PMID-sentid Pub_year Sent_text comp_official_name comp_offset protein_name organism prot_offset 34035463-0 2021 Platycodin D, a natural component of Platycodon grandiflorum, prevents both lysosome- and TMPRSS2-driven SARS-CoV-2 infection by hindering membrane fusion. platycodin D 0-12 transmembrane serine protease 2 Homo sapiens 90-97 34054222-4 2021 Key findings and conclusions: EGCG, via activating Nrf2, can suppress ACE2 (a cellular receptor for SARS-CoV-2) and TMPRSS2, which mediate cell entry of the virus. epigallocatechin gallate 30-34 transmembrane serine protease 2 Homo sapiens 116-123 34052981-3 2021 METHODS: In the present study molecular docking technique was applied to test binding affinity of ciprofloxacin and levofloxacin-two commercially available fluoroquinolones, to SARS-CoV-2 S-, E- and TMPRSS2 proteins, RNA-dependent RNA polymerase and papain-like protease (PLPRO). Fluoroquinolones 156-172 transmembrane serine protease 2 Homo sapiens 199-206 34052981-6 2021 In the case of TMPRSS2 protein and PLPRO protease the best docked ligand was levofloxacin and in the case of E proteins and RNA-dependent RNA polymerase the best docked ligands were levofloxacin and dexamethasone. Levofloxacin 77-89 transmembrane serine protease 2 Homo sapiens 15-22 34052981-6 2021 In the case of TMPRSS2 protein and PLPRO protease the best docked ligand was levofloxacin and in the case of E proteins and RNA-dependent RNA polymerase the best docked ligands were levofloxacin and dexamethasone. Dexamethasone 199-212 transmembrane serine protease 2 Homo sapiens 15-22 34052981-7 2021 Moreover, a molecular dynamics study also reveals that ciprofloxacin and levofloxacin form a stable complex with E- and TMPRSS2 proteins, RNA polymerase and papain-like protease (PLPRO). Ciprofloxacin 55-68 transmembrane serine protease 2 Homo sapiens 120-127 34052981-7 2021 Moreover, a molecular dynamics study also reveals that ciprofloxacin and levofloxacin form a stable complex with E- and TMPRSS2 proteins, RNA polymerase and papain-like protease (PLPRO). Levofloxacin 73-85 transmembrane serine protease 2 Homo sapiens 120-127 34052981-0 2021 The application of in silico experimental model in the assessment of ciprofloxacin and levofloxacin interaction with main SARS-CoV-2 targets: S-, E- and TMPRSS2 proteins, RNA-dependent RNA polymerase and papain-like protease (PLpro)-preliminary molecular docking analysis. Ciprofloxacin 69-82 transmembrane serine protease 2 Homo sapiens 153-160 34052981-0 2021 The application of in silico experimental model in the assessment of ciprofloxacin and levofloxacin interaction with main SARS-CoV-2 targets: S-, E- and TMPRSS2 proteins, RNA-dependent RNA polymerase and papain-like protease (PLpro)-preliminary molecular docking analysis. Levofloxacin 87-99 transmembrane serine protease 2 Homo sapiens 153-160 34052981-3 2021 METHODS: In the present study molecular docking technique was applied to test binding affinity of ciprofloxacin and levofloxacin-two commercially available fluoroquinolones, to SARS-CoV-2 S-, E- and TMPRSS2 proteins, RNA-dependent RNA polymerase and papain-like protease (PLPRO). Ciprofloxacin 98-111 transmembrane serine protease 2 Homo sapiens 199-206 34052981-3 2021 METHODS: In the present study molecular docking technique was applied to test binding affinity of ciprofloxacin and levofloxacin-two commercially available fluoroquinolones, to SARS-CoV-2 S-, E- and TMPRSS2 proteins, RNA-dependent RNA polymerase and papain-like protease (PLPRO). Levofloxacin 116-128 transmembrane serine protease 2 Homo sapiens 199-206 34042026-7 2022 In this review, we discuss the current state of the art of developing inhibitors against the entry proteases furin, the transmembrane serine protease type-II (TMPRSS2), trypsin, and cathepsin L. Serine 134-140 transmembrane serine protease 2 Homo sapiens 159-166 34035463-3 2021 Here, we show that platycodin D (PD), a triterpenoid saponin abundant in Platycodon grandiflorum (PG), a dietary and medicinal herb commonly used in East Asia, effectively blocks the two main SARS-CoV-2 infection routes via lysosome- and transmembrane protease serine 2 (TMPRSS2)-driven entry. platycodin D 19-31 transmembrane serine protease 2 Homo sapiens 238-269 34035463-3 2021 Here, we show that platycodin D (PD), a triterpenoid saponin abundant in Platycodon grandiflorum (PG), a dietary and medicinal herb commonly used in East Asia, effectively blocks the two main SARS-CoV-2 infection routes via lysosome- and transmembrane protease serine 2 (TMPRSS2)-driven entry. platycodin D 19-31 transmembrane serine protease 2 Homo sapiens 271-278 34016183-8 2021 Previous studies have shown that people with ACE2 polymorphism who have type 2 transmembrane serine proteases (TMPRSS2) are at high risk of SARS-CoV-2 infection. Serine 93-99 transmembrane serine protease 2 Homo sapiens 111-118 33556871-3 2021 Meanwhile, host-targeted drugs that inhibit cellular transmembrane serine protease (TMPRSS2) can prevent SARS-CoV-2 from entering cells, and its combination with chloroquine and dihydroorotate dehydrogenase (DHODH) inhibitors can limit the spread of SARS-CoV-2 and reduce the morbidity and mortality of patients with COVID-19. Serine 67-73 transmembrane serine protease 2 Homo sapiens 84-91 34001215-3 2021 Camostat mesylate acts as an inhibitor of the host cell serine protease TMPRSS2 and prevents the virus from entering the cell. Serine 56-62 transmembrane serine protease 2 Homo sapiens 72-79 33667455-4 2021 Valproic acid could reduce angiotensin-converting enzyme 2 and transmembrane serine protease 2 expression, required for SARS-CoV-2 viral entry, and modulate the immune cellular and cytokine response to infection, thereby reducing end-organ damage. Valproic Acid 0-13 transmembrane serine protease 2 Homo sapiens 63-94 33979601-8 2021 In turn, pre-treatment of erythroid cells with dexamethasone significantly diminished ACE2/TMPRSS2 expression and subsequently reduced their infectivity with SARS-CoV-2. Dexamethasone 47-60 transmembrane serine protease 2 Homo sapiens 91-98 33556871-3 2021 Meanwhile, host-targeted drugs that inhibit cellular transmembrane serine protease (TMPRSS2) can prevent SARS-CoV-2 from entering cells, and its combination with chloroquine and dihydroorotate dehydrogenase (DHODH) inhibitors can limit the spread of SARS-CoV-2 and reduce the morbidity and mortality of patients with COVID-19. Chloroquine 162-173 transmembrane serine protease 2 Homo sapiens 84-91 32306862-6 2021 Moreover, four promising inhibitors were identified against TMPRSS2; Rubitecan and Loprazolam drugs, and compounds ZINC000015988935 and ZINC000103558522. triazulenone 83-93 transmembrane serine protease 2 Homo sapiens 60-67 33556379-4 2021 RA-differentiation induced an upregulation of ace2 and tmprss2 gene expression while inducing downregulation of ctsb and ctsl. Tretinoin 0-2 transmembrane serine protease 2 Homo sapiens 55-62 33706067-1 2021 While the angiotensin converting enzyme 2 (ACE2) protein is defined as the primary severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) receptor, the viral serine molecule might be mobilized by the host"s transmembrane protease serine subtype 2 (TMPRSS2) enzyme from the viral spike (S) protein and hijack the host"s N-acetyl-D-galactosamine (GalNAc) metabolism. Serine 164-170 transmembrane serine protease 2 Homo sapiens 254-261 33689451-0 2021 Ribavirin shows antiviral activity against SARS-CoV-2 and downregulates the activity of TMPRSS2 and the expression of ACE2 In Vitro. Ribavirin 0-9 transmembrane serine protease 2 Homo sapiens 88-95 33689451-5 2021 According to the detailed molecular techniques, Ribavirin was shown to decrease the expression of TMPRSS2 both at mRNA and protein levels 48 hours after treatment. Ribavirin 48-57 transmembrane serine protease 2 Homo sapiens 98-105 33689451-7 2021 Finally, proteolytic activity assays showed that Ribavirin also showed an inhibitory effect on TMPRSS2 enzyme. Ribavirin 49-58 transmembrane serine protease 2 Homo sapiens 95-102 33689451-8 2021 Based on these results, we hypothesized that Ribavirin may inhibit the expression of TMPRSS2 by modulating the formation of inhibitory G-quadruplex structures at the TMPRSS2 promoter. Ribavirin 45-54 transmembrane serine protease 2 Homo sapiens 85-92 33689451-8 2021 Based on these results, we hypothesized that Ribavirin may inhibit the expression of TMPRSS2 by modulating the formation of inhibitory G-quadruplex structures at the TMPRSS2 promoter. Ribavirin 45-54 transmembrane serine protease 2 Homo sapiens 166-173 33689451-9 2021 As a conclusion, Ribavirin is a potential antiviral drug for the treatment against SARS-CoV-2, and it interferes with the effect of TMPRSS2 and ACE2 expression. Ribavirin 17-26 transmembrane serine protease 2 Homo sapiens 132-139 33903855-0 2021 Efficacy of the TMPRSS2 inhibitor camostat mesilate in patients hospitalized with Covid-19-a double-blind randomized controlled trial. camostat 34-51 transmembrane serine protease 2 Homo sapiens 16-23 33903855-4 2021 Within 48 h of admission, participants were randomly assigned in a 2:1 ratio to receive the TMPRSS2 inhibitor camostat mesilate 200 mg three times daily for 5 days or placebo. camostat 110-127 transmembrane serine protease 2 Homo sapiens 92-99 32936429-4 2021 A tentative hypothesis to explain these findings is the role of angiotensin-converting enzyme 2 (ACE2) and serine protease TMPRSS2 involved in viral infection. Serine 107-113 transmembrane serine protease 2 Homo sapiens 123-130 33969249-2 2021 Transmembrane serine protease 2 (TMPRSS2) is regarded as one of the main proteases implicated in the coronavirus S protein priming, an important step for binding of the S protein to the angiotensin-converting enzyme 2 (ACE2) receptor before cell entry. Serine 14-20 transmembrane serine protease 2 Homo sapiens 33-40 33394891-3 2021 SARS-CoV-2 enters host cells via angiotensin converting enzyme-2 (ACE2) and the serine protease TMPRSS2. Serine 80-86 transmembrane serine protease 2 Homo sapiens 96-103 33991451-2 2021 Viral entry is dependent on the binding of the viral spike protein to the angiotensin converting enzyme II protein (ACE2) on the host cell surface, followed by proteolytic cleavage by a host serine protease such as TMPRSS2. Serine 191-197 transmembrane serine protease 2 Homo sapiens 215-222 33996911-1 2021 Camostat, nafamostat, and bromhexine are inhibitors of the transmembrane serine protease TMPRSS2. nafamostat 10-20 transmembrane serine protease 2 Homo sapiens 89-96 33996911-1 2021 Camostat, nafamostat, and bromhexine are inhibitors of the transmembrane serine protease TMPRSS2. Bromhexine 26-36 transmembrane serine protease 2 Homo sapiens 89-96 33996911-1 2021 Camostat, nafamostat, and bromhexine are inhibitors of the transmembrane serine protease TMPRSS2. Serine 73-79 transmembrane serine protease 2 Homo sapiens 89-96 33996911-3 2021 However, while camostat and nafamostat inhibit TMPRSS2 by forming a covalent adduct, the mode of action of bromhexine remains unclear. camostat 15-23 transmembrane serine protease 2 Homo sapiens 47-54 33996911-3 2021 However, while camostat and nafamostat inhibit TMPRSS2 by forming a covalent adduct, the mode of action of bromhexine remains unclear. nafamostat 28-38 transmembrane serine protease 2 Homo sapiens 47-54 33981629-8 2021 Results: Among the TLR agonists, the TLR3 agonist Poly(I:C) significantly increased ACE2 and TMPRSS2 mRNA expression in HNECs (ACE2 36.212+-11.600-fold change, p<0.0001; TMPRSS2 5.598+-2.434-fold change, p=0.031). Poly I-C 50-59 transmembrane serine protease 2 Homo sapiens 93-100 33981629-8 2021 Results: Among the TLR agonists, the TLR3 agonist Poly(I:C) significantly increased ACE2 and TMPRSS2 mRNA expression in HNECs (ACE2 36.212+-11.600-fold change, p<0.0001; TMPRSS2 5.598+-2.434-fold change, p=0.031). Poly I-C 50-59 transmembrane serine protease 2 Homo sapiens 170-177 33969249-5 2021 Results: We identified the human extracellular serine protease inhibitor (serpin) alpha 1 anti-trypsin (A1AT) as a novel TMPRSS2 inhibitor. Serine 47-53 transmembrane serine protease 2 Homo sapiens 121-128 33969249-6 2021 Structural modeling revealed that A1AT docked to an extracellular domain of TMPRSS2 in a conformation that is suitable for catalysis, resembling similar serine protease inhibitor complexes. Serine 153-159 transmembrane serine protease 2 Homo sapiens 76-83 33922918-13 2021 The SARS-CoV-2 priming proteases Tmprss2, Cathepsin L, and Furin mRNA were upregulated by DHT in the kidney. Dihydrotestosterone 90-93 transmembrane serine protease 2 Homo sapiens 33-40 33919991-3 2021 In this study, we show that L-carnitine tartrate supplementation in humans and rodents led to significant decreases of key host dependency factors, notably angiotensin-converting enzyme 2 (ACE2), transmembrane protease serine 2 (TMPRSS2), and Furin, which are responsible for viral attachment, viral spike S-protein cleavage, and priming for viral fusion and entry. Carnitine 28-39 transmembrane serine protease 2 Homo sapiens 196-227 33886690-6 2021 Next, SARS-2-S-driven entry was efficiently activated by not only TMPRSS2, but also the TMPRSS13 protease, thus broadening the cell tropism of SARS-CoV-2. sars-2-s 6-14 transmembrane serine protease 2 Homo sapiens 66-73 33919991-3 2021 In this study, we show that L-carnitine tartrate supplementation in humans and rodents led to significant decreases of key host dependency factors, notably angiotensin-converting enzyme 2 (ACE2), transmembrane protease serine 2 (TMPRSS2), and Furin, which are responsible for viral attachment, viral spike S-protein cleavage, and priming for viral fusion and entry. Carnitine 28-39 transmembrane serine protease 2 Homo sapiens 229-236 33868970-7 2022 Results and conclusion: The phytochemicals like limonin, gedunin, eribulin, pedunculagin, limonin glycoside and betunilic acid bind at the active site of both furin and TMPRSS2. Glycosides 98-107 transmembrane serine protease 2 Homo sapiens 169-176 33868970-7 2022 Results and conclusion: The phytochemicals like limonin, gedunin, eribulin, pedunculagin, limonin glycoside and betunilic acid bind at the active site of both furin and TMPRSS2. betunilic acid 112-126 transmembrane serine protease 2 Homo sapiens 169-176 33608407-10 2021 Paradoxically, Bromhexine enhanced cell-cell fusion in the presence of TMPRSS2, while its metabolite Ambroxol exhibited inhibitory activity in some conditions. Bromhexine 15-25 transmembrane serine protease 2 Homo sapiens 71-78 33608407-13 2021 Bromhexine, reportedly an inhibitor of TMPRSS2, is currently tested in clinical trials against coronavirus disease 2019. Bromhexine 0-10 transmembrane serine protease 2 Homo sapiens 39-46 33868970-10 2022 Among the drugs, the drug nafamostat may be more beneficial than the camostat in suppressing the activity of TMPRSS2. nafamostat 26-36 transmembrane serine protease 2 Homo sapiens 109-116 33647240-0 2021 Low risk of the TMPRSS2 inhibitor camostat mesylate and its metabolite GBPA to act as perpetrators of drug-drug interactions. camostat 34-51 transmembrane serine protease 2 Homo sapiens 16-23 33842191-8 2021 These studies suggested that bromocriptine can be the best candidate for TMPRSS2, Main protease, and RdRp protein. Bromocriptine 29-42 transmembrane serine protease 2 Homo sapiens 73-80 33918670-6 2021 In human Caco-2 colon epithelial cells as well as the lung cell line A549 stably expressing ACE2 and TMPRSS2, quinine also showed antiviral activity. Quinine 110-117 transmembrane serine protease 2 Homo sapiens 101-108 33821268-6 2021 The mechanism of the protease inhibitors nafamostat and camostat extend beyond inhibition of TMPRSS2 to coagulation-induced spike cleavage. nafamostat 41-51 transmembrane serine protease 2 Homo sapiens 93-100 33647240-0 2021 Low risk of the TMPRSS2 inhibitor camostat mesylate and its metabolite GBPA to act as perpetrators of drug-drug interactions. 4-(4-guanidinobenzoyloxy)phenylacetic acid 71-75 transmembrane serine protease 2 Homo sapiens 16-23 33609069-8 2021 Analyses of functional annotation and enrichment in TMPRSS2 showed that TMPRSS2 is mostly enriched in regulation of viral entry into host cells, protein processing and serine-type peptidase activity. Serine 168-174 transmembrane serine protease 2 Homo sapiens 52-59 33609069-8 2021 Analyses of functional annotation and enrichment in TMPRSS2 showed that TMPRSS2 is mostly enriched in regulation of viral entry into host cells, protein processing and serine-type peptidase activity. Serine 168-174 transmembrane serine protease 2 Homo sapiens 72-79 33164230-10 2021 There is growing evidence that androgen-enabled expression of ACE2 receptors and the serine protease TMPRSS2, two permissive elements engaging the SARS-CoV-2 spike protein for infection, may contribute to severe COVID-19 in men. Serine 85-91 transmembrane serine protease 2 Homo sapiens 101-108 33694182-4 2021 The expression of CYP1A1, PSA, KLK2, TMPRSS2, and AR mRNA levels was decreased which results in reducing the production of PSA and DHT in the presence of testosterone. Testosterone 154-166 transmembrane serine protease 2 Homo sapiens 37-44 33786727-8 2022 A number of bonding interactions in terms of hydrogen bond and hydrophobic interactions were observed between the proposed molecules and ligand-interacting amino acids of the TMPRSS2. Hydrogen 45-53 transmembrane serine protease 2 Homo sapiens 175-182 33188579-4 2021 Angiotensin-converting enzyme 2 (ACE2) and type II transmembrane serine protease (TMPRSS2) are the main host cell factors for the Severe Acute Respiratory Syndrome-Coronavirus 2 (SARS-CoV-2) entry but so far it is unclear if human MSCs express or do not these two proteins. Serine 65-71 transmembrane serine protease 2 Homo sapiens 82-89 33790352-2 2021 Keeping this hypothesis intact, the present study describes for the first-time, Grazoprevir, an FDA approved anti-viral drug primarily approved for Hepatitis C Virus (HCV), mediated multiple pathway control via synergistic inhibition of viral entry targeting host cell Angiotensin-Converting Enzyme 2 (ACE-2)/transmembrane serine protease 2 (TMPRSS2) and viral replication targeting RNA-dependent RNA polymerase (RdRP). grazoprevir 80-91 transmembrane serine protease 2 Homo sapiens 309-340 33790352-2 2021 Keeping this hypothesis intact, the present study describes for the first-time, Grazoprevir, an FDA approved anti-viral drug primarily approved for Hepatitis C Virus (HCV), mediated multiple pathway control via synergistic inhibition of viral entry targeting host cell Angiotensin-Converting Enzyme 2 (ACE-2)/transmembrane serine protease 2 (TMPRSS2) and viral replication targeting RNA-dependent RNA polymerase (RdRP). grazoprevir 80-91 transmembrane serine protease 2 Homo sapiens 342-349 33606519-7 2021 This study, for the first time, reports the molecules like cyclosporine, calcitriol, and estradiol as candidate drugs with the binding ability to the host proteases, TMPRSS2, and cathepsin B/L. Cyclosporine 59-71 transmembrane serine protease 2 Homo sapiens 166-173 33741941-5 2021 We further demonstrate that alpha1AT binds and inactivates the serine protease TMPRSS2, which enzymatically primes the SARS-CoV-2 spike protein for membrane fusion. Serine 63-69 transmembrane serine protease 2 Homo sapiens 79-86 33722999-1 2021 BACKGROUND: Bromhexine is a potent inhibitor of transmembrane serine protease 2 and appears to have an antiviral effect in controlling influenza and parainfluenza infection; however, its efficacy in COVID-19 is controversial. Bromhexine 12-22 transmembrane serine protease 2 Homo sapiens 48-79 33758885-0 2021 Magnesium Treatment on Methylation Changes of Transmembrane Serine Protease 2 (TMPRSS2). Magnesium 0-9 transmembrane serine protease 2 Homo sapiens 46-77 33758885-0 2021 Magnesium Treatment on Methylation Changes of Transmembrane Serine Protease 2 (TMPRSS2). Magnesium 0-9 transmembrane serine protease 2 Homo sapiens 79-86 33758885-2 2021 Objectives: To test the hypothesis that Mg treatment leads to DNA methylation changes in TMPRSS2 . Magnesium 40-42 transmembrane serine protease 2 Homo sapiens 89-96 33758885-10 2021 These findings, if confirmed, provide another mechanism for the role of Mg intervention for the prevention of COVID-19 and treatment of early and mild disease by modifying the phenotype of the TMPRSS2 genotype. Magnesium 72-74 transmembrane serine protease 2 Homo sapiens 193-200 33706759-8 2021 ACE2 and TMPRSS2 were also expressed in FSP-1+ lung fibroblasts in bleomycin-induced pulmonary fibrosis, and when combined with PM exposure, they were further upregulated. Bleomycin 67-76 transmembrane serine protease 2 Homo sapiens 9-16 33750821-4 2021 In vivo studies indicate that 8P9R or the combination of repurposed drugs (umifenovir also known as arbidol, chloroquine and camostat which is a TMPRSS2 inhibitor), simultaneously interfering with the two entry pathways of coronaviruses, can significantly suppress SARS-CoV-2 replication in hamsters and SARS-CoV in mice. umifenovir 75-85 transmembrane serine protease 2 Homo sapiens 145-152 33750821-4 2021 In vivo studies indicate that 8P9R or the combination of repurposed drugs (umifenovir also known as arbidol, chloroquine and camostat which is a TMPRSS2 inhibitor), simultaneously interfering with the two entry pathways of coronaviruses, can significantly suppress SARS-CoV-2 replication in hamsters and SARS-CoV in mice. umifenovir 100-107 transmembrane serine protease 2 Homo sapiens 145-152 33750821-4 2021 In vivo studies indicate that 8P9R or the combination of repurposed drugs (umifenovir also known as arbidol, chloroquine and camostat which is a TMPRSS2 inhibitor), simultaneously interfering with the two entry pathways of coronaviruses, can significantly suppress SARS-CoV-2 replication in hamsters and SARS-CoV in mice. camostat 125-133 transmembrane serine protease 2 Homo sapiens 145-152 33606519-7 2021 This study, for the first time, reports the molecules like cyclosporine, calcitriol, and estradiol as candidate drugs with the binding ability to the host proteases, TMPRSS2, and cathepsin B/L. Calcitriol 73-83 transmembrane serine protease 2 Homo sapiens 166-173 33664446-6 2021 In addition, eicosapentaenoic acid showed higher efficacy than linolenic acid in reducing activity of TMPRSS2 and cathepsin L proteases, but neither of the fatty acids affected their expression at the protein level. Eicosapentaenoic Acid 13-34 transmembrane serine protease 2 Homo sapiens 102-109 33606519-7 2021 This study, for the first time, reports the molecules like cyclosporine, calcitriol, and estradiol as candidate drugs with the binding ability to the host proteases, TMPRSS2, and cathepsin B/L. Estradiol 89-98 transmembrane serine protease 2 Homo sapiens 166-173 33664446-6 2021 In addition, eicosapentaenoic acid showed higher efficacy than linolenic acid in reducing activity of TMPRSS2 and cathepsin L proteases, but neither of the fatty acids affected their expression at the protein level. alpha-Linolenic Acid 63-77 transmembrane serine protease 2 Homo sapiens 102-109 33606519-11 2021 The molecular docking and MD simulation results showed strong and stable binding of cyclosporine A (CsA) with TMPRSS2 and CTSL genes. Cyclosporine 84-98 transmembrane serine protease 2 Homo sapiens 110-117 33606519-11 2021 The molecular docking and MD simulation results showed strong and stable binding of cyclosporine A (CsA) with TMPRSS2 and CTSL genes. Cyclosporine 100-103 transmembrane serine protease 2 Homo sapiens 110-117 33791156-7 2021 Through an initiate pilot screening with around 100 compounds, Flupirtine, a selective neuronal potassium channel opener, was identified as a potential TMPRSS2 inhibitor from an FDA-approved drug library by using this screening platform, and showed inhibitory effect on the TMPRSS-dependent infection of SARS-CoV-2 Spike-pseudotyped lentiviral particles. flupirtine 63-73 transmembrane serine protease 2 Homo sapiens 152-159 33791156-1 2021 Transmembrane serine protease (TMPRSS2) plays an oncogenic role in prostate cancer as the fusion gene with ERG, and has also been demonstrated to be essential for the cellular entry of severe acute respiratory syndrome coronaviruses (SARS-CoV). Serine 14-20 transmembrane serine protease 2 Homo sapiens 31-38 33791156-8 2021 This study describes a platform proven effective for rapidly screening of TMPRSS2 inhibitors, and suggests that Flupirtine may be worthy of further consideration of repurposing to treat COVID-19 patients. flupirtine 112-122 transmembrane serine protease 2 Homo sapiens 74-81 33676899-0 2021 Camostat mesylate inhibits SARS-CoV-2 activation by TMPRSS2-related proteases and its metabolite GBPA exerts antiviral activity. camostat 0-17 transmembrane serine protease 2 Homo sapiens 52-59 33676899-8 2021 The Camostat metabolite GBPA inhibited recombinant TMPRSS2 with reduced efficiency as compared to Camostat mesylate. gbpa 24-28 transmembrane serine protease 2 Homo sapiens 51-58 33676899-11 2021 INTERPRETATION: Our results suggest that SARS-CoV-2 can use TMPRSS2 and closely related proteases for spread in the upper respiratory tract and that spread in the human lung can be blocked by Camostat mesylate and its metabolite GBPA. gbpa 229-233 transmembrane serine protease 2 Homo sapiens 60-67 33626084-6 2021 This pattern of ACE2 expression contrasted with that of transmembrane protease serine type 2 (TMPRSS2), which was significantly increased in full-term newborn and adult NHP lungs compared to preterm NHP lungs. Serine 79-85 transmembrane serine protease 2 Homo sapiens 94-101 33671076-2 2021 Although TMPRSS2 is a well-characterized type II transmembrane serine protease (TTSP), the role of other TTSPs on the replication of SARS-CoV-2 remains to be elucidated. Serine 63-69 transmembrane serine protease 2 Homo sapiens 9-16 33708781-1 2021 Purpose: On the basis that spironolactone is involved in ACE2 expression and TMPRSS2 activity, previous studies have suggested that spironolactone may influence the infectivity of COVID-19. Spironolactone 27-41 transmembrane serine protease 2 Homo sapiens 77-84 33708781-1 2021 Purpose: On the basis that spironolactone is involved in ACE2 expression and TMPRSS2 activity, previous studies have suggested that spironolactone may influence the infectivity of COVID-19. Spironolactone 132-146 transmembrane serine protease 2 Homo sapiens 77-84 33558541-0 2021 Distinct mechanisms for TMPRSS2 expression explain organ-specific inhibition of SARS-CoV-2 infection by enzalutamide. enzalutamide 104-116 transmembrane serine protease 2 Homo sapiens 24-31 33570381-5 2021 However, we observed a substantial drop in antiviral potency upon expression of TMPRSS2, a transmembrane serine protease that acts in an alternative viral entry pathway to the lysosomal cathepsins. Serine 105-111 transmembrane serine protease 2 Homo sapiens 80-87 33563156-3 2022 METHOD: In this work two home-made databases from synthetic quinolines and coumarins were virtually docked against viral proteases (3CL and PL), human cell surface proteases (TMPRSS2 and furin) and spike proteins (S1 and S2). Quinolines 60-70 transmembrane serine protease 2 Homo sapiens 175-182 33558541-3 2021 Among these drugs, a second-generation antiandrogen agent, enzalutamide, was proposed because it reduces the expression of transmembrane serine protease 2 (TMPRSS2), a key component mediating SARS-CoV-2-driven entry, in prostate cancer cells. enzalutamide 59-71 transmembrane serine protease 2 Homo sapiens 123-154 33563156-3 2022 METHOD: In this work two home-made databases from synthetic quinolines and coumarins were virtually docked against viral proteases (3CL and PL), human cell surface proteases (TMPRSS2 and furin) and spike proteins (S1 and S2). Coumarins 75-84 transmembrane serine protease 2 Homo sapiens 175-182 33558541-3 2021 Among these drugs, a second-generation antiandrogen agent, enzalutamide, was proposed because it reduces the expression of transmembrane serine protease 2 (TMPRSS2), a key component mediating SARS-CoV-2-driven entry, in prostate cancer cells. enzalutamide 59-71 transmembrane serine protease 2 Homo sapiens 156-163 33563156-7 2022 Two compounds, quinoline-1 and coumarin-24, were found to be effective on three targets - S2, TMPRSS2 and furin - simultaneously, with good predicted affinity between -7.54 to -8.85 kcal/mol. quinoline 15-24 transmembrane serine protease 2 Homo sapiens 94-101 33465165-0 2021 Hydroxychloroquine-mediated inhibition of SARS-CoV-2 entry is attenuated by TMPRSS2. Hydroxychloroquine 0-18 transmembrane serine protease 2 Homo sapiens 76-83 33563156-7 2022 Two compounds, quinoline-1 and coumarin-24, were found to be effective on three targets - S2, TMPRSS2 and furin - simultaneously, with good predicted affinity between -7.54 to -8.85 kcal/mol. coumarin 31-39 transmembrane serine protease 2 Homo sapiens 94-101 33176395-3 2021 Camostat mesylate, an orally available well-known serine protease inhibitor, is a potent inhibitor of TMPRSS2 and has been hypothesized as a potential antiviral drug against COVID-19. camostat 0-17 transmembrane serine protease 2 Homo sapiens 102-109 33465165-8 2021 We also show that hydroxychloroquine efficiently blocks viral entry mediated by cathepsin L, but not by TMPRSS2, and that a combination of hydroxychloroquine and a clinically-tested TMPRSS2 inhibitor prevents SARS-CoV-2 infection more potently than either drug alone. Hydroxychloroquine 18-36 transmembrane serine protease 2 Homo sapiens 182-189 33564221-1 2021 The type II transmembrane serine protease TMPRSS2 facilitates the entry of coronaviruses, such as SARS-CoV-2, into host cells by cleaving the S1/S2 interface of the viral spike protein. Serine 26-32 transmembrane serine protease 2 Homo sapiens 42-49 33564221-5 2021 Based on the binding mode of GBPA, residues K342 and W461 have been identified as potential contacts involved in TMPRSS2 selective binding and activity. gbpa 29-33 transmembrane serine protease 2 Homo sapiens 113-120 33564221-5 2021 Based on the binding mode of GBPA, residues K342 and W461 have been identified as potential contacts involved in TMPRSS2 selective binding and activity. croconazole 44-48 transmembrane serine protease 2 Homo sapiens 113-120 32851697-7 2021 As for TMPRSS2, 90.7% of TE1 cells, 31.5% of CTBs, 22.1% of EVTs and 70.8% of STBs were TMPRSS2 positive. stbs 78-82 transmembrane serine protease 2 Homo sapiens 88-95 33512650-0 2021 Strong Binding of Leupeptin with TMPRSS2 Protease May Be an Alternative to Camostat and Nafamostat for SARS-CoV-2 Repurposed Drug: Evaluation from Molecular Docking and Molecular Dynamics Simulations. leupeptin 18-27 transmembrane serine protease 2 Homo sapiens 33-40 33512650-8 2021 The docking study reveals that leupeptin molecule strongly binds with TMPRSS2 protein than the other two drug molecules. leupeptin 31-40 transmembrane serine protease 2 Homo sapiens 70-77 33512650-10 2021 Furthermore, leupeptin forms interactions with the key amino acids of TMPRSS2 and the same have been maintained during the MD simulations. leupeptin 13-22 transmembrane serine protease 2 Homo sapiens 70-77 33512650-11 2021 This structural and dynamical information is useful to evaluate these drugs to be used as repurposed drugs, however, the strong binding profile of leupeptin with TMPRSS2, suggests, it may be considered as a repurposed drug for COVID-19 disease after clinical trial. leupeptin 147-156 transmembrane serine protease 2 Homo sapiens 162-169 33035337-4 2021 SARS-CoV-2 uses human angiotensin-converting enzyme 2 (ACE2) for viral entry and transmembrane serine protease family member II (TMPRSS2) for spike protein priming. Serine 95-101 transmembrane serine protease 2 Homo sapiens 129-136 33477294-10 2021 It has been proposed that spironolactone may prevent acute lung injury in COVID-19 infection due to its pleiotropic effects with favorable renin-angiotensin-aldosterone system (RAAS) and ACE2 expression, reduction in transmembrane serine protease 2 (TMPRSS2) activity and antiandrogenic action, and therefore it may prove to act as additional protection for patients at highest risk of severe pneumonia. Spironolactone 26-40 transmembrane serine protease 2 Homo sapiens 217-248 33477294-10 2021 It has been proposed that spironolactone may prevent acute lung injury in COVID-19 infection due to its pleiotropic effects with favorable renin-angiotensin-aldosterone system (RAAS) and ACE2 expression, reduction in transmembrane serine protease 2 (TMPRSS2) activity and antiandrogenic action, and therefore it may prove to act as additional protection for patients at highest risk of severe pneumonia. Spironolactone 26-40 transmembrane serine protease 2 Homo sapiens 250-257 33488517-9 2020 ACE2 receptor and TMPRSS2 serine protease were colocalized in adrenocortical cells in zona fasciculata and zona reticularis. Serine 26-32 transmembrane serine protease 2 Homo sapiens 18-25 33098835-6 2021 Bioactive peptides with unique amino acid sequences can mitigate such targets including, type II transmembrane serine proteases (TMPRSS2) inhibition, furin cleavage, and renin-angiotensin-aldosterone system (RAAS) members. Serine 111-117 transmembrane serine protease 2 Homo sapiens 129-136 32452644-2 2021 The key steps of virus life cycle have been recently clarified, highlighting the role of host type 2 angiotensin-converting enzyme (ACE2) and TMPRSS2 serine protease in virus-cell binding and entry, respectively. Serine 150-156 transmembrane serine protease 2 Homo sapiens 142-149 33130280-7 2021 The catalytic triad consisting of Serine-441, Histidine-296 and Aspartic acid-345 was identified as active binding site of TMPRSS2 using existing ligands. Serine 34-40 transmembrane serine protease 2 Homo sapiens 123-130 33130280-7 2021 The catalytic triad consisting of Serine-441, Histidine-296 and Aspartic acid-345 was identified as active binding site of TMPRSS2 using existing ligands. Histidine 46-55 transmembrane serine protease 2 Homo sapiens 123-130 33130280-7 2021 The catalytic triad consisting of Serine-441, Histidine-296 and Aspartic acid-345 was identified as active binding site of TMPRSS2 using existing ligands. Aspartic Acid 64-77 transmembrane serine protease 2 Homo sapiens 123-130 33397514-5 2021 Interestingly, serine protease transmembrane serine protease 2 (TMPRSS2) had less expression in cardiomyocytes, but CTSB and CTSL, which belonged to cell protease, could be found to be enriched in cardiomyocytes. Serine 15-21 transmembrane serine protease 2 Homo sapiens 64-71 33397514-5 2021 Interestingly, serine protease transmembrane serine protease 2 (TMPRSS2) had less expression in cardiomyocytes, but CTSB and CTSL, which belonged to cell protease, could be found to be enriched in cardiomyocytes. Serine 45-51 transmembrane serine protease 2 Homo sapiens 64-71 33372179-4 2020 Since AT2 cells express the SARS-CoV-2 receptors angiotensin converting enzyme (ACE2) and transmembrane protease/serine subfamily member 2 (TMPRSS2), their expression should decline as AT2 cells are depleted by hyperoxia. Serine 113-119 transmembrane serine protease 2 Homo sapiens 140-147 33382023-6 2020 Molecular docking score and MMGBSA Binding energy of Fisetin was better than Nafamostat, a known inhibitor of TMPRSS2. nafamostat 77-87 transmembrane serine protease 2 Homo sapiens 110-117 33382023-11 2020 Significant decrease in TMPRSS2-Fisetin and TMPRSS2-Nafamostat complex fluctuation occurred around His 41, Glu 44, Gly 136, Ser 186 in RMSF study. Histidine 99-102 transmembrane serine protease 2 Homo sapiens 24-31 33382023-11 2020 Significant decrease in TMPRSS2-Fisetin and TMPRSS2-Nafamostat complex fluctuation occurred around His 41, Glu 44, Gly 136, Ser 186 in RMSF study. Histidine 99-102 transmembrane serine protease 2 Homo sapiens 44-51 33382023-11 2020 Significant decrease in TMPRSS2-Fisetin and TMPRSS2-Nafamostat complex fluctuation occurred around His 41, Glu 44, Gly 136, Ser 186 in RMSF study. Glutamic Acid 107-110 transmembrane serine protease 2 Homo sapiens 24-31 33382023-11 2020 Significant decrease in TMPRSS2-Fisetin and TMPRSS2-Nafamostat complex fluctuation occurred around His 41, Glu 44, Gly 136, Ser 186 in RMSF study. Glutamic Acid 107-110 transmembrane serine protease 2 Homo sapiens 44-51 33382023-11 2020 Significant decrease in TMPRSS2-Fisetin and TMPRSS2-Nafamostat complex fluctuation occurred around His 41, Glu 44, Gly 136, Ser 186 in RMSF study. Glycine 115-118 transmembrane serine protease 2 Homo sapiens 24-31 33382023-11 2020 Significant decrease in TMPRSS2-Fisetin and TMPRSS2-Nafamostat complex fluctuation occurred around His 41, Glu 44, Gly 136, Ser 186 in RMSF study. Glycine 115-118 transmembrane serine protease 2 Homo sapiens 44-51 33382023-11 2020 Significant decrease in TMPRSS2-Fisetin and TMPRSS2-Nafamostat complex fluctuation occurred around His 41, Glu 44, Gly 136, Ser 186 in RMSF study. Serine 124-127 transmembrane serine protease 2 Homo sapiens 24-31 33382023-11 2020 Significant decrease in TMPRSS2-Fisetin and TMPRSS2-Nafamostat complex fluctuation occurred around His 41, Glu 44, Gly 136, Ser 186 in RMSF study. Serine 124-127 transmembrane serine protease 2 Homo sapiens 44-51 33505639-0 2021 Spontaneous binding of potential COVID-19 drugs (Camostat and Nafamostat) to human serine protease TMPRSS2. Serine 83-89 transmembrane serine protease 2 Homo sapiens 99-106 33505639-2 2021 Recent studies showed that two drugs, Camostat and Nafamostat, might be repurposed to treat COVID-19 by inhibiting human TMPRSS2 required for proteolytic activation of viral spike (S) glycoprotein. camostat 38-46 transmembrane serine protease 2 Homo sapiens 121-128 33505639-2 2021 Recent studies showed that two drugs, Camostat and Nafamostat, might be repurposed to treat COVID-19 by inhibiting human TMPRSS2 required for proteolytic activation of viral spike (S) glycoprotein. nafamostat 51-61 transmembrane serine protease 2 Homo sapiens 121-128 32972339-6 2021 The priming of the spike (S) protein of the virus by proteolytic cleavage by the trans-membrane serine protease-2 (TMPRSS2) is necessary for fusion of the virus to the host cell after it binds to its receptor angiotensin converting enzyme-2 (ACE2). Serine 96-102 transmembrane serine protease 2 Homo sapiens 115-122 33239231-5 2021 First, AAT is a serine protease inhibitor (SERPIN) shown to inhibit TMPRSS-2, the host serine protease that cleaves the spike protein of SARS-CoV-2, a necessary preparatory step for the virus to bind its cell surface receptor ACE2 to gain intracellular entry. Serine 16-22 transmembrane serine protease 2 Homo sapiens 68-76 33239231-5 2021 First, AAT is a serine protease inhibitor (SERPIN) shown to inhibit TMPRSS-2, the host serine protease that cleaves the spike protein of SARS-CoV-2, a necessary preparatory step for the virus to bind its cell surface receptor ACE2 to gain intracellular entry. Serine 87-93 transmembrane serine protease 2 Homo sapiens 68-76 33141332-3 2021 The current body of evidence indicates that SARS-CoV-2 requires the membrane-bound angiotensin-converting enzyme 2 (ACE2) and the membrane-bound serine protease TMPRSS2 to enter cells. Serine 145-151 transmembrane serine protease 2 Homo sapiens 161-168 33290397-2 2020 The host serine protease TMPRSS2 and cysteine proteases Cathepsin B/L can activate S, making two independent entry pathways accessible to SARS-CoV-2. Serine 9-15 transmembrane serine protease 2 Homo sapiens 25-32 33375616-1 2020 The human serine protease serine 2 TMPRSS2 is involved in the priming of proteins of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and represents a possible target for COVID-19 therapy. Serine 10-16 transmembrane serine protease 2 Homo sapiens 35-42 33375616-1 2020 The human serine protease serine 2 TMPRSS2 is involved in the priming of proteins of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and represents a possible target for COVID-19 therapy. Serine 26-32 transmembrane serine protease 2 Homo sapiens 35-42 33375616-7 2020 Several well-studied drugs can downregulate the expression of TMPRSS2 in human cells, including acetaminophen (paracetamol) and curcumin. Acetaminophen 96-109 transmembrane serine protease 2 Homo sapiens 62-69 33375616-7 2020 Several well-studied drugs can downregulate the expression of TMPRSS2 in human cells, including acetaminophen (paracetamol) and curcumin. Acetaminophen 111-122 transmembrane serine protease 2 Homo sapiens 62-69 33375616-7 2020 Several well-studied drugs can downregulate the expression of TMPRSS2 in human cells, including acetaminophen (paracetamol) and curcumin. Curcumin 128-136 transmembrane serine protease 2 Homo sapiens 62-69 33390952-9 2020 In addition, theaflavin-3-gallate could inhibit protein expression of ACE2 and TMPRSS2 without significant cytotoxicity. Theaflavin 3-gallate 13-33 transmembrane serine protease 2 Homo sapiens 79-86 33390952-10 2020 Our results suggest that GB-1 and theaflavin-3-gallate could act as potential candidates for prophylaxis or treatment of SARS-CoV-2 infection through inhibiting protein expression of ACE2 and TMPRSS2 for the further study. Theaflavin 3-gallate 34-54 transmembrane serine protease 2 Homo sapiens 192-199 33390974-6 2020 An analysis of the pharmacology of HCQ in COVID-19 reveals certain possible reasons for this failure-a pharmacokinetic failure due to failure to achieve adequate drug concentration at the target site and attenuation of its inhibitory effect due to the presence of TMPRSS2 in airway epithelial cells. Hydroxychloroquine 35-38 transmembrane serine protease 2 Homo sapiens 264-271 32808185-3 2020 Angiotensin-converting enzyme 2 (ACE2) and Transmembrane serine protease (TMPRSS2) are the main cell entry receptors of SARS-CoV-2. Serine 57-63 transmembrane serine protease 2 Homo sapiens 74-81 33415017-0 2020 Tannic acid suppresses SARS-CoV-2 as a dual inhibitor of the viral main protease and the cellular TMPRSS2 protease. Tannins 0-11 transmembrane serine protease 2 Homo sapiens 98-105 33415017-1 2020 The cell surface protein TMPRSS2 (transmembrane protease serine 2) is an androgen-responsive serine protease important for prostate cancer progression and therefore an attractive therapeutic target. Serine 57-63 transmembrane serine protease 2 Homo sapiens 25-32 33415017-6 2020 Here we show that screening of these compounds identified tannic acid a potent inhibitor of both SARS-CoV-2 Mpro and TMPRSS2. Tannins 58-69 transmembrane serine protease 2 Homo sapiens 117-124 33415017-7 2020 Molecular analysis demonstrated that tannic acid formed a thermodynamically stable complex with the two proteins at a KD of 1.1 mM for Mpro and 1.77 mM for TMPRSS2. Tannins 37-48 transmembrane serine protease 2 Homo sapiens 156-163 33415017-8 2020 Tannic acid inhibited the activities of the two proteases with an IC50 of 13.4 mM for Mpro and 2.31 mM for TMPRSS2. Tannins 0-11 transmembrane serine protease 2 Homo sapiens 107-114 33278189-4 2020 The virus requires proteolytic processing of its spike protein by transmembrane protease receptor serine type 2 (TMPRSS2) to enable binding to cellular ACE2. Serine 98-104 transmembrane serine protease 2 Homo sapiens 113-120 33278189-5 2020 Since TMPRSS2 contains an androgen promoter, it may be downregulated by the antiandrogenic actions of spironolactone. Spironolactone 102-116 transmembrane serine protease 2 Homo sapiens 6-13 33278189-11 2020 We review the evidence that spironolactone may be the preferred RASSi to increase PN1 and decrease TMPRSS2, furin and plasmin activities and thereby to reduce viral cell binding, entry, infectivity and bad outcomes. Spironolactone 28-42 transmembrane serine protease 2 Homo sapiens 99-106 32808185-8 2020 The expression level of TMPRSS2 was increased noticeably with a number of medications such as metformin. Metformin 94-103 transmembrane serine protease 2 Homo sapiens 24-31 33049583-7 2020 In the compositions of GB-2, we discovered that 50 mug/mL of theaflavin could inhibit protein expression of ACE2 and TMPRSS2. theaflavin 61-71 transmembrane serine protease 2 Homo sapiens 117-124 33049583-9 2020 In conclusion, our results suggest that GB-2 and theaflavin could act as potential compounds for ACE2 and TMPRSS2 inhibitors in the further clinical study. theaflavin 49-59 transmembrane serine protease 2 Homo sapiens 106-113 33245731-8 2020 TMPRSS2, inflammatory cytokines G-CSF, M-CSF, IL-1alpha, IL-6 and MCP-1 are suppressed by MEKi alone or with remdesivir. remdesivir 109-119 transmembrane serine protease 2 Homo sapiens 0-7 33330557-12 2020 Studies have found that ACE2 and TMPRSS2 are expressed in the testis and male reproductive tract and are regulated by testosterone. Testosterone 118-130 transmembrane serine protease 2 Homo sapiens 33-40 33218024-0 2020 Target-Centered Drug Repurposing Predictions of Human Angiotensin-Converting Enzyme 2 (ACE2) and Transmembrane Protease Serine Subtype 2 (TMPRSS2) Interacting Approved Drugs for Coronavirus Disease 2019 (COVID-19) Treatment through a Drug-Target Interaction Deep Learning Model. Serine 120-126 transmembrane serine protease 2 Homo sapiens 138-145 33218024-7 2020 Furthermore, three of the top 30 drugs with strong affinity prediction for the TMPRSS2 are anti-hepatitis C virus (HCV) drugs, including ombitasvir, daclatasvir, and paritaprevir. ombitasvir 137-147 transmembrane serine protease 2 Homo sapiens 79-86 33218024-7 2020 Furthermore, three of the top 30 drugs with strong affinity prediction for the TMPRSS2 are anti-hepatitis C virus (HCV) drugs, including ombitasvir, daclatasvir, and paritaprevir. daclatasvir 149-160 transmembrane serine protease 2 Homo sapiens 79-86 33218024-7 2020 Furthermore, three of the top 30 drugs with strong affinity prediction for the TMPRSS2 are anti-hepatitis C virus (HCV) drugs, including ombitasvir, daclatasvir, and paritaprevir. paritaprevir 166-178 transmembrane serine protease 2 Homo sapiens 79-86 33218024-8 2020 Notably, of the top 30 drugs, AT1R blocker eprosartan and neuropsychiatric drug lisuride showed similar gene expression profiles to potential TMPRSS2 inhibitors. eprosartan 43-53 transmembrane serine protease 2 Homo sapiens 142-149 33218024-8 2020 Notably, of the top 30 drugs, AT1R blocker eprosartan and neuropsychiatric drug lisuride showed similar gene expression profiles to potential TMPRSS2 inhibitors. Lisuride 80-88 transmembrane serine protease 2 Homo sapiens 142-149 33328008-2 2020 Angiotensin-converting enzyme 2 (ACE2), one of the binding sites for SARS-CoV-2 infection in humans, can bind to viral spike proteins, allowing transmembrane serine protease (TMPRSS2) to activate S-protein to trigger infection and induce the production of various inflammatory factors such as interleukin-1, interferon-l, and tumor necrosis factor. Serine 158-164 transmembrane serine protease 2 Homo sapiens 175-182 33391794-1 2020 Angiotensin-converting enzyme 2 (ACE2) and serine protease TMPRSS2 have been implicated in cell entry for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the virus responsible for coronavirus disease 2019 (COVID-19). Serine 43-49 transmembrane serine protease 2 Homo sapiens 59-66 33200134-0 2020 Ozone exposure upregulates the expression of host susceptibility protein TMPRSS2 to SARS-CoV-2. Ozone 0-5 transmembrane serine protease 2 Homo sapiens 73-80 32960480-4 2020 The plasma serine protease inhibitor alpha-1 antitrypsin was suggested to protect from COVID-19 by inhibiting TMPRSS2, a cell surface serine protease essential for the SARS-CoV-2 cell entry. Serine 11-17 transmembrane serine protease 2 Homo sapiens 110-117 33170176-11 2020 In addition, we identified possible interactions among hydroxytyrosol and alpha-cyclodextrin with the protein Spike and the human proteins ACE2 and TMPRSS2. 3,4-dihydroxyphenylethanol 55-69 transmembrane serine protease 2 Homo sapiens 148-155 33170176-11 2020 In addition, we identified possible interactions among hydroxytyrosol and alpha-cyclodextrin with the protein Spike and the human proteins ACE2 and TMPRSS2. alpha-cyclodextrin 74-92 transmembrane serine protease 2 Homo sapiens 148-155 31894360-6 2020 S-saponin treatment induces a decrease in AR expression in a time- and dose-dependent manner and a potent decrease in the expression of its target genes, including prostate-specific antigen (PSA), transmembrane protease, serin 2 (TMPRSS2), and NK3 homeobox 1 (NKX3.1). sakurasosaponin 0-9 transmembrane serine protease 2 Homo sapiens 230-237 32857620-0 2020 Azithromycin Downregulates Gene Expression of IL-1beta and Pathways Involving TMPRSS2 and TMPRSS11D Required by SARS-CoV-2. Azithromycin 0-12 transmembrane serine protease 2 Homo sapiens 78-85 32857620-8 2020 RESULTS: Cell cultures treated with 10microg of azithromycin significantly downregulated receptor-mediated endocytosis canonical pathways involving TMPRSS2 and TMPRSS11D genes. Azithromycin 48-60 transmembrane serine protease 2 Homo sapiens 148-155 32857620-11 2020 CONCLUSIONS: This proof of concept demonstrates azithromycin downregulates pathways involving serine proteases TMPRSS2 and TMPRSS11D required for SARS-CoV-2 activation and its cell-to-cell transmission while downregulating pro-inflammatory cytokine IL-1beta, NDST-1 and their associated pathways. Azithromycin 48-60 transmembrane serine protease 2 Homo sapiens 111-118 32857620-11 2020 CONCLUSIONS: This proof of concept demonstrates azithromycin downregulates pathways involving serine proteases TMPRSS2 and TMPRSS11D required for SARS-CoV-2 activation and its cell-to-cell transmission while downregulating pro-inflammatory cytokine IL-1beta, NDST-1 and their associated pathways. Serine 94-100 transmembrane serine protease 2 Homo sapiens 111-118 32890967-3 2020 SARS-CoV-2 entry into host cells is characterized by viral spike protein interaction with cellular angiotensin-converting enzyme 2 (ACE2) and serine protease TMPRSS2. Serine 142-148 transmembrane serine protease 2 Homo sapiens 158-165 32960480-4 2020 The plasma serine protease inhibitor alpha-1 antitrypsin was suggested to protect from COVID-19 by inhibiting TMPRSS2, a cell surface serine protease essential for the SARS-CoV-2 cell entry. Serine 134-140 transmembrane serine protease 2 Homo sapiens 110-117 32829149-8 2020 We highlight 376 approved, investigational or experimental drugs targeting S1A serine proteases that may also inhibit TMPRSS2. Serine 79-85 transmembrane serine protease 2 Homo sapiens 118-125 32441816-4 2020 Therefore, this study aimed to assess the presence of angiotensin-converting enzyme 2 (ACE2)/transmembrane serine proteases 2 (TMPRSS2) expression in salivary glands using publicly available databases. Serine 107-113 transmembrane serine protease 2 Homo sapiens 127-134 33125431-1 2020 Angiotensin-converting enzyme 2 (ACE2) has been implicated in the pathogenesis of chronic kidney disease (CKD) and is a membrane receptor for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the virus responsible for coronavirus disease (COVID-19), whereas transmembrane protease, serine 2 (TMPRSS2) is involved in viral attachment. Serine 294-300 transmembrane serine protease 2 Homo sapiens 304-311 32829149-10 2020 We discuss how experimental drugs targeting related serine proteases might be repurposed as TMPRSS2 inhibitors to treat coronaviruses. Serine 52-58 transmembrane serine protease 2 Homo sapiens 92-99 32768580-3 2020 This study investigates the N720D variant, positioned in the collectrin-like domain (CLD) at proximity to type II transmembrane serine protease (TMPRSS2) cleavage site. Serine 128-134 transmembrane serine protease 2 Homo sapiens 145-152 33111622-3 2022 The aim of this study was to investigate the interactions of twenty-three phytochemicals belonging to different flavonoid subgroups with the receptor binding domain (RBD) of the spike glycoprotein of 2019-nCoV, and cellular proteases [transmembrane serine protease 2 (TMPRSS2), cathepsin B and L (CatB/L)]. Flavonoids 112-121 transmembrane serine protease 2 Homo sapiens 235-266 33111622-3 2022 The aim of this study was to investigate the interactions of twenty-three phytochemicals belonging to different flavonoid subgroups with the receptor binding domain (RBD) of the spike glycoprotein of 2019-nCoV, and cellular proteases [transmembrane serine protease 2 (TMPRSS2), cathepsin B and L (CatB/L)]. Flavonoids 112-121 transmembrane serine protease 2 Homo sapiens 268-275 33137894-3 2020 The TMPRSS2 gene encodes a Transmembrane Protease Serine-2 protein (TMPS2) that belongs to the serine protease family. Serine 50-56 transmembrane serine protease 2 Homo sapiens 4-11 33137894-3 2020 The TMPRSS2 gene encodes a Transmembrane Protease Serine-2 protein (TMPS2) that belongs to the serine protease family. Serine 50-56 transmembrane serine protease 2 Homo sapiens 68-73 33137894-3 2020 The TMPRSS2 gene encodes a Transmembrane Protease Serine-2 protein (TMPS2) that belongs to the serine protease family. Serine 95-101 transmembrane serine protease 2 Homo sapiens 4-11 33137894-3 2020 The TMPRSS2 gene encodes a Transmembrane Protease Serine-2 protein (TMPS2) that belongs to the serine protease family. Serine 95-101 transmembrane serine protease 2 Homo sapiens 68-73 33089728-0 2022 Prevention of SARS-CoV-2 cell entry: insight from in silico interaction of drug-like alkaloids with spike glycoprotein, human ACE2, and TMPRSS2. Alkaloids 85-94 transmembrane serine protease 2 Homo sapiens 136-143 33089728-5 2022 These alkaloids were docked for their interactions with SARS-CoV-2 spike glycoprotein, ACE2, and TMPRSS2. Alkaloids 6-15 transmembrane serine protease 2 Homo sapiens 97-104 33089728-9 2022 10-Hydroxyusambarensine and Cryptospirolepine were docked in a similar binding pattern to the S1-specificy pocket of TMPRSS2 as camostat (reference inhibitor). 10'-hydroxyusambarensine 0-23 transmembrane serine protease 2 Homo sapiens 117-124 33089728-9 2022 10-Hydroxyusambarensine and Cryptospirolepine were docked in a similar binding pattern to the S1-specificy pocket of TMPRSS2 as camostat (reference inhibitor). cryptospirolepine 28-45 transmembrane serine protease 2 Homo sapiens 117-124 33052338-2 2020 Transmembrane serine protease 2 (TMPRSS2) is regarded as one of the main proteases implicated in the coronavirus S protein priming, an important step for binding of the S protein to the angiotensin-converting enzyme 2 (ACE2) receptor before cell entry. Serine 14-20 transmembrane serine protease 2 Homo sapiens 33-40 33007239-4 2020 Cleavage and the syncytium are abolished by treatment with the furin inhibitors decanoyl-RVKR-chloromethylketone (CMK) and naphthofluorescein, but not by the transmembrane protease serine 2 (TMPRSS2) inhibitor camostat. decanoylRVKRchloromethylketone 114-117 transmembrane serine protease 2 Homo sapiens 191-198 33007239-4 2020 Cleavage and the syncytium are abolished by treatment with the furin inhibitors decanoyl-RVKR-chloromethylketone (CMK) and naphthofluorescein, but not by the transmembrane protease serine 2 (TMPRSS2) inhibitor camostat. naphthofluorescein 123-141 transmembrane serine protease 2 Homo sapiens 191-198 33066495-6 2020 Interestingly, GPR30 appears to exhibit greater co-localisation with TMPRSS2 in key tissues like lung and prostate, suggesting that BPA exposure may impact on the local expression of these SARS-CoV-2 infection mediators. bisphenol A 132-135 transmembrane serine protease 2 Homo sapiens 69-76 33052338-4 2020 Herein, we identified the human extracellular serine protease inhibitor (serpin) alpha 1 antitrypsin (A1AT) as a novel TMPRSS2 inhibitor. Serine 46-52 transmembrane serine protease 2 Homo sapiens 119-126 33052338-5 2020 Structural modeling revealed that A1AT docked to an extracellular domain of TMPRSS2 in a conformation that is suitable for catalysis, resembling similar serine protease-inhibitor complexes. Serine 153-159 transmembrane serine protease 2 Homo sapiens 76-83 32730844-5 2020 Repositioning approved, investigational and experimental drugs on the serine protease domain of TMPRSS2 could thus be valuable. Serine 70-76 transmembrane serine protease 2 Homo sapiens 96-103 33117437-3 2020 The observed role of androgens in transcription of transmembrane protease serine-2, which facilitates COVID-19 anchoring to angiotensin-converting enzyme 2 cell surface receptors, seems to suggest that higher testosterone levels might be detrimental for outcomes. Testosterone 209-221 transmembrane serine protease 2 Homo sapiens 51-82 32730844-3 2020 A putative target to interfere with the virus is the host transmembrane serine protease family member II (TMPRSS2). Serine 72-78 transmembrane serine protease 2 Homo sapiens 106-113 33193689-1 2020 Type 2 transmembrane serine protease (TMPRSS2) is a new member of the serine proteases, and studies have shown that TMPRSS2 plays a role in the occurrence of prostate malignancies and is closely related to the occurrence of the coronavirus disease 2019 (COVID-19). Serine 21-27 transmembrane serine protease 2 Homo sapiens 38-45 32721806-5 2020 Current data shows that spironolactone may concurrently mitigate abnormal ACE2 expression, correct the balances membrane-attached and free circulating ACE2 and between angiotensin II and Angiotensin-(1-7) (Ang-(1-7)), suppress androgen-mediated TMPRSS2 activity, and inhibit obesity-related RAAS dysfunctions, with consequent decrease of viral priming. Spironolactone 24-38 transmembrane serine protease 2 Homo sapiens 245-252 33193689-1 2020 Type 2 transmembrane serine protease (TMPRSS2) is a new member of the serine proteases, and studies have shown that TMPRSS2 plays a role in the occurrence of prostate malignancies and is closely related to the occurrence of the coronavirus disease 2019 (COVID-19). Serine 21-27 transmembrane serine protease 2 Homo sapiens 116-123 33193689-1 2020 Type 2 transmembrane serine protease (TMPRSS2) is a new member of the serine proteases, and studies have shown that TMPRSS2 plays a role in the occurrence of prostate malignancies and is closely related to the occurrence of the coronavirus disease 2019 (COVID-19). Serine 70-76 transmembrane serine protease 2 Homo sapiens 38-45 33193689-1 2020 Type 2 transmembrane serine protease (TMPRSS2) is a new member of the serine proteases, and studies have shown that TMPRSS2 plays a role in the occurrence of prostate malignancies and is closely related to the occurrence of the coronavirus disease 2019 (COVID-19). Serine 70-76 transmembrane serine protease 2 Homo sapiens 116-123 32974340-11 2020 Further, we discovered unique signatures of genes in ACE2 + TMPRSS2 + STBs and EVTs. stbs 70-74 transmembrane serine protease 2 Homo sapiens 60-67 33042994-8 2020 Following the binding of the S1 receptor-binding domain (RBD) to ACE2, transmembrane protease/serine subfamily 2 (TMPRSS2) cleaves the S2 domain to facilitate membrane fusion. Serine 94-100 transmembrane serine protease 2 Homo sapiens 114-121 32726128-5 2020 Testosterone on the contrary enhances the levels of the two most critical molecules, angiotensin-converting enzyme 2 (ACE2) and the transmembrane protease serine-type 2 (TMPRSS2), transcriptionally and posttranslationally, thereby increasing viral load and delaying viral clearance in men as compared with women. Testosterone 0-12 transmembrane serine protease 2 Homo sapiens 170-177 32726128-5 2020 Testosterone on the contrary enhances the levels of the two most critical molecules, angiotensin-converting enzyme 2 (ACE2) and the transmembrane protease serine-type 2 (TMPRSS2), transcriptionally and posttranslationally, thereby increasing viral load and delaying viral clearance in men as compared with women. Serine 155-161 transmembrane serine protease 2 Homo sapiens 170-177 32641482-7 2020 Interestingly, overexpression of serine protease TMPRSS2 or amphotericin treatment significantly neutralized the IFN-inducible transmembrane 3 (IFITM3) restriction of human coronavirus (CoV) entry, but did not compromise the effect of LY6E on the entry of human coronaviruses. Serine 33-39 transmembrane serine protease 2 Homo sapiens 49-56 32992731-2 2020 Proposed mechanisms involve host cell membrane-bound angiotensin-converting enzyme 2 (ACE2), type II transmembrane serine proteases (TTSPs), such as transmembrane serine protease isoform 2 (TMPRSS2), lysosomal endopeptidase Cathepsin L (CTSL), subtilisin-like proprotein peptidase furin (FURIN), and even potentially membrane bound heparan sulfate proteoglycans. Serine 115-121 transmembrane serine protease 2 Homo sapiens 190-197 32992731-2 2020 Proposed mechanisms involve host cell membrane-bound angiotensin-converting enzyme 2 (ACE2), type II transmembrane serine proteases (TTSPs), such as transmembrane serine protease isoform 2 (TMPRSS2), lysosomal endopeptidase Cathepsin L (CTSL), subtilisin-like proprotein peptidase furin (FURIN), and even potentially membrane bound heparan sulfate proteoglycans. Serine 163-169 transmembrane serine protease 2 Homo sapiens 190-197 32992731-2 2020 Proposed mechanisms involve host cell membrane-bound angiotensin-converting enzyme 2 (ACE2), type II transmembrane serine proteases (TTSPs), such as transmembrane serine protease isoform 2 (TMPRSS2), lysosomal endopeptidase Cathepsin L (CTSL), subtilisin-like proprotein peptidase furin (FURIN), and even potentially membrane bound heparan sulfate proteoglycans. Heparitin Sulfate 332-347 transmembrane serine protease 2 Homo sapiens 190-197 32924827-8 2022 The results indicated that, Ritonavir has the highest potency to block SARS-CoV-2 main protease and human TMPRSS2, a host cell factor that aids viral infection. Ritonavir 28-37 transmembrane serine protease 2 Homo sapiens 106-113 32842606-9 2020 Further, we have performed molecular dynamics (MD) simulations to analyze the stability of the protein-ligand complexes for the three top inhibitors of TMPRSS2 namely, qingdainone, edgeworoside C and adlumidine, and of cathepsin L namely, ararobinol, (+)-oxoturkiyenine and 3alpha,17alpha-cinchophylline. qingdainone 168-179 transmembrane serine protease 2 Homo sapiens 152-159 32842606-9 2020 Further, we have performed molecular dynamics (MD) simulations to analyze the stability of the protein-ligand complexes for the three top inhibitors of TMPRSS2 namely, qingdainone, edgeworoside C and adlumidine, and of cathepsin L namely, ararobinol, (+)-oxoturkiyenine and 3alpha,17alpha-cinchophylline. edgeworoside C 181-195 transmembrane serine protease 2 Homo sapiens 152-159 32842606-9 2020 Further, we have performed molecular dynamics (MD) simulations to analyze the stability of the protein-ligand complexes for the three top inhibitors of TMPRSS2 namely, qingdainone, edgeworoside C and adlumidine, and of cathepsin L namely, ararobinol, (+)-oxoturkiyenine and 3alpha,17alpha-cinchophylline. Adlumidine 200-210 transmembrane serine protease 2 Homo sapiens 152-159 32842606-9 2020 Further, we have performed molecular dynamics (MD) simulations to analyze the stability of the protein-ligand complexes for the three top inhibitors of TMPRSS2 namely, qingdainone, edgeworoside C and adlumidine, and of cathepsin L namely, ararobinol, (+)-oxoturkiyenine and 3alpha,17alpha-cinchophylline. NSC658573 239-249 transmembrane serine protease 2 Homo sapiens 152-159 32842606-9 2020 Further, we have performed molecular dynamics (MD) simulations to analyze the stability of the protein-ligand complexes for the three top inhibitors of TMPRSS2 namely, qingdainone, edgeworoside C and adlumidine, and of cathepsin L namely, ararobinol, (+)-oxoturkiyenine and 3alpha,17alpha-cinchophylline. (+)-Oxoturkiyenine 251-269 transmembrane serine protease 2 Homo sapiens 152-159 32842606-9 2020 Further, we have performed molecular dynamics (MD) simulations to analyze the stability of the protein-ligand complexes for the three top inhibitors of TMPRSS2 namely, qingdainone, edgeworoside C and adlumidine, and of cathepsin L namely, ararobinol, (+)-oxoturkiyenine and 3alpha,17alpha-cinchophylline. Deoxycholic Acid 274-280 transmembrane serine protease 2 Homo sapiens 152-159 32842606-9 2020 Further, we have performed molecular dynamics (MD) simulations to analyze the stability of the protein-ligand complexes for the three top inhibitors of TMPRSS2 namely, qingdainone, edgeworoside C and adlumidine, and of cathepsin L namely, ararobinol, (+)-oxoturkiyenine and 3alpha,17alpha-cinchophylline. 17alpha-cinchophylline 281-303 transmembrane serine protease 2 Homo sapiens 152-159 32824674-4 2020 High testosterone levels could upregulate transmembrane serine protease 2 (TMPRSS2), facilitating the entry of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) into host cells via angiotensin-converting enzyme 2 (ACE2). Testosterone 5-17 transmembrane serine protease 2 Homo sapiens 42-73 32824674-4 2020 High testosterone levels could upregulate transmembrane serine protease 2 (TMPRSS2), facilitating the entry of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) into host cells via angiotensin-converting enzyme 2 (ACE2). Testosterone 5-17 transmembrane serine protease 2 Homo sapiens 75-82 32824674-6 2020 Clinical studies on TMPRSS2 inhibitors, such as camostat, nafamostat, and bromhexine, are ongoing. nafamostat 58-68 transmembrane serine protease 2 Homo sapiens 20-27 32824674-6 2020 Clinical studies on TMPRSS2 inhibitors, such as camostat, nafamostat, and bromhexine, are ongoing. Bromhexine 74-84 transmembrane serine protease 2 Homo sapiens 20-27 32974340-12 2020 The ACE2 + TMPRSS2 + STBs are highly differentiated cells and express genes involving mitochondrial metabolism and glucose transport. Glucose 115-122 transmembrane serine protease 2 Homo sapiens 11-18 32793908-5 2020 Chloroquine or hydroxychloroquine increase cleaved active SP-domain of TMPRSS2, and this is potentiated by MEKi. Chloroquine 0-11 transmembrane serine protease 2 Homo sapiens 71-78 32818215-4 2020 Among these, homoharringtonine and halofuginone appear the most potent agents, reducing endogenous TMPRSS2 expression at sub-micromolar concentrations. Homoharringtonine 13-30 transmembrane serine protease 2 Homo sapiens 99-106 32818215-4 2020 Among these, homoharringtonine and halofuginone appear the most potent agents, reducing endogenous TMPRSS2 expression at sub-micromolar concentrations. halofuginone 35-47 transmembrane serine protease 2 Homo sapiens 99-106 32818215-6 2020 We further demonstrate that halofuginone modulates TMPRSS2 levels through proteasomal-mediated degradation that involves the E3 ubiquitin ligase component DDB1- and CUL4-associated factor 1 (DCAF1). halofuginone 28-40 transmembrane serine protease 2 Homo sapiens 51-58 32793911-0 2020 Camostat mesylate inhibits SARS-CoV-2 activation by TMPRSS2-related proteases and its metabolite GBPA exerts antiviral activity. camostat 0-17 transmembrane serine protease 2 Homo sapiens 52-59 32793911-2 2020 The protease inhibitor camostat mesylate inhibits SARS-CoV-2 infection of lung cells by blocking the virus-activating host cell protease TMPRSS2. camostat 23-40 transmembrane serine protease 2 Homo sapiens 137-144 32793911-7 2020 The camostat metabolite GBPA inhibited the activity of recombinant TMPRSS2 with reduced efficiency as compared to camostat mesylate and was rapidly generated in the presence of serum. gbpa 24-28 transmembrane serine protease 2 Homo sapiens 67-74 32793908-5 2020 Chloroquine or hydroxychloroquine increase cleaved active SP-domain of TMPRSS2, and this is potentiated by MEKi. Hydroxychloroquine 15-33 transmembrane serine protease 2 Homo sapiens 71-78 32793908-8 2020 TMPRSS2, inflammatory cytokines G-CSF, M- CSF, IL-1a, IL-6 and MCP-1 are suppressed by MEKi alone or in combination with remdesivir. remdesivir 121-131 transmembrane serine protease 2 Homo sapiens 0-7 32741259-3 2020 SARS-CoV and SARS-CoV-2 employ the host cellular serine protease TMPRSS2 for spike (S) protein priming for viral entry into host cells. Serine 49-55 transmembrane serine protease 2 Homo sapiens 65-72 32515982-6 2020 It is suggested that H2S may block SARS-CoV-2 entry into host cells by interfering with ACE2 and TMPRSS2, inhibit SARS-CoV-2 replication by attenuating virus assembly/release, and protect SARS-CoV-2-induced lung damage by suppressing immune response and inflammation development. Deuterium 21-24 transmembrane serine protease 2 Homo sapiens 97-104 32741259-7 2020 Camostat and bromhexine are known TMPRSS2 inhibitor drugs, hence these were used as control molecules throughout the study. camostat 0-8 transmembrane serine protease 2 Homo sapiens 34-41 32741259-7 2020 Camostat and bromhexine are known TMPRSS2 inhibitor drugs, hence these were used as control molecules throughout the study. Bromhexine 13-23 transmembrane serine protease 2 Homo sapiens 34-41 32741259-8 2020 Based on better dock score, binding-free energy and binding interactions compared to the control molecules, six molecules (Neohesperidin, Myricitrin, Quercitrin, Naringin, Icariin, and Ambroxol) were found to be promising against the TMPRSS2. neohesperidin 123-136 transmembrane serine protease 2 Homo sapiens 234-241 32741259-8 2020 Based on better dock score, binding-free energy and binding interactions compared to the control molecules, six molecules (Neohesperidin, Myricitrin, Quercitrin, Naringin, Icariin, and Ambroxol) were found to be promising against the TMPRSS2. myricitrin 138-148 transmembrane serine protease 2 Homo sapiens 234-241 32741259-8 2020 Based on better dock score, binding-free energy and binding interactions compared to the control molecules, six molecules (Neohesperidin, Myricitrin, Quercitrin, Naringin, Icariin, and Ambroxol) were found to be promising against the TMPRSS2. quercitrin 150-160 transmembrane serine protease 2 Homo sapiens 234-241 32741259-8 2020 Based on better dock score, binding-free energy and binding interactions compared to the control molecules, six molecules (Neohesperidin, Myricitrin, Quercitrin, Naringin, Icariin, and Ambroxol) were found to be promising against the TMPRSS2. naringin 162-170 transmembrane serine protease 2 Homo sapiens 234-241 32741259-8 2020 Based on better dock score, binding-free energy and binding interactions compared to the control molecules, six molecules (Neohesperidin, Myricitrin, Quercitrin, Naringin, Icariin, and Ambroxol) were found to be promising against the TMPRSS2. icariin 172-179 transmembrane serine protease 2 Homo sapiens 234-241 32741259-8 2020 Based on better dock score, binding-free energy and binding interactions compared to the control molecules, six molecules (Neohesperidin, Myricitrin, Quercitrin, Naringin, Icariin, and Ambroxol) were found to be promising against the TMPRSS2. Ambroxol 185-193 transmembrane serine protease 2 Homo sapiens 234-241 32953840-0 2020 Erratum to dexmedetomidine promotes breast cancer cell migration through Rab11-mediated secretion of exosomal TMPRSS2. Dexmedetomidine 11-26 transmembrane serine protease 2 Homo sapiens 110-117 32458206-5 2020 Using bromhexine at a dosage that selectively inhibits TMPRSS2 and, in so doing, inhibits TMPRSS2-specific viral entry is likely to be effective against SARS-CoV-2. Bromhexine 6-16 transmembrane serine protease 2 Homo sapiens 55-62 32638018-7 2020 Inversely, the most important S protein cleavage protease TMPRSS2 (transmembrane protease serine protease-2) in the heart exhibits an extremely lower expression than that in the lung (adjusted P < 0.0001), which may restrict entry of SARS-CoV-2 into cardiac cells. Serine 90-96 transmembrane serine protease 2 Homo sapiens 58-65 32458206-5 2020 Using bromhexine at a dosage that selectively inhibits TMPRSS2 and, in so doing, inhibits TMPRSS2-specific viral entry is likely to be effective against SARS-CoV-2. Bromhexine 6-16 transmembrane serine protease 2 Homo sapiens 90-97 32743585-4 2020 Because AT2 cells express the SARS-CoV-2 receptors angiotensin converting enzyme (ACE2) and transmembrane protease/serine subfamily member 2 (TMPRSS2), we expected their expression would decline as AT2 cells were depleted by hyperoxia. Serine 115-121 transmembrane serine protease 2 Homo sapiens 142-149 32864545-5 2020 Androgens upregulate the protease TMPRSS2 (type II transmembrane serine protease-2), which facilitates efficient virus-host cell fusion with the epithelium of the lungs, thus increasing susceptibility to SARS-CoV-2 infection and development of severe COVID-19. Serine 65-71 transmembrane serine protease 2 Homo sapiens 34-41 32864545-6 2020 Owing to low levels of steroid hormones, prepubertal children may have low expression of TMPRSS2, thereby limiting the viral entry into host cells. Steroids 23-30 transmembrane serine protease 2 Homo sapiens 89-96 32672528-1 2021 Transmembrane serine protease 2 (TMPRSS2) has been established as one of the host proteins that facilitate entry of coronaviruses into host cells. Serine 14-20 transmembrane serine protease 2 Homo sapiens 33-40 32672528-7 2021 Two lead compounds, ZINC64606047 and ZINC05296775, were identified having binding affinities higher than those of the reference inhibitors, favorable interactions with TMPRSS2 active site residues and good ADME and medicinal chemistry properties. ZINC64606047 20-32 transmembrane serine protease 2 Homo sapiens 168-175 32672528-7 2021 Two lead compounds, ZINC64606047 and ZINC05296775, were identified having binding affinities higher than those of the reference inhibitors, favorable interactions with TMPRSS2 active site residues and good ADME and medicinal chemistry properties. zinc05296775 37-49 transmembrane serine protease 2 Homo sapiens 168-175 32662421-3 2020 The novel coronavirus canonically utilizes the angiotensin-converting enzyme 2 (ACE2) receptor and the serine protease TMPRSS2 for cell entry. Serine 103-109 transmembrane serine protease 2 Homo sapiens 119-126 32664879-9 2020 We further discussed that polymorphisms in ACE2 or TMPRSS2 could guide effective treatments (i.e., hydroxychloroquine and camostat) for COVID-19. Hydroxychloroquine 99-117 transmembrane serine protease 2 Homo sapiens 51-58 32664879-9 2020 We further discussed that polymorphisms in ACE2 or TMPRSS2 could guide effective treatments (i.e., hydroxychloroquine and camostat) for COVID-19. camostat 122-130 transmembrane serine protease 2 Homo sapiens 51-58 32664949-4 2020 It is cleaved by type II transmembrane serine protease (TMPRSS)2 and disintegrin and metallopeptidase domain (ADAM)17 to assist viral entry into host cells. Serine 39-45 transmembrane serine protease 2 Homo sapiens 56-64 32589459-1 2020 PURPOSE: The spike proteins of SARS-CoV-2 interact with ACE2 or basigin/CD147 receptors, regulating human-to-human transmissions of COVID-19 together with serine protease TMPRSS2. Serine 155-161 transmembrane serine protease 2 Homo sapiens 171-178 32412310-2 2020 Prostate cancer is one of the most common cancers among men and raises particular interest during the pandemic as recent reports show that the TMPRSS2 (and other serine proteases), which facilitate the entry, replication and budding of the virion from a cell, can be inhibited using androgen deprivation therapy. Serine 162-168 transmembrane serine protease 2 Homo sapiens 143-150 32278065-8 2020 SARS-CoV uses the angiotensin-converting enzyme 2 (ACE2) and the serine protease TMPRSS2 for S protein priming. Serine 65-71 transmembrane serine protease 2 Homo sapiens 81-88 32511372-5 2020 We found that the potent Nrf2 activating composition PB125 downregulates ACE2 and TMPRSS2 mRNA expression in human liver-derived HepG2 cells. pb125 53-58 transmembrane serine protease 2 Homo sapiens 83-90 32334052-0 2020 Repurposing the mucolytic cough suppressant and TMPRSS2 protease inhibitor bromhexine for the prevention and management of SARS-CoV-2 infection. Bromhexine 75-85 transmembrane serine protease 2 Homo sapiens 48-55 32469279-0 2022 Withanone and Withaferin-A are predicted to interact with transmembrane protease serine 2 (TMPRSS2) and block entry of SARS-CoV-2 into cells. withanone 0-9 transmembrane serine protease 2 Homo sapiens 58-89 32469279-0 2022 Withanone and Withaferin-A are predicted to interact with transmembrane protease serine 2 (TMPRSS2) and block entry of SARS-CoV-2 into cells. withanone 0-9 transmembrane serine protease 2 Homo sapiens 91-98 32469279-0 2022 Withanone and Withaferin-A are predicted to interact with transmembrane protease serine 2 (TMPRSS2) and block entry of SARS-CoV-2 into cells. withaferin 14-24 transmembrane serine protease 2 Homo sapiens 58-89 32469279-0 2022 Withanone and Withaferin-A are predicted to interact with transmembrane protease serine 2 (TMPRSS2) and block entry of SARS-CoV-2 into cells. withaferin 14-24 transmembrane serine protease 2 Homo sapiens 91-98 32410502-2 2021 TMPRSS2 encodes a transmembrane serine protease which plays a crucial role in SARS-CoV-2 cell entry. Serine 32-38 transmembrane serine protease 2 Homo sapiens 0-7 32574272-5 2020 Host proteases, e.g., cathepsins, furin, or members of the type II transmembrane serine proteases (TTSP) family, such as Transmembrane protease serine 2 (TMPRSS2), are involved in virus entry by proteolytically activating virus ligands. Serine 81-87 transmembrane serine protease 2 Homo sapiens 121-152 32574272-5 2020 Host proteases, e.g., cathepsins, furin, or members of the type II transmembrane serine proteases (TTSP) family, such as Transmembrane protease serine 2 (TMPRSS2), are involved in virus entry by proteolytically activating virus ligands. Serine 81-87 transmembrane serine protease 2 Homo sapiens 154-161 32325025-3 2020 (Cell) identify ACE2 as a SARS-CoV-2 receptor, and the latter show its entry mechanism depends on cellular serine protease TMPRSS2. Serine 107-113 transmembrane serine protease 2 Homo sapiens 123-130 32572552-3 2020 The current body of evidence indicates that SARS-CoV-2 requires the membrane-bound angiotensin-converting enzyme 2 (ACE2) and the membrane-bound serine protease TMPRSS2 to enter cells. Serine 145-151 transmembrane serine protease 2 Homo sapiens 161-168 32360480-4 2020 Such drugs comprise inhibitors of TMPRSS2 serine protease and inhibitors of angiotensin-converting enzyme 2 (ACE2). Serine 42-48 transmembrane serine protease 2 Homo sapiens 34-41 32360584-0 2020 Possible use of the mucolytic drug, bromhexine hydrochloride, as a prophylactic agent against SARS-CoV-2 infection based on its action on the Transmembrane Serine Protease 2. Bromhexine 36-60 transmembrane serine protease 2 Homo sapiens 142-173 32595355-4 2020 One of the important SARS-CoV-2 targets namely type 2 transmembrane serine protease (TMPRSS2) was screened with NPC"s NIH small molecule library which includes approved drugs by FDA and compounds in clinical investigation. Serine 68-74 transmembrane serine protease 2 Homo sapiens 85-92 32595355-7 2020 Both binding energy results as well as crucial residues in ligand binding were also compared with a positive control TMPRSS2 inhibitor, Camostat mesylate. camostat 136-153 transmembrane serine protease 2 Homo sapiens 117-124 32595355-8 2020 Based on these numerical calculations we proposed a compound (benzquercin) as strong TMPRSS2 inhibitor. benzquercin 62-73 transmembrane serine protease 2 Homo sapiens 85-92 32595355-9 2020 If these results can be validated by in vitro and in vivo studies, benzquercin can be considered to be used as inhibitor of TMPRSS2 at the clinical studies. benzquercin 67-78 transmembrane serine protease 2 Homo sapiens 124-131 32595360-0 2020 Interaction of certain monoterpenoid hydrocarbons with the receptor binding domain of 2019 novel coronavirus (2019-nCoV), transmembrane serine protease 2 (TMPRSS2), cathepsin B, and cathepsin L (CatB/L) and their pharmacokinetic properties. monoterpenoid hydrocarbons 23-49 transmembrane serine protease 2 Homo sapiens 122-153 32595360-0 2020 Interaction of certain monoterpenoid hydrocarbons with the receptor binding domain of 2019 novel coronavirus (2019-nCoV), transmembrane serine protease 2 (TMPRSS2), cathepsin B, and cathepsin L (CatB/L) and their pharmacokinetic properties. monoterpenoid hydrocarbons 23-49 transmembrane serine protease 2 Homo sapiens 155-162 32595360-2 2020 The aim of this study was to investigate the molecular interactions between monoterpenoids and spike protein of 2019-nCoV together with the cellular proteases [transmembrane serine protease 2 (TMPRSS2), cathepsin B (CatB), and cathepsin L (CatL)]. Monoterpenes 76-90 transmembrane serine protease 2 Homo sapiens 160-191 32595360-2 2020 The aim of this study was to investigate the molecular interactions between monoterpenoids and spike protein of 2019-nCoV together with the cellular proteases [transmembrane serine protease 2 (TMPRSS2), cathepsin B (CatB), and cathepsin L (CatL)]. Monoterpenes 76-90 transmembrane serine protease 2 Homo sapiens 193-200 32545518-5 2020 We found that the potent Nrf2-activating composition PB125 downregulates ACE2 and TMPRSS2 mRNA expression in human liver-derived HepG2 cells. pb125 53-58 transmembrane serine protease 2 Homo sapiens 83-90 32532094-2 2020 We previously found that nafamostat mesylate, an existing drug used for disseminated intravascular coagulation (DIC), effectively blocked Middle East respiratory syndrome coronavirus (MERS-CoV) S protein-mediated cell fusion by targeting transmembrane serine protease 2 (TMPRSS2), and inhibited MERS-CoV infection of human lung epithelium-derived Calu-3 cells. nafamostat 25-35 transmembrane serine protease 2 Homo sapiens 238-269 32532094-2 2020 We previously found that nafamostat mesylate, an existing drug used for disseminated intravascular coagulation (DIC), effectively blocked Middle East respiratory syndrome coronavirus (MERS-CoV) S protein-mediated cell fusion by targeting transmembrane serine protease 2 (TMPRSS2), and inhibited MERS-CoV infection of human lung epithelium-derived Calu-3 cells. nafamostat 25-35 transmembrane serine protease 2 Homo sapiens 271-278 32532094-3 2020 Here we established a quantitative fusion assay dependent on severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) S protein, angiotensin I converting enzyme 2 (ACE2) and TMPRSS2, and found that nafamostat mesylate potently inhibited the fusion while camostat mesylate was about 10-fold less active. nafamostat 202-221 transmembrane serine protease 2 Homo sapiens 178-185 32582302-4 2020 The SARS-CoV-2 virus responsible for the infection depends on two human genes: the human receptor angiotensin converting enzyme 2 (ACE2) for cell invasion, and the serine protease TMPRSS2 for S protein priming. Serine 164-170 transmembrane serine protease 2 Homo sapiens 180-187 32276929-2 2020 The modulation of its expression by sex steroids could contribute to the male predominance of severe infections, and given that TMPRSS2 has no known indispensable functions, and inhibitors are available, it is an appealing target for prevention or treatment of respiratory viral infections. Steroids 40-48 transmembrane serine protease 2 Homo sapiens 128-135 32574273-12 2020 Finally, a direct effect of GL or GA to reduce virus transmission exists, which may involve reduced expression of type 2 transmembrane serine protease (TMPRSS2), which is required for virus uptake. Glycyrrhizic Acid 28-30 transmembrane serine protease 2 Homo sapiens 152-159 32574273-12 2020 Finally, a direct effect of GL or GA to reduce virus transmission exists, which may involve reduced expression of type 2 transmembrane serine protease (TMPRSS2), which is required for virus uptake. Glycyrrhetinic Acid 34-36 transmembrane serine protease 2 Homo sapiens 152-159 32574273-12 2020 Finally, a direct effect of GL or GA to reduce virus transmission exists, which may involve reduced expression of type 2 transmembrane serine protease (TMPRSS2), which is required for virus uptake. Serine 135-141 transmembrane serine protease 2 Homo sapiens 152-159 32313004-3 2020 The CDX and the derived-cell line conserve 16% of primary tumor (PT) and 56% of CTC mutations, as well as 83% of PT copy-number aberrations including clonal TMPRSS2-ERG fusion and NKX3.1 loss. Cefadroxil 4-7 transmembrane serine protease 2 Homo sapiens 157-164 32404436-4 2020 Expression of two mucosa-specific serine proteases, TMPRSS2 and TMPRSS4, facilitated SARS-CoV-2 spike fusogenic activity and promoted virus entry into host cells. Serine 34-40 transmembrane serine protease 2 Homo sapiens 52-59 32408547-0 2020 Virtual Screening of Natural Products against Type II Transmembrane Serine Protease (TMPRSS2), the Priming Agent of Coronavirus 2 (SARS-CoV-2). Serine 68-74 transmembrane serine protease 2 Homo sapiens 85-92 32408547-12 2020 The low-molecular-weight compound NPC306344 showed significant interaction with the active site residues of TMPRSS2, with a binding energy score of -14.69. npc306344 34-43 transmembrane serine protease 2 Homo sapiens 108-115 32376987-0 2020 Inhibition of Influenza A virus propagation by benzoselenoxanthenes stabilizing TMPRSS2 Gene G-quadruplex and hence down-regulating TMPRSS2 expression. benzoselenoxanthenes 47-67 transmembrane serine protease 2 Homo sapiens 80-87 32376987-0 2020 Inhibition of Influenza A virus propagation by benzoselenoxanthenes stabilizing TMPRSS2 Gene G-quadruplex and hence down-regulating TMPRSS2 expression. benzoselenoxanthenes 47-67 transmembrane serine protease 2 Homo sapiens 132-139 32376987-2 2020 The transmembrane serine protease TMPRSS2 was previously identified as the essential protease that can cleave hemagglutinin of many subtypes of influenza virus and spike protein of coronavirus. Serine 18-24 transmembrane serine protease 2 Homo sapiens 34-41 32376987-3 2020 Herein, we found that a guanine rich tract, capable of forming intramolecular G-quadruplex in the presence of potassium ions, in the promoter region of human TMPRSS2 gene was quite important for gene transcriptional activity, hence affecting its function. Guanine 24-31 transmembrane serine protease 2 Homo sapiens 158-165 32376987-3 2020 Herein, we found that a guanine rich tract, capable of forming intramolecular G-quadruplex in the presence of potassium ions, in the promoter region of human TMPRSS2 gene was quite important for gene transcriptional activity, hence affecting its function. Potassium 110-119 transmembrane serine protease 2 Homo sapiens 158-165 31871879-7 2019 The downstream targets of androgen receptors, such as PSA, TMPRSS2, and TMEPA1, were found decreased in the presence of kaempferol in qPCR data. Androgens 26-34 transmembrane serine protease 2 Homo sapiens 59-66 32219716-4 2020 Moreover, GA not only suppressed the expression of androgen target genes (TMPRSS2, PSA, and NKX3.1), but also enhanced the suppressive effect of anti-androgens (bicalutamide and flutamide) on LNCaP cell growth. 18alpha-glycyrrhetinic acid 10-12 transmembrane serine protease 2 Homo sapiens 74-81 31614005-0 2020 Targeting the TMPRSS2/ERG fusion mRNA using liposomal nanovectors enhances docetaxel treatment in prostate cancer. docetaxel 75-84 transmembrane serine protease 2 Homo sapiens 14-21 32142651-4 2020 Here, we demonstrate that SARS-CoV-2 uses the SARS-CoV receptor ACE2 for entry and the serine protease TMPRSS2 for S protein priming. Serine 87-93 transmembrane serine protease 2 Homo sapiens 103-110 32511288-2 2020 We have focused on identifying repurposing candidates for the transmembrane serine protease family member II (TMPRSS2), which is critical for entry of coronaviruses into cells. Serine 76-82 transmembrane serine protease 2 Homo sapiens 110-117 32985199-4 2020 SARS-CoV-2 has been shown to use the SARS-CoV receptor ACE2 for entry and serine protease TMPRSS2 for S protein priming. Serine 74-80 transmembrane serine protease 2 Homo sapiens 90-97 32661206-3 2020 Cellular receptor ACE2, serine protease TMPRSS2 and exopeptidase CD26 (also known as DPP4) are the three membrane bound proteins potentially implicated in SARS-CoV-2 infection. Serine 24-30 transmembrane serine protease 2 Homo sapiens 40-47 31871879-7 2019 The downstream targets of androgen receptors, such as PSA, TMPRSS2, and TMEPA1, were found decreased in the presence of kaempferol in qPCR data. Kaempferols 120-130 transmembrane serine protease 2 Homo sapiens 59-66 31638934-0 2019 TMPRSS2-ERG fusions confer efficacy of enzalutamide in an in vivo bone tumor growth model. enzalutamide 39-51 transmembrane serine protease 2 Homo sapiens 0-7 31638934-4 2019 We hypothesize that enzalutamide treatment will be more effective in cells/tumors with TMPRSS2-ERG translocations because these tumors have increased AR signaling. enzalutamide 20-32 transmembrane serine protease 2 Homo sapiens 87-94 30718921-0 2019 TMPRSS2-ERG activates NO-cGMP signaling in prostate cancer cells. Cyclic GMP 25-29 transmembrane serine protease 2 Homo sapiens 0-7 31391268-5 2019 Knockdown of TMPRSS2 expression was performed using a previously described antisense peptide-conjugated phosphorodiamidate morpholino oligomer, T-ex5, that interferes with splicing of TMPRSS2 pre-mRNA, resulting in the expression of enzymatically inactive TMPRSS2. DIAMIDOPHOSPHATE 104-122 transmembrane serine protease 2 Homo sapiens 13-20 31391268-5 2019 Knockdown of TMPRSS2 expression was performed using a previously described antisense peptide-conjugated phosphorodiamidate morpholino oligomer, T-ex5, that interferes with splicing of TMPRSS2 pre-mRNA, resulting in the expression of enzymatically inactive TMPRSS2. DIAMIDOPHOSPHATE 104-122 transmembrane serine protease 2 Homo sapiens 184-191 31391268-5 2019 Knockdown of TMPRSS2 expression was performed using a previously described antisense peptide-conjugated phosphorodiamidate morpholino oligomer, T-ex5, that interferes with splicing of TMPRSS2 pre-mRNA, resulting in the expression of enzymatically inactive TMPRSS2. DIAMIDOPHOSPHATE 104-122 transmembrane serine protease 2 Homo sapiens 184-191 30807643-0 2019 The influence of treatment sequence in the prognostic value of TMPRSS2-ERG as biomarker of taxane resistance in castration-resistant prostate cancer. taxane 91-97 transmembrane serine protease 2 Homo sapiens 63-70 30807643-1 2019 TMPRSS2-ERG expression in blood has been correlated with low docetaxel benefit in metastatic castration-resistant prostate cancer (mCRPC). Docetaxel 61-70 transmembrane serine protease 2 Homo sapiens 0-7 30807643-9 2019 In patients without prior A/E, blood and tumor TMPRSS2-ERG independently predicted lower PSA-PFS (HR 3.3, 95% CI 1.4-7.9 and HR 1.8, 95% CI 1.02-3.3, respectively) to taxanes. Taxoids 167-174 transmembrane serine protease 2 Homo sapiens 47-54 30718921-7 2019 This study strongly suggests that targeting NO-cGMP signaling pathways may be a novel therapeutic strategy to treat PCa with TMPRSS2-ERG gene fusion. Cyclic GMP 47-51 transmembrane serine protease 2 Homo sapiens 125-132 29773553-6 2018 TMPRSS2-ERG gene fusion status was also associated with an enhanced androgen-regulated gene expression, along with altered intratumoral androgen metabolism, demonstrated by reduced testosterone concentrations and increased DHT/testosterone ratios in TMPRSS2-ERG-positive tumors. Testosterone 181-193 transmembrane serine protease 2 Homo sapiens 0-7 30626688-1 2019 Transmembrane serine protease TMPRSS2 activates the spike protein of highly pathogenic human coronaviruses such as severe acute respiratory syndrome-related coronavirus (SARS-CoV) and Middle East respiratory syndrome-related coronavirus (MERS-CoV). Serine 14-20 transmembrane serine protease 2 Homo sapiens 30-37 30626688-10 2019 Transmembrane protease serine type 2 (TMPRSS2), a protease belonging to the type II transmembrane serine protease family, cleaves the coronavirus spike protein, making it a potential therapeutic target for coronavirus infections. Serine 23-29 transmembrane serine protease 2 Homo sapiens 38-45 30626688-10 2019 Transmembrane protease serine type 2 (TMPRSS2), a protease belonging to the type II transmembrane serine protease family, cleaves the coronavirus spike protein, making it a potential therapeutic target for coronavirus infections. Serine 98-104 transmembrane serine protease 2 Homo sapiens 38-45 30280407-12 2019 Riluzole also significantly inhibited AR transcription activity by decreasing its target genes expression (PSA, TMPRSS2, and KLK2). Riluzole 0-8 transmembrane serine protease 2 Homo sapiens 112-119 30254184-8 2018 Galiellalactone significantly reduced the expression of the AR target genes PSA (P < 0.001), TMPRSS2 (P < 0.001), and FKBP5 (P = 0.003) in benign tissue cultures (n = 24). galiellalactone 0-15 transmembrane serine protease 2 Homo sapiens 96-103 30413791-11 2018 These findings suggest that cleavage at S2" is carried out by proteases recognizing a single arginine, most likely TMPRSS2 and cathepsin L. Arginine 93-101 transmembrane serine protease 2 Homo sapiens 115-122 30260630-4 2018 Herein, we propose a "mix-to-go" colloidal strategy that utilizes the electrostatic attraction between negatively charged target sequences and positively charged silver nanoparticles (AgNPs) to induce aggregation of AgNPs to profile a panel of clinically validated urinary prostate cancer (PCa) RNA biomarkers ( TMPRSS2:ERG, T2:ERG; prostate cancer antigen 3, PCA3; and kallikrein-related peptidase 2, KLK2). Silver 162-168 transmembrane serine protease 2 Homo sapiens 312-319 30108097-0 2018 A Prospective Study of Aspirin Use and Prostate Cancer Risk by TMPRSS2:ERG Status. Aspirin 23-30 transmembrane serine protease 2 Homo sapiens 63-70 30108097-1 2018 Background: In a case-control study, aspirin use was associated with a lower risk of a common prostate cancer molecular subtype, the TMPRSS2:ERG gene fusion. Aspirin 37-44 transmembrane serine protease 2 Homo sapiens 133-140 29773553-6 2018 TMPRSS2-ERG gene fusion status was also associated with an enhanced androgen-regulated gene expression, along with altered intratumoral androgen metabolism, demonstrated by reduced testosterone concentrations and increased DHT/testosterone ratios in TMPRSS2-ERG-positive tumors. Dihydrotestosterone 223-226 transmembrane serine protease 2 Homo sapiens 0-7 29773553-6 2018 TMPRSS2-ERG gene fusion status was also associated with an enhanced androgen-regulated gene expression, along with altered intratumoral androgen metabolism, demonstrated by reduced testosterone concentrations and increased DHT/testosterone ratios in TMPRSS2-ERG-positive tumors. Dihydrotestosterone 223-226 transmembrane serine protease 2 Homo sapiens 250-257 29773553-6 2018 TMPRSS2-ERG gene fusion status was also associated with an enhanced androgen-regulated gene expression, along with altered intratumoral androgen metabolism, demonstrated by reduced testosterone concentrations and increased DHT/testosterone ratios in TMPRSS2-ERG-positive tumors. Testosterone 227-239 transmembrane serine protease 2 Homo sapiens 0-7 29773553-6 2018 TMPRSS2-ERG gene fusion status was also associated with an enhanced androgen-regulated gene expression, along with altered intratumoral androgen metabolism, demonstrated by reduced testosterone concentrations and increased DHT/testosterone ratios in TMPRSS2-ERG-positive tumors. Testosterone 227-239 transmembrane serine protease 2 Homo sapiens 250-257 29773553-7 2018 TMPRSS2-ERG-positive and -negative prostate cancer specimens have distinct intratumoral androgen profiles, possibly due to activation of testosterone-independent DHT biosynthesis via the alternative pathway in TMPRSS2-ERG-positive tumors. Testosterone 137-149 transmembrane serine protease 2 Homo sapiens 0-7 29773553-7 2018 TMPRSS2-ERG-positive and -negative prostate cancer specimens have distinct intratumoral androgen profiles, possibly due to activation of testosterone-independent DHT biosynthesis via the alternative pathway in TMPRSS2-ERG-positive tumors. Dihydrotestosterone 162-165 transmembrane serine protease 2 Homo sapiens 0-7 29773553-8 2018 Thus, patients with TMPRSS2-ERG-positive prostate cancer may benefit from novel inhibitors targeting the alternative DHT biosynthesis. Dihydrotestosterone 117-120 transmembrane serine protease 2 Homo sapiens 20-27 29217279-5 2018 These results suggest that circulating HCoVs in the field generally use cell-surface TMPRSS2 for cell entry, not endosomal cathepsins, in human airway epithelial cells. hcovs 39-44 transmembrane serine protease 2 Homo sapiens 85-92 29381490-5 2018 The 22Rv1 cell line responded to testosterone by increasing the nuclear entry of AR, AR-V7, and phosphorylated AR and by increasing the levels of prostate-specific antigen and TMPRSS2. Testosterone 33-45 transmembrane serine protease 2 Homo sapiens 176-183 29465803-6 2018 In contrast, we find that the TMPRSS2:ERG fusion-positive cell lines VCaP and DuCaP do not show signs of synthetic lethality, but are sensitive to cytotoxic effects caused by olaparib. olaparib 175-183 transmembrane serine protease 2 Homo sapiens 30-37 29285272-11 2017 Mechanism dissection suggest that baicalein can suppress AR target genes (PSA, TMPRSS2, and TMEPA1) expression in both androgen responsive LNCaP cells and castration resistant CWR22Rv1 cells, that may involve the inhibiting the AR N/C dimerization and AR-coactivators interaction. baicalein 34-43 transmembrane serine protease 2 Homo sapiens 79-86 29540675-5 2018 Over-expression of these MIR222HGs increased androgen-independent cell growth and repressed the expression of androgen receptor-regulated dihydrotestosterone (DHT)-induced KLK3, TMPRSS2, and FKBP5 in HSPC LNCaP cells, hallmarks of the CRPC phenotype. Dihydrotestosterone 138-157 transmembrane serine protease 2 Homo sapiens 178-185 29540675-5 2018 Over-expression of these MIR222HGs increased androgen-independent cell growth and repressed the expression of androgen receptor-regulated dihydrotestosterone (DHT)-induced KLK3, TMPRSS2, and FKBP5 in HSPC LNCaP cells, hallmarks of the CRPC phenotype. Dihydrotestosterone 159-162 transmembrane serine protease 2 Homo sapiens 178-185 28636671-6 2017 The cleavage fragments produced by trypsin and TMPRSS2 differed in their decoration with N-glycans, suggesting that these proteases cleave different SARS S glycoforms. n-glycans 89-98 transmembrane serine protease 2 Homo sapiens 47-54 28123608-5 2017 Here we show anti-proliferative activity of the newly described PIM1 inhibitor NMS-P645 in combination with the PI3K inhibitor GDC-0941 in TMPRSS2/ERG positive and negative PCa cells. 2-(1H-indazol-4-yl)-6-(4-methanesulfonylpiperazin-1-ylmethyl)-4-morpholin-4-ylthieno(3,2-d)pyrimidine 127-135 transmembrane serine protease 2 Homo sapiens 139-146 28652740-7 2017 Here, we propose to develop an assay for prostate cancer diagnosis using oligonucleotide-functionalized quantum dot and magnetic microparticle for optical detection of rearranged TMPRSS2-ERG fusion genes at a low concentration in urine. Oligonucleotides 73-88 transmembrane serine protease 2 Homo sapiens 179-186 28652740-9 2017 Here, we show detection of multiple TMPRSS2-ERG fusion genes using color-coded oligonucleotides in cell lysate and urine. Oligonucleotides 79-95 transmembrane serine protease 2 Homo sapiens 36-43 26948395-1 2016 TMPRSS2-ERG rearrangement is a genetic alteration exclusive to prostate cancer, associated with taxane resistance in preclinical models. taxane 96-102 transmembrane serine protease 2 Homo sapiens 0-7 27707886-5 2017 Furthermore, ABBV-075 disrupted DHT-stimulated recruitment of BET family member BRD4 to gene-regulatory regions cooccupied by AR, including the well-established PSA and TMPRSS2 enhancers. mivebresib 13-21 transmembrane serine protease 2 Homo sapiens 169-176 27707886-5 2017 Furthermore, ABBV-075 disrupted DHT-stimulated recruitment of BET family member BRD4 to gene-regulatory regions cooccupied by AR, including the well-established PSA and TMPRSS2 enhancers. Dihydrotestosterone 32-35 transmembrane serine protease 2 Homo sapiens 169-176 27707886-8 2017 ABBV-075 was also a potent inhibitor of MYC and the TMPRSS2-ETS fusion protein, important parallel transcription factor drivers of CRPC. mivebresib 0-8 transmembrane serine protease 2 Homo sapiens 52-59 27707886-9 2017 IMPLICATIONS: The ability of BET family inhibitor ABBV-075 to inhibit transcription activation downstream of the initiating events of transcription factors like AR and TMPRSS2:ETS fusion proteins provides a promising therapeutic option for CRPC patients who have developed resistance to second-generation antiandrogens. mivebresib 50-58 transmembrane serine protease 2 Homo sapiens 168-175 26948395-7 2016 Moreover, TMPRSS2-ERG also predicted low PSA-PFS to cabazitaxel. cabazitaxel 52-63 transmembrane serine protease 2 Homo sapiens 10-17 26948395-9 2016 Tissue TMPRSS2-ERG expression correlated with lower PSA-PFS (p=0.02) to docetaxel. Docetaxel 72-81 transmembrane serine protease 2 Homo sapiens 7-14 26948395-13 2016 In the present study we show that the detection of TMPRSS2-ERG in blood from metastatic resistant prostate cancer patients predicts resistance to docetaxel and it may be useful to select treatment and to avoid possible toxicities in refractory patients. Docetaxel 146-155 transmembrane serine protease 2 Homo sapiens 51-58 29345891-4 2016 Herein, we described a new strategy for non-invasive TMPRSS2-ERG detection in patient urinary samples by coupling of isothermal reverse transcription-recombinase polymerization amplification (RT-RPA) to amplify TMPRSS2-ERG transcripts and surface-enhanced Raman scattering (SERS) to directly detect the amplicons. sers 274-278 transmembrane serine protease 2 Homo sapiens 53-60 27342909-2 2016 Our aim was to analyze the dynamic modulation, determined by ADT, of the expression of selected genes involved in the pathogenesis and progression of prostate cancer (TMPRSS2:ERG, WNT11, SPINK1, CHGA, AR, and SPDEF) using real-time polymerase chain reaction in a series of 59 surgical samples of prostate carcinomas, including 37 cases preoperatively treated with ADT and 22 untreated cases, and in 43 corresponding biopsies. adt 61-64 transmembrane serine protease 2 Homo sapiens 167-174 27342909-2 2016 Our aim was to analyze the dynamic modulation, determined by ADT, of the expression of selected genes involved in the pathogenesis and progression of prostate cancer (TMPRSS2:ERG, WNT11, SPINK1, CHGA, AR, and SPDEF) using real-time polymerase chain reaction in a series of 59 surgical samples of prostate carcinomas, including 37 cases preoperatively treated with ADT and 22 untreated cases, and in 43 corresponding biopsies. adt 364-367 transmembrane serine protease 2 Homo sapiens 167-174 27342909-5 2016 The effect of ADT on CHGA gene up-modulation was almost exclusively detected in cases positive for the TMPRSS2:ERG fusion. adt 14-17 transmembrane serine protease 2 Homo sapiens 103-110 29345891-4 2016 Herein, we described a new strategy for non-invasive TMPRSS2-ERG detection in patient urinary samples by coupling of isothermal reverse transcription-recombinase polymerization amplification (RT-RPA) to amplify TMPRSS2-ERG transcripts and surface-enhanced Raman scattering (SERS) to directly detect the amplicons. sers 274-278 transmembrane serine protease 2 Homo sapiens 211-218 26935606-0 2016 Functional analysis of the TMPRSS2:ERG fusion gene in cisplatin-induced cell death. Cisplatin 54-63 transmembrane serine protease 2 Homo sapiens 27-34 26944919-8 2016 Moreover, expression of AR variant 7 (ARv7) and TMPRSS2-ERG fusion gene were greatly inhibited after combined treatment with AD and edelfosine in VCaP cells. edelfosine 132-142 transmembrane serine protease 2 Homo sapiens 48-55 26986253-9 2016 CONCLUSIONS: These findings provide some suggestive evidence that higher pre-diagnostic free testosterone levels are associated with an increased risk of developing TMPRSS2:ERG-positive prostate cancer. Testosterone 93-105 transmembrane serine protease 2 Homo sapiens 165-172 26935606-5 2016 By contrast, VCaP cells, which do contain TMPRSS2:ERG, were sensitized to cisplatin-induced apoptosis through siRNA inhibition of the fusion gene. Cisplatin 74-83 transmembrane serine protease 2 Homo sapiens 42-49 27023109-0 2016 Knocking Down TMPRSS2-ERG Fusion Oncogene by siRNA Could be an Alternative Treatment to Flutamide. Flutamide 88-97 transmembrane serine protease 2 Homo sapiens 14-21 27023109-4 2016 Therefore, concomitant or subsequent association of FLU to siRNA TMPRSS2-ERG was performed in VCaP cells and in SCID mice bearing xenografted VCaP tumors. Flutamide 52-55 transmembrane serine protease 2 Homo sapiens 65-72 26623558-6 2016 For the first time, the impact of the ERG translocation on the metabolome was demonstrated, highlighting an altered fatty acid oxidation in TMPRSS2-ERG translocation positive PCa specimens. Fatty Acids 116-126 transmembrane serine protease 2 Homo sapiens 140-147 26503111-0 2016 Aspirin and NSAID use in association with molecular subtypes of prostate cancer defined by TMPRSS2:ERG fusion status. Aspirin 0-7 transmembrane serine protease 2 Homo sapiens 91-98 25933120-7 2015 To propose a concrete therapeutic approach, siRNA TMPRSS2-ERG IV was conjugated to squalene, which can self-organize as nanoparticles in water. Squalene 83-91 transmembrane serine protease 2 Homo sapiens 50-57 26571387-2 2015 In VCaP cells, a human prostate cancer cell line overexpressing both AR and the TMPRSS2-ERG gene fusion, an androgen response element (ARE)-targeted Py-Im polyamide significantly downregulates AR driven gene expression. py-im 149-154 transmembrane serine protease 2 Homo sapiens 80-87 26571387-2 2015 In VCaP cells, a human prostate cancer cell line overexpressing both AR and the TMPRSS2-ERG gene fusion, an androgen response element (ARE)-targeted Py-Im polyamide significantly downregulates AR driven gene expression. Nylons 155-164 transmembrane serine protease 2 Homo sapiens 80-87 26095298-5 2015 Most influenza virus strains contain a HA sequence with a single arginine at the cleavage site suitable for processing by the trypsin-like serine proteases human airway trypsin-like protease (HAT) and transmembrane protease serine 2 (TMPRSS2), albeit a minority of viruses possesses HA cleavage site motifs that are processed by other proteases. Arginine 65-73 transmembrane serine protease 2 Homo sapiens 201-232 25728532-2 2015 We hypothesized that men with TMPRSS2:ERG positive tumors are more responsive to androgen deprivation therapy (ADT). adt 111-114 transmembrane serine protease 2 Homo sapiens 30-37 25728532-10 2015 CONCLUSIONS: Our results, combined with those from earlier studies, provide suggestive evidence that men with TMPRSS2:ERG positive tumors may have longer prostate cancer survival after ADT. adt 185-188 transmembrane serine protease 2 Homo sapiens 110-117 25933120-7 2015 To propose a concrete therapeutic approach, siRNA TMPRSS2-ERG IV was conjugated to squalene, which can self-organize as nanoparticles in water. Water 137-142 transmembrane serine protease 2 Homo sapiens 50-57 25933120-9 2015 In conclusion, this study offers a new prospect of treatment for prostate cancer based on siRNA-squalene nanoparticles targeting TMPRSS2-ERG junction oncogene. Squalene 96-104 transmembrane serine protease 2 Homo sapiens 129-136 25088707-0 2014 Pyrrole-imidazole polyamide targeted to break fusion sites in TMPRSS2 and ERG gene fusion represses prostate tumor growth. N-[5-[[4-[[5-[[5-[[5-[[5-[[3-[3-(Dimethylamino)propylamino]-3-Oxidanylidene-Propyl]carbamoyl]-1-Methyl-Pyrrol-3-Yl]carbamoyl]-1-Methyl-Pyrrol-3-Yl]carbamoyl]-1-Methyl-Pyrrol-3-Yl]carbamoyl]-1-Methyl-Pyrrol-3-Yl]amino]-4-Oxidanylidene-Butyl]carbamoyl]-1-Methyl-Pyrrol-3-Yl]-1-Methyl-4-[[1-Methyl-4-[(1-Methylimidazol-2-Yl)carbonylamino]pyrrol-2-Yl]carbonylamino]imidazole-2-Carboxamide 0-27 transmembrane serine protease 2 Homo sapiens 62-69 25088707-3 2014 In the present study, we designed a PI polyamide targeting TMPRSS2-ERG translocation breakpoints and assessed its effect on human prostate cancer cells. pi polyamide 36-48 transmembrane serine protease 2 Homo sapiens 59-66 24926821-10 2014 Our findings suggest that patients with TMPRSS2:ETS negative tumors may be more responsive to VDR-mediated growth inhibition and that TMPRSS2:ETS status should be considered in future clinical trials. ets 48-51 transmembrane serine protease 2 Homo sapiens 40-47 25266362-6 2014 Three peptides, shared across almost all fusion protein products, were determined to be the most abundant peptides, providing "signature" peptides for detection of ERG over-expression resulting from TMPRSS2-ERG gene fusion. Peptides 6-14 transmembrane serine protease 2 Homo sapiens 199-206 24926821-2 2014 The majority of human PCas express a transmembrane protease serine 2 (TMPRSS2):erythroblast transformation-specific (ETS) fusion gene, but most preclinical studies have been performed in PCa models lacking TMPRSS2:ETS in part due to the limited availability of model systems expressing endogenous TMPRSS2:ETS. ets 214-217 transmembrane serine protease 2 Homo sapiens 70-77 24926821-10 2014 Our findings suggest that patients with TMPRSS2:ETS negative tumors may be more responsive to VDR-mediated growth inhibition and that TMPRSS2:ETS status should be considered in future clinical trials. ets 142-145 transmembrane serine protease 2 Homo sapiens 134-141 24926821-5 2014 In TMPRSS2:ETS positive VCaP cells, depletion of TMPRSS2:ETS substantially reduced 1,25D-mediated CYP24A1 induction. ets 11-14 transmembrane serine protease 2 Homo sapiens 3-10 24505269-5 2014 Novel associations between TMPRSS2-ERG and alterations in the tumor stroma, for example, increased vascular density, hyaluronan and PDGFRbeta and decreased Caveolin-1, all known to be associated with an aggressive disease, were found. Hyaluronic Acid 117-127 transmembrane serine protease 2 Homo sapiens 27-34 24926821-5 2014 In TMPRSS2:ETS positive VCaP cells, depletion of TMPRSS2:ETS substantially reduced 1,25D-mediated CYP24A1 induction. ets 11-14 transmembrane serine protease 2 Homo sapiens 49-56 24926821-5 2014 In TMPRSS2:ETS positive VCaP cells, depletion of TMPRSS2:ETS substantially reduced 1,25D-mediated CYP24A1 induction. ets 57-60 transmembrane serine protease 2 Homo sapiens 3-10 24926821-5 2014 In TMPRSS2:ETS positive VCaP cells, depletion of TMPRSS2:ETS substantially reduced 1,25D-mediated CYP24A1 induction. ets 57-60 transmembrane serine protease 2 Homo sapiens 49-56 24926821-6 2014 Artificial expression of the type VI+72 TMPRSS2:ETS isoform in LNCaP cells synergized with 1,25D to greatly increase CYP24A1 expression. ets 48-51 transmembrane serine protease 2 Homo sapiens 40-47 25043536-0 2014 KLK3, PCA3, and TMPRSS2-ERG expression in the peripheral blood mononuclear cell fraction from castration-resistant prostate cancer patients and response to docetaxel treatment. Docetaxel 156-165 transmembrane serine protease 2 Homo sapiens 16-23 24764242-8 2014 Treatment with the DNA methylation inhibitor 5-Aza-2"-deoxycytidine reversed the low expression levels of TMPRSS2 in the AR-negative PCa cells. Decitabine 45-67 transmembrane serine protease 2 Homo sapiens 106-113 24600012-3 2014 The type II transmembrane serine protease TMPRSS2 is expressed in the respiratory tract and is capable of activating a variety of respiratory viruses, including low-pathogenic (LP) IAVs possessing a single arginine residue at the cleavage site. Arginine 206-214 transmembrane serine protease 2 Homo sapiens 42-49 24527392-3 2014 Here, we show that retinoic acid (RA) regulates early human prostate epithelial differentiation by activating a tightly coexpressed set of 80 genes (e.g., TMPRSS2). Tretinoin 19-32 transmembrane serine protease 2 Homo sapiens 155-162 24527392-3 2014 Here, we show that retinoic acid (RA) regulates early human prostate epithelial differentiation by activating a tightly coexpressed set of 80 genes (e.g., TMPRSS2). Tretinoin 34-36 transmembrane serine protease 2 Homo sapiens 155-162 25043536-9 2014 In response to docetaxel treatment, KLK3 levels decreased in 80% (95% CI 60-100%), PCA3 in 89% (95% CI 68-100%), and TMPRSS2-ERG in 86% (95% CI 60-100%) of patients. Docetaxel 15-24 transmembrane serine protease 2 Homo sapiens 117-124 24824408-1 2014 OBJECTIVE: To investigate the association between the length of the polymorphic trinucleotide CAG microsatellite repeats in exon 1 of the AR gene and the risk of prostate cancer containing TMPRSS2:ETS fusion genes. trinucleotide 80-93 transmembrane serine protease 2 Homo sapiens 189-196 23395110-5 2013 The acyclic urea that exhibited the strongest effect on the inhibition of the PRMT1 activity also showed the greatest effect on the expression of some androgen receptor target genes (TMPRSS2 and FKBP5), which may be related with its enzymatic activity. Urea 12-16 transmembrane serine protease 2 Homo sapiens 183-190 24227843-4 2014 Here, we show that arginine and lysine residues within ACE2 amino acids 697 to 716 are essential for cleavage by TMPRSS2 and HAT and that ACE2 processing is required for augmentation of SARS-S-driven entry by these proteases. Arginine 19-27 transmembrane serine protease 2 Homo sapiens 113-120 24227843-4 2014 Here, we show that arginine and lysine residues within ACE2 amino acids 697 to 716 are essential for cleavage by TMPRSS2 and HAT and that ACE2 processing is required for augmentation of SARS-S-driven entry by these proteases. Lysine 32-38 transmembrane serine protease 2 Homo sapiens 113-120 24227843-6 2014 Expression of TMPRSS2 increased cellular uptake of soluble SARS-S, suggesting that protease-dependent augmentation of viral entry might be due to increased uptake of virions into target cells. sars-s 59-65 transmembrane serine protease 2 Homo sapiens 14-21 24227843-7 2014 Finally, TMPRSS2 was found to compete with the metalloprotease ADAM17 for ACE2 processing, but only cleavage by TMPRSS2 resulted in augmented SARS-S-driven entry. sars-s 142-148 transmembrane serine protease 2 Homo sapiens 112-119 23527573-10 2013 On the basis of the inhibitor studies, a series of new fluorogenic substrates containing a D-arginine residue at the P3 position was synthesized, some of them were efficiently cleaved by TMPRSS2. D-Arginine 91-101 transmembrane serine protease 2 Homo sapiens 187-194 23192983-4 2013 Here we show that 15-deoxy-Delta(12,14)-prostaglandin J(2) (15d-PGJ(2)), an endogenously produced antiinflammatory prostaglandin, targets the AR and acts as a potent AR inhibitor, rapidly repressing AR target genes, such as FKBP51 and TMPRSS2 in prostate cancer cells. 15-deoxy-delta(12,14)-prostaglandin j 18-55 transmembrane serine protease 2 Homo sapiens 235-242 23192983-4 2013 Here we show that 15-deoxy-Delta(12,14)-prostaglandin J(2) (15d-PGJ(2)), an endogenously produced antiinflammatory prostaglandin, targets the AR and acts as a potent AR inhibitor, rapidly repressing AR target genes, such as FKBP51 and TMPRSS2 in prostate cancer cells. Prostaglandins 40-53 transmembrane serine protease 2 Homo sapiens 235-242 23192983-7 2013 Chromatin immunoprecipitation assays indicate that the inhibitory effect of 15d-PGJ(2) on FKBP51 and TMPRSS2 expression occurs in parallel with the inhibition of the AR binding to the regulatory regions of these genes. 15d-pgj 76-83 transmembrane serine protease 2 Homo sapiens 101-108 23399562-5 2013 Fenofibrate induces cell cycle arrest in G1 phase and apoptosis in LNCaP cells, reduces the expressions of androgen receptor (AR) and AR target genes (prostate-specific antigen and TMPRSS2), and inhibits Akt phosphorylation. Fenofibrate 0-11 transmembrane serine protease 2 Homo sapiens 181-188 23192983-4 2013 Here we show that 15-deoxy-Delta(12,14)-prostaglandin J(2) (15d-PGJ(2)), an endogenously produced antiinflammatory prostaglandin, targets the AR and acts as a potent AR inhibitor, rapidly repressing AR target genes, such as FKBP51 and TMPRSS2 in prostate cancer cells. -pgj 63-67 transmembrane serine protease 2 Homo sapiens 235-242 22415461-5 2012 We tested the effect of dutasteride, a 5alpha-reductase inhibitor, in TMPRSS2-ERG fusion-positive VCaP cell proliferation and cell invasion. Dutasteride 24-35 transmembrane serine protease 2 Homo sapiens 70-77 23565244-9 2013 VCaP cells, which harbor the TMPRSS2-ERG gene fusion and PC3 cells that stably express a similar construct (fusion III) showed enhanced sensitivity towards rucaparib, which, in turn, increased the radiation response to a similar extent as the DNA-PKcs inhibitor NU7441. rucaparib 156-165 transmembrane serine protease 2 Homo sapiens 29-36 23554889-0 2013 Celastrol suppresses tumor cell growth through targeting an AR-ERG-NF-kappaB pathway in TMPRSS2/ERG fusion gene expressing prostate cancer. celastrol 0-9 transmembrane serine protease 2 Homo sapiens 88-95 23072892-5 2012 We further demonstrate that benzylsulfonyl-d-arginine-proline-4-amidinobenzylamide (BAPA), which is a potent inhibitor of HAT and TMPRSS2, efficiently suppresses virus propagation in TMPRSS2-expressing human airway epithelial cells by inhibition of HA cleavage. benzylsulfonyl-d-arginine-proline-4-amidinobenzylamide 28-82 transmembrane serine protease 2 Homo sapiens 130-137 23072892-5 2012 We further demonstrate that benzylsulfonyl-d-arginine-proline-4-amidinobenzylamide (BAPA), which is a potent inhibitor of HAT and TMPRSS2, efficiently suppresses virus propagation in TMPRSS2-expressing human airway epithelial cells by inhibition of HA cleavage. benzylsulfonyl-d-arginine-proline-4-amidinobenzylamide 28-82 transmembrane serine protease 2 Homo sapiens 183-190 23072892-5 2012 We further demonstrate that benzylsulfonyl-d-arginine-proline-4-amidinobenzylamide (BAPA), which is a potent inhibitor of HAT and TMPRSS2, efficiently suppresses virus propagation in TMPRSS2-expressing human airway epithelial cells by inhibition of HA cleavage. 2,5-bis(3-oxobutanoylamino)benzenesulfonic acid 84-88 transmembrane serine protease 2 Homo sapiens 130-137 23072892-5 2012 We further demonstrate that benzylsulfonyl-d-arginine-proline-4-amidinobenzylamide (BAPA), which is a potent inhibitor of HAT and TMPRSS2, efficiently suppresses virus propagation in TMPRSS2-expressing human airway epithelial cells by inhibition of HA cleavage. 2,5-bis(3-oxobutanoylamino)benzenesulfonic acid 84-88 transmembrane serine protease 2 Homo sapiens 183-190 22415461-6 2012 We also evaluated the effect of dutasteride on the TMPRSS2-ERG fusion gene expression. Dutasteride 32-43 transmembrane serine protease 2 Homo sapiens 51-58 22558251-3 2012 Here, we show that both HAT and TMPRSS2 are coexpressed with 2,6-linked sialic acids, the major receptor determinant of human influenza viruses, throughout the human respiratory tract. 2,6-linked sialic acids 61-84 transmembrane serine protease 2 Homo sapiens 32-39 22212979-8 2012 RESULTS: Upon stimulation with 1 nM DHT, AR and RNA Pol II were recruited onto PSA and TMPRSS2 enhancer regions to a greater extent (P < 0.05) in AR-overexpressing cells compared to control cells. Dihydrotestosterone 36-39 transmembrane serine protease 2 Homo sapiens 87-94 23251544-2 2012 Our recent results from a systematic chemical biology sensitivity screen covering most known drugs and drug-like molecules indicated that aldehyde dehydrogenase inhibitor disulfiram is one of the most potent cancer-specific inhibitors of prostate cancer cell growth, including TMPRSS2-ERG fusion positive cancers. Disulfiram 171-181 transmembrane serine protease 2 Homo sapiens 277-284 23251544-4 2012 METHODS AND FINDINGS: In this study, we utilized a chemical biology drug sensitivity screen to explore disulfiram mechanistic details and to identify compounds potentiating the effect of disulfiram in TMPRSS2-ERG fusion positive prostate cancer cells. Disulfiram 187-197 transmembrane serine protease 2 Homo sapiens 201-208 22313860-5 2012 Embedded in this study was peripheral blood sampling for TMPRSS2-ERG and SPINK1, two genes that are believed to define prostate cancer genotypes, to assess their utility as biomarkers This study suggests that at the delivered doses, cytarabine has limited efficacy and significant myelotoxicity suggesting, it does not have a role in the treatment of docetaxel-refractory CRPC. Cytarabine 233-243 transmembrane serine protease 2 Homo sapiens 57-64 22154085-5 2012 Furthermore, our data indicated that CTS could modulate AR transactivation and suppress the DHT-mediated AR target genes (PSA, TMPRSS2, and TMEPA1) expression in both androgen responsive PCa LNCaP cells and castration resistant CWR22rv1 cells. cryptotanshinone 37-40 transmembrane serine protease 2 Homo sapiens 127-134 22154085-5 2012 Furthermore, our data indicated that CTS could modulate AR transactivation and suppress the DHT-mediated AR target genes (PSA, TMPRSS2, and TMEPA1) expression in both androgen responsive PCa LNCaP cells and castration resistant CWR22rv1 cells. Dihydrotestosterone 92-95 transmembrane serine protease 2 Homo sapiens 127-134 21394739-8 2011 RESULTS: Expression of the TMPRSS2/ERG fusions in PC3 cells increased radiation sensitivity and decreased paclitaxel sensitivity. Paclitaxel 106-116 transmembrane serine protease 2 Homo sapiens 27-34 21802835-0 2011 TMPRSS2-ERG status in circulating tumor cells as a predictive biomarker of sensitivity in castration-resistant prostate cancer patients treated with abiraterone acetate. Abiraterone Acetate 149-168 transmembrane serine protease 2 Homo sapiens 0-7 21802835-6 2011 MEASUREMENTS: TMPRSS2-ERG status was characterized by a sensitive, analytically valid reverse transcription polymerase chain reaction assay in CTCs enriched from ethylene-diaminetetraacetic acid anticoagulated blood obtained prior to AA treatment. Edetic Acid 162-194 transmembrane serine protease 2 Homo sapiens 14-21 21178489-4 2011 This study suggests that ERG activation plays a role in prostaglandin signaling because knockdown of ERG expression in TMPRSS2-ERG fusion containing CaP cells leads to altered levels of the 15-hydroxy-prostaglandin dehydrogenase (HPGD), a tumor suppressor and prostaglandin catabolizing enzyme, and prostaglandin E2 (PGE2) . Prostaglandins 56-69 transmembrane serine protease 2 Homo sapiens 119-126 21178489-4 2011 This study suggests that ERG activation plays a role in prostaglandin signaling because knockdown of ERG expression in TMPRSS2-ERG fusion containing CaP cells leads to altered levels of the 15-hydroxy-prostaglandin dehydrogenase (HPGD), a tumor suppressor and prostaglandin catabolizing enzyme, and prostaglandin E2 (PGE2) . Dinoprostone 317-321 transmembrane serine protease 2 Homo sapiens 119-126 21519790-11 2011 We found that VPA and TSA induce apoptosis, upregulate p21/Waf1/CIP1, repress TMPRSS2-ERG expression and affect acetylation status of p53 in VCaP cells. Valproic Acid 14-17 transmembrane serine protease 2 Homo sapiens 78-85 21519790-11 2011 We found that VPA and TSA induce apoptosis, upregulate p21/Waf1/CIP1, repress TMPRSS2-ERG expression and affect acetylation status of p53 in VCaP cells. trichostatin A 22-25 transmembrane serine protease 2 Homo sapiens 78-85 21178489-4 2011 This study suggests that ERG activation plays a role in prostaglandin signaling because knockdown of ERG expression in TMPRSS2-ERG fusion containing CaP cells leads to altered levels of the 15-hydroxy-prostaglandin dehydrogenase (HPGD), a tumor suppressor and prostaglandin catabolizing enzyme, and prostaglandin E2 (PGE2) . Prostaglandins 201-214 transmembrane serine protease 2 Homo sapiens 119-126 21178489-4 2011 This study suggests that ERG activation plays a role in prostaglandin signaling because knockdown of ERG expression in TMPRSS2-ERG fusion containing CaP cells leads to altered levels of the 15-hydroxy-prostaglandin dehydrogenase (HPGD), a tumor suppressor and prostaglandin catabolizing enzyme, and prostaglandin E2 (PGE2) . Dinoprostone 299-315 transmembrane serine protease 2 Homo sapiens 119-126 29147215-9 2010 LNCaP cell lines were analyzed for the effect of EGCG and SB on the expression profile of TMPRSS2-ERG. epigallocatechin gallate 49-53 transmembrane serine protease 2 Homo sapiens 90-97 29147215-9 2010 LNCaP cell lines were analyzed for the effect of EGCG and SB on the expression profile of TMPRSS2-ERG. Silybin 58-60 transmembrane serine protease 2 Homo sapiens 90-97 20736744-11 2010 The TMPRSS2 dual-color break-apart FISH probe cocktail provides a simple and reliable method for the detection of TMPRSS2-related genetic alterations in formalin-fixed paraffin-embedded tissue. Formaldehyde 153-161 transmembrane serine protease 2 Homo sapiens 4-11 20631123-7 2010 Finally, TMPRSS2 was found to be coexpressed with the major receptor determinant of human influenza viruses, 2,6-linked sialic acids, in human alveolar epithelium, indicating that viral target cells in the human respiratory tract express TMPRSS2. 2,6-linked sialic acids 109-132 transmembrane serine protease 2 Homo sapiens 9-16 20631123-7 2010 Finally, TMPRSS2 was found to be coexpressed with the major receptor determinant of human influenza viruses, 2,6-linked sialic acids, in human alveolar epithelium, indicating that viral target cells in the human respiratory tract express TMPRSS2. 2,6-linked sialic acids 109-132 transmembrane serine protease 2 Homo sapiens 238-245 20736744-11 2010 The TMPRSS2 dual-color break-apart FISH probe cocktail provides a simple and reliable method for the detection of TMPRSS2-related genetic alterations in formalin-fixed paraffin-embedded tissue. Formaldehyde 153-161 transmembrane serine protease 2 Homo sapiens 114-121 20736744-11 2010 The TMPRSS2 dual-color break-apart FISH probe cocktail provides a simple and reliable method for the detection of TMPRSS2-related genetic alterations in formalin-fixed paraffin-embedded tissue. Paraffin 168-176 transmembrane serine protease 2 Homo sapiens 4-11 20736744-11 2010 The TMPRSS2 dual-color break-apart FISH probe cocktail provides a simple and reliable method for the detection of TMPRSS2-related genetic alterations in formalin-fixed paraffin-embedded tissue. Paraffin 168-176 transmembrane serine protease 2 Homo sapiens 114-121 19293179-3 2009 TMPRSS2-ERG, TMPRSS2-ETV1, and SLC45A3-ERG rearrangements account for roughly 90% of ETS fusion prostate cancer. ets 85-88 transmembrane serine protease 2 Homo sapiens 0-7 20616363-0 2010 Detection of TMPRSS2-ETS fusions by a multiprobe fluorescence in situ hybridization assay for the early diagnosis of prostate cancer: a pilot study. ets 21-24 transmembrane serine protease 2 Homo sapiens 13-20 20601956-3 2010 We show that androgen signaling promotes co-recruitment of androgen receptor and topoisomerase II beta (TOP2B) to sites of TMPRSS2-ERG genomic breakpoints, triggering recombinogenic TOP2B-mediated DSBs. dsbs 197-201 transmembrane serine protease 2 Homo sapiens 123-130 19584279-1 2009 It seems clear that androgen receptor (AR)-regulated expression of the TMPRSS2:ERG fusion gene plays an early role in prostate cancer (PC) development or progression, but the extent to which TMPRSS2:ERG is down-regulated in response to androgen deprivation therapy (ADT) and whether AR reactivates TMPRSS2:ERG expression in castration-resistant PC (CRPC) have not been determined. adt 266-269 transmembrane serine protease 2 Homo sapiens 191-198 19584279-1 2009 It seems clear that androgen receptor (AR)-regulated expression of the TMPRSS2:ERG fusion gene plays an early role in prostate cancer (PC) development or progression, but the extent to which TMPRSS2:ERG is down-regulated in response to androgen deprivation therapy (ADT) and whether AR reactivates TMPRSS2:ERG expression in castration-resistant PC (CRPC) have not been determined. adt 266-269 transmembrane serine protease 2 Homo sapiens 191-198 19584279-3 2009 To further assess whether TMPRSS2:ERG expression is initially down-regulated in response to ADT, we examined VCaP cells, which express the TMPRSS2:ERG fusion gene, and xenografts. adt 92-95 transmembrane serine protease 2 Homo sapiens 26-33 19339269-4 2009 Here, we collected blood every month from 89 patients (54 chemotherapy-naive patients and 35 docetaxel-treated patients) treated in phase I/phase II clinical trials of an orally available, highly specific CYP17 inhibitor, abiraterone acetate, that ablates the synthesis of androgens and estrogens that drive TMPRSS2-ERG fusions. Abiraterone Acetate 222-241 transmembrane serine protease 2 Homo sapiens 308-315 20382709-5 2010 In both LNCaP prostate cancer cells and human semen, TMPRSS2 protein was detected predominantly as inactive zymogen forms as part of an array of multiple noncovalent and disulfide-linked complexes, suggesting that TMPRSS2 activity may be regulated by unconventional mechanisms. Disulfides 170-179 transmembrane serine protease 2 Homo sapiens 53-60 20147525-0 2010 1{alpha},25-Dihydroxyvitamin D3 inhibits growth of VCaP prostate cancer cells despite inducing the growth-promoting TMPRSS2:ERG gene fusion. Calcitriol 0-31 transmembrane serine protease 2 Homo sapiens 116-123 20147525-4 2010 Here we show that the natural VDR agonist 1alpha,25-dihydroxyvitamin D(3) and its synthetic analog EB1089 increase expression of TMPRSS2:ERG mRNA in VCaP prostate cancer cells; this results in increased ETS-related gene (ERG) protein expression and ERG activity as demonstrated by an increase in the ERG target gene CACNA1D. 1,25-dihydroxyvitamin D 42-70 transmembrane serine protease 2 Homo sapiens 129-136 20124490-6 2010 The higher-dose dutasteride treatment group was found to include significantly fewer cancers with TMPRSS2-ERG genetic fusions. Dutasteride 16-27 transmembrane serine protease 2 Homo sapiens 98-105 19293179-3 2009 TMPRSS2-ERG, TMPRSS2-ETV1, and SLC45A3-ERG rearrangements account for roughly 90% of ETS fusion prostate cancer. ets 85-88 transmembrane serine protease 2 Homo sapiens 13-20 11741986-7 2002 The sequence of the protease domain carried the essential triad His, Asp, and Ser and showed some similarity to that of TMPRSS2, hepsin, HAT, MT-SP1, TMPRSS3, and corin, sharing 45.5, 41.9, 41.3, 40.3, 39.1, and 38.5% identity, respectively. Histidine 64-67 transmembrane serine protease 2 Homo sapiens 120-127 18474293-0 2008 Detection of the TMPRSS2-ETS fusion gene in prostate carcinomas: retrospective analysis of 55 formalin-fixed and paraffin-embedded samples with clinical data. Formaldehyde 94-102 transmembrane serine protease 2 Homo sapiens 17-24 18474293-0 2008 Detection of the TMPRSS2-ETS fusion gene in prostate carcinomas: retrospective analysis of 55 formalin-fixed and paraffin-embedded samples with clinical data. Paraffin 113-121 transmembrane serine protease 2 Homo sapiens 17-24 15537383-8 2005 Treatment of LNCaP cells with the cellular immunopurified TMPRSS2 protease induced a transient increase in intracellular calcium, which is indicative of G-protein-coupled-receptor activation. Calcium 121-128 transmembrane serine protease 2 Homo sapiens 58-65 12711008-6 2003 After stimulation of cells by DHT (10nM), synthetic androgen R1881 (1 nM), or organic pesticides (difenoconazole, fentinacetate, tetramethrin) TMPRSS2 mRNA expression was down-regulated by the factor 0.6 after 24h of DHT treatment. difenoconazole 98-112 transmembrane serine protease 2 Homo sapiens 143-150 12711008-6 2003 After stimulation of cells by DHT (10nM), synthetic androgen R1881 (1 nM), or organic pesticides (difenoconazole, fentinacetate, tetramethrin) TMPRSS2 mRNA expression was down-regulated by the factor 0.6 after 24h of DHT treatment. phentin acetate 114-127 transmembrane serine protease 2 Homo sapiens 143-150 12711008-6 2003 After stimulation of cells by DHT (10nM), synthetic androgen R1881 (1 nM), or organic pesticides (difenoconazole, fentinacetate, tetramethrin) TMPRSS2 mRNA expression was down-regulated by the factor 0.6 after 24h of DHT treatment. tetramethrin 129-141 transmembrane serine protease 2 Homo sapiens 143-150 12711008-6 2003 After stimulation of cells by DHT (10nM), synthetic androgen R1881 (1 nM), or organic pesticides (difenoconazole, fentinacetate, tetramethrin) TMPRSS2 mRNA expression was down-regulated by the factor 0.6 after 24h of DHT treatment. Dihydrotestosterone 217-220 transmembrane serine protease 2 Homo sapiens 143-150 12711008-8 2003 In contrast, TMPRSS2 expression was up-regulated by the factor 0.9 when cells were stimulated by tetramethrin. tetramethrin 97-109 transmembrane serine protease 2 Homo sapiens 13-20 18719366-6 2008 Of note, curcumin downregulated transcript encoded by the potentially causal TMPRSS2-ERG gene fusion, a common oncogenic alteration noted in 50-70% of prostate cancer patients. Curcumin 9-17 transmembrane serine protease 2 Homo sapiens 77-84 18471784-7 2008 On the other hand, inhibition of UGT2B115/17 expression by small interfering RNA (siRNA) resulted in an induced response to DHT of androgen-receptor target genes such as PSA, KLK4, NKX3.1, TMPRSS2, SLC16A6 and VEGF. Dihydrotestosterone 124-127 transmembrane serine protease 2 Homo sapiens 189-196 15537383-9 2005 This calcium mobilization was inhibited by cellular pre-treatment with a specific PAR-2 antagonist, but not with a PAR-1 antagonist; inhibition of the protease activity also failed to mobilize calcium, suggesting that TMPRSS2 is capable of cleaving and thereby activating the PAR-2 receptor. Calcium 5-12 transmembrane serine protease 2 Homo sapiens 218-225 11741986-7 2002 The sequence of the protease domain carried the essential triad His, Asp, and Ser and showed some similarity to that of TMPRSS2, hepsin, HAT, MT-SP1, TMPRSS3, and corin, sharing 45.5, 41.9, 41.3, 40.3, 39.1, and 38.5% identity, respectively. Aspartic Acid 69-72 transmembrane serine protease 2 Homo sapiens 120-127 11741986-7 2002 The sequence of the protease domain carried the essential triad His, Asp, and Ser and showed some similarity to that of TMPRSS2, hepsin, HAT, MT-SP1, TMPRSS3, and corin, sharing 45.5, 41.9, 41.3, 40.3, 39.1, and 38.5% identity, respectively. Serine 78-81 transmembrane serine protease 2 Homo sapiens 120-127 11745466-7 2001 Mutations in the TMPRSS2 gene were screened using DNA isolated from paraffin-embedded prostate cancer tissues from 9 patients with aggressive prostate cancer and from 9 patients with nonaggressive disease. Paraffin 68-76 transmembrane serine protease 2 Homo sapiens 17-24 33972944-4 2021 Attractive pharmacological targets to impede viral entry include type-II transmembrane serine proteases (TTSPs), such as TMPRSS2, whose essential role in the virus lifecycle is responsible for the cleavage and priming of the viral spike protein 5-7 . Serine 87-93 transmembrane serine protease 2 Homo sapiens 121-128 33972944-5 2021 Here, we identify and characterize a small-molecule compound, N-0385, as the most potent inhibitor of TMPRSS2 reported to date. Ms-QFR-Kbt 62-68 transmembrane serine protease 2 Homo sapiens 102-109 33817867-4 2021 This brief opinion critically discusses the potential of Silymarin, a flavonolignan with diverse pharmacological activity having antiinflammatory, antioxidant, antiplatelet, and antiviral properties, with versatile immune-cytokine regulatory functions, that able to bind with transmembrane protease serine 2 (TMPRSS2) and induce endogenous antiviral cytokine interferon-stimulated gene 15, for the management of COVID-19. Silymarin 57-66 transmembrane serine protease 2 Homo sapiens 276-307 33817867-4 2021 This brief opinion critically discusses the potential of Silymarin, a flavonolignan with diverse pharmacological activity having antiinflammatory, antioxidant, antiplatelet, and antiviral properties, with versatile immune-cytokine regulatory functions, that able to bind with transmembrane protease serine 2 (TMPRSS2) and induce endogenous antiviral cytokine interferon-stimulated gene 15, for the management of COVID-19. Silymarin 57-66 transmembrane serine protease 2 Homo sapiens 309-316 33817867-5 2021 Silymarin inhibits the expression of host cell surface receptor TMPRSS2 with a docking binding energy corresponding to -1,350.61 kcal/mol and a full fitness score of -8.11. Silymarin 0-9 transmembrane serine protease 2 Homo sapiens 64-71 34915414-1 2022 The interactions of four sulfonylated Phe(3-Am)-derived inhibitors (MI-432, MI-463, MI-482 and MI-1900) of type II transmembrane serine proteases (TTSP) such as transmembrane protease serine 2 (TMPRSS2) were examined with serum albumin and cytochrome P450 (CYP) isoenzymes. Phenylalanine 38-41 transmembrane serine protease 2 Homo sapiens 161-192 33824725-1 2021 SARS-CoV-2 utilizes the angiotensin-converting enzyme 2 (ACE2) receptor and transmembrane serine protease (TMPRSS2) to infect human lung cells. Serine 90-96 transmembrane serine protease 2 Homo sapiens 107-114 33762412-0 2021 Host serine proteases TMPRSS2 and TMPRSS11D mediate proteolytic activation and trypsin-independent infection in group A rotaviruses. Serine 5-11 transmembrane serine protease 2 Homo sapiens 22-29 34915414-1 2022 The interactions of four sulfonylated Phe(3-Am)-derived inhibitors (MI-432, MI-463, MI-482 and MI-1900) of type II transmembrane serine proteases (TTSP) such as transmembrane protease serine 2 (TMPRSS2) were examined with serum albumin and cytochrome P450 (CYP) isoenzymes. Phenylalanine 38-41 transmembrane serine protease 2 Homo sapiens 194-201 34915414-1 2022 The interactions of four sulfonylated Phe(3-Am)-derived inhibitors (MI-432, MI-463, MI-482 and MI-1900) of type II transmembrane serine proteases (TTSP) such as transmembrane protease serine 2 (TMPRSS2) were examined with serum albumin and cytochrome P450 (CYP) isoenzymes. 3-am 42-46 transmembrane serine protease 2 Homo sapiens 161-192 34915414-1 2022 The interactions of four sulfonylated Phe(3-Am)-derived inhibitors (MI-432, MI-463, MI-482 and MI-1900) of type II transmembrane serine proteases (TTSP) such as transmembrane protease serine 2 (TMPRSS2) were examined with serum albumin and cytochrome P450 (CYP) isoenzymes. 3-am 42-46 transmembrane serine protease 2 Homo sapiens 194-201 34915414-1 2022 The interactions of four sulfonylated Phe(3-Am)-derived inhibitors (MI-432, MI-463, MI-482 and MI-1900) of type II transmembrane serine proteases (TTSP) such as transmembrane protease serine 2 (TMPRSS2) were examined with serum albumin and cytochrome P450 (CYP) isoenzymes. Serine 129-135 transmembrane serine protease 2 Homo sapiens 161-192 34915414-1 2022 The interactions of four sulfonylated Phe(3-Am)-derived inhibitors (MI-432, MI-463, MI-482 and MI-1900) of type II transmembrane serine proteases (TTSP) such as transmembrane protease serine 2 (TMPRSS2) were examined with serum albumin and cytochrome P450 (CYP) isoenzymes. Serine 129-135 transmembrane serine protease 2 Homo sapiens 194-201 34915500-2 2022 This study elucidates pulmonary expression patterns SARS-CoV-2 entry factors (ACE2 and transmembrane protease serine subtype 2, TMPRSS2) and RAAS components in lethal COVID-19. Serine 110-116 transmembrane serine protease 2 Homo sapiens 128-135 34561887-5 2022 The viral particle incorporates the S protein, which has already undergone S1/S2 cleavage by furin, and then undergoes further cleavage at the S2" site, mediated by the type II transmembrane serine protease TMPRSS2, after binding to the receptor ACE2 to facilitate membrane fusion at the plasma membrane. Serine 191-197 transmembrane serine protease 2 Homo sapiens 207-214 34826419-0 2022 Hydroxychloroquine treatment on SARS-CoV-2 receptor ACE2, TMPRSS2 and NRP1 expression in human primary pterygium and conjunctival cells. Hydroxychloroquine 0-18 transmembrane serine protease 2 Homo sapiens 58-65 34826419-2 2022 Its infection depends on the binding of spike protein to the host cell receptor angiotensin-converting enzyme 2 (ACE2), type II transmembrane serine protease (TMPRSS2) and neuropilin-1 (NRP1). Serine 142-148 transmembrane serine protease 2 Homo sapiens 159-166 34293137-2 2021 ACE2 and TMPRSS2, host molecules required for viral entry, are regulated by sex steroids and expressed in the placenta. Steroids 80-88 transmembrane serine protease 2 Homo sapiens 9-16 34947999-7 2021 Here, we demonstrate by using a SARS-CoV-2 spike pseudotyped lentivirus particles (SSPL) system and patient-isolated SARS-CoV-2 VOCs to infect transgenic A549ACE2/TMPRSS2 and Calu-3 human lung cells that all three carrageenan types exert antiviral activity. Carrageenan 214-225 transmembrane serine protease 2 Homo sapiens 163-170 34913352-2 2021 In the lower respiratory system, the virus uses angiotensin-converting enzyme 2 (ACE2) receptor in conjunction with serine protease TMPRSS2, expressed by alveolar type II (ATII) cells as one of the SARS-CoV-2 target cells, to enter. Serine 116-122 transmembrane serine protease 2 Homo sapiens 132-139 34692233-5 2021 Consistently, the combination of the CTPB inhibitor CA-074 methyl ester and the TMPRSS2 inhibitor Camostat reduced the viral load to 0.0078+-0.0057%. camostat 98-106 transmembrane serine protease 2 Homo sapiens 80-87 34606834-4 2021 Angiotensin-converting enzyme 2 (ACE2) and transmembrane protease/serine subfamily member 2 (TMPRSS2) are essential proteins involved in the cell entry of SARS-CoV-2. Serine 66-72 transmembrane serine protease 2 Homo sapiens 93-100 34875734-2 2021 The virus enters host cells through angiotensin-converting enzyme 2 (ACE2) and transmembrane protease serine subtype 2 (TMPRSS2). Serine 102-108 transmembrane serine protease 2 Homo sapiens 120-127 34876760-4 2022 Polyunsaturated fatty acids control protein complex formation in lipid rafts associated with the function of two SARS-CoV-2 entry gateways: angiotensin-converting enzyme-2 and cellular protease transmembrane protease serine-2. Fatty Acids, Unsaturated 0-27 transmembrane serine protease 2 Homo sapiens 194-225 34677831-8 2021 Here we show that treatment of A549 human lung epithelial cells for 7 days with 25 mM d-galactose, an inducer of diabetic-like and oxidative stress cellular phenotypes, leads to increased mRNA levels of ACE2, TMPRSS2, and FURIN, along with reduced SERPINA1 mRNA. Galactose 86-97 transmembrane serine protease 2 Homo sapiens 209-216 34787160-4 2021 Thus, four potential drugs (bromhexine, camostat, gabexate, and nafamostat) were used to explore the mechanism of binding with TMPRSS2 in this work. Bromhexine 28-38 transmembrane serine protease 2 Homo sapiens 127-134 34787160-4 2021 Thus, four potential drugs (bromhexine, camostat, gabexate, and nafamostat) were used to explore the mechanism of binding with TMPRSS2 in this work. camostat 40-48 transmembrane serine protease 2 Homo sapiens 127-134 34787160-4 2021 Thus, four potential drugs (bromhexine, camostat, gabexate, and nafamostat) were used to explore the mechanism of binding with TMPRSS2 in this work. Gabexate 50-58 transmembrane serine protease 2 Homo sapiens 127-134 34787160-4 2021 Thus, four potential drugs (bromhexine, camostat, gabexate, and nafamostat) were used to explore the mechanism of binding with TMPRSS2 in this work. nafamostat 64-74 transmembrane serine protease 2 Homo sapiens 127-134 34787160-6 2021 Through the results of calculating binding free energy by nine methods, the binding affinity of camostat, gabexate, and nafamostat to TMPRSS2 showed great advantages compared with bromhexine, where the nafamostat was surprisingly found to present two reasonable binding conformations (forward and reverse directions). camostat 96-104 transmembrane serine protease 2 Homo sapiens 134-141 34787160-6 2021 Through the results of calculating binding free energy by nine methods, the binding affinity of camostat, gabexate, and nafamostat to TMPRSS2 showed great advantages compared with bromhexine, where the nafamostat was surprisingly found to present two reasonable binding conformations (forward and reverse directions). Gabexate 106-114 transmembrane serine protease 2 Homo sapiens 134-141 34787160-6 2021 Through the results of calculating binding free energy by nine methods, the binding affinity of camostat, gabexate, and nafamostat to TMPRSS2 showed great advantages compared with bromhexine, where the nafamostat was surprisingly found to present two reasonable binding conformations (forward and reverse directions). nafamostat 120-130 transmembrane serine protease 2 Homo sapiens 134-141 34787160-6 2021 Through the results of calculating binding free energy by nine methods, the binding affinity of camostat, gabexate, and nafamostat to TMPRSS2 showed great advantages compared with bromhexine, where the nafamostat was surprisingly found to present two reasonable binding conformations (forward and reverse directions). nafamostat 202-212 transmembrane serine protease 2 Homo sapiens 134-141 34787160-8 2021 In addition, compared with gabexate, the dimethylamino group in camostat forms more van der Waals interactions with surrounding hot-spots His296 and Val280, resulting in a stronger affinity to TMPRSS2. Gabexate 27-35 transmembrane serine protease 2 Homo sapiens 193-200 34787160-11 2021 The guanidinium groups of the drugs have powerful interactions with adjacent residues due to the formation of more hydrogen bonds, suggesting that this may be the critical site for drug design against TMPRSS2. Guanidine 4-15 transmembrane serine protease 2 Homo sapiens 201-208 34787160-11 2021 The guanidinium groups of the drugs have powerful interactions with adjacent residues due to the formation of more hydrogen bonds, suggesting that this may be the critical site for drug design against TMPRSS2. Hydrogen 115-123 transmembrane serine protease 2 Homo sapiens 201-208 34749700-13 2021 Further, FA-treated mammalian cells showed significant overexpression of ACE-2, NRP-1 and TMPRSS2 genes except with L-lactic acid and oleic acid caused downregulation of NRP-1 gene, while 17-octadecynoic acid caused insignificant effect. Lactic Acid 116-129 transmembrane serine protease 2 Homo sapiens 90-97 34749700-13 2021 Further, FA-treated mammalian cells showed significant overexpression of ACE-2, NRP-1 and TMPRSS2 genes except with L-lactic acid and oleic acid caused downregulation of NRP-1 gene, while 17-octadecynoic acid caused insignificant effect. Oleic Acid 134-144 transmembrane serine protease 2 Homo sapiens 90-97 34677831-0 2021 d-Galactose treatment increases ACE2, TMPRSS2, and FURIN and reduces SERPINA1 mRNA expression in A549 human lung epithelial cells. Galactose 0-11 transmembrane serine protease 2 Homo sapiens 38-45 34677831-3 2021 SARS-CoV-2 initially infects respiratory tract epithelial cells by binding to the host cell membrane ACE2, followed by proteolytic priming for cell entry by the host cell membrane serine protease TMPRSS2. Serine 180-186 transmembrane serine protease 2 Homo sapiens 196-203 34967175-6 2021 Based on the analysis of 72 articles using the MEDLINE database (PubMed), it can be concluded that testosterone is involved in the co-regulation of the synthesis of angiotensin-converting enzyme-2 and transmembrane serine protease-2, facilitating the penetration of SARS-CoV-2 into target cells and promoting easier infection in men. Testosterone 99-111 transmembrane serine protease 2 Homo sapiens 201-232 34658235-6 2021 Mechanistically, we demonstrate that the atovaquone antiviral activity against SARS-CoV-2 is partially dependent on the expression of TMPRSS2 and that the drug can disrupt the interaction of the spike protein with the viral receptor, ACE2. Atovaquone 41-51 transmembrane serine protease 2 Homo sapiens 134-141 34829773-7 2021 OM-85 significantly reduced the expression of ACE2 (p < 0.001), TMPRSS2 (p < 0.001), DPP4 (p < 0.005), and cellular heparan sulfate (p < 0.01), while ADAM17 (p < 0.02) expression was significantly upregulated. om-85 0-5 transmembrane serine protease 2 Homo sapiens 64-71 34635581-1 2021 The host cell serine protease TMPRSS2 is an attractive therapeutic target for COVID-19 drug discovery. Serine 14-20 transmembrane serine protease 2 Homo sapiens 30-37 34635581-3 2021 Utilizing rational structure-based drug design (SBDD) coupled to substrate specificity screening of TMPRSS2, we have discovered covalent small-molecule ketobenzothiazole (kbt) TMPRSS2 inhibitors which are structurally distinct from and have significantly improved activity over the existing known inhibitors Camostat and Nafamostat. ketobenzothiazole 152-169 transmembrane serine protease 2 Homo sapiens 100-107 34635581-3 2021 Utilizing rational structure-based drug design (SBDD) coupled to substrate specificity screening of TMPRSS2, we have discovered covalent small-molecule ketobenzothiazole (kbt) TMPRSS2 inhibitors which are structurally distinct from and have significantly improved activity over the existing known inhibitors Camostat and Nafamostat. ketobenzothiazole 152-169 transmembrane serine protease 2 Homo sapiens 176-183 34406858-4 2021 Similarly, inhibition of TMPRSS2 protease activity by camostat mesylate or nafamostat mesylate prevents infection mediated by the TMPRSS2-dependent and cathepsin-independent pathway. camostat 54-71 transmembrane serine protease 2 Homo sapiens 25-32 34690521-3 2022 Through molecular docking and dynamic simulation studies, we used the FDA-approved drug mezonavir against the most important viral targets, including spike (S) glycoprotein, Transmembrane serine protease 2 (TMPRSS2), RNA-dependent RNA polymerase (RdRp), Main protease (Mpro), human angiotensin-converting enzyme 2 (ACE-2), and furin. mezonavir 88-97 transmembrane serine protease 2 Homo sapiens 174-205 34690521-3 2022 Through molecular docking and dynamic simulation studies, we used the FDA-approved drug mezonavir against the most important viral targets, including spike (S) glycoprotein, Transmembrane serine protease 2 (TMPRSS2), RNA-dependent RNA polymerase (RdRp), Main protease (Mpro), human angiotensin-converting enzyme 2 (ACE-2), and furin. mezonavir 88-97 transmembrane serine protease 2 Homo sapiens 207-214 34406864-11 2021 Therefore, this study revealed that, at least, TMPRSS2 is involved in HE cleavage and suggested that nafamostat could be a candidate for therapeutic drugs of ICV infection. nafamostat 101-111 transmembrane serine protease 2 Homo sapiens 47-54 34406864-15 2021 This study revealed that transmembrane protease serine S1, members 2 (TMPRSS2), and not human airway trypsin-like protease (HAT), is involved in HE cleavage. Serine 48-54 transmembrane serine protease 2 Homo sapiens 70-77 34406858-4 2021 Similarly, inhibition of TMPRSS2 protease activity by camostat mesylate or nafamostat mesylate prevents infection mediated by the TMPRSS2-dependent and cathepsin-independent pathway. camostat 54-71 transmembrane serine protease 2 Homo sapiens 130-137 34406858-4 2021 Similarly, inhibition of TMPRSS2 protease activity by camostat mesylate or nafamostat mesylate prevents infection mediated by the TMPRSS2-dependent and cathepsin-independent pathway. nafamostat 75-94 transmembrane serine protease 2 Homo sapiens 25-32 34406858-4 2021 Similarly, inhibition of TMPRSS2 protease activity by camostat mesylate or nafamostat mesylate prevents infection mediated by the TMPRSS2-dependent and cathepsin-independent pathway. nafamostat 75-94 transmembrane serine protease 2 Homo sapiens 130-137 34635175-1 2021 BACKGROUND: SARS-CoV-2 uses the angiotensin-converting enzyme 2 (ACE2) and neuropilin-1 (NRP1) receptors for entry into cells, and the serine protease TMPRSS2 for S protein priming. Serine 135-141 transmembrane serine protease 2 Homo sapiens 151-158 34393265-4 2021 Here, we performed a theoretical investigation of the same by studying the binding of the molecules with SARS-COV-2 Spike protein, the complex formed by Spike and ACE2 human receptor and a human serine protease TMPRSS2 which aids in cleavage of the Spike protein to initiate the viral activation in the body. Serine 195-201 transmembrane serine protease 2 Homo sapiens 211-218 34393265-8 2021 We tested the stability of the docked complexes by running Molecular Dynamics (MD) simulations where we observed the stability of the quinoline analogues with the Spike-ACE2 and TMPRSS2 nevertheless the quinolines were not stable with the Spike protein alone. quinoline 134-143 transmembrane serine protease 2 Homo sapiens 178-185 34393265-11 2021 We also observed that a Fluoride based compound: 3-(3-(Trifluoromethyl)phenyl)quinoline helps the inhibitor to bind with both Spike-ACE2 and TMPRSS2 with equal probability. Fluorides 24-32 transmembrane serine protease 2 Homo sapiens 141-148 34572459-0 2021 Hydrogen Sulfide Inhibits TMPRSS2 in Human Airway Epithelial Cells: Implications for SARS-CoV-2 Infection. Hydrogen Sulfide 0-16 transmembrane serine protease 2 Homo sapiens 26-33 34393265-11 2021 We also observed that a Fluoride based compound: 3-(3-(Trifluoromethyl)phenyl)quinoline helps the inhibitor to bind with both Spike-ACE2 and TMPRSS2 with equal probability. 3-[3-(Trifluoromethyl)phenyl]quinoline 49-87 transmembrane serine protease 2 Homo sapiens 141-148 34590967-7 2021 PCA discloses the evidence of the structural similarities to the corresponding complexes of L1, L2, and L6 with the complex of TMPRSS2(TM) and Nafamostat mesylate (TM-NAM). nafamostat 143-162 transmembrane serine protease 2 Homo sapiens 127-134 34132421-2 2021 The virus enters into humans by attachment of its Spike protein (S) to the ACE receptor present on the lung epithelial cell surface followed by cleavage of S protein by the cellular transmembrane serine protease (TMPRSS2). Serine 196-202 transmembrane serine protease 2 Homo sapiens 213-220 34282808-12 2021 ACE2 expression was suppressed in ENP tissues; however, a combination of poly(I:C) and IL-13 induced ACE2/TMPRSS2 upregulation in ENP. Poly I-C 73-82 transmembrane serine protease 2 Homo sapiens 106-113 34572459-7 2021 Considering that respiratory epithelial cells can be directly exposed to H2S by inhalation, here we tested the in vitro effects of H2S-donors on TMPRSS2 and ACE2 expression in human upper and lower airway epithelial cells. Deuterium 131-134 transmembrane serine protease 2 Homo sapiens 145-152 34572459-8 2021 We showed that H2S significantly reduces the expression of TMPRSS2 without modifying ACE2 expression both in respiratory cell lines and primary human upper and lower airway epithelial cells. Deuterium 15-18 transmembrane serine protease 2 Homo sapiens 59-66 34174588-5 2021 The expression of TMPRSS2 was increased by PgLPS, IL1beta, or PGE2 while BSG was elevated by PgLPS and IL1beta. Dinoprostone 62-66 transmembrane serine protease 2 Homo sapiens 18-25 34575594-2 2021 Nafamostat mesylate (NFM) suppresses transmembrane serine protease 2 and SARS-CoV-2 S protein-mediated fusion. nafamostat 0-19 transmembrane serine protease 2 Homo sapiens 37-68 34534255-6 2021 Furthermore, tranexamic acid exerted inhibitory effects on TMPRSS2 protease activity. Tranexamic Acid 13-28 transmembrane serine protease 2 Homo sapiens 59-66 34576032-4 2021 Differentiated iCMs expressed the primary SARS-CoV2 receptor angiotensin-converting enzyme-II (ACE2) and the transmembrane protease serine type 2 (TMPRSS2) receptor suggesting the susceptibility of iCMs to SARS-CoV2. Serine 132-138 transmembrane serine protease 2 Homo sapiens 147-154 34160253-0 2021 Structural basis of covalent inhibitory mechanism of TMPRSS2-related serine proteases by camostat. Serine 69-75 transmembrane serine protease 2 Homo sapiens 53-60 34578348-0 2021 Nafamostat-Interferon-alpha Combination Suppresses SARS-CoV-2 Infection In Vitro and In Vivo by Cooperatively Targeting Host TMPRSS2. nafamostat-interferon-alpha 0-27 transmembrane serine protease 2 Homo sapiens 125-132 34392451-7 2021 However, type II transmembrane serine protease (TMPRSS2) is able to inhibit the ENaC, but it is utilized in the case of SARS-CoV-2 cell entry, therefore the ENaC remains activated. Serine 31-37 transmembrane serine protease 2 Homo sapiens 48-55 34449057-2 2021 Interestingly, identified mutations mainly occur in the spike (S) protein which interacts with the ACE2 receptor and is cleaved via serine protease TMPRSS2. Serine 132-138 transmembrane serine protease 2 Homo sapiens 148-155 34116393-0 2021 Magnesium treatment on methylation changes of transmembrane serine protease 2 (TMPRSS2). Magnesium 0-9 transmembrane serine protease 2 Homo sapiens 46-77 34116393-0 2021 Magnesium treatment on methylation changes of transmembrane serine protease 2 (TMPRSS2). Magnesium 0-9 transmembrane serine protease 2 Homo sapiens 79-86 34116393-2 2021 This study aims to test the hypothesis that magnesium (Mg) treatment leads to DNA methylation changes in TMPRSS2. Magnesium 44-53 transmembrane serine protease 2 Homo sapiens 105-112 34116393-2 2021 This study aims to test the hypothesis that magnesium (Mg) treatment leads to DNA methylation changes in TMPRSS2. Magnesium 55-57 transmembrane serine protease 2 Homo sapiens 105-112 34116393-8 2021 CONCLUSIONS: Among individuals ages < 65 y with calcium-to-magnesium intake ratios equal to or over 2.6, reducing the ratio to around 2.3 increased 5-methylcytosine modifications (i.e., cg16371860) and reduced 5-hydroxymethylcytosine modifications (i.e., cg26337277) in the TMPRSS2 gene. Calcium 48-55 transmembrane serine protease 2 Homo sapiens 274-281 34116393-8 2021 CONCLUSIONS: Among individuals ages < 65 y with calcium-to-magnesium intake ratios equal to or over 2.6, reducing the ratio to around 2.3 increased 5-methylcytosine modifications (i.e., cg16371860) and reduced 5-hydroxymethylcytosine modifications (i.e., cg26337277) in the TMPRSS2 gene. Magnesium 59-68 transmembrane serine protease 2 Homo sapiens 274-281 34116393-8 2021 CONCLUSIONS: Among individuals ages < 65 y with calcium-to-magnesium intake ratios equal to or over 2.6, reducing the ratio to around 2.3 increased 5-methylcytosine modifications (i.e., cg16371860) and reduced 5-hydroxymethylcytosine modifications (i.e., cg26337277) in the TMPRSS2 gene. cg26337277 255-265 transmembrane serine protease 2 Homo sapiens 274-281 34116393-9 2021 These findings, if confirmed, provide another mechanism for the role of Mg intervention in the prevention of COVID-19 and treatment of early and mild disease by modifying the phenotype of the TMPRSS2 genotype. Magnesium 72-74 transmembrane serine protease 2 Homo sapiens 192-199 34340553-0 2021 The TMPRSS2 Inhibitor Nafamostat Reduces SARS-CoV-2 Pulmonary Infection in Mouse Models of COVID-19. nafamostat 22-32 transmembrane serine protease 2 Homo sapiens 4-11 34444960-5 2021 In summary, hesperidin is a potential TMPRSS2 inhibitor for the reduction of the SARS-CoV-2 infection. Hesperidin 12-22 transmembrane serine protease 2 Homo sapiens 38-45 34703545-5 2021 We show that otamixaban suppresses TMPRSS2 activity and SARS-CoV-2 infection of a human lung cell line, although with lower potency than camostat or nafamostat. otamixaban 13-23 transmembrane serine protease 2 Homo sapiens 35-42 34527703-5 2021 To help the virus enter efficiently, the S protein is further activated by the serine protease 2 (TMPRSS2), provided that the S has been cleaved by furin previously. Serine 79-85 transmembrane serine protease 2 Homo sapiens 98-105 34427179-8 2021 MDS analysis indicated bisdemethoxycurcumin (BDMC), carvacrol and thymol as better inhibitors than the camostat due to their stable binding with TMPRSS2 in its oxyanion hole and inducing subtle modification in the spatial arrangement of the catalytic triad residues. bisdemethoxycurcumin 23-43 transmembrane serine protease 2 Homo sapiens 145-152 34427179-8 2021 MDS analysis indicated bisdemethoxycurcumin (BDMC), carvacrol and thymol as better inhibitors than the camostat due to their stable binding with TMPRSS2 in its oxyanion hole and inducing subtle modification in the spatial arrangement of the catalytic triad residues. bisdemethoxycurcumin 45-49 transmembrane serine protease 2 Homo sapiens 145-152 34427179-8 2021 MDS analysis indicated bisdemethoxycurcumin (BDMC), carvacrol and thymol as better inhibitors than the camostat due to their stable binding with TMPRSS2 in its oxyanion hole and inducing subtle modification in the spatial arrangement of the catalytic triad residues. carvacrol 52-61 transmembrane serine protease 2 Homo sapiens 145-152 34427179-8 2021 MDS analysis indicated bisdemethoxycurcumin (BDMC), carvacrol and thymol as better inhibitors than the camostat due to their stable binding with TMPRSS2 in its oxyanion hole and inducing subtle modification in the spatial arrangement of the catalytic triad residues. Thymol 66-72 transmembrane serine protease 2 Homo sapiens 145-152 34415218-2 2021 In this study, we used combined molecular docking, molecular dynamics simulations and binding free energy analyses to investigate the potentials of vitamin D3 and its hydroxyderivatives as TMPRSS2 inhibitor and to inhibit the SARS-CoV-2 receptor binding domain (RBD) binding to angiotensin-converting enzyme 2 (ACE2), as well as to unveil molecular and structural basis of 1,25(OH)2D3 capability to inhibit ACE2 and SARS-CoV-2 RBD interactions. Cholecalciferol 148-158 transmembrane serine protease 2 Homo sapiens 189-196 34415218-2 2021 In this study, we used combined molecular docking, molecular dynamics simulations and binding free energy analyses to investigate the potentials of vitamin D3 and its hydroxyderivatives as TMPRSS2 inhibitor and to inhibit the SARS-CoV-2 receptor binding domain (RBD) binding to angiotensin-converting enzyme 2 (ACE2), as well as to unveil molecular and structural basis of 1,25(OH)2D3 capability to inhibit ACE2 and SARS-CoV-2 RBD interactions. Calcitriol 373-384 transmembrane serine protease 2 Homo sapiens 189-196 34415218-3 2021 The results show that vitamin D3 and its hydroxyderivatives are favorable to bind active site of TMPRSS2 and the binding site(s) between ACE2 and SARS-CoV2-RBD, which indicate that vitamin D3 and its biologically active hydroxyderivatives can serve as TMPRSS2 inhibitor and can inhibit ACE2 binding of SARS-CoV-2 RBD to prevent SARS-CoV-2 entry. Cholecalciferol 22-32 transmembrane serine protease 2 Homo sapiens 97-104 34415218-3 2021 The results show that vitamin D3 and its hydroxyderivatives are favorable to bind active site of TMPRSS2 and the binding site(s) between ACE2 and SARS-CoV2-RBD, which indicate that vitamin D3 and its biologically active hydroxyderivatives can serve as TMPRSS2 inhibitor and can inhibit ACE2 binding of SARS-CoV-2 RBD to prevent SARS-CoV-2 entry. Cholecalciferol 22-32 transmembrane serine protease 2 Homo sapiens 252-259 34415218-3 2021 The results show that vitamin D3 and its hydroxyderivatives are favorable to bind active site of TMPRSS2 and the binding site(s) between ACE2 and SARS-CoV2-RBD, which indicate that vitamin D3 and its biologically active hydroxyderivatives can serve as TMPRSS2 inhibitor and can inhibit ACE2 binding of SARS-CoV-2 RBD to prevent SARS-CoV-2 entry. Cholecalciferol 181-191 transmembrane serine protease 2 Homo sapiens 97-104 34415218-3 2021 The results show that vitamin D3 and its hydroxyderivatives are favorable to bind active site of TMPRSS2 and the binding site(s) between ACE2 and SARS-CoV2-RBD, which indicate that vitamin D3 and its biologically active hydroxyderivatives can serve as TMPRSS2 inhibitor and can inhibit ACE2 binding of SARS-CoV-2 RBD to prevent SARS-CoV-2 entry. Cholecalciferol 181-191 transmembrane serine protease 2 Homo sapiens 252-259 34353250-4 2022 Studies suggests SARS-CoV-2 entry via olfactory epithelium (OE) and the expression of type 2 transmembrane serine protease (TMPRSS2) in addition to angiotensin converting enzyme 2 (ACE2) can facilitate SARS-CoV-2 neurotropism. Serine 107-113 transmembrane serine protease 2 Homo sapiens 124-131 34445373-1 2021 Human ACE2 and the serine protease TMPRSS2 of novel SARS-CoV-2 are primary entry receptors in host cells. Serine 19-25 transmembrane serine protease 2 Homo sapiens 35-42 34370633-0 2022 Molecular Modeling Targeting Transmembrane Serine Protease 2 (TMPRSS2) as an Alternative Drug Target Against Coronaviruses. Serine 43-49 transmembrane serine protease 2 Homo sapiens 62-69 34100014-4 2021 Similarly, inhibition of TMPRSS2 protease activity by camostat mesylate or nafamostat mesylate prevents infection mediated by the TMPRSS2-dependent and cathepsin-independent pathway. camostat 54-71 transmembrane serine protease 2 Homo sapiens 25-32 34100014-4 2021 Similarly, inhibition of TMPRSS2 protease activity by camostat mesylate or nafamostat mesylate prevents infection mediated by the TMPRSS2-dependent and cathepsin-independent pathway. camostat 54-71 transmembrane serine protease 2 Homo sapiens 130-137 34100014-4 2021 Similarly, inhibition of TMPRSS2 protease activity by camostat mesylate or nafamostat mesylate prevents infection mediated by the TMPRSS2-dependent and cathepsin-independent pathway. nafamostat 75-94 transmembrane serine protease 2 Homo sapiens 25-32 34100014-4 2021 Similarly, inhibition of TMPRSS2 protease activity by camostat mesylate or nafamostat mesylate prevents infection mediated by the TMPRSS2-dependent and cathepsin-independent pathway. nafamostat 75-94 transmembrane serine protease 2 Homo sapiens 130-137 34336361-2 2021 Recent studies have shown that transmembrane serine protease 2 (TMPRSS2), a protease known for similar role in previous coronavirus infections, severe acute respiratory syndrome (SARS), and Middle East respiratory syndrome (MERS), is responsible for the proteolytic cleavage of the SARS-CoV-2 spike protein, enabling host cell fusion of the virus. Serine 45-51 transmembrane serine protease 2 Homo sapiens 64-71 34351542-5 2021 Two pentacyclic terpenoids (24-methylene cycloartenol and isoiguesteri) interacted with the hACE2 binding hotspots for the SARS-CoV-2 spike protein, while the abietane diterpenes were found accommodated within the S1-specificity pocket, interacting strongly with the active site residues TMPRSS2. isoiguesteri 58-70 transmembrane serine protease 2 Homo sapiens 288-295 34351542-5 2021 Two pentacyclic terpenoids (24-methylene cycloartenol and isoiguesteri) interacted with the hACE2 binding hotspots for the SARS-CoV-2 spike protein, while the abietane diterpenes were found accommodated within the S1-specificity pocket, interacting strongly with the active site residues TMPRSS2. Abietanes 159-178 transmembrane serine protease 2 Homo sapiens 288-295 34118289-4 2021 Nine withanolides were tested in silico for their potential to target and inhibit (i) cell surface receptor protein (TMPRSS2) that is required for entry of virus to host cells and (ii) viral protein (the main protease Mpro) that is essential for virus replication. Withanolides 5-17 transmembrane serine protease 2 Homo sapiens 117-124 34118289-5 2021 We report that the withanolides possess capacity to inhibit the activity of TMPRSS2 and Mpro. Withanolides 19-31 transmembrane serine protease 2 Homo sapiens 76-83 34118289-6 2021 Furthermore, withanolide-treated cells showed downregulation of TMPRSS2 expression and inhibition of SARS-CoV-2 replication in vitro, suggesting that Ashwagandha may provide a useful resource for COVID-19 treatment. Withanolides 13-24 transmembrane serine protease 2 Homo sapiens 64-71 34210968-0 2021 The antiandrogen enzalutamide downregulates TMPRSS2 and reduces cellular entry of SARS-CoV-2 in human lung cells. enzalutamide 17-29 transmembrane serine protease 2 Homo sapiens 44-51 34306988-3 2021 Our in silico approach suggested that unique phytocompounds such as emodin, thymol and carvacrol, and artemisinin could physically bind SARS-CoV-2 spike glycoproteins (6VXX and 6VYB), SARS-CoV-2 B.1.351 South Africa variant of Spike glycoprotein (7NXA), and even with ACE2 and prevent the SARS-CoV-2 binding to the host ACE2, TMPRSS2 and neutrapilin-1 receptors. Thymol 76-82 transmembrane serine protease 2 Homo sapiens 326-333 34306988-3 2021 Our in silico approach suggested that unique phytocompounds such as emodin, thymol and carvacrol, and artemisinin could physically bind SARS-CoV-2 spike glycoproteins (6VXX and 6VYB), SARS-CoV-2 B.1.351 South Africa variant of Spike glycoprotein (7NXA), and even with ACE2 and prevent the SARS-CoV-2 binding to the host ACE2, TMPRSS2 and neutrapilin-1 receptors. carvacrol 87-96 transmembrane serine protease 2 Homo sapiens 326-333 34306988-3 2021 Our in silico approach suggested that unique phytocompounds such as emodin, thymol and carvacrol, and artemisinin could physically bind SARS-CoV-2 spike glycoproteins (6VXX and 6VYB), SARS-CoV-2 B.1.351 South Africa variant of Spike glycoprotein (7NXA), and even with ACE2 and prevent the SARS-CoV-2 binding to the host ACE2, TMPRSS2 and neutrapilin-1 receptors. artemisinin 102-113 transmembrane serine protease 2 Homo sapiens 326-333 34306988-9 2021 Emodin showed best interactions with TMPRSS 2 and ACE2 with Etotal of -7.1 and -7.3 KJ mol-1 respectively, whereas artemisinin interacts with TMPRSS 2 and ACE2 with Etotal of -6.9 and -7.4 KJ mol-1 respectively. Emodin 0-6 transmembrane serine protease 2 Homo sapiens 37-45 34306988-9 2021 Emodin showed best interactions with TMPRSS 2 and ACE2 with Etotal of -7.1 and -7.3 KJ mol-1 respectively, whereas artemisinin interacts with TMPRSS 2 and ACE2 with Etotal of -6.9 and -7.4 KJ mol-1 respectively. artemisinin 115-126 transmembrane serine protease 2 Homo sapiens 142-150 34230470-0 2021 EZH2-induced lysine K362 methylation enhances TMPRSS2-ERG oncogenic activity in prostate cancer. lysine k362 13-24 transmembrane serine protease 2 Homo sapiens 46-53 34225789-12 2021 DISCUSSION: In this trial, we repurpose the FDA approved LHRH antagonist degarelix, commonly used for prostate cancer, to suppress TMPRSS2, a host cell surface protease required for SARS-CoV-2 cell entry. acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ILys-prolyl-alaninamide 73-82 transmembrane serine protease 2 Homo sapiens 131-138 34096226-1 2021 Angiotensin-converting enzyme II (ACE2) in association with type II transmembrane serine protease (TMPRSS2) is considered the main receptor of SARS-CoV-2. Serine 82-88 transmembrane serine protease 2 Homo sapiens 99-106 34210968-4 2021 We show here that treatment with the antiandrogen enzalutamide-a well-tolerated drug widely used in advanced prostate cancer-reduces TMPRSS2 levels in human lung cells and in mouse lung. enzalutamide 50-62 transmembrane serine protease 2 Homo sapiens 133-140 34138966-7 2021 Our study also demonstrates that brazilin and theaflavin-3,3"-digallate, and to a still greater extent, curcumin, decrease the activity of transmembrane serine protease 2 both in cell-free and cell-based assays. brazilin 33-41 transmembrane serine protease 2 Homo sapiens 139-170 34209110-1 2021 Positively charged groups that mimic arginine or lysine in a natural substrate of trypsin are necessary for drugs to inhibit the trypsin-like serine protease TMPRSS2 that is involved in the viral entry and spread of coronaviruses, including SARS-CoV-2. Arginine 37-45 transmembrane serine protease 2 Homo sapiens 158-165 34209110-1 2021 Positively charged groups that mimic arginine or lysine in a natural substrate of trypsin are necessary for drugs to inhibit the trypsin-like serine protease TMPRSS2 that is involved in the viral entry and spread of coronaviruses, including SARS-CoV-2. Lysine 49-55 transmembrane serine protease 2 Homo sapiens 158-165 34209110-1 2021 Positively charged groups that mimic arginine or lysine in a natural substrate of trypsin are necessary for drugs to inhibit the trypsin-like serine protease TMPRSS2 that is involved in the viral entry and spread of coronaviruses, including SARS-CoV-2. Serine 142-148 transmembrane serine protease 2 Homo sapiens 158-165 34209110-6 2021 These results suggest that the proposed compounds, in addition to Camostat and Nafamostat, could be effective TMPRSS2 inhibitors for COVID-19 treatment by occupying the S1 pocket with the hallmark positively charged groups. nafamostat 79-89 transmembrane serine protease 2 Homo sapiens 110-117 34181691-4 2021 The serine protease TMPRSS2 has been shown to be important for S protein priming and viral entry, however, little is known about its regulation. Serine 4-10 transmembrane serine protease 2 Homo sapiens 20-27 34181691-5 2021 SPINT2 is a member of the family of Kunitz type serine protease inhibitors and has been shown to inhibit TMPRSS2. Serine 48-54 transmembrane serine protease 2 Homo sapiens 105-112 34201505-2 2021 Following the binding between S1 subunit and ACE2 receptor, different serine proteases, including TMPRSS2 and furin, trigger and participate in the fusion of the viral envelope with the host cell membrane. Serine 70-76 transmembrane serine protease 2 Homo sapiens 98-105 34162861-4 2021 We identify homoharringtonine and halofuginone as the most attractive agents, reducing endogenous TMPRSS2 expression at sub-micromolar concentrations. Homoharringtonine 12-29 transmembrane serine protease 2 Homo sapiens 98-105 34162861-4 2021 We identify homoharringtonine and halofuginone as the most attractive agents, reducing endogenous TMPRSS2 expression at sub-micromolar concentrations. halofuginone 34-46 transmembrane serine protease 2 Homo sapiens 98-105 34162861-6 2021 We further demonstrate that halofuginone modulates TMPRSS2 levels through proteasomal-mediated degradation that involves the E3 ubiquitin ligase component DDB1- and CUL4-associated factor 1 (DCAF1). halofuginone 28-40 transmembrane serine protease 2 Homo sapiens 51-58 34138966-7 2021 Our study also demonstrates that brazilin and theaflavin-3,3"-digallate, and to a still greater extent, curcumin, decrease the activity of transmembrane serine protease 2 both in cell-free and cell-based assays. Curcumin 104-112 transmembrane serine protease 2 Homo sapiens 139-170 34138966-7 2021 Our study also demonstrates that brazilin and theaflavin-3,3"-digallate, and to a still greater extent, curcumin, decrease the activity of transmembrane serine protease 2 both in cell-free and cell-based assays. theaflavin-3,3'-digallate 46-71 transmembrane serine protease 2 Homo sapiens 139-170 34079462-6 2021 Marine sponge produces classes of compounds that can inhibit the viral cysteine protease (Mpro) such as esculetin and ilimaquinone and human serine protease (TMPRSS2) such as pseudotheonamide C and D and aeruginosin 98B. Pseudotheonamide C 175-193 transmembrane serine protease 2 Homo sapiens 158-165 34150618-4 2021 In addition, HG122 reduced the mRNA expression of PSA and TMPRSS2 which are target genes of AR, resulting in cell growth inhibition and metastasis suppression of CRPC, without affecting the expression of AR mRNA level. HG122 13-18 transmembrane serine protease 2 Homo sapiens 58-65 34127969-3 2021 Serine proteases (SPs) including furin and TMPRSS2 cleave SARS-CoV-2 spike protein, facilitating viral entry. Serine 0-6 transmembrane serine protease 2 Homo sapiens 43-50 34514079-4 2021 Transmembrane serine-type 2 (TMPRSS2) is a SARS CoV-2 enzyme that is essential for viral fusion with the host cell. Serine 14-20 transmembrane serine protease 2 Homo sapiens 29-36 34104394-6 2021 Whereas low testosterone levels may be protective against the initial susceptibility (due to a restoration of immunological functions and a block of TMPRSS2), low testosterone may stimulate a worse clinical course in the advanced COVID-19 infection as it could exacerbate or activate the cytokine storm. Testosterone 12-24 transmembrane serine protease 2 Homo sapiens 149-156 34131661-1 2021 The host cell serine protease TMPRSS2 is an attractive therapeutic target for COVID-19 drug discovery. Serine 14-20 transmembrane serine protease 2 Homo sapiens 30-37 34131661-3 2021 Utilizing rational structure-based drug design (SBDD) coupled to substrate specificity screening of TMPRSS2, we have discovered a novel class of small molecule ketobenzothiazole TMPRSS2 inhibitors with significantly improved activity over existing irreversible inhibitors Camostat and Nafamostat. ketobenzothiazole 160-177 transmembrane serine protease 2 Homo sapiens 100-107 34131661-3 2021 Utilizing rational structure-based drug design (SBDD) coupled to substrate specificity screening of TMPRSS2, we have discovered a novel class of small molecule ketobenzothiazole TMPRSS2 inhibitors with significantly improved activity over existing irreversible inhibitors Camostat and Nafamostat. ketobenzothiazole 160-177 transmembrane serine protease 2 Homo sapiens 178-185 34063247-3 2021 FRET assay was applied to investigate the inhibitory effects of SB on the two proteases involved in SARS-CoV-2 infection, Mpro and TMPRSS2. Antimony 64-66 transmembrane serine protease 2 Homo sapiens 131-138 34063247-7 2021 Furthermore, SB extracts effectively inhibited SARS-CoV-2 Vpp infection through a TMPRSS2-dependent mechanism. Antimony 13-15 transmembrane serine protease 2 Homo sapiens 82-89 34063247-10 2021 Thus, SB may effectively prevent SARS-CoV-2 infection and replication through inhibiting Mpro and TMPRSS2 protease activities. Antimony 6-8 transmembrane serine protease 2 Homo sapiens 98-105 34075338-0 2021 Structural insights and inhibition mechanism of TMPRSS2 by experimentally known inhibitors Camostat mesylate, Nafamostat and Bromhexine hydrochloride to control SARS-coronavirus-2: A molecular modeling approach. camostat 91-108 transmembrane serine protease 2 Homo sapiens 48-55 34075338-0 2021 Structural insights and inhibition mechanism of TMPRSS2 by experimentally known inhibitors Camostat mesylate, Nafamostat and Bromhexine hydrochloride to control SARS-coronavirus-2: A molecular modeling approach. nafamostat 110-120 transmembrane serine protease 2 Homo sapiens 48-55 34075338-0 2021 Structural insights and inhibition mechanism of TMPRSS2 by experimentally known inhibitors Camostat mesylate, Nafamostat and Bromhexine hydrochloride to control SARS-coronavirus-2: A molecular modeling approach. Bromhexine 125-149 transmembrane serine protease 2 Homo sapiens 48-55 34075338-3 2021 Similarly, a transmembrane serine protease, TMPRSS2 of the host cell plays a significant role in the proteolytic cleavage of viral "S" protein helpful for the priming of ACE2 receptors and viral entry into human cells. Serine 27-33 transmembrane serine protease 2 Homo sapiens 44-51 34075338-5 2021 Hence, we have used a molecular dynamics (MD) simulated homology model of TMPRSS2 to study the inhibition mechanism of experimentally known inhibitors Camostat mesylate, Nafamostat and Bromhexine hydrochloride (BHH) using molecular modeling techniques. camostat 151-168 transmembrane serine protease 2 Homo sapiens 74-81 34075338-5 2021 Hence, we have used a molecular dynamics (MD) simulated homology model of TMPRSS2 to study the inhibition mechanism of experimentally known inhibitors Camostat mesylate, Nafamostat and Bromhexine hydrochloride (BHH) using molecular modeling techniques. nafamostat 170-180 transmembrane serine protease 2 Homo sapiens 74-81 34075338-5 2021 Hence, we have used a molecular dynamics (MD) simulated homology model of TMPRSS2 to study the inhibition mechanism of experimentally known inhibitors Camostat mesylate, Nafamostat and Bromhexine hydrochloride (BHH) using molecular modeling techniques. Bromhexine 185-209 transmembrane serine protease 2 Homo sapiens 74-81 34075338-5 2021 Hence, we have used a molecular dynamics (MD) simulated homology model of TMPRSS2 to study the inhibition mechanism of experimentally known inhibitors Camostat mesylate, Nafamostat and Bromhexine hydrochloride (BHH) using molecular modeling techniques. Bromhexine 211-214 transmembrane serine protease 2 Homo sapiens 74-81 34075338-7 2021 Molecular docking analysis revealed that Camostat mesylate and its structural analogue Nafamostat interact strongly with residues His296 and Ser441 present in the catalytic triad of TMPRSS2, whereas BHH binds with Ala386 along with other residues. nafamostat 87-97 transmembrane serine protease 2 Homo sapiens 182-189 34075338-7 2021 Molecular docking analysis revealed that Camostat mesylate and its structural analogue Nafamostat interact strongly with residues His296 and Ser441 present in the catalytic triad of TMPRSS2, whereas BHH binds with Ala386 along with other residues. Bromhexine 199-202 transmembrane serine protease 2 Homo sapiens 182-189 34667827-5 2021 Then, we generate a pharmacophore model from TMPRSS2 active site consequently, and the developed models were employed for the screening of one million molecules from the Enamine database. cyclopentyl enamine 170-177 transmembrane serine protease 2 Homo sapiens 45-52 34075338-9 2021 MM-PBSA calculations also revealed the stronger binding of Camostat mesylate to TMPRSS2 active site residues as compared to Nafamostat and BHH. poly(tetramethylene succinate-co-tetramethylene adipate) 3-7 transmembrane serine protease 2 Homo sapiens 80-87 34853776-0 2021 PFOA induces alteration in DNA methylation regulators and SARS-CoV-2 targets Ace2 and Tmprss2 in mouse lung tissues. perfluorooctanoic acid 0-4 transmembrane serine protease 2 Homo sapiens 86-93 34796023-5 2021 SARS-CoV-2 enters the body with the help of the target proteins: angiotensin-converting enzyme 2 (ACE2) and associated serine protease TMPRSS2 of the nasal epithelium. Serine 119-125 transmembrane serine protease 2 Homo sapiens 135-142 34693818-12 2021 The type II transmembrane serine proteases TMPRSS2 and histone acetyltransferases (HAT) are host cell proteases that are recruited by the virus to cleave ACE2 surface protein S which facilitates the viral entry. Serine 26-32 transmembrane serine protease 2 Homo sapiens 43-50 35430474-2 2022 It is mediated by the binding of viral spike proteins to human cells via entry and replication processes involving human angiotensin converting enzyme-2 (hACE2), transmembrane serine protease (TMPRSS2) and cathepsin L (Cath L). Serine 176-182 transmembrane serine protease 2 Homo sapiens 193-200 35596627-7 2022 Mapping the activity of silibinin indicated its excellent binding inhibition activity against SARS-CoV-2 S protein, Mpro and RdRP at IC50 0.029, 0.021, and 0.042 muM, respectively, while it showed no inhibition activity against TMPRSS2 at its IC50(SARS-CoV-2) . Silybin 24-33 transmembrane serine protease 2 Homo sapiens 228-235 35578172-0 2022 Molecular docking analysis reveals the functional inhibitory effect of Genistein and Quercetin on TMPRSS2: SARS-COV-2 cell entry facilitator spike protein. Genistein 71-80 transmembrane serine protease 2 Homo sapiens 98-105 35578172-0 2022 Molecular docking analysis reveals the functional inhibitory effect of Genistein and Quercetin on TMPRSS2: SARS-COV-2 cell entry facilitator spike protein. Quercetin 85-94 transmembrane serine protease 2 Homo sapiens 98-105 35578172-6 2022 RESULTS: Docking analysis using PyRx version 0.8 along with AutoDockVina reveals that among the screened phyto compounds, Genistein shows the maximum binding affinity towards the hydrophobic substrate-binding site of TMPRSS2 with three hydrogen bonds interaction ( - 7.5 kcal/mol). Genistein 122-131 transmembrane serine protease 2 Homo sapiens 217-224 35578172-6 2022 RESULTS: Docking analysis using PyRx version 0.8 along with AutoDockVina reveals that among the screened phyto compounds, Genistein shows the maximum binding affinity towards the hydrophobic substrate-binding site of TMPRSS2 with three hydrogen bonds interaction ( - 7.5 kcal/mol). Hydrogen 236-244 transmembrane serine protease 2 Homo sapiens 217-224 35578172-7 2022 On the other hand, molecular docking analysis using Schrodinger identified Quercetin as the most potent phyto compound with a maximum binding affinity towards the hydrophilic catalytic site of TMPRSS2 ( - 7.847 kcal/mol) with three hydrogen bonds interaction. Quercetin 75-84 transmembrane serine protease 2 Homo sapiens 193-200 35578172-7 2022 On the other hand, molecular docking analysis using Schrodinger identified Quercetin as the most potent phyto compound with a maximum binding affinity towards the hydrophilic catalytic site of TMPRSS2 ( - 7.847 kcal/mol) with three hydrogen bonds interaction. Hydrogen 232-240 transmembrane serine protease 2 Homo sapiens 193-200 35578172-10 2022 CONCLUSION: The compounds, Quercetin and Genistein, can inhibit the TMPRSS2 guided priming of the spike protein. Quercetin 27-36 transmembrane serine protease 2 Homo sapiens 68-75 35578172-10 2022 CONCLUSION: The compounds, Quercetin and Genistein, can inhibit the TMPRSS2 guided priming of the spike protein. Genistein 41-50 transmembrane serine protease 2 Homo sapiens 68-75 35578172-12 2022 The critical finding is that compared to Genistein, Quercetin exhibits higher binding affinity with the catalytic unit of TMPRSS2 and forms a stable complex with the target. Genistein 41-50 transmembrane serine protease 2 Homo sapiens 122-129 35578172-12 2022 The critical finding is that compared to Genistein, Quercetin exhibits higher binding affinity with the catalytic unit of TMPRSS2 and forms a stable complex with the target. Quercetin 52-61 transmembrane serine protease 2 Homo sapiens 122-129 35504352-0 2022 Transmembrane serine protease 2 (TMPRSS2) proteolytically activates the epithelial sodium channel (ENaC) by cleaving the channel"s gamma-subunit. Sodium 83-89 transmembrane serine protease 2 Homo sapiens 0-31 35549865-9 2022 Of interest, restoration of NO by L-arginine may attenuate SARS-CoV-2 infection through different mechanisms, including reduction binding of SARS-CoV-2 to ACE2, inhibition of transmembrane protease serine type 2 (TMPRSS2) a critical for activation of SARS-CoV-2 spike protein and cellular entry, inhibition proliferation and replication of SARS-CoV-2, and prevention of SARS-CoV-2-induced coagulopathy. Arginine 34-44 transmembrane serine protease 2 Homo sapiens 213-220 35521985-6 2022 Bromhexine is a specific TMPRSS2 inhibitor that potentially inhibits the infectivity cycle of SARS-CoV-2. Bromhexine 0-10 transmembrane serine protease 2 Homo sapiens 25-32 35521985-8 2022 The findings of these studies have shown that bromhexine is effective in improving the clinical outcomes of COVID-19 and has prophylactic effects by inhibiting TMPRSS2 and viral penetration into the host cells. Bromhexine 46-56 transmembrane serine protease 2 Homo sapiens 160-167 35104687-1 2022 BACKGROUND: The human protein transmembrane protease serine type 2 (TMPRSS2) plays a key role in SARS-CoV-2 infection, as it is required to activate the virus" spike protein, facilitating entry into target cells. Serine 53-59 transmembrane serine protease 2 Homo sapiens 68-75 35104687-13 2022 Moreover, our results identify TMPRSS2 as a promising drug target, with a potential role for camostat mesilate, a drug approved for the treatment of chronic pancreatitis and postoperative reflux esophagitis, in the treatment of COVID-19. camostat 93-110 transmembrane serine protease 2 Homo sapiens 31-38 35344983-4 2022 Attractive pharmacological targets to impede viral entry include type-II transmembrane serine proteases (TTSPs), such as TMPRSS2, whose essential role in the virus lifecycle is to cleave the viral spike protein to expose the fusion peptide for cell entry5,6. Serine 87-93 transmembrane serine protease 2 Homo sapiens 121-128 35504352-0 2022 Transmembrane serine protease 2 (TMPRSS2) proteolytically activates the epithelial sodium channel (ENaC) by cleaving the channel"s gamma-subunit. Sodium 83-89 transmembrane serine protease 2 Homo sapiens 33-40 35631327-4 2022 The catalytic activity of TMPRSS2 can be blocked by the trypsin-like serine protease inhibitor camostat, which impairs infection by SARS-CoV-2. Serine 69-75 transmembrane serine protease 2 Homo sapiens 26-33 35412356-1 2022 The SARS-CoV-2 coronavirus, which causes COVID-19, uses a viral surface spike protein for host cell entry and the human cell-surface transmembrane serine protease, TMPRSS2, to process the spike protein. Serine 147-153 transmembrane serine protease 2 Homo sapiens 164-171 35412356-5 2022 For camostat 200 mg dosed four times daily, 90% inhibition of TMPRSS2 is predicted to occur but with only about 40% viral entry inhibition. camostat 4-12 transmembrane serine protease 2 Homo sapiens 62-69 35412356-13 2022 The present work used a one-compartment pharmacokinetic (PK)/pharmacodynamic (PD) mathematical model for camostat and the active metabolite FOY-251, incorporating TMPRSS2 reversible covalent inhibition by FOY-251, and empirical equations linking TMPRSS2 inhibition of SARS-CoV-2 cell entry. Gabexate 140-143 transmembrane serine protease 2 Homo sapiens 163-170 35412405-1 2022 INTRODUCTION: The main route of transmission of SARS-CoV-2 is the upper respiratory tract via cell membranes, including angiotensin-converting enzyme 2 (ACE2) and transmembrane host-associated serine protease transmembrane serine protease 2 (TMPRSS2). Serine 193-199 transmembrane serine protease 2 Homo sapiens 242-249 35412405-1 2022 INTRODUCTION: The main route of transmission of SARS-CoV-2 is the upper respiratory tract via cell membranes, including angiotensin-converting enzyme 2 (ACE2) and transmembrane host-associated serine protease transmembrane serine protease 2 (TMPRSS2). Serine 223-229 transmembrane serine protease 2 Homo sapiens 242-249 35458558-3 2022 Furthermore, the expression patterns of SARS-CoV-2 entry factors, such as the receptor angiotensin-converting enzyme 2 (ACE2), as well as transmembrane protease serine subtype 2 (TMPRSS2) and cathepsin L (CTSL), cellular proteases involved in SARS-CoV-2 spike protein activation, are largely unexplored in most species. Serine 161-167 transmembrane serine protease 2 Homo sapiens 179-186 35440617-0 2022 Author Correction: Enoxaparin augments alpha-1-antitrypsin inhibition of TMPRSS2, a promising drug combination against COVID-19. Enoxaparin 19-29 transmembrane serine protease 2 Homo sapiens 73-80 35455738-2 2022 Angiotensin-Converting Enzyme 2 (ACE2) and TransMembrane Protease Serine S1 member 2 (TMPRSS2) are enzymes that play crucial roles in SARS-CoV-2 entry into human host cells. Serine 66-72 transmembrane serine protease 2 Homo sapiens 86-93 35338216-0 2022 Enoxaparin augments alpha-1-antitrypsin inhibition of TMPRSS2, a promising drug combination against COVID-19. Enoxaparin 0-10 transmembrane serine protease 2 Homo sapiens 54-61 35455823-3 2022 Furthermore, spironolactone, a type of MRA, has been suggested to have a beneficial effect on SARS-CoV-2 outcomes through its dual action as an MRA and antiandrogen, resulting in reduced transmembrane protease receptor serine type 2 (TMPRSS2)-related viral entry to host cells. Spironolactone 13-27 transmembrane serine protease 2 Homo sapiens 234-241 35338216-8 2022 In conclusion, enoxaparin enhances AAT inhibition of both TMPRSS2 and coronavirus infection. Enoxaparin 15-25 transmembrane serine protease 2 Homo sapiens 58-65 35455942-4 2022 Here, we show for the first time that deficiency or pharmacological inhibition of the cellular lysine-methyltransferase SMYD2 decreases TMPRSS2 expression on both mRNA and protein levels. Lysine 95-101 transmembrane serine protease 2 Homo sapiens 136-143 35378747-3 2022 While ACE2 and TMPRSS2 genes are upregulated in the cortex of alcohol-dependent individuals, information on expression in specific brain regions and neural populations implicated in SARS-CoV-2 neuroinvasion, particularly monoaminergic neurons, is limited. Alcohols 62-69 transmembrane serine protease 2 Homo sapiens 15-22 35378747-4 2022 We sought to clarify how chronic alcohol exposure affects ACE2 and TMPRSS2 expression in monoaminergic brainstem circuits and other putative SARS-CoV-2 entry points. Alcohols 33-40 transmembrane serine protease 2 Homo sapiens 67-74 35378747-9 2022 Whereas ACE2 was detected in most brain regions, TMPRSS2 was only detected in the olfactory bulb and DRN but was not significantly altered after CIE. Our results suggest that previous alcohol exposure may increase the risk of SARS-CoV-2 neuroinvasion and render brain circuits involved in cardiovascular and respiratory function as well as emotional processing more vulnerable to infection, making adverse outcomes more likely. Alcohols 184-191 transmembrane serine protease 2 Homo sapiens 49-56 35331159-1 2022 BACKGROUND: Host factors such as angiotensin-converting enzyme 2 (ACE2) and the transmembrane protease, serine-subtype-2 (TMPRSS2) are important factors for SARS-CoV-2 infection. Serine 104-110 transmembrane serine protease 2 Homo sapiens 122-129 35338216-1 2022 The cell surface serine protease Transmembrane Protease 2 (TMPRSS2) is required to cleave the spike protein of SARS-CoV-2 for viral entry into cells. Serine 17-23 transmembrane serine protease 2 Homo sapiens 59-66 35331159-3 2022 METHODS: We investigated telmisartan, linagliptin and empagliflozin induced effects on renal and cardiac expression of ACE2, TMPRSS2 and key enzymes involved in RAAS (REN, AGTR2, AGT) under high-salt conditions in a non-diabetic experimental 5/6 nephrectomy (5/6 Nx) model. Linagliptin 38-49 transmembrane serine protease 2 Homo sapiens 125-132 35338216-2 2022 We determined whether negatively-charged heparin enhanced TMPRSS2 inhibition by alpha-1-antitrypsin (AAT). Heparin 41-48 transmembrane serine protease 2 Homo sapiens 58-65 35338216-5 2022 Detailed molecular modeling was undertaken with the heparin-TMPRSS2-AAT ternary complex. Heparin 52-59 transmembrane serine protease 2 Homo sapiens 60-67 35331159-3 2022 METHODS: We investigated telmisartan, linagliptin and empagliflozin induced effects on renal and cardiac expression of ACE2, TMPRSS2 and key enzymes involved in RAAS (REN, AGTR2, AGT) under high-salt conditions in a non-diabetic experimental 5/6 nephrectomy (5/6 Nx) model. empagliflozin 54-67 transmembrane serine protease 2 Homo sapiens 125-132 35338216-6 2022 Enoxaparin enhanced AAT inhibition of both TMPRSS2 activity and infection of hAEc with HCoV-229E. Enoxaparin 0-10 transmembrane serine protease 2 Homo sapiens 43-50 35338216-7 2022 Underlying these findings, detailed molecular modeling revealed that: (i) the reactive center loop of AAT adopts an inhibitory-competent conformation compared with the crystal structure of TMPRSS2 bound to an exogenous (nafamostat) or endogenous (HAI-2) TMPRSS2 inhibitor and (ii) negatively-charged heparin bridges adjacent electropositive patches at the TMPRSS2-AAT interface, neutralizing otherwise repulsive forces. Heparin 300-307 transmembrane serine protease 2 Homo sapiens 189-196 35277472-2 2022 Here, we show AKT serine/threonine kinase-dependent epigenetic control of ACE2 and TMPRSS2 expression by high-cannabidiol (CBD) cannabis extracts and their individual components. Serine 18-24 transmembrane serine protease 2 Homo sapiens 83-90 35294338-7 2022 The mechanism of the protease inhibitors nafamostat and camostat may extend beyond inhibition of TMPRSS2 to coagulation-induced spike cleavage. nafamostat 41-51 transmembrane serine protease 2 Homo sapiens 97-104 35345416-2 2022 Coronaviruses, as well as influenza viruses, depend on host type 2 transmembrane serine protease, TMPRSS2, for entry and propagation in the human cell. Serine 81-87 transmembrane serine protease 2 Homo sapiens 98-105 35345416-11 2022 Among these hits, ZINC000143375720 shows the most stable binding interaction with TMPRSS2. zinc000143375720 18-34 transmembrane serine protease 2 Homo sapiens 82-89 35320487-2 2022 So far, it is known that severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) primarily infects the type II pneumocytes in humans, with the help of transmembrane serine protease type 2 (TMPRSS2). Serine 170-176 transmembrane serine protease 2 Homo sapiens 194-201 35301316-5 2022 The biological and pathological importance of these RG4s is then exemplified by a canonical 3-quartet RG4 within Tmprss2, which can inhibit Tmprss2 translation and prevent SARS-CoV-2 entry. RG-4 52-56 transmembrane serine protease 2 Homo sapiens 113-120 35301316-5 2022 The biological and pathological importance of these RG4s is then exemplified by a canonical 3-quartet RG4 within Tmprss2, which can inhibit Tmprss2 translation and prevent SARS-CoV-2 entry. RG-4 52-56 transmembrane serine protease 2 Homo sapiens 140-147 35301316-5 2022 The biological and pathological importance of these RG4s is then exemplified by a canonical 3-quartet RG4 within Tmprss2, which can inhibit Tmprss2 translation and prevent SARS-CoV-2 entry. RG-4 102-105 transmembrane serine protease 2 Homo sapiens 113-120 35301316-5 2022 The biological and pathological importance of these RG4s is then exemplified by a canonical 3-quartet RG4 within Tmprss2, which can inhibit Tmprss2 translation and prevent SARS-CoV-2 entry. RG-4 102-105 transmembrane serine protease 2 Homo sapiens 140-147 35359837-6 2022 ACE2 and transmembrane serine proteinase 2 (TMPRSS2) mRNA were expressed in ALI and airway organoids at levels similar to those of native (i.e., non-cultured) human bronchial epithelial cells, whereas furin expression was more faithfully represented in ALI. Serine 23-29 transmembrane serine protease 2 Homo sapiens 44-51 35277472-2 2022 Here, we show AKT serine/threonine kinase-dependent epigenetic control of ACE2 and TMPRSS2 expression by high-cannabidiol (CBD) cannabis extracts and their individual components. high-cannabidiol 105-121 transmembrane serine protease 2 Homo sapiens 83-90 35277472-2 2022 Here, we show AKT serine/threonine kinase-dependent epigenetic control of ACE2 and TMPRSS2 expression by high-cannabidiol (CBD) cannabis extracts and their individual components. Cannabidiol 123-126 transmembrane serine protease 2 Homo sapiens 83-90 35277472-5 2022 CBD and terpene PTWT2.2 profoundly inhibited ACE2 and TMPRSS2 expression, both individually and in combination. Cannabidiol 0-3 transmembrane serine protease 2 Homo sapiens 54-61 35277472-5 2022 CBD and terpene PTWT2.2 profoundly inhibited ACE2 and TMPRSS2 expression, both individually and in combination. Terpenes 8-15 transmembrane serine protease 2 Homo sapiens 54-61 35072549-5 2022 Two known TMPRSS2 inhibitors, namely camostat and nafamostat, approved drugs for the treatment of pancreatitis, are under clinical trials as potential drugs against COVID-19. camostat 37-45 transmembrane serine protease 2 Homo sapiens 10-17 35170548-1 2022 Transmembrane serine proteinase 2 (TMPRSS2), which is an essential serine protease for priming spike protein of SARS-CoV-2, was found in low expression in many cancer tissue including lung cancer. Serine 14-20 transmembrane serine protease 2 Homo sapiens 35-42 35072549-5 2022 Two known TMPRSS2 inhibitors, namely camostat and nafamostat, approved drugs for the treatment of pancreatitis, are under clinical trials as potential drugs against COVID-19. nafamostat 50-60 transmembrane serine protease 2 Homo sapiens 10-17 34862332-2 2022 Angiotensin-converting enzyme-2 (ACE2) is the receptor responsible for coronavirus binding, while subsequent cell entry relies on priming by the serine protease TMPRSS2 (transmembrane protease, serine 2). Serine 145-151 transmembrane serine protease 2 Homo sapiens 161-168 35101449-7 2022 Furthermore, one TFQ derivative, compound 7, showed a better therapeutic index than TFQ on TMPRSS2, and may therefore inhibit the infectibility of SARS-CoV-2, including that of several mutant variants. tafenoquine 17-20 transmembrane serine protease 2 Homo sapiens 91-98 35101449-7 2022 Furthermore, one TFQ derivative, compound 7, showed a better therapeutic index than TFQ on TMPRSS2, and may therefore inhibit the infectibility of SARS-CoV-2, including that of several mutant variants. tafenoquine 84-87 transmembrane serine protease 2 Homo sapiens 91-98 34862332-2 2022 Angiotensin-converting enzyme-2 (ACE2) is the receptor responsible for coronavirus binding, while subsequent cell entry relies on priming by the serine protease TMPRSS2 (transmembrane protease, serine 2). Serine 194-200 transmembrane serine protease 2 Homo sapiens 161-168 35226423-1 2022 BACKGROUND: Angiotensin-converting enzyme 2 (ACE2) and transmembrane protease serine subtype 2 (TMPRSS2) are key proteins mediating viral entry of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Serine 78-84 transmembrane serine protease 2 Homo sapiens 96-103 35046573-3 2022 Several mAbs (LY-CoV555, LY-CoV016, REGN10933, REGN10987 and CT-P59) completely lost neutralizing activity against B.1.1.529 virus in both Vero-TMPRSS2 and Vero-hACE2-TMPRSS2 cells, whereas others were reduced (COV2-2196 and COV2-2130 combination, ~12-fold decrease) or minimally affected (S309). Lysine 14-16 transmembrane serine protease 2 Homo sapiens 144-151 35046573-3 2022 Several mAbs (LY-CoV555, LY-CoV016, REGN10933, REGN10987 and CT-P59) completely lost neutralizing activity against B.1.1.529 virus in both Vero-TMPRSS2 and Vero-hACE2-TMPRSS2 cells, whereas others were reduced (COV2-2196 and COV2-2130 combination, ~12-fold decrease) or minimally affected (S309). Lysine 14-16 transmembrane serine protease 2 Homo sapiens 167-174 35193695-1 2022 OBJECTIVE: To determine the effect of polymorphisms and mutations in angiotensin-converting enzyme 2 (ACE2) and Type 2 transmembrane serine proteases (TMPRSS2) genes on susceptibility to corona virus disease 2019 (COVID-19) and patient prognosis. Serine 133-139 transmembrane serine protease 2 Homo sapiens 151-158 35269785-6 2022 In this work, a combination of experimental methods (biochemical inhibition assays, surface plasmon resonance, and quartz crystal microbalance with dissipation monitoring) confirms the potential role of TA in the prevention of SARS-CoV-2 infectivity through the inhibition of extracellular RBD/ACE2 interactions and TMPRSS2 and 3CLpro activity. Tannins 203-205 transmembrane serine protease 2 Homo sapiens 316-323 35215982-2 2022 Nafamostat, a potent TMPRSS2 inhibitor as well as a candidate for anti-SARS-CoV-2 drug, possesses the same acyl substructure as camostat, but is known to have a greater antiviral effect. nafamostat 0-10 transmembrane serine protease 2 Homo sapiens 21-28 35157239-7 2022 Out of selected phytoconstituents, vicenin 2, rosmarinic acid, and orientin were found to have the highest efficacy in terms of molecular interaction and drug-likeness properties against ACE2 and TMPRSS2 host receptor proteins. rosmarinic acid 46-61 transmembrane serine protease 2 Homo sapiens 196-203 35215982-3 2022 A unique aspect of the molecular binding of nafamostat has been recently reported to be the formation of a covalent bond between its acyl substructure and Ser441 in TMPRSS2. nafamostat 44-54 transmembrane serine protease 2 Homo sapiens 165-172 35215982-5 2022 In silico analysis showed that Asp435 significantly contributes to the binding of nafamostat and camostat to TMPRSS2, while Glu299 interacts strongly only with nafamostat. nafamostat 82-92 transmembrane serine protease 2 Homo sapiens 109-116 35215982-6 2022 The estimated binding affinity for each compound with TMPRSS2 was actually consistent with the higher activity of nafamostat; however, the evaluation of the newly synthesized nafamostat derivatives revealed that the predicted binding affinity did not correlate with their anti-SARS-CoV-2 activity measured by the cytopathic effect (CPE) inhibition assay. nafamostat 114-124 transmembrane serine protease 2 Homo sapiens 54-61 35215982-8 2022 These results strongly indicate that the ease of covalent bond formation with Ser441 in TMPRSS2 possibly plays a major role in the anti-SARS-CoV-2 effect of nafamostat and its derivatives. nafamostat 157-167 transmembrane serine protease 2 Homo sapiens 88-95 35063125-6 2022 Moreover, entry of SARS-CoV-2 into BCECs could be reduced by anti-spike-, anti-angiotensin-converting enzyme 2 (ACE2)-, and anti-neuropilin-1 (NRP1)-specific antibodies or the transmembrane protease serine subtype 2 (TMPRSS2) inhibitor nafamostat. Serine 199-205 transmembrane serine protease 2 Homo sapiens 217-224 35063125-6 2022 Moreover, entry of SARS-CoV-2 into BCECs could be reduced by anti-spike-, anti-angiotensin-converting enzyme 2 (ACE2)-, and anti-neuropilin-1 (NRP1)-specific antibodies or the transmembrane protease serine subtype 2 (TMPRSS2) inhibitor nafamostat. nafamostat 236-246 transmembrane serine protease 2 Homo sapiens 217-224 35079032-0 2022 Ozone exposure upregulates the expression of host susceptibility protein TMPRSS2 to SARS-CoV-2. Ozone 0-5 transmembrane serine protease 2 Homo sapiens 73-80 35103351-0 2022 Estradiol reduces ACE2 and TMPRSS2 mRNA levels in A549 human lung epithelial cells. Estradiol 0-9 transmembrane serine protease 2 Homo sapiens 27-34 35103351-3 2022 SARS-CoV-2 infects respiratory tract epithelial cells by binding to their cell membrane ACE2, followed by priming for cell entry by the host cell membrane serine protease TMPRSS2. Serine 155-161 transmembrane serine protease 2 Homo sapiens 171-178 35103351-6 2022 Treatment of A549 human lung epithelial cells with 17-beta-estradiol reduced the cellular mRNA levels of ACE2 and TMPRSS2 mRNA, while not affecting FURIN expression. Estradiol 51-68 transmembrane serine protease 2 Homo sapiens 114-121 35103351-8 2022 Studies into the molecular pathways by which 17-beta-estradiol reduces ACE2 and TMPRSS2 mRNA expression in lung epithelial cells are needed for assessing its potential protective value against severe Covid-19. Estradiol 45-62 transmembrane serine protease 2 Homo sapiens 80-87 35160229-0 2022 Angiotensin-Converting Enzyme 2 (ACE2), Transmembrane Peptidase Serine 2 (TMPRSS2), and Furin Expression Increases in the Lungs of Patients with Idiopathic Pulmonary Fibrosis (IPF) and Lymphangioleiomyomatosis (LAM): Implications for SARS-CoV-2 (COVID-19) Infections. Serine 64-70 transmembrane serine protease 2 Homo sapiens 74-81 35103059-1 2022 Background: Bromhexine hydrochloride has been suggested as a TMPRSS2 protease blocker that precludes the penetration of SARS-CoV-2 into cells. Bromhexine 12-36 transmembrane serine protease 2 Homo sapiens 61-68 35154056-6 2022 By contrast, an important SARS-CoV-2 infection-associated factor, type II transmembrane serine protease (TMPRSS2), was poorly expressed in placenta. Serine 88-94 transmembrane serine protease 2 Homo sapiens 105-112 35039793-7 2022 The receptor ACE2 mediates the entry of SARS-CoV-2 into the host cells, whereas the serine protease TMPRSS2 primes the viral S protein. Serine 84-90 transmembrane serine protease 2 Homo sapiens 100-107 35039793-8 2022 In this study, Metadichol was found to be 270 times more potent an inhibitor of TMPRSS2 (EC50 = 96 ng/mL) than camostat mesylate (EC50 = 26000 ng/mL). metadichol 15-25 transmembrane serine protease 2 Homo sapiens 81-88 35017320-12 2022 KEGG and GO analyses and GSEA implied that multiple immune- and metabolism-related pathways were significantly linked with TMPRSS2 expression. gsea 25-29 transmembrane serine protease 2 Homo sapiens 123-130 35128036-2 2022 Because the androgen-responsive serine protease TMPRSS2 is involved in cleaving the SARS-CoV-2 spike protein allowing the virus to enter the cell, therefore, direct TMPRSS2 inhibition will inhibit virus activation and disease progression which make it an important target for drug discovery. Serine 32-38 transmembrane serine protease 2 Homo sapiens 48-55 34997794-2 2022 Published data revealed associations of COVID-19 susceptibility and severity with host genetic polymorphisms in renin-angiotensin-aldosterone system (RAAS)-related genes including angiotensin-converting enzyme (ACE)1, ACE2, and transmembrane protease (TMPRSS)2. Aldosterone 130-141 transmembrane serine protease 2 Homo sapiens 228-260 34983356-10 2022 However, the combination of dipeptidyl peptidase-4 (DDP4) inhibitors and spironolactone/eplerenone seems to be more effective by reducing soluble ACE2 level, antagonizing TMPRSS2, maintaining ACE2 on cell membrane and reducing risk of viral entry into the cells. Spironolactone 73-87 transmembrane serine protease 2 Homo sapiens 171-178 34983356-10 2022 However, the combination of dipeptidyl peptidase-4 (DDP4) inhibitors and spironolactone/eplerenone seems to be more effective by reducing soluble ACE2 level, antagonizing TMPRSS2, maintaining ACE2 on cell membrane and reducing risk of viral entry into the cells. Eplerenone 88-98 transmembrane serine protease 2 Homo sapiens 171-178 35128036-2 2022 Because the androgen-responsive serine protease TMPRSS2 is involved in cleaving the SARS-CoV-2 spike protein allowing the virus to enter the cell, therefore, direct TMPRSS2 inhibition will inhibit virus activation and disease progression which make it an important target for drug discovery. Serine 32-38 transmembrane serine protease 2 Homo sapiens 165-172