PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 32819975-11 2020 The ability of FUS+GEM to control primary tumor outgrowth was moderately enhanced by either neoadjuvant or adjuvant treatment with anti-PD-1. fusarubin 15-18 programmed cell death 1 Mus musculus 136-140 32662325-3 2021 Upon the sulfamide drug adsorption onto the stated nanocages, the energy levels of the highest occupied molecular orbital (HOMO) and the lowest unoccupied molecular orbital (LUMO) were significantly changed, resulting in a decrease in the values of bandgap (E g) that caused enhance in their electrical conductivity. fusarubin 9-18 ras homolog family member G Homo sapiens 22-23 32662325-5 2021 Finally, The QTAIM analysis was investigated for both types of structural aspects and electronic properties (such as rho, " " ^"2" rho, G(r), V (r) and H(r)) associated with adsorption of sulfamide molecule on the stated nanocages. fusarubin 188-197 ras homolog family member G Homo sapiens 131-137 32656213-6 2020 We demonstrate that FUS may directly stimulate mechanosensory PANX1 localized in endoplasmic reticulum to evoke calcium release from internal stores. fusarubin 20-23 pannexin 1 Homo sapiens 62-67 32028085-4 2020 In this study, we demonstrated that FUS increases MSC transplantation into brain tissue by >2-fold, and that this finding might be related to the activation of intercellular adhesion molecule-1 in endothelial and subendothelial cells and vascular adhesion molecule-1 in endothelial cells. fusarubin 36-39 intercellular adhesion molecule 1 Homo sapiens 160-193 32492056-4 2020 Building on this established technique, we propose to develop FUS-enabled liquid biopsy technique (FUS-LBx) to enhance the release of brain tumor biomarkers (e.g., DNA, RNA, and proteins) into the circulation. fusarubin 62-65 labial homeobox homolog Mus musculus 103-106 32492056-12 2020 This study suggests that FUS-LBx could be a safe and effective brain-tumor biomarker release technique, and MRI could be used to develop image-guided FUS-LBx. fusarubin 25-28 labial homeobox homolog Mus musculus 29-32 32492056-12 2020 This study suggests that FUS-LBx could be a safe and effective brain-tumor biomarker release technique, and MRI could be used to develop image-guided FUS-LBx. fusarubin 150-153 labial homeobox homolog Mus musculus 154-157 32361864-7 2020 Caspase 3 induction in C6 cells relative to control showed increases of 109%, 110%, and 278% for 5-ALA, FUS, and SDT groups, respectively (p < 0.05). fusarubin 104-107 caspase 3 Homo sapiens 0-9 32361864-8 2020 For the C6 cells, caspase 3 staining positivity was 2.1%, 6.7%, 11.2%, and 39.8% for control, 5-ALA, FUS, and SDT groups, respectively. fusarubin 101-104 caspase 3 Homo sapiens 18-27 32270718-7 2020 The expression of P16 and Ki-67 in the treated cervical tissues was significantly lower than that before treatment, and the expression of Fas was found up-regulated (all p < .05).Conclusion: FUS therapy appears to be a feasible and effective treatment for patients with HPV positive CIN1. fusarubin 191-194 cyclin dependent kinase inhibitor 2A Homo sapiens 18-21 32206098-8 2020 Results: CRT-NP plus FUS (CFUS) upregulated CRT expression, expanded the population of melanoma TRP-2 specific functional CD4+ and CD8+ T cells and tumor-suppressing M1 phenotype, and increased PD-1 and PD-L1 marker expression in the T cells. fusarubin 21-24 tRNA proline 2 Mus musculus 96-101 32206098-8 2020 Results: CRT-NP plus FUS (CFUS) upregulated CRT expression, expanded the population of melanoma TRP-2 specific functional CD4+ and CD8+ T cells and tumor-suppressing M1 phenotype, and increased PD-1 and PD-L1 marker expression in the T cells. fusarubin 21-24 CD274 antigen Mus musculus 203-208 31575487-10 2020 Western blotting was used to evaluate the correlation between FUS-induced epileptic suppression and the PI3K-mTOR signaling pathway. fusarubin 62-65 mechanistic target of rapamycin kinase Rattus norvegicus 109-113 32270718-8 2020 FUS therapy may help to reduce the expression of p16 and Ki-67 and enhance the expression of Fas in the treated cervical tissues to regulate cell proliferation and increase apoptosis, and thus prevent the disease from evolving into high grade lesions. fusarubin 0-3 cyclin dependent kinase inhibitor 2A Homo sapiens 49-52 31065903-5 2019 RESULTS: IL-8 levels were significantly higher in the AqH of patients with BU and FUS than in the AqH of control subjects (p < 0.001 and p < 0.001, respectively). fusarubin 82-85 C-X-C motif chemokine ligand 8 Homo sapiens 9-13 31508507-6 2019 Several compounds (phenylarsonic acid, phenylbaronic acid, sulfamide) exhibited favorable Kis for SmCA versus two human isoforms. fusarubin 59-68 U2AF homology motif kinase 1 Homo sapiens 90-93 29339208-5 2018 Next, we demonstrated that FUS-aided MB-shBirc5-lipo-NGR exhibited a higher transfection efficiency compared with the control group. fusarubin 27-30 reticulon 4 receptor Homo sapiens 53-56 31470629-8 2019 The effects of FUS were more potent than those of AFU, with FUS up-regulating p21 expression in a p53-dependent manner, as detected by Western blot analyses, likely the consequence of decreased ERK phosphorylation and increased p38 expression (both of which increase p21 stability). fusarubin 15-18 H3 histone pseudogene 16 Homo sapiens 78-81 31470629-8 2019 The effects of FUS were more potent than those of AFU, with FUS up-regulating p21 expression in a p53-dependent manner, as detected by Western blot analyses, likely the consequence of decreased ERK phosphorylation and increased p38 expression (both of which increase p21 stability). fusarubin 15-18 tumor protein p53 Homo sapiens 98-101 31470629-8 2019 The effects of FUS were more potent than those of AFU, with FUS up-regulating p21 expression in a p53-dependent manner, as detected by Western blot analyses, likely the consequence of decreased ERK phosphorylation and increased p38 expression (both of which increase p21 stability). fusarubin 15-18 mitogen-activated protein kinase 1 Homo sapiens 194-197 31470629-8 2019 The effects of FUS were more potent than those of AFU, with FUS up-regulating p21 expression in a p53-dependent manner, as detected by Western blot analyses, likely the consequence of decreased ERK phosphorylation and increased p38 expression (both of which increase p21 stability). fusarubin 15-18 mitogen-activated protein kinase 14 Homo sapiens 228-231 31470629-8 2019 The effects of FUS were more potent than those of AFU, with FUS up-regulating p21 expression in a p53-dependent manner, as detected by Western blot analyses, likely the consequence of decreased ERK phosphorylation and increased p38 expression (both of which increase p21 stability). fusarubin 15-18 H3 histone pseudogene 16 Homo sapiens 267-270 31470629-8 2019 The effects of FUS were more potent than those of AFU, with FUS up-regulating p21 expression in a p53-dependent manner, as detected by Western blot analyses, likely the consequence of decreased ERK phosphorylation and increased p38 expression (both of which increase p21 stability). fusarubin 60-63 H3 histone pseudogene 16 Homo sapiens 78-81 31470629-8 2019 The effects of FUS were more potent than those of AFU, with FUS up-regulating p21 expression in a p53-dependent manner, as detected by Western blot analyses, likely the consequence of decreased ERK phosphorylation and increased p38 expression (both of which increase p21 stability). fusarubin 60-63 tumor protein p53 Homo sapiens 98-101 31470629-8 2019 The effects of FUS were more potent than those of AFU, with FUS up-regulating p21 expression in a p53-dependent manner, as detected by Western blot analyses, likely the consequence of decreased ERK phosphorylation and increased p38 expression (both of which increase p21 stability). fusarubin 60-63 mitogen-activated protein kinase 14 Homo sapiens 228-231 31470629-8 2019 The effects of FUS were more potent than those of AFU, with FUS up-regulating p21 expression in a p53-dependent manner, as detected by Western blot analyses, likely the consequence of decreased ERK phosphorylation and increased p38 expression (both of which increase p21 stability). fusarubin 60-63 H3 histone pseudogene 16 Homo sapiens 267-270 31470629-9 2019 FUS also decreased Akt phosphorylation and resulted in increased Fas ligand production and caspase-8/3-dependent apoptosis. fusarubin 0-3 AKT serine/threonine kinase 1 Homo sapiens 19-22 31470629-9 2019 FUS also decreased Akt phosphorylation and resulted in increased Fas ligand production and caspase-8/3-dependent apoptosis. fusarubin 0-3 Fas ligand Homo sapiens 65-75 31470629-9 2019 FUS also decreased Akt phosphorylation and resulted in increased Fas ligand production and caspase-8/3-dependent apoptosis. fusarubin 0-3 caspase 8 Homo sapiens 91-102 30981691-4 2019 Taking our previously discovered CXCR4 modulator RB-108 as the lead compound, a series of derivatives were synthesized structurally modifying and optimizing the amide and sulfamide side chains. fusarubin 171-180 C-X-C motif chemokine receptor 4 Rattus norvegicus 33-38 31057396-5 2019 The potential molecular mechanism of FUS assisting NK cell therapy was also initially explored through evaluating the expression of ICAM1 and CX3CL1 by qRT-PCR. fusarubin 37-40 intercellular adhesion molecule 1 Homo sapiens 132-137 31057396-5 2019 The potential molecular mechanism of FUS assisting NK cell therapy was also initially explored through evaluating the expression of ICAM1 and CX3CL1 by qRT-PCR. fusarubin 37-40 C-X3-C motif chemokine ligand 1 Homo sapiens 142-148 31057396-7 2019 The qRT-PCR results also showed that CX3CL1 may be involved in the process of FUS-assisted NK cell infiltration. fusarubin 78-81 C-X3-C motif chemokine ligand 1 Homo sapiens 37-43 30074266-4 2018 The synthesized sulfamide/phenolic sulfamide derivatives were investigated as cholinesterase inhibitors and their relative role in AChE versus BChE inhibition was defined. fusarubin 16-25 butyrylcholinesterase Homo sapiens 78-92 30074266-4 2018 The synthesized sulfamide/phenolic sulfamide derivatives were investigated as cholinesterase inhibitors and their relative role in AChE versus BChE inhibition was defined. fusarubin 16-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 131-135 30074266-4 2018 The synthesized sulfamide/phenolic sulfamide derivatives were investigated as cholinesterase inhibitors and their relative role in AChE versus BChE inhibition was defined. fusarubin 16-25 butyrylcholinesterase Homo sapiens 143-147 30150769-6 2018 In this study, we aimed to evaluate whether the use of FUS-induced BBB opening to enhance GSK-3 inhibitor delivery, which would bring additive effect of Abeta plaque clearance by FUS with the reduction of Abeta plaque synthesis by GSK-3 inhibitor in an AD mice model. fusarubin 55-58 glycogen synthase kinase 3 beta Mus musculus 90-95 30150769-6 2018 In this study, we aimed to evaluate whether the use of FUS-induced BBB opening to enhance GSK-3 inhibitor delivery, which would bring additive effect of Abeta plaque clearance by FUS with the reduction of Abeta plaque synthesis by GSK-3 inhibitor in an AD mice model. fusarubin 55-58 glycogen synthase kinase 3 beta Mus musculus 231-236 30150769-6 2018 In this study, we aimed to evaluate whether the use of FUS-induced BBB opening to enhance GSK-3 inhibitor delivery, which would bring additive effect of Abeta plaque clearance by FUS with the reduction of Abeta plaque synthesis by GSK-3 inhibitor in an AD mice model. fusarubin 179-182 glycogen synthase kinase 3 beta Mus musculus 90-95 30150769-7 2018 FUS-induced BBB opening on APPswe/PSEN1-dE9 transgenic mice was performed unilaterally, with the contralateral hemisphere serving as a reference. fusarubin 0-3 presenilin 1 Mus musculus 34-39 29109793-4 2017 Methods: Differential expression of NFkappaB signaling pathway genes was assessed in rats at 6 h and 4 days following a FUS-mediated increase in BBB permeability. fusarubin 120-123 nuclear factor kappa B subunit 1 Homo sapiens 36-44 28738704-4 2017 The comparison with the structure of hCA II in complex with its sulphamide analogue revealed that the two inhibitors adopt a completely different binding mode within the hCA II active site. fusarubin 64-74 carbonic anhydrase 2 Homo sapiens 37-43 28738704-4 2017 The comparison with the structure of hCA II in complex with its sulphamide analogue revealed that the two inhibitors adopt a completely different binding mode within the hCA II active site. fusarubin 64-74 carbonic anhydrase 2 Homo sapiens 170-176 27749053-0 2016 Sulfamide as Zinc Binding Motif in Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa). fusarubin 0-9 carboxypeptidase B2 Homo sapiens 74-117 28511006-7 2017 After only a single treatment, our strategy led to therapeutically relevant levels of GDNF protein content in the FUS-targeted regions in the striatum of the 6-OHDA-induced rat model of PD, which lasted at least up to 10 weeks. fusarubin 114-117 glial cell derived neurotrophic factor Rattus norvegicus 86-90 27345430-5 2016 Immunohistochemistry staining of BDNF revealed that FUS-enhanced IN delivery achieved similar locally enhanced delivery as the established FUS technique. fusarubin 52-55 brain derived neurotrophic factor Mus musculus 33-37 27235980-2 2016 We have previously demonstrated that a separated gene-carrying liposome and MBs administration plus FUS exposure can deliver genes into the brain, with the successful expression of the reporter gene and glial cell line-derived neurotrophic factor (GDNF) gene. fusarubin 100-103 glial cell line derived neurotrophic factor Mus musculus 203-246 27068142-0 2016 Acetylcholinesterase and carbonic anhydrase inhibitory properties of novel urea and sulfamide derivatives incorporating dopaminergic 2-aminotetralin scaffolds. fusarubin 84-93 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-20 27563403-0 2016 Design, Synthesis, and Characterization of Sulfamide and Sulfamate Nucleotidomimetic Inhibitors of hHint1. fusarubin 43-52 histidine triad nucleotide binding protein 1 Homo sapiens 99-105 27068142-3 2016 The novel urea and sulfamide derivatives were tested for inhibition of hCA I, II and AChE enzymes. fusarubin 19-28 carbonic anhydrase 1 Homo sapiens 71-76 27068142-3 2016 The novel urea and sulfamide derivatives were tested for inhibition of hCA I, II and AChE enzymes. fusarubin 19-28 acetylcholinesterase (Cartwright blood group) Homo sapiens 85-89 26611920-4 2016 Since this sulfamide MEK inhibitor displayed an exceptionally favorable PK profile with low brain penetration potential despite being highly oral bioavailable, we elected to keep the sulfamide capping group intact while taming its unwanted off-target activity by optimizing the structural surroundings. fusarubin 11-20 mitogen-activated protein kinase kinase 7 Homo sapiens 21-24 26795114-0 2016 Sulfamide derivatives with selective carbonic anhydrase VII inhibitory action. fusarubin 0-9 carbonic anhydrase 7 Homo sapiens 37-59 26611920-4 2016 Since this sulfamide MEK inhibitor displayed an exceptionally favorable PK profile with low brain penetration potential despite being highly oral bioavailable, we elected to keep the sulfamide capping group intact while taming its unwanted off-target activity by optimizing the structural surroundings. fusarubin 183-192 mitogen-activated protein kinase kinase 7 Homo sapiens 21-24 26985287-3 2016 Potency optimization afforded two tool compounds, sulfonamide EPZ031686 and sulfamide EPZ030456, with cellular potency at a level sufficient to probe the in vitro biology of SMYD3 inhibition. fusarubin 76-85 SET and MYND domain containing 3 Mus musculus 174-179 26071631-8 2015 With longitudinal observation of IVIS monitoring, animals with FUS treatment showed significant promotion of LpDNA release into the CNS and demonstrated enhanced expression of genes upon sonication with FUS-BBB opening, while both the luciferase and GDNF protein expression were successfully measured via Western blotting. fusarubin 63-66 glial cell derived neurotrophic factor Homo sapiens 250-254 25071945-4 2014 With OCT scanning, the dynamic change in vessels during FUS exposure can be observed and studied. fusarubin 56-59 plexin A2 Homo sapiens 5-8 25586140-5 2015 The objective of the study was to investigate whether safe and efficient NTN delivery can be achieved through FUS-induced BBB opening via intravenous administration, and thus trigger the neuroregeneration cascade in the nigrostriatal pathway. fusarubin 110-113 neurturin Mus musculus 73-76 25586140-7 2015 FUS significantly enhanced the delivery of NTN compared with the direct injection technique, whereas triggering of the signaling cascade was detected downstream to the neuronal nuclei. fusarubin 0-3 neurturin Mus musculus 43-46 25921269-8 2015 These results show that hCA I, II, and AChE were effectively inhibited by the novel sulfamoylcarbamates 17-21 and sulfamide derivatives 22-26. fusarubin 114-123 carbonic anhydrase 1 Homo sapiens 24-29 25223956-6 2014 Among these compounds, the novel sulfamide derivative 17 showed the most potent inhibitory effect against hCA I (Ki : 153.88 nM), while sulfamide derivative 26 showed the highest inhibitory potential against hCA II (Ki : 117.80 nM). fusarubin 33-42 carbonic anhydrase 1 Homo sapiens 106-111 25223956-6 2014 Among these compounds, the novel sulfamide derivative 17 showed the most potent inhibitory effect against hCA I (Ki : 153.88 nM), while sulfamide derivative 26 showed the highest inhibitory potential against hCA II (Ki : 117.80 nM). fusarubin 136-145 carbonic anhydrase 2 Homo sapiens 208-214 25198897-0 2014 Design, synthesis and biological evaluation of sulfamide and triazole benzodiazepines as novel p53-MDM2 inhibitors. fusarubin 47-56 tumor protein p53 Homo sapiens 95-98 25198897-0 2014 Design, synthesis and biological evaluation of sulfamide and triazole benzodiazepines as novel p53-MDM2 inhibitors. fusarubin 47-56 MDM2 proto-oncogene Homo sapiens 99-103 24587228-7 2014 The experimental results showed that MBs/FUS significantly increased the cerebral content of EPO by bettering vascular permeability. fusarubin 41-44 erythropoietin Rattus norvegicus 93-96 24651609-11 2014 These results provide new opportunities for the development of specific PPARalpha-activating drugs focused on sulfamide derivatives with a long alkyl chain for the treatment of metabolic dysfunction. fusarubin 110-119 peroxisome proliferator activated receptor alpha Rattus norvegicus 72-81 24157370-1 2013 Introducing a sulfamide moiety to our coumarin derivatives afforded enhanced Raf/MEK inhibitory activity concomitantly with an acceptable PK profile. fusarubin 14-23 mitogen-activated protein kinase kinase 7 Homo sapiens 81-84 24224693-2 2013 Especially when a sulfonamide or sulfamide moiety was added, resulting compounds exhibited not only potent CB1R activity but also a desired tPSA value over 90 A(2), a threshold considered to possess a low probability to cross BBB, leading to the identification of compound 4 (B/P = 1/64) as a peripherally restricted CB1R antagonist. fusarubin 33-42 cannabinoid receptor 1 (brain) Mus musculus 107-111 24224693-2 2013 Especially when a sulfonamide or sulfamide moiety was added, resulting compounds exhibited not only potent CB1R activity but also a desired tPSA value over 90 A(2), a threshold considered to possess a low probability to cross BBB, leading to the identification of compound 4 (B/P = 1/64) as a peripherally restricted CB1R antagonist. fusarubin 33-42 zinc finger protein 185 Mus musculus 278-286 24224693-2 2013 Especially when a sulfonamide or sulfamide moiety was added, resulting compounds exhibited not only potent CB1R activity but also a desired tPSA value over 90 A(2), a threshold considered to possess a low probability to cross BBB, leading to the identification of compound 4 (B/P = 1/64) as a peripherally restricted CB1R antagonist. fusarubin 33-42 cannabinoid receptor 1 (brain) Mus musculus 317-321 24157370-0 2013 The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors. fusarubin 4-13 zinc fingers and homeoboxes 2 Homo sapiens 120-123 24157370-0 2013 The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors. fusarubin 4-13 mitogen-activated protein kinase kinase 7 Homo sapiens 124-127 24128000-3 2013 Crystallographic studies on the complex of hCA II with the lead sulfamide derivative of this series clarified the binding mode of this type of inhibitors in the enzyme active site cavity. fusarubin 64-73 carbonic anhydrase 2 Homo sapiens 43-49 24157370-1 2013 Introducing a sulfamide moiety to our coumarin derivatives afforded enhanced Raf/MEK inhibitory activity concomitantly with an acceptable PK profile. fusarubin 14-23 zinc fingers and homeoboxes 2 Homo sapiens 77-80 24128000-5 2013 In vivo testing of the lead molecule in the sulfamide series, in cotreatment with doxorubicin, demonstrated a chemosensitization of CA IX containing tumors. fusarubin 44-53 carbonic anhydrase 9 Homo sapiens 132-137 23707300-4 2013 We demonstrate that transcranial FUS application leads to a significant reduction in plaque burden four days after a single treatment in the TgCRND8 mouse model of AD and that endogenous antibodies are found bound to Abeta plaques. fusarubin 33-36 amyloid beta (A4) precursor protein Mus musculus 217-222 23474388-4 2013 Sulfamide 28 was identified as a highly potent MEK inhibitor with nanomolar cell potency against B-RAF (V600E) as well as Ras-mutated cell lines, high metabolic stability and resulting long half-lives. fusarubin 0-9 mitogen-activated protein kinase kinase 7 Homo sapiens 47-50 23849171-7 2013 CONCLUSIONS: A newly designed nitroimidazole and sulfamide dual targeting drug reduces hypoxic extracellular acidification, slows down tumor growth at nontoxic doses and sensitizes tumors to irradiation all in a CAIX dependent manner, suggesting no "off-target" effects. fusarubin 49-58 carbonic anhydrase 9 Homo sapiens 212-216 23543430-4 2013 Small-molecule BACE1 inhibitors of the hydroxyethylamine, hydantoin, and sulfamide classes were functionalized by biotin PEG linkers of varying lengths forming probes that were bound to streptavidin donor beads. fusarubin 73-82 beta-secretase 1 Homo sapiens 15-20 23474388-4 2013 Sulfamide 28 was identified as a highly potent MEK inhibitor with nanomolar cell potency against B-RAF (V600E) as well as Ras-mutated cell lines, high metabolic stability and resulting long half-lives. fusarubin 0-9 B-Raf proto-oncogene, serine/threonine kinase Homo sapiens 97-102 23200251-2 2013 CA VIII, X and XI thus obtained showed high catalytic activity (67.3-92.0% of the activity of hCA II and much higher compared to hCA I) and were inhibited in the milli-micromolar range by inorganic anions, sulfamide, sulfamic acid, phenylboronic acid and phenylarsonic acid. fusarubin 206-215 carbonic anhydrase 8 Homo sapiens 0-7 23046583-13 2012 Accumulation of FUS in the cytoplasm may retain RNA targets and recruit additional RNA-binding proteins, such as PABP-1, into stress-granule like aggregates that coalesce into permanent inclusions that could negatively affect RNA metabolism. fusarubin 16-19 poly(A) binding protein, cytoplasmic 1 Mus musculus 113-119 22921802-6 2012 We demonstrate that FUS can non-invasively deliver siRNA-Htt directly to the striatum leading to a significant reduction of Htt expression in a dose dependent manner. fusarubin 20-23 huntingtin Homo sapiens 57-60 22921802-6 2012 We demonstrate that FUS can non-invasively deliver siRNA-Htt directly to the striatum leading to a significant reduction of Htt expression in a dose dependent manner. fusarubin 20-23 huntingtin Homo sapiens 124-127 22984865-2 2012 Herein, we describe the discovery of a novel class of BACE-1 inhibitors represented by sulfamide 14g, using a medicinal chemistry strategy to optimize central nervous system (CNS) penetration by minimizing hydrogen bond donors (HBDs) and reducing P-glycoprotein (P-gp) mediated efflux. fusarubin 87-96 beta-site APP cleaving enzyme 1 Mus musculus 54-60 22984865-2 2012 Herein, we describe the discovery of a novel class of BACE-1 inhibitors represented by sulfamide 14g, using a medicinal chemistry strategy to optimize central nervous system (CNS) penetration by minimizing hydrogen bond donors (HBDs) and reducing P-glycoprotein (P-gp) mediated efflux. fusarubin 87-96 phosphoglycolate phosphatase Mus musculus 247-261 22984865-2 2012 Herein, we describe the discovery of a novel class of BACE-1 inhibitors represented by sulfamide 14g, using a medicinal chemistry strategy to optimize central nervous system (CNS) penetration by minimizing hydrogen bond donors (HBDs) and reducing P-glycoprotein (P-gp) mediated efflux. fusarubin 87-96 phosphoglycolate phosphatase Mus musculus 263-267 21861133-7 2012 In summary, treatment with FUS, in combination with a dose of microbubbles, can enhance BBB permeability through a caveolae-mediated transcellular approach by upregulating the expression level of caveolin-1 and, consequently, the amount of caveolae. fusarubin 27-30 caveolin 1 Rattus norvegicus 196-206 22506561-3 2012 The SAR for steroid inhibition of G6PD has been substantially developed; the 3beta-alcohol can be replaced with 3beta-H-bond donors such as sulfamide, sulfonamide, urea, and carbamate. fusarubin 140-149 sarcosine dehydrogenase Homo sapiens 4-7 22506561-3 2012 The SAR for steroid inhibition of G6PD has been substantially developed; the 3beta-alcohol can be replaced with 3beta-H-bond donors such as sulfamide, sulfonamide, urea, and carbamate. fusarubin 140-149 glucose-6-phosphate dehydrogenase Homo sapiens 34-38 22443542-10 2012 CONCLUSIONS: These data demonstrate that the overexpression of Fus/Caz causes in vivo toxicity by disrupting neuromuscular junctions (NMJs) and inducing apoptosis in motor neurons. fusarubin 63-66 cabeza Drosophila melanogaster 67-70 22355253-5 2012 Analysis according to gender did not show any influence of sex on the association of miR-146a and Ets-1 with FUS. fusarubin 109-112 ETS proto-oncogene 1, transcription factor Homo sapiens 98-103 19272776-2 2009 Herein, we report on the synthesis of sulfamide based inhibitors designed around a lysine scaffold and their structure-activity relationships against HDAC1 and HDAC6 isotypes as well as 293T cells. fusarubin 38-47 histone deacetylase 1 Homo sapiens 150-155 21875798-3 2011 Sulfonamide and sulfamide with high polar surface area and good activity at CB1 were rationally designed and pharmacologically tested. fusarubin 16-25 cannabinoid receptor 1 Homo sapiens 76-79 20099854-3 2010 SUMO-AMSN (4a) and Ub-AMSN (4b) contain a sulfamide group as a nonhydrolyzable mimic of the phosphate group in the cognate Ub/Ubl-AMP adenylate intermediate in the first half-reaction, and these constructs selectively inhibit SUMO E1 and Ub E1, respectively, in a dose-dependent manner. fusarubin 42-51 small nucleolar RNA, H/ACA box 73A Homo sapiens 231-243 19272776-2 2009 Herein, we report on the synthesis of sulfamide based inhibitors designed around a lysine scaffold and their structure-activity relationships against HDAC1 and HDAC6 isotypes as well as 293T cells. fusarubin 38-47 histone deacetylase 6 Homo sapiens 160-165 17127063-7 2007 The best hCA VI inhibitors were cyanide, azide, sulfamide, and sulfamate, with inhibition constants in the range of 70-90microM. fusarubin 48-57 carbonic anhydrase 6 Homo sapiens 9-15 17346964-5 2007 The additional two hydrogen bonds in which N-hydroxysulfamide bound to hCA II is involved as compared to the corresponding adduct of sulfamide may explain its higher affinity for the enzyme, also providing hints for the design of tight-binding CA inhibitors possessing an organic moiety substituting the NH group in the N-hydroxysulfamide structure. fusarubin 52-61 carbonic anhydrase 2 Homo sapiens 71-77 18618322-5 2009 Inhibition data of the cytosolic isozymes hCA I - hCA III with a large number of anions (halides, pseudohalides, bicarbonate, carbonate, nitrate, nitrite, hydrosulfide, sulfate, sulfamic acid, sulfamide, etc. fusarubin 193-202 carbonic anhydrase 1 Homo sapiens 42-47 18618322-5 2009 Inhibition data of the cytosolic isozymes hCA I - hCA III with a large number of anions (halides, pseudohalides, bicarbonate, carbonate, nitrate, nitrite, hydrosulfide, sulfate, sulfamic acid, sulfamide, etc. fusarubin 193-202 HCA1 Homo sapiens 42-45 18217703-4 2008 An extensive SAR study led to sulfamide (R)- 22b, which inhibited the strand transfer with an IC50 of 7 nM and HIV infection in MT4 cells with a CIC95 of 44 nM, and ketoamide (S)- 28c that inhibited strand transfer with an IC50 of 12 nM and the HIV infection in MT4 cells with a CIC95 of 13 nM and exhibited a good pharmacokinetic profile when dosed orally to preclinical species. fusarubin 30-39 sarcosine dehydrogenase Homo sapiens 13-16 17627576-12 2007 Overview of analysis favours substituents with high electronegativity and less bulk at R and R" positions of the parent nucleus, provides a basis to design new Sulfamide derivatives possessing potent and selective carbonic anhydrase-II inhibitory activity. fusarubin 160-169 carbonic anhydrase 2 Homo sapiens 214-235 17228882-0 2007 Novel sulfamide analogs of oleoylethanolamide showing in vivo satiety inducing actions and PPARalpha activation. fusarubin 6-15 peroxisome proliferator activated receptor alpha Rattus norvegicus 91-100 16999776-8 2006 From structure-activity comparisons, the sulfamate is more effective than the sulfamide in inhibiting carbonic anhydrase I and II, but the sulfamate does not confer selectivity. fusarubin 78-87 carbonic anhydrase 1 Homo sapiens 102-129 17125255-1 2006 The sulfamide analogue of the antiepileptic drug topiramate is a 210 times less potent inhibitor of isozyme II of the zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1) compared to topiramate but effectively inhibits isozymes CA VA, VB, VII, XIII, and XIV (KI in the range of 21-35 nM). fusarubin 4-13 carbonic anhydrase 5A Homo sapiens 223-228 17125255-3 2006 As shown by X-ray crystallography, the sulfamide analogue binds to CA II with the deprotonated sulfamide moiety coordinated to Zn(II) and with the organic scaffold making an extended network of hydrogen bonds with Thr199, Gln92, His94, Asn62, and Thr200. fusarubin 39-48 carbonic anhydrase 2 Homo sapiens 67-72 17125255-3 2006 As shown by X-ray crystallography, the sulfamide analogue binds to CA II with the deprotonated sulfamide moiety coordinated to Zn(II) and with the organic scaffold making an extended network of hydrogen bonds with Thr199, Gln92, His94, Asn62, and Thr200. fusarubin 95-104 carbonic anhydrase 2 Homo sapiens 67-72 16710859-3 2006 Among the enzymes for which sulfamide-based inhibitors were designed, are the carbonic anhydrases (CAs), a large number of proteases belonging to the aspartic protease (HIV-1 protease, gamma-secretase), serine protease (elastase, chymase, tryptase, and thrombin among others), and metalloprotease (carboxypeptidase A (CPA) and matrix metalloproteinases (MMP)) families. fusarubin 28-37 carboxypeptidase A1 Homo sapiens 318-321 16710859-4 2006 Some steroid sulfatase (STS) and protein tyrosine phosphatase inhibitors belonging to the sulfamide class of derivatives have also been reported. fusarubin 90-99 steroid sulfatase Homo sapiens 5-22 16759092-0 2006 Inhibition of carbonic anhydrase-II by sulfamate and sulfamide groups: an investigation involving direct thermodynamic binding measurements. fusarubin 53-62 carbonic anhydrase 2 Homo sapiens 14-35 16759092-1 2006 This paper examines the relative effectiveness of bioisosteric sulfamate and sulfamide derivatives for inhibition of human carbonic anhydrase-II (CA-II) by using a direct binding assay based on the ThermoFluor method (Matulis et al. fusarubin 77-86 carbonic anhydrase 2 Homo sapiens 123-144 16759092-1 2006 This paper examines the relative effectiveness of bioisosteric sulfamate and sulfamide derivatives for inhibition of human carbonic anhydrase-II (CA-II) by using a direct binding assay based on the ThermoFluor method (Matulis et al. fusarubin 77-86 carbonic anhydrase 2 Homo sapiens 146-151 16759092-11 2006 It appears that the sulfamide group is less suitable than the sulfamate group for obtaining potent inhibition of CA-II. fusarubin 20-29 carbonic anhydrase 2 Homo sapiens 113-118 16311805-0 2005 Alternative method of Boc-removal from sulfamide using silica-phenyl sulfonic acid in conjunction with microwave heating. fusarubin 39-48 BOC cell adhesion associated, oncogene regulated Homo sapiens 22-25 20141508-2 2006 Amongst the enzymes for which sulfamide-based inhibitors were designed are the carbonic anhydrases (CAs), and a large number of proteases belonging to the aspartic protease (HIV-1 protease, gamma-secretase), serine protease (elastase, chymase, tryptase and thrombin, among others) and metalloproteinase (carboxypeptidase A [CPA] and matrix metalloproteinase [MMP]) families. fusarubin 30-39 carboxypeptidase A1 Homo sapiens 324-327 20141508-3 2006 Some steroid sulfatase (STS) and protein tyrosine phosphatase inhibitors belonging to the sulfamide class of derivatives have also been reported. fusarubin 90-99 steroid sulfatase Homo sapiens 5-22 20141508-5 2006 This is achieved either by directly coordinating to the metal ion found in some metalloenzymes (CAs, CPA, STS), usually by means of one of the nitrogen atoms present in the sulfamide motif, or, as in the case of the cyclic sulfamides, acting as HIV protease inhibitors interacting with the catalytically critical aspartic acid residues of the active site by means of an oxygen atom belonging to the HN-SO(2)-NH motif that substitutes a catalytically essential water molecule. fusarubin 173-182 carboxypeptidase A1 Homo sapiens 101-104 15771438-0 2005 Comparison of sulfamate and sulfamide groups for the inhibition of carbonic anhydrase-II by using topiramate as a structural platform. fusarubin 28-37 carbonic anhydrase 2 Homo sapiens 67-88 15771438-1 2005 This paper examines the relative effectiveness of sulfamate and sulfamide groups for the inhibition of carbonic anhydrase-II (CA-II). fusarubin 64-73 carbonic anhydrase 2 Homo sapiens 103-124 15771438-1 2005 This paper examines the relative effectiveness of sulfamate and sulfamide groups for the inhibition of carbonic anhydrase-II (CA-II). fusarubin 64-73 carbonic anhydrase 2 Homo sapiens 126-131 15686897-1 2005 The identification, design, and synthesis of a series of novel sulfamide- and urea-based small-molecule antagonists of the protein-protein interaction IL-2/IL-2Ralpha are described. fusarubin 63-72 interleukin 2 Homo sapiens 151-155 15686897-1 2005 The identification, design, and synthesis of a series of novel sulfamide- and urea-based small-molecule antagonists of the protein-protein interaction IL-2/IL-2Ralpha are described. fusarubin 63-72 interleukin 2 receptor subunit alpha Homo sapiens 156-166 15686897-2 2005 Installation of a furan carboxylic acid fragment onto a low-micromolar sulfamide resulted in a 23-fold improvement in activity, providing a sub-micromolar, nonpeptidic IL-2 inhibitor (IC(50)=0.60 microM). fusarubin 71-80 interleukin 2 Homo sapiens 168-172 15454240-2 2004 The inhibition of the newly discovered cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isozyme XIII of murine origin (mCA XIII) has been investigated with a series of anions, such as the physiological ones (bicarbonate, chloride), or the metal complexing anions (cyanate, cyanide, azide, hydrogen sulfide, etc), nitrate, nitrite, sulfate, sulfamate, sulfamide as well as with phenylboronic and phenylarsonic acids. fusarubin 348-357 carbonic anhydrase 13 Mus musculus 116-124 15501038-5 2004 Excellent hCA IV inhibitory properties showed sulfamic acid, sulfamide, phenylboronic acid and phenylarsonic acid, with K(i)"s in the range of 0.87-0.93 microM, whereas their affinities for the other investigated isozymes were in the millimolar range. fusarubin 61-70 carbonic anhydrase 4 Homo sapiens 10-16 15454240-3 2004 The best mCA XIII inhibitors were cyanate, thiocyanate, cyanide and sulfamide, with K(I)-s in the range of 0.25microM-0.74 mM, whereas fluoride, iodide, azide, carbonate and hydrogen sulfide were less effective (K(I)-s in the range of 3.0-5.5mM). fusarubin 68-77 carbonic anhydrase 13 Mus musculus 9-17 12431056-0 2002 Sulfamide-based inhibitors for carboxypeptidase A. fusarubin 0-9 carboxypeptidase A1 Homo sapiens 31-49 12904065-5 2003 The sulfamide and sulfonamide derivatization at the N-terminal position in general afforded highly potent thrombin inhibitors but with moderate oral absorption, while the well-absorbable N-carbamate derivatives exhibited limited metabolic stability in S9 fractions. fusarubin 4-13 coagulation factor II Rattus norvegicus 106-114 15231731-3 2004 Based on cDNA microarrays and protein analysis, we found that FUS at the intermediate peak pressure of 1.5 MPa induced a complex signaling cascade with upregulation of proapoptotic genes [e.g., p53, p21, Thy1 (CD 90)]. fusarubin 62-65 tumor protein p53 Homo sapiens 194-197 15231731-3 2004 Based on cDNA microarrays and protein analysis, we found that FUS at the intermediate peak pressure of 1.5 MPa induced a complex signaling cascade with upregulation of proapoptotic genes [e.g., p53, p21, Thy1 (CD 90)]. fusarubin 62-65 H3 histone pseudogene 16 Homo sapiens 199-202 15231731-3 2004 Based on cDNA microarrays and protein analysis, we found that FUS at the intermediate peak pressure of 1.5 MPa induced a complex signaling cascade with upregulation of proapoptotic genes [e.g., p53, p21, Thy1 (CD 90)]. fusarubin 62-65 Thy-1 cell surface antigen Homo sapiens 204-208 15231731-3 2004 Based on cDNA microarrays and protein analysis, we found that FUS at the intermediate peak pressure of 1.5 MPa induced a complex signaling cascade with upregulation of proapoptotic genes [e.g., p53, p21, Thy1 (CD 90)]. fusarubin 62-65 Thy-1 cell surface antigen Homo sapiens 210-215 15231731-4 2004 Simultaneously, FUS downregulated cellular survival components (e.g., bcl-2, SOD). fusarubin 16-19 BCL2 apoptosis regulator Homo sapiens 70-75 15080932-0 2004 Sulfamide derivatives as transition state analogue inhibitors for carboxypeptidase A. fusarubin 0-9 carboxypeptidase A1 Homo sapiens 66-84 12617903-1 2003 A novel class of effective CAIs has been identified, starting from a very weak carbonic anhydrase inhibitor (CAI), sulfamide, whose X-ray crystal structure in the adduct with hCA II has recently been reported. fusarubin 115-124 carbonic anhydrase 2 Homo sapiens 175-181 12617904-1 2003 A series of sugar sulfamate/sulfamide derivatives were prepared and assayed as inhibitors of three carbonic anhydrase (CA) isozymes, hCA I, hCA II and bCA IV. fusarubin 28-37 cytochrome P450 family 24 subfamily A member 1 Homo sapiens 133-157 11731425-10 2001 Immunohistochemistry of the resected specimen demonstrated that FUS homogeneously induced lethal and sublethal tumor damage with consecutive up-regulation of p53 and loss of proliferative activity. fusarubin 64-67 tumor protein p53 Homo sapiens 158-161 12362982-0 2002 Sulfamide antifolates inhibiting thymidylate synthase: synthesis, enzyme inhibition and cytotoxicity. fusarubin 0-9 thymidylate synthase Mus musculus 33-53 10560733-0 1999 4-Chlorobenzyl sulfonamide and sulfamide derivatives of histamine homologues: the design of potent histamine H3 receptor antagonists. fusarubin 31-40 histamine receptor H3 Homo sapiens 99-120 11916140-4 2001 The new sulfamide/sulfamates were effective CA II and CA IV inhibitors, but showed no inhibitory activity against isozyme I. fusarubin 8-17 carbonic anhydrase 2 Homo sapiens 44-49 11916140-4 2001 The new sulfamide/sulfamates were effective CA II and CA IV inhibitors, but showed no inhibitory activity against isozyme I. fusarubin 8-17 carbonic anhydrase 4 Homo sapiens 54-59 33799460-5 2021 Congeners with attached sulfamide substituents retained Aurora A inhibitory activity. fusarubin 24-33 aurora kinase A Homo sapiens 56-64 10507774-5 1999 In patients treated with fluorouracil derivatives (FUs), the expression of TP significantly correlated with favourable prognosis and with unfavourable prognosis in those not treated with FUs. fusarubin 51-54 thymidine phosphorylase Homo sapiens 75-77 10507774-5 1999 In patients treated with fluorouracil derivatives (FUs), the expression of TP significantly correlated with favourable prognosis and with unfavourable prognosis in those not treated with FUs. fusarubin 187-190 thymidine phosphorylase Homo sapiens 75-77 10507774-6 1999 The patients with TP-positive tumours, the prognosis of patients treated with FUs was significantly better than that of those not treated with FUs. fusarubin 78-81 thymidine phosphorylase Homo sapiens 18-20 10507774-6 1999 The patients with TP-positive tumours, the prognosis of patients treated with FUs was significantly better than that of those not treated with FUs. fusarubin 143-146 thymidine phosphorylase Homo sapiens 18-20 10507774-7 1999 In patients with TP-positive tumours, treatment with FUs and lymph node metastasis were independent prognostic factors according to the Cox proportional hazards model. fusarubin 53-56 thymidine phosphorylase Homo sapiens 17-19 10507774-9 1999 The determination of the expression of TP might be useful for predicting the efficacy of post-operative chemotherapy using FUs to prevent recurrence in advanced gastric carcinoma patients who undergo curative gastrectomy. fusarubin 123-126 thymidine phosphorylase Homo sapiens 39-41 9083478-2 1997 The structure of the urea 2 showed a conformation similar to that reported for the related urea 3 by Lam et al., while the sulfamide 1 adopted an unanticipated conformation in which the P1" and P2" side chains were transposed. fusarubin 123-132 crystallin gamma F, pseudogene Homo sapiens 186-196 34605896-0 2022 FUS-induced neurotoxicity is prevented by inhibiting GSK-3beta in a drosophila model of amyotrophic lateral sclerosis. fusarubin 0-3 shaggy Drosophila melanogaster 53-62 34734364-10 2022 By 2 weeks post-FUS, we noted emergence of adaptive resistance mechanisms, including upregulation of TIGIT on CD4 + T cells and CD155 on non-immune tumor and stromal cells. fusarubin 16-19 T cell immunoreceptor with Ig and ITIM domains Mus musculus 101-106 34734364-10 2022 By 2 weeks post-FUS, we noted emergence of adaptive resistance mechanisms, including upregulation of TIGIT on CD4 + T cells and CD155 on non-immune tumor and stromal cells. fusarubin 16-19 CD4 antigen Mus musculus 110-113 34530052-5 2021 In vitro studies demonstrated sustained release of basic fibroblast growth factor (bFGF) from the ARSs using repeated applications of FUS. fusarubin 134-137 fibroblast growth factor 2 Mus musculus 51-81 34530052-5 2021 In vitro studies demonstrated sustained release of basic fibroblast growth factor (bFGF) from the ARSs using repeated applications of FUS. fusarubin 134-137 fibroblast growth factor 2 Mus musculus 83-87 34605896-5 2022 Here, we report GSK-3beta as a potential modulator of FUS-induced toxicity. fusarubin 54-57 shaggy Drosophila melanogaster 16-25 34605896-8 2022 In addition, we found that the levels of FUS proteins were significantly reduced by co-overexpression of Slimb, a F-box protein, in FUS-expressing flies, indicating that Slimb is critical for the suppressive effect of Shaggy/GSK-3beta inhibition on FUS-induced toxicity in Drosophila. fusarubin 41-44 supernumerary limbs Drosophila melanogaster 105-110 34605896-8 2022 In addition, we found that the levels of FUS proteins were significantly reduced by co-overexpression of Slimb, a F-box protein, in FUS-expressing flies, indicating that Slimb is critical for the suppressive effect of Shaggy/GSK-3beta inhibition on FUS-induced toxicity in Drosophila. fusarubin 41-44 supernumerary limbs Drosophila melanogaster 170-175 34605896-8 2022 In addition, we found that the levels of FUS proteins were significantly reduced by co-overexpression of Slimb, a F-box protein, in FUS-expressing flies, indicating that Slimb is critical for the suppressive effect of Shaggy/GSK-3beta inhibition on FUS-induced toxicity in Drosophila. fusarubin 41-44 shaggy Drosophila melanogaster 218-234 34605896-8 2022 In addition, we found that the levels of FUS proteins were significantly reduced by co-overexpression of Slimb, a F-box protein, in FUS-expressing flies, indicating that Slimb is critical for the suppressive effect of Shaggy/GSK-3beta inhibition on FUS-induced toxicity in Drosophila. fusarubin 132-135 supernumerary limbs Drosophila melanogaster 105-110 34605896-8 2022 In addition, we found that the levels of FUS proteins were significantly reduced by co-overexpression of Slimb, a F-box protein, in FUS-expressing flies, indicating that Slimb is critical for the suppressive effect of Shaggy/GSK-3beta inhibition on FUS-induced toxicity in Drosophila. fusarubin 132-135 supernumerary limbs Drosophila melanogaster 170-175 34605896-8 2022 In addition, we found that the levels of FUS proteins were significantly reduced by co-overexpression of Slimb, a F-box protein, in FUS-expressing flies, indicating that Slimb is critical for the suppressive effect of Shaggy/GSK-3beta inhibition on FUS-induced toxicity in Drosophila. fusarubin 132-135 shaggy Drosophila melanogaster 218-234 34605896-8 2022 In addition, we found that the levels of FUS proteins were significantly reduced by co-overexpression of Slimb, a F-box protein, in FUS-expressing flies, indicating that Slimb is critical for the suppressive effect of Shaggy/GSK-3beta inhibition on FUS-induced toxicity in Drosophila. fusarubin 249-252 supernumerary limbs Drosophila melanogaster 105-110 34605896-8 2022 In addition, we found that the levels of FUS proteins were significantly reduced by co-overexpression of Slimb, a F-box protein, in FUS-expressing flies, indicating that Slimb is critical for the suppressive effect of Shaggy/GSK-3beta inhibition on FUS-induced toxicity in Drosophila. fusarubin 249-252 supernumerary limbs Drosophila melanogaster 170-175 34605896-8 2022 In addition, we found that the levels of FUS proteins were significantly reduced by co-overexpression of Slimb, a F-box protein, in FUS-expressing flies, indicating that Slimb is critical for the suppressive effect of Shaggy/GSK-3beta inhibition on FUS-induced toxicity in Drosophila. fusarubin 249-252 shaggy Drosophila melanogaster 218-234 34605896-9 2022 These findings revealed a novel mechanism of neuronal protective effect through SCFSlimb-mediated FUS degradation via GSK-3beta inhibition, and provided in vivo evidence of the potential for modulating FUS-induced ALS progression using GSK-3beta inhibitors. fusarubin 98-101 shaggy Drosophila melanogaster 118-127 34605896-9 2022 These findings revealed a novel mechanism of neuronal protective effect through SCFSlimb-mediated FUS degradation via GSK-3beta inhibition, and provided in vivo evidence of the potential for modulating FUS-induced ALS progression using GSK-3beta inhibitors. fusarubin 202-205 shaggy Drosophila melanogaster 236-245 35179290-3 2022 Since sulfamide realizes the optimal balance in the relationships among composition, structure, and properties, in addition to very short absorption of 160 nm, it achieves multiple optical performance records among the non-pi-conjugated DUV NLO materials, including the strongest SHG efficiency (about 4 times that of KDP), the largest birefringence (obv. fusarubin 6-15 WNK lysine deficient protein kinase 1 Homo sapiens 318-321 34405679-3 2021 Here, we developed a kind of nanoprobe-loaded MBs (AV-ICG-NPs@MBs) which can monitor the apoptotic cells that occur during FUS-mediated BBB opening through encapsulating the annexin V-targeted nanoprobes AV-ICG-NPs into the cavity of lipid-PLGA hybrid MBs. fusarubin 123-126 annexin A5 Homo sapiens 174-183 34393708-6 2021 The water diffusion caused by FUS-BBBD was analyzed using the apparent diffusion coefficient (ADC), axial diffusivity, radial diffusivity (RD), and fractional anisotropy, obtained at 5 min, 24 and 48 h, as well as the water channel expression of aquaporin-4 (AQP-4) immunostaining at 48 h after FUS-induced BBBD. fusarubin 30-33 aquaporin 4 Rattus norvegicus 246-257 34393708-6 2021 The water diffusion caused by FUS-BBBD was analyzed using the apparent diffusion coefficient (ADC), axial diffusivity, radial diffusivity (RD), and fractional anisotropy, obtained at 5 min, 24 and 48 h, as well as the water channel expression of aquaporin-4 (AQP-4) immunostaining at 48 h after FUS-induced BBBD. fusarubin 30-33 aquaporin 4 Rattus norvegicus 259-264 34393708-9 2021 When we applied higher sonication conditions, the ADC and RD showed enhancement until 48 h, and became comparable to contralateral values at 72 h. AQP-4 expression was upregulated after FUS-induced BBBD in both sonication conditions at 48 h. The results of this study provide preliminary evidence on how mechanical forces from FUS alter water dynamics through diffusion tensor imaging (DTI) measures and AQP4 expression. fusarubin 186-189 aquaporin 4 Rattus norvegicus 147-152 34393708-9 2021 When we applied higher sonication conditions, the ADC and RD showed enhancement until 48 h, and became comparable to contralateral values at 72 h. AQP-4 expression was upregulated after FUS-induced BBBD in both sonication conditions at 48 h. The results of this study provide preliminary evidence on how mechanical forces from FUS alter water dynamics through diffusion tensor imaging (DTI) measures and AQP4 expression. fusarubin 186-189 aquaporin 4 Rattus norvegicus 404-408 34393708-9 2021 When we applied higher sonication conditions, the ADC and RD showed enhancement until 48 h, and became comparable to contralateral values at 72 h. AQP-4 expression was upregulated after FUS-induced BBBD in both sonication conditions at 48 h. The results of this study provide preliminary evidence on how mechanical forces from FUS alter water dynamics through diffusion tensor imaging (DTI) measures and AQP4 expression. fusarubin 327-330 aquaporin 4 Rattus norvegicus 147-152 34393708-9 2021 When we applied higher sonication conditions, the ADC and RD showed enhancement until 48 h, and became comparable to contralateral values at 72 h. AQP-4 expression was upregulated after FUS-induced BBBD in both sonication conditions at 48 h. The results of this study provide preliminary evidence on how mechanical forces from FUS alter water dynamics through diffusion tensor imaging (DTI) measures and AQP4 expression. fusarubin 327-330 aquaporin 4 Rattus norvegicus 404-408 6761818-0 1982 [Medium term effect (3 months) of hypoglycemic sulfamide treatment (gliclazide) on insulin secretion of the non-insulin dependent diabetic]. fusarubin 47-56 insulin Homo sapiens 83-90 6761818-0 1982 [Medium term effect (3 months) of hypoglycemic sulfamide treatment (gliclazide) on insulin secretion of the non-insulin dependent diabetic]. fusarubin 47-56 insulin Homo sapiens 112-119 33989819-10 2021 FUS stimulation of TRPV1-expressing neurons at the striatum repeatedly evoked locomotor behavior in freely moving mice. fusarubin 0-3 transient receptor potential cation channel, subfamily V, member 1 Mus musculus 19-24 33600879-7 2021 Following FUS-triggered delivery, sham nanodroplets induced a 22.6 +- 21% increase in local c-Fos expression, whereas pentobarbital-loaded nanodroplets induced a 21.7 +- 13% decrease (n = 6). fusarubin 10-13 Fos proto-oncogene, AP-1 transcription factor subunit Rattus norvegicus 92-97 33992926-4 2021 Several compounds showed good inhibition of PDE4B in vitro and the SAR indicated superiority of aminosulfonamide moiety over aminocarboxamide in terms of PDE4B inhibition. fusarubin 96-112 phosphodiesterase 4B, cAMP-specific a Danio rerio 44-49 33992926-4 2021 Several compounds showed good inhibition of PDE4B in vitro and the SAR indicated superiority of aminosulfonamide moiety over aminocarboxamide in terms of PDE4B inhibition. fusarubin 96-112 phosphodiesterase 4B, cAMP-specific a Danio rerio 154-159 33992926-6 2021 The participation of aminosulfonamide moiety in PDE4B inhibition and the reason for selectivity though moderate shown by 3q and 3u was revealed by the in silico docking studies. fusarubin 21-37 phosphodiesterase 4B, cAMP-specific a Danio rerio 48-53 33608142-5 2021 A 40% increase in accumulation of transferrin receptor-targeting liposomes was observed in the FUS-treated hemisphere, whereas the isotype immunoglobulin G liposomes showed no increased accumulation. fusarubin 95-98 transferrin receptor Rattus norvegicus 34-54 33476735-4 2021 We demonstrate that timing of antibody injection relative to FUS BBB/BTB disruption is a critical determinant of mCD47 access, with post-FUS injection conferring superlative antibody delivery to gliomas. fusarubin 61-64 CD47 antigen (Rh-related antigen, integrin-associated signal transducer) Mus musculus 113-118 33476735-5 2021 We also show that mCD47 delivery across the BBB/BTB with repeat sessions of FUS can significantly constrain tumor outgrowth and extend survival in glioma-bearing mice. fusarubin 76-79 CD47 antigen (Rh-related antigen, integrin-associated signal transducer) Mus musculus 18-23 33476735-7 2021 Moreover, our results confirm that mCD47 delivery with FUS is a promising therapeutic strategy for GB therapy. fusarubin 55-58 CD47 antigen (Rh-related antigen, integrin-associated signal transducer) Mus musculus 35-40 33639877-13 2021 Eyes with FUS had significantly higher aqueous humor (AH) cytokine levels (VEGF, bFGF, IL-6, IL-8 and IL-10) compared with the control eyes (P < 0.05). fusarubin 10-13 vascular endothelial growth factor A Homo sapiens 75-79 33639877-13 2021 Eyes with FUS had significantly higher aqueous humor (AH) cytokine levels (VEGF, bFGF, IL-6, IL-8 and IL-10) compared with the control eyes (P < 0.05). fusarubin 10-13 fibroblast growth factor 2 Homo sapiens 81-85 33639877-13 2021 Eyes with FUS had significantly higher aqueous humor (AH) cytokine levels (VEGF, bFGF, IL-6, IL-8 and IL-10) compared with the control eyes (P < 0.05). fusarubin 10-13 interleukin 6 Homo sapiens 87-91 33639877-13 2021 Eyes with FUS had significantly higher aqueous humor (AH) cytokine levels (VEGF, bFGF, IL-6, IL-8 and IL-10) compared with the control eyes (P < 0.05). fusarubin 10-13 C-X-C motif chemokine ligand 8 Homo sapiens 93-97 33639877-13 2021 Eyes with FUS had significantly higher aqueous humor (AH) cytokine levels (VEGF, bFGF, IL-6, IL-8 and IL-10) compared with the control eyes (P < 0.05). fusarubin 10-13 interleukin 10 Homo sapiens 102-107 33393538-1 2021 The regioselective gamma-C-H amination of the side-chain of saturated 2-alkyl nitrogen heterocycles is reported, proceeding through a sulfamide-directed 1,6-radical translocation. fusarubin 134-143 interleukin 2 receptor subunit gamma Homo sapiens 19-26 33447034-9 2021 Furthermore, the FUS-assisted MBs-LPHNspCas9/MGMT-cRGD enhanced the therapeutic effects of TMZ in glioblastoma, inhibited tumor growth, and prolonged survival of tumor-bearing mice, with a high level of biosafety. fusarubin 17-20 O-6-methylguanine-DNA methyltransferase Mus musculus 45-49 33287379-5 2020 FUS-Cav significantly increases the sensitivity of cancer cells to RT and HT by reducing long-term clonogenic survival, short-term cell metabolic activity, cell invasion, and induction of sonoporation. fusarubin 0-3 caveolin 2 Homo sapiens 4-7