PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 9154923-0 1997 Effect of nuclear protein HMG1 on in vitro slippage synthesis of the tandem repeat dTG x dCA. dolutegravir 83-86 high mobility group box 1 Rattus norvegicus 26-30 9154923-3 1997 We show here that HMG1 (modeled by the second HMG box motif from HMG1 of the rat, HMGb) binds to complexes formed from annealing unequal lengths of dTG x dCA and inhibits the in vitro elongation of these complexes by the Klenow fragment of DNA polymerase I at 37 degrees C. At 46 degrees C, HMGb enhances the elongation. dolutegravir 148-151 high mobility group box 1 Rattus norvegicus 18-22 9154923-3 1997 We show here that HMG1 (modeled by the second HMG box motif from HMG1 of the rat, HMGb) binds to complexes formed from annealing unequal lengths of dTG x dCA and inhibits the in vitro elongation of these complexes by the Klenow fragment of DNA polymerase I at 37 degrees C. At 46 degrees C, HMGb enhances the elongation. dolutegravir 148-151 high mobility group box 1 Rattus norvegicus 65-69 7743202-4 1995 Treatment with sigma receptor agonist DTG potentiated the hypoxia/hypoglycemia-induced decrease in the CA1 presynaptic potential, whereas SKF10047 which possesses an affinity for phencyclidine site attenuated the decrease of potential. dolutegravir 38-41 carbonic anhydrase 1 Rattus norvegicus 103-106 7536037-2 1995 DTG and ETG retain the inhibitory effect of TG on the sarcoplasmic reticulum (SR) ATPase, displaying a 2 and 10 microM Ki, respectively. dolutegravir 0-3 dynein axonemal heavy chain 8 Homo sapiens 82-88 7536037-3 1995 Steady state and lifetime fluorescence measurements are consistent with energy transfer between tryptophanyl residues assigned to the ATPase membrane-bound region and DTG. dolutegravir 167-170 dynein axonemal heavy chain 8 Homo sapiens 134-140 7536037-4 1995 This phenomenon exhibits saturation behavior, occurs in the presence of DTG concentrations producing ATPase inhibition, and is partially prevented by inhibitory concentrations of TG. dolutegravir 72-75 dynein axonemal heavy chain 8 Homo sapiens 101-107 7536037-5 1995 Although long range conformational effects of TG binding affect the fluorescence properties of endogenous tryptophans as well as of a fluorescein 5"-isothiocyanate (FITC) label of the ATPase extramembranous region, no significant energy transfer was detected between DTG and the FITC label. dolutegravir 267-270 dynein axonemal heavy chain 8 Homo sapiens 184-190 7753753-5 1995 One site, called rem1, was defined with 100 nM alaproclate and bound sigma 2 ligands with high affinity, e.g. haloperidol, GBR 12909, DTG and (+)-3-PPP. dolutegravir 134-137 RRAD and GEM like GTPase 1 Rattus norvegicus 17-21 34954655-2 2022 This study investigates the effect of dolutegravir (DTG) exposure on the functional expression of the reduced folate carrier (RFC), proton-coupled folate transporter (PCFT), and folate receptor-alpha (FRalpha) in the placenta. dolutegravir 38-50 solute carrier family 46 member 1 Homo sapiens 132-165 1532832-1 1992 We have reported previously that the high affinity sigma ligand DTG potentiates N-methyl-D-aspartate (NMDA)-induced excitation of pyramidal neurons in the CA3 region of rat dorsal hippocampus. dolutegravir 64-67 carbonic anhydrase 3 Rattus norvegicus 155-158 1532832-3 1992 At low doses, the sigma ligands DTG, JO-1784, JO-1783, AdipG, DnBG, APDQ, BD-737 and (+)-pentazocine dose-dependently enhanced selectively NMDA-induced activation of CA3 pyramidal neurons (with the exception of BD-737 which also presented a late potentiation of the neuronal response to quisqualate). dolutegravir 32-35 carbonic anhydrase 3 Rattus norvegicus 166-169 7532890-2 1994 We report that MKT1 encodes a 92,979 Da protein with serine-rich regions and the retroviral protease signature, DTG, but with no substantial homology to proteins presently in the databases. dolutegravir 112-115 Mkt1p Saccharomyces cerevisiae S288C 15-19 25350530-8 2014 While rilpivirine and dolutegravir inhibit mainly the renal transporter OCT2 in the basolateral membrane of the proximal tubular cell, cobicistat predominantly inhibits the renal transporter MATE1 in the luminal membrane. dolutegravir 22-34 POU class 2 homeobox 2 Homo sapiens 72-76 34954655-2 2022 This study investigates the effect of dolutegravir (DTG) exposure on the functional expression of the reduced folate carrier (RFC), proton-coupled folate transporter (PCFT), and folate receptor-alpha (FRalpha) in the placenta. dolutegravir 38-50 folate receptor alpha Homo sapiens 178-199 34954655-2 2022 This study investigates the effect of dolutegravir (DTG) exposure on the functional expression of the reduced folate carrier (RFC), proton-coupled folate transporter (PCFT), and folate receptor-alpha (FRalpha) in the placenta. dolutegravir 38-50 FOS like 1, AP-1 transcription factor subunit Homo sapiens 201-208 34954655-2 2022 This study investigates the effect of dolutegravir (DTG) exposure on the functional expression of the reduced folate carrier (RFC), proton-coupled folate transporter (PCFT), and folate receptor-alpha (FRalpha) in the placenta. dolutegravir 52-55 solute carrier family 46 member 1 Homo sapiens 132-165 34954655-2 2022 This study investigates the effect of dolutegravir (DTG) exposure on the functional expression of the reduced folate carrier (RFC), proton-coupled folate transporter (PCFT), and folate receptor-alpha (FRalpha) in the placenta. dolutegravir 52-55 solute carrier family 46 member 1 Homo sapiens 167-171 34954655-2 2022 This study investigates the effect of dolutegravir (DTG) exposure on the functional expression of the reduced folate carrier (RFC), proton-coupled folate transporter (PCFT), and folate receptor-alpha (FRalpha) in the placenta. dolutegravir 52-55 folate receptor alpha Homo sapiens 178-199 34954655-2 2022 This study investigates the effect of dolutegravir (DTG) exposure on the functional expression of the reduced folate carrier (RFC), proton-coupled folate transporter (PCFT), and folate receptor-alpha (FRalpha) in the placenta. dolutegravir 52-55 FOS like 1, AP-1 transcription factor subunit Homo sapiens 201-208 34954655-6 2022 FINDINGS: In placental cells, clinically relevant DTG exposure for 3h or 6h was associated with a modest but significant reduction in the expression of RFC and PCFT both at the mRNA and protein levels, as well as decreased uptake of RFC and PCFT substrates (3H)-methotrexate and (3H)-folic acid, respectively. dolutegravir 50-53 solute carrier family 46, member 1 Mus musculus 160-164 34954655-6 2022 FINDINGS: In placental cells, clinically relevant DTG exposure for 3h or 6h was associated with a modest but significant reduction in the expression of RFC and PCFT both at the mRNA and protein levels, as well as decreased uptake of RFC and PCFT substrates (3H)-methotrexate and (3H)-folic acid, respectively. dolutegravir 50-53 solute carrier family 46, member 1 Mus musculus 241-245 34954655-7 2022 In pregnant mice, DTG administration was associated with an increase in both placental RFC and PCFT mRNA expression, accompanied by a decrease in placental FRalpha mRNA under folate-deficient dietary conditions. dolutegravir 18-21 solute carrier family 46, member 1 Mus musculus 95-99 34954655-7 2022 In pregnant mice, DTG administration was associated with an increase in both placental RFC and PCFT mRNA expression, accompanied by a decrease in placental FRalpha mRNA under folate-deficient dietary conditions. dolutegravir 18-21 FOS like 1, AP-1 transcription factor subunit Homo sapiens 156-163 34880680-13 2021 Utilization of dolutegravir-based regimens should be encouraged to attain a normal CD4 count earlier. dolutegravir 15-27 CD4 molecule Homo sapiens 83-86 34528449-3 2021 Results: A novel cis-eQTL, rs28967009, was identified for UGT1A1, which is predicted to upregulate UGT1A1 expression thereby potentially affecting the metabolism of dolutegravir and irinotecan, which are extensively prescribed in SA for HIV and colorectal cancer treatment, respectively. dolutegravir 165-177 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 58-64 34784398-5 2021 However, a CD4+/CD8+ >1 was observed in 25% of patients treated with Raltegravir and half of those treated with Dolutegravir. dolutegravir 112-124 CD4 molecule Homo sapiens 11-14 34784398-5 2021 However, a CD4+/CD8+ >1 was observed in 25% of patients treated with Raltegravir and half of those treated with Dolutegravir. dolutegravir 112-124 CD8a molecule Homo sapiens 16-19 34784398-9 2021 Dolutegravir showed a tendency to statistically significant changes in IL-4 and IL-10. dolutegravir 0-12 interleukin 4 Homo sapiens 71-75 34784398-9 2021 Dolutegravir showed a tendency to statistically significant changes in IL-4 and IL-10. dolutegravir 0-12 interleukin 10 Homo sapiens 80-85 34328253-15 2021 Unbound dolutegravir >= 431 nM induced expression of CYP3A4 (>= two-fold) in a dose-dependent manner, while 1.44 muM of unbound dolutegravir induced CYP2B6 expression 2.2 +- 0.3-fold (P = 0.0004). dolutegravir 8-20 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-59 34328253-15 2021 Unbound dolutegravir >= 431 nM induced expression of CYP3A4 (>= two-fold) in a dose-dependent manner, while 1.44 muM of unbound dolutegravir induced CYP2B6 expression 2.2 +- 0.3-fold (P = 0.0004). dolutegravir 8-20 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 149-155 34328253-15 2021 Unbound dolutegravir >= 431 nM induced expression of CYP3A4 (>= two-fold) in a dose-dependent manner, while 1.44 muM of unbound dolutegravir induced CYP2B6 expression 2.2 +- 0.3-fold (P = 0.0004). dolutegravir 128-140 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 149-155 34328253-16 2021 CONCLUSIONS: In summary, this in vitro study suggests that dolutegravir has the potential to increase hepatic clearance of levonorgestrel by inducing both CYP3A and non-CYP3A enzymes. dolutegravir 59-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 155-160 34328253-16 2021 CONCLUSIONS: In summary, this in vitro study suggests that dolutegravir has the potential to increase hepatic clearance of levonorgestrel by inducing both CYP3A and non-CYP3A enzymes. dolutegravir 59-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 169-174 34551678-7 2021 Urinary beta2microglobulin significantly increased at week 24 with DTG and EVG/c but remained unchanged in the RAL arm. dolutegravir 67-70 beta-2-microglobulin Homo sapiens 8-26 34555326-14 2021 INTERPRETATION: Clinicians and people with HIV should be aware of associations between weight gain and use of dolutegravir, tenofovir alafenamide, and raltegravir, particularly given the potential consequences of weight gain, such as insulin resistance, dyslipidaemia, and hypertension. dolutegravir 110-122 insulin Homo sapiens 234-241 34528449-3 2021 Results: A novel cis-eQTL, rs28967009, was identified for UGT1A1, which is predicted to upregulate UGT1A1 expression thereby potentially affecting the metabolism of dolutegravir and irinotecan, which are extensively prescribed in SA for HIV and colorectal cancer treatment, respectively. dolutegravir 165-177 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 99-105 34528449-4 2021 Conclusion: As increased UGT1A1 expression could affect the clinical outcome of dolutegravir and irinotecan treatment by increasing drug clearance, patients with the rs28967009A variant may require increased drug doses to reach therapeutic levels or should be prescribed alternative drugs. dolutegravir 80-92 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 25-31 34120186-0 2021 Switching from boosted PIs to dolutegravir decreases soluble CD14 and adiponectin in high cardiovascular risk people living with HIV. dolutegravir 30-42 CD14 molecule Homo sapiens 61-65 34575401-5 2021 Drug-drug interactions (DDIs) of UGT1A1 substrates dolutegravir and raltegravir with UGT1A1 inhibitor atazanavir have been simulated, and the role of intestinal metabolism in these clinical DDIs examined. dolutegravir 51-63 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 33-39 34120186-0 2021 Switching from boosted PIs to dolutegravir decreases soluble CD14 and adiponectin in high cardiovascular risk people living with HIV. dolutegravir 30-42 adiponectin, C1Q and collagen domain containing Homo sapiens 70-81 34120186-5 2021 Soluble CD14 (-11%, P < 0.001) and adiponectin (-11%, P < 0.001) significantly declined and high-sensitive C-reactive protein (-13%, P = 0.069) and oxidized LDL (-13%, P = 0.084) tended to decrease with dolutegravir. dolutegravir 203-215 CD14 molecule Homo sapiens 8-12 34120186-5 2021 Soluble CD14 (-11%, P < 0.001) and adiponectin (-11%, P < 0.001) significantly declined and high-sensitive C-reactive protein (-13%, P = 0.069) and oxidized LDL (-13%, P = 0.084) tended to decrease with dolutegravir. dolutegravir 203-215 adiponectin, C1Q and collagen domain containing Homo sapiens 35-46 34120186-5 2021 Soluble CD14 (-11%, P < 0.001) and adiponectin (-11%, P < 0.001) significantly declined and high-sensitive C-reactive protein (-13%, P = 0.069) and oxidized LDL (-13%, P = 0.084) tended to decrease with dolutegravir. dolutegravir 203-215 C-reactive protein Homo sapiens 107-125 34120186-6 2021 Switching to dolutegravir remained significantly associated with soluble CD14 and adiponectin reductions after adjustment for baseline variables. dolutegravir 13-25 CD14 molecule Homo sapiens 73-77 34120186-6 2021 Switching to dolutegravir remained significantly associated with soluble CD14 and adiponectin reductions after adjustment for baseline variables. dolutegravir 13-25 adiponectin, C1Q and collagen domain containing Homo sapiens 82-93 34120186-8 2021 CONCLUSIONS: Switching from boosted PIs to dolutegravir in PLWH with high cardiovascular risk led to soluble CD14 and adiponectin reductions at 48 weeks. dolutegravir 43-55 CD14 molecule Homo sapiens 109-113 34120186-8 2021 CONCLUSIONS: Switching from boosted PIs to dolutegravir in PLWH with high cardiovascular risk led to soluble CD14 and adiponectin reductions at 48 weeks. dolutegravir 43-55 adiponectin, C1Q and collagen domain containing Homo sapiens 118-129 35099526-0 2022 Corrigendum to: CYP2B6 Genotype and Weight Gain Differences Between Dolutegravir and Efavirenz. dolutegravir 68-80 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 16-22 34909672-4 2021 The metabolism pathways of dolutegravir and bictegravir are similar, both including CYP3A and UGT1A1, and both agents are substrates to different drug transporters. dolutegravir 27-39 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 84-89 34909672-4 2021 The metabolism pathways of dolutegravir and bictegravir are similar, both including CYP3A and UGT1A1, and both agents are substrates to different drug transporters. dolutegravir 27-39 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 94-100 35551149-7 2022 RESULTS: Through Week 48, changes in biomarkers did not significantly differ between dolutegravir + rilpivirine and CAR groups, except for increases in soluble CD14 and decreases in fatty acid binding protein-2, which favored dolutegravir + rilpivirine. dolutegravir 85-97 CD14 molecule Homo sapiens 160-164 35551149-7 2022 RESULTS: Through Week 48, changes in biomarkers did not significantly differ between dolutegravir + rilpivirine and CAR groups, except for increases in soluble CD14 and decreases in fatty acid binding protein-2, which favored dolutegravir + rilpivirine. dolutegravir 226-238 fatty acid binding protein 2 Homo sapiens 182-210 35512135-7 2022 Of nine polymorphisms previously associated with dolutegravir pharmacokinetics, the lowest P-value with AUCVAR was UGT1A1 rs887829 (P = 1.8 x 10-4), which was also associated with log10 bilirubin (P = 8.6 x 10-13). dolutegravir 49-61 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 115-121 35512135-11 2022 CONCLUSIONS: In South Africa, rs887829 and rs28899168 in the UGT1A locus were independently associated with dolutegravir AUCVAR. dolutegravir 108-120 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 61-66 35409412-5 2022 With molecular docking, we showed that both Etravirine and Dolutegravir are preferentially bound to primary ACE2-interacting residues on the RBD domain, implying that these two drug blocks may prohibit the viral attachment of SARS-CoV-2. dolutegravir 59-71 angiotensin converting enzyme 2 Homo sapiens 108-112 35409412-8 2022 These data implied that Etravirine and Dolutegravir may serve as general spike inhibitors against dominant viral variants of SARS-CoV-2. dolutegravir 39-51 surface glycoprotein Severe acute respiratory syndrome coronavirus 2 73-78 35019724-6 2022 Unexpectedly, CD8 T cells treated with dolutegravir showed a similar killing ability 7 dpi compared to emtricitabine or rilpivirine treated cells. dolutegravir 39-51 CD8a molecule Homo sapiens 14-17 35357907-6 2022 The median times between the date of effective marketing of generic TDF/FTC and the date of de-simplification of EFV/TDF/FTC and RPV/TDF/FTC were 723 (IQR: 369-1119) and 234 (IQR: 142-264) days, respectively; this time was 155 (IQR: 28 - 287) days for de-simplification of DTG/ABC/3TC. dolutegravir 273-276 sex determining region Y Homo sapiens 68-71 35357907-6 2022 The median times between the date of effective marketing of generic TDF/FTC and the date of de-simplification of EFV/TDF/FTC and RPV/TDF/FTC were 723 (IQR: 369-1119) and 234 (IQR: 142-264) days, respectively; this time was 155 (IQR: 28 - 287) days for de-simplification of DTG/ABC/3TC. dolutegravir 273-276 sex determining region Y Homo sapiens 117-120 35512127-0 2022 Dolutegravir Suppresses Thermogenesis via Disrupting UCP1 Expression and Mitochondrial Function in Brown/Beige Adipocytes in preclinical models. dolutegravir 0-12 uncoupling protein 1 (mitochondrial, proton carrier) Mus musculus 53-57 35512127-5 2022 RESULTS: Two-week administration of DTG to female mice reduced energy expenditure, which was accompanied by decreased uncoupling protein 1 (UCP1) expression in brown/beige adipose tissues. dolutegravir 36-39 uncoupling protein 1 (mitochondrial, proton carrier) Mus musculus 118-138 35512127-5 2022 RESULTS: Two-week administration of DTG to female mice reduced energy expenditure, which was accompanied by decreased uncoupling protein 1 (UCP1) expression in brown/beige adipose tissues. dolutegravir 36-39 uncoupling protein 1 (mitochondrial, proton carrier) Mus musculus 140-144 35512127-6 2022 In vitro studies showed that DTG significantly reduced brown adipogenic markers, especially UCP1 in brown and beige adipocytes while drugs from other classes did not. dolutegravir 29-32 uncoupling protein 1 (mitochondrial, proton carrier) Mus musculus 92-96 35512127-7 2022 Furthermore, a loss of UCP1 by DTG led to a decrease in mitochondrial complex IV component, followed by a reduction in mitochondrial respiratory capacity and reduced insulin-stimulated glucose uptake. dolutegravir 31-34 uncoupling protein 1 (mitochondrial, proton carrier) Mus musculus 23-27 35512127-8 2022 CONCLUSION: Our findings show that DTG targets UCP1 and mitochondrial functions in brown and beige adipocytes and disrupts thermogenic functions in preclinical models providing the potential mechanisms by which DTG suppresses energy expenditure leading to weight-gain. dolutegravir 35-38 uncoupling protein 1 (mitochondrial, proton carrier) Mus musculus 47-51 35411401-9 2022 CONCLUSIONS: Forty-eight weeks after switching from a PI-based to a dolutegravir-based regimen, patients with Framingham score >10% or aged >50 years showed improvement of several atherogenic lipid features, including LDL particle phenotype, ox-LDL and Lp-PLA2. dolutegravir 68-80 phospholipase A2 group VII Homo sapiens 253-260 35422637-0 2022 Comparison of Renal Function Biomarkers of Serum Creatinine and Cystatin C in HIV-Infected People on Dolutegravir-Containing Therapy. dolutegravir 101-113 cystatin C Homo sapiens 64-74 35432298-0 2022 Similar CD4/CD8 Ratio Recovery After Initiation of Dolutegravir Plus Lamivudine Versus Dolutegravir or Bictegravir-Based Three-Drug Regimens in Naive Adults With HIV. dolutegravir 51-63 CD4 molecule Homo sapiens 8-11 35432298-0 2022 Similar CD4/CD8 Ratio Recovery After Initiation of Dolutegravir Plus Lamivudine Versus Dolutegravir or Bictegravir-Based Three-Drug Regimens in Naive Adults With HIV. dolutegravir 51-63 CD8a molecule Homo sapiens 12-15 35432298-0 2022 Similar CD4/CD8 Ratio Recovery After Initiation of Dolutegravir Plus Lamivudine Versus Dolutegravir or Bictegravir-Based Three-Drug Regimens in Naive Adults With HIV. dolutegravir 87-99 CD4 molecule Homo sapiens 8-11 35432298-11 2022 Conclusions: In this large cohort study in people with HIV, ART initiation with dolutegravir plus lamivudine vs. dolutegravir or bictegravir-based triple antiretroviral therapy showed no difference in the rates of CD4/CD8 normalization at 48 weeks. dolutegravir 80-92 artemin Homo sapiens 60-63 34983388-17 2022 Treatment with ABC/DTG/3TC was associated with higher risk of treatment failure. dolutegravir 19-22 ATP binding cassette subfamily B member 6 (Langereis blood group) Homo sapiens 15-18 35017453-2 2022 High levels of raltegravir and dolutegravir can potentially cause bilirubin toxicity as they compete for albumin binding and follow the same metabolic pathway through UGT1A1. dolutegravir 31-43 albumin Homo sapiens 105-112 35017453-2 2022 High levels of raltegravir and dolutegravir can potentially cause bilirubin toxicity as they compete for albumin binding and follow the same metabolic pathway through UGT1A1. dolutegravir 31-43 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 167-173 33601161-5 2021 Furthermore, two carboxylic acid derivatives (DP4 and DP5) could be identified, which can be explained as the result of the hydrolysis of the exocyclic amide bond of dolutegravir and DP1, respectively. dolutegravir 166-178 transcription factor Dp family member 3 Homo sapiens 46-49 33653604-3 2021 We studied the effect of 24-weeks antiretroviral combination therapy with abacavir, lamivudine, and dolutegravir on HML-2 levels in 29 ALS patients. dolutegravir 100-112 C-type lectin domain containing 10A Homo sapiens 116-121 32667979-2 2021 In a Phase 1 dolutegravir-efavirenz interaction study, mean dolutegravir Cmin decreased by 60% and 85% among CYP2B6 normal and slow/intermediate metabolizers, respectively. dolutegravir 13-25 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 109-115 33601161-5 2021 Furthermore, two carboxylic acid derivatives (DP4 and DP5) could be identified, which can be explained as the result of the hydrolysis of the exocyclic amide bond of dolutegravir and DP1, respectively. dolutegravir 166-178 harakiri, BCL2 interacting protein Homo sapiens 54-57 33601161-6 2021 During the fragmentation process of dolutegravir and its degradation products DP1 to DP3 a formal addition of oxygen resulting in the respective carboxylic acid fragments was detected. dolutegravir 36-48 prostaglandin D2 receptor Homo sapiens 78-81 33601161-6 2021 During the fragmentation process of dolutegravir and its degradation products DP1 to DP3 a formal addition of oxygen resulting in the respective carboxylic acid fragments was detected. dolutegravir 36-48 APC regulator of WNT signaling pathway Homo sapiens 85-88 33625064-8 2021 In target gene analyses, the lowest P-values for the dolutegravir and tenofovir groups were ABCG2 rs4148149 (P = 7.0x10-4) and ABCC10 rs67861980 (P = 1.0x10-2), respectively, which were not significant after correction for multiple testing. dolutegravir 53-65 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 92-97 33483020-1 2021 The present study aims to develop Chitosan-based polymeric nanoparticles of anti-HIV drug Dolutegravir, to aid appropriate dose adjustment and ease of oral administration as milk and food admixture for children. dolutegravir 90-102 activation induced cytidine deaminase Homo sapiens 107-110 33637050-8 2021 A higher proportion of patients on DTG achieved VS compared to PI/rs [Range:33.1%(13.6,50.4)-45.3%(24.1,61.6)] and RAL [16.7%(3.3,31.2)] in patients with VL > 100,000 copies/mL at baseline, and similar VS was achieved in patients with CD4+ <= 200 cells/muL at baseline. dolutegravir 35-38 RAS like proto-oncogene A Homo sapiens 115-118 33637050-8 2021 A higher proportion of patients on DTG achieved VS compared to PI/rs [Range:33.1%(13.6,50.4)-45.3%(24.1,61.6)] and RAL [16.7%(3.3,31.2)] in patients with VL > 100,000 copies/mL at baseline, and similar VS was achieved in patients with CD4+ <= 200 cells/muL at baseline. dolutegravir 35-38 CD4 molecule Homo sapiens 235-238 33637050-8 2021 A higher proportion of patients on DTG achieved VS compared to PI/rs [Range:33.1%(13.6,50.4)-45.3%(24.1,61.6)] and RAL [16.7%(3.3,31.2)] in patients with VL > 100,000 copies/mL at baseline, and similar VS was achieved in patients with CD4+ <= 200 cells/muL at baseline. dolutegravir 35-38 tripartite motif containing 37 Homo sapiens 253-256 33637050-9 2021 DTG also achieved greater increase in CD4+ cells from baseline compared to EFV [32.6(10.7,54.7)], ritonavir-boosted darunavir [DRV/r:25.7(3.6,48.1)] and BIC [24.7(1.5,47.7)]. dolutegravir 0-3 CD4 molecule Homo sapiens 38-41 33637050-10 2021 Patients receiving DTG had lower odds of discontinuing therapy by W96 compared to PI/rs, EFV, RAL and EVG/c. dolutegravir 19-22 RAS like proto-oncogene A Homo sapiens 94-97 33501995-7 2021 The Cr-eGFR changes between darunavir/cobicistat and darunavir/cobicistat with rilpivirine and/or dolutegravir showed more significant decreases in patients taking two or more IPTCrS at 12, 24 and 48 weeks. dolutegravir 98-110 epidermal growth factor receptor Homo sapiens 7-11 33501995-9 2021 CONCLUSIONS: Concomitant use of darunavir/cobicistat plus IPTCrS dolutegravir, rilpivirine, or both produced an additive effect in the expected Cr-eGFR decrease. dolutegravir 65-77 epidermal growth factor receptor Homo sapiens 147-151 33625064-8 2021 In target gene analyses, the lowest P-values for the dolutegravir and tenofovir groups were ABCG2 rs4148149 (P = 7.0x10-4) and ABCC10 rs67861980 (P = 1.0x10-2), respectively, which were not significant after correction for multiple testing. dolutegravir 53-65 ATP binding cassette subfamily C member 10 Homo sapiens 127-133 33625064-9 2021 In genome-wide analyses the lowest P-values for dolutegravir, was rs7590091 in TMEM163 (P = 3.7x10-8), rs17137701 in LOC105379130 (P = 6.4x10- 8) for TAF, and rs76771105 in LOC105371716 (P = 9.7x10-8) for TDF. dolutegravir 48-60 transmembrane protein 163 Homo sapiens 79-86 32166319-0 2020 The integrase inhibitors dolutegravir and raltegravir exert pro-adipogenic and profibrotic effects and induce insulin resistance in human/simian adipose tissue and human adipocytes. dolutegravir 25-37 insulin Homo sapiens 110-117 33436439-2 2021 We previously reported that, in vitro, the lab-adapted HIV-1 NL4-3 strain can acquire resistance to the integrase inhibitor dolutegravir (DTG) by acquiring mutations in the envelope glycoprotein (Env) that enhance viral cell-cell transmission. dolutegravir 124-136 endogenous retrovirus group K member 20 Homo sapiens 173-194 33436439-2 2021 We previously reported that, in vitro, the lab-adapted HIV-1 NL4-3 strain can acquire resistance to the integrase inhibitor dolutegravir (DTG) by acquiring mutations in the envelope glycoprotein (Env) that enhance viral cell-cell transmission. dolutegravir 124-136 endogenous retrovirus group K member 20 Homo sapiens 196-199 33436439-2 2021 We previously reported that, in vitro, the lab-adapted HIV-1 NL4-3 strain can acquire resistance to the integrase inhibitor dolutegravir (DTG) by acquiring mutations in the envelope glycoprotein (Env) that enhance viral cell-cell transmission. dolutegravir 138-141 endogenous retrovirus group K member 20 Homo sapiens 173-194 33436439-2 2021 We previously reported that, in vitro, the lab-adapted HIV-1 NL4-3 strain can acquire resistance to the integrase inhibitor dolutegravir (DTG) by acquiring mutations in the envelope glycoprotein (Env) that enhance viral cell-cell transmission. dolutegravir 138-141 endogenous retrovirus group K member 20 Homo sapiens 196-199 33200210-0 2021 Long-term efficacy of dolutegravir plus lamivudine for maintenance of HIV viral suppression in adults with and without historical resistance to lamivudine: Week 96 results of ART-PRO pilot study. dolutegravir 22-34 artemin Homo sapiens 175-178 33436439-7 2021 These Env mutants exhibit reduced susceptibility to DTG, with effects on replication and Env structure that are HIV-1 strain dependent. dolutegravir 52-55 endogenous retrovirus group K member 20 Homo sapiens 6-9 32737482-9 2020 At 48 weeks, patients who switched to dolutegravir had lower mean progression of both right (+4 versus +14.6 mum) and left (-6.1 versus +1.6 mum) CIMT and also a smaller increase in mean PWV (+0.18 versus +0.39 m/s) than patients continuing on boosted PIs, although differences were not statistically significant. dolutegravir 38-50 CIMT Homo sapiens 146-150 32701823-0 2020 Switching to Bictegravir/Emtricitabine/Tenofovir Alafenamide (B/F/TAF) from Dolutegravir (DTG)+F/TAF or DTG+F/Tenofovir Disoproxil Fumarate (TDF) in the Presence of Pre-Existing NRTI Resistance. dolutegravir 76-88 TATA-box binding protein associated factor 8 Homo sapiens 66-69 32701823-0 2020 Switching to Bictegravir/Emtricitabine/Tenofovir Alafenamide (B/F/TAF) from Dolutegravir (DTG)+F/TAF or DTG+F/Tenofovir Disoproxil Fumarate (TDF) in the Presence of Pre-Existing NRTI Resistance. dolutegravir 90-93 TATA-box binding protein associated factor 8 Homo sapiens 66-69 33179568-4 2022 Comparison of docking and MD simulation results of complexes of drugs with that of inhibitor N3 (experimentally obtained) suggests EGCG, withaferin, dolutegravir, artesunate as potential inhibitors of the main protease (Mpro). dolutegravir 149-161 NEWENTRY Severe acute respiratory syndrome-related coronavirus 220-224 32737482-12 2020 CONCLUSIONS: Relative to continuing on boosted PIs, switching to dolutegravir in virologically suppressed patients with high cardiovascular risk showed consistent favourable although non-significant trends on CIMT progression at 48 weeks. dolutegravir 65-77 CIMT Homo sapiens 209-213 32566255-0 2020 Biochemical activity of RAGs is impeded by Dolutegravir, an HIV integrase inhibitor. dolutegravir 43-55 ephrin A5 Homo sapiens 24-28 33335931-13 2020 Conclusions: Neuropsychiatric symptoms in patients on DTG/ABC/3TC could resolve or improve after switching to EVG/COBI/FTC/TAF. dolutegravir 54-57 TATA-box binding protein associated factor 8 Homo sapiens 123-126 32960272-0 2021 CYP2B6 Genotype and Weight Gain Differences Between Dolutegravir and Efavirenz. dolutegravir 52-64 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 0-6 32310900-11 2020 Children with dolutegravir exposure had some suggestion of increased risk of neurologic case (aRR = 2.43, 95% CI 0.75--7.84), which was observed consistently across several sensitivity analyses. dolutegravir 14-26 arrestin beta 2 Homo sapiens 94-101 32667674-6 2020 CD4 mean increase was 257.8 (249.3; 266.2) cells/mm3, and it was lower with TAF/FTC/EVG/CBT and TDF/FTC/RPV compared with ABC/3TC/DTG. dolutegravir 130-133 CD4 molecule Homo sapiens 0-3 32668455-2 2021 We evaluated whether people receiving dolutegravir (DTG) plus F/TAF or F/tenofovir disoproxil fumarate (TDF) with viral suppression can switch to B/F/TAF without compromising safety or efficacy, regardless of pre-existing NRTI resistance. dolutegravir 52-55 TATA-box binding protein associated factor 8 Homo sapiens 150-153 32668455-12 2021 INTERPRETATION: The single-tablet regimen B/F/TAF is a safe, effective option for people virologically suppressed on DTG plus either F/TDF or F/TAF, including in individuals with pre-existing resistance to NRTIs. dolutegravir 117-120 TATA-box binding protein associated factor 8 Homo sapiens 46-49 32303561-2 2020 Because DTG is a substrate of the efflux transporter ABCG2 and ABCG2 is highly polymorphic, we asked whether dose adjustment of DTG is needed for ABCG2-deficient individuals. dolutegravir 8-11 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 53-58 32566255-8 2020 Binding and nicking studies showed that, Dolutegravir could decrease the binding efficiency of RAG1 domains and cleavage on DNA substrates, but not as considerably as Elvitegravir. dolutegravir 41-53 recombination activating 1 Homo sapiens 95-99 31971958-0 2020 HIV antiretroviral drugs, dolutegravir, maraviroc and ritonavir-boosted atazanavir use different pathways to affect inflammation, senescence and insulin sensitivity in human coronary endothelial cells. dolutegravir 26-38 insulin Homo sapiens 145-152 32577427-11 2020 Conclusions: Naive PWH with lower CD4 counts and those on TAF/FTC or TDF/FTC backbones were at higher risk of weight increase in the course of DTG-based ART. dolutegravir 143-146 CD4 molecule Homo sapiens 34-37 32011683-0 2020 Genetic influence of ABCG2, UGT1A1 and NR1I2 on dolutegravir plasma pharmacokinetics. dolutegravir 48-60 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 21-26 32011683-0 2020 Genetic influence of ABCG2, UGT1A1 and NR1I2 on dolutegravir plasma pharmacokinetics. dolutegravir 48-60 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 28-34 32011683-0 2020 Genetic influence of ABCG2, UGT1A1 and NR1I2 on dolutegravir plasma pharmacokinetics. dolutegravir 48-60 nuclear receptor subfamily 1 group I member 2 Homo sapiens 39-44 32011683-2 2020 We sought to ascertain the contributory effect of SNPs in four key genes linked to dolutegravir disposition (UGT1A1, ABCG2, CYP3A and NR1I2) on plasma dolutegravir pharmacokinetics. dolutegravir 83-95 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 109-115 32011683-2 2020 We sought to ascertain the contributory effect of SNPs in four key genes linked to dolutegravir disposition (UGT1A1, ABCG2, CYP3A and NR1I2) on plasma dolutegravir pharmacokinetics. dolutegravir 83-95 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 117-122 32011683-2 2020 We sought to ascertain the contributory effect of SNPs in four key genes linked to dolutegravir disposition (UGT1A1, ABCG2, CYP3A and NR1I2) on plasma dolutegravir pharmacokinetics. dolutegravir 83-95 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 124-129 32011683-2 2020 We sought to ascertain the contributory effect of SNPs in four key genes linked to dolutegravir disposition (UGT1A1, ABCG2, CYP3A and NR1I2) on plasma dolutegravir pharmacokinetics. dolutegravir 83-95 nuclear receptor subfamily 1 group I member 2 Homo sapiens 134-139 32011683-2 2020 We sought to ascertain the contributory effect of SNPs in four key genes linked to dolutegravir disposition (UGT1A1, ABCG2, CYP3A and NR1I2) on plasma dolutegravir pharmacokinetics. dolutegravir 151-163 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 109-115 32011683-2 2020 We sought to ascertain the contributory effect of SNPs in four key genes linked to dolutegravir disposition (UGT1A1, ABCG2, CYP3A and NR1I2) on plasma dolutegravir pharmacokinetics. dolutegravir 151-163 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 117-122 32011683-2 2020 We sought to ascertain the contributory effect of SNPs in four key genes linked to dolutegravir disposition (UGT1A1, ABCG2, CYP3A and NR1I2) on plasma dolutegravir pharmacokinetics. dolutegravir 151-163 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 124-129 32011683-2 2020 We sought to ascertain the contributory effect of SNPs in four key genes linked to dolutegravir disposition (UGT1A1, ABCG2, CYP3A and NR1I2) on plasma dolutegravir pharmacokinetics. dolutegravir 151-163 nuclear receptor subfamily 1 group I member 2 Homo sapiens 134-139 32011683-8 2020 CONCLUSIONS: This study showed a pharmacogenetic association between dolutegravir pharmacokinetics and variants in the ABCG2, UGT1A1 and NR1I2 genes, particularly when combined. dolutegravir 69-81 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 119-124 32011683-8 2020 CONCLUSIONS: This study showed a pharmacogenetic association between dolutegravir pharmacokinetics and variants in the ABCG2, UGT1A1 and NR1I2 genes, particularly when combined. dolutegravir 69-81 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 126-132 32011683-8 2020 CONCLUSIONS: This study showed a pharmacogenetic association between dolutegravir pharmacokinetics and variants in the ABCG2, UGT1A1 and NR1I2 genes, particularly when combined. dolutegravir 69-81 nuclear receptor subfamily 1 group I member 2 Homo sapiens 137-142 32109250-2 2020 An off-target inhibition of the endogenous ligand binding to the human melanocortin 4 receptor (MC4R) has been suggested as a potential mechanism for clinical body weight gain following initiation of dolutegravir, an INSTI. dolutegravir 200-212 melanocortin 4 receptor Homo sapiens 71-94 32109250-2 2020 An off-target inhibition of the endogenous ligand binding to the human melanocortin 4 receptor (MC4R) has been suggested as a potential mechanism for clinical body weight gain following initiation of dolutegravir, an INSTI. dolutegravir 200-212 melanocortin 4 receptor Homo sapiens 96-100 31971958-8 2020 RESULTS: Dolutegravir reduced inflammation by decreasing NFkappaB activation and IL-6/IL-8/sICAM-1/sVCAM-1 secretion, as did maraviroc with a milder effect. dolutegravir 9-21 interleukin 6 Homo sapiens 81-85 31971958-8 2020 RESULTS: Dolutegravir reduced inflammation by decreasing NFkappaB activation and IL-6/IL-8/sICAM-1/sVCAM-1 secretion, as did maraviroc with a milder effect. dolutegravir 9-21 C-X-C motif chemokine ligand 8 Homo sapiens 86-90 31971958-14 2020 In USP18-silenced cells, basal insulin resistance was increased, but dolutegravir and atazanavir/r kept their effect on insulin sensitivity, indicating that USP18 was dispensable. dolutegravir 69-81 insulin Homo sapiens 120-127 31971958-16 2020 Dolutegravir and atazanavir/r, but not maraviroc, exerted opposite effects on inflammation and senescence that involved USP18. dolutegravir 0-12 ubiquitin specific peptidase 18 Homo sapiens 120-125 31971958-18 2020 Thus, in endothelial cells, dolutegravir and atazanavir/r oppositely affected pathways leading to inflammation, senescence and insulin resistance. dolutegravir 28-40 insulin Homo sapiens 127-134 32235038-10 2020 Cross-intolerance was low, and only 5/55 patients with prior DTG intolerability had to discontinue BIC/F/TAF due to NPAEs. dolutegravir 61-64 TATA-box binding protein associated factor 8 Homo sapiens 105-108 31119275-8 2019 Typical dolutegravir apparent clearance (CL/F) was 0.93 L/h with 32% between-subject variability, the apparent volume of distribution was 20.2 L and the absorption rate constant was fixed to 2.24 h-1. dolutegravir 8-20 crooked neck pre-mRNA splicing factor 1 Homo sapiens 41-45 31478469-0 2019 Reduced soluble CD14 levels after switching from a dual regimen with lamivudine plus boosted protease inhibitors to lamivudine plus dolutegravir in virologically suppressed HIV-infected patients. dolutegravir 132-144 CD14 molecule Homo sapiens 16-20 31339677-16 2019 CONCLUSIONS: Treatment with DTG combined with either of two tenofovir prodrugs (TAF and TDF) showed noninferior efficacy to treatment with the standard-care regimen. dolutegravir 28-31 TATA-box binding protein associated factor 8 Homo sapiens 80-83 31339677-17 2019 There was significantly more weight gain with the DTG-containing regimens, especially in combination with TAF, than with the standard-care regimen. dolutegravir 50-53 TATA-box binding protein associated factor 8 Homo sapiens 106-109 31339677-1 2019 BACKGROUND: Two drugs under consideration for inclusion in antiretroviral therapy (ART) regimens for human immunodeficiency virus (HIV) infection are dolutegravir (DTG) and tenofovir alafenamide fumarate (TAF). dolutegravir 150-162 TATA-box binding protein associated factor 8 Homo sapiens 205-208 30934067-13 2019 Results of Sensitivity Analysis: Women"s deaths averted with DTG exceeded pediatric deaths added with EFV unless dolutegravir-associated NTD risk was 1.5% or greater. dolutegravir 113-125 fuzzy planar cell polarity protein Homo sapiens 137-140 31339677-1 2019 BACKGROUND: Two drugs under consideration for inclusion in antiretroviral therapy (ART) regimens for human immunodeficiency virus (HIV) infection are dolutegravir (DTG) and tenofovir alafenamide fumarate (TAF). dolutegravir 164-167 TATA-box binding protein associated factor 8 Homo sapiens 205-208 31146698-9 2019 CD4+ count increase was significantly greater with DTG than PIs (difference: 23.63-31.47 cells/muL) and efavirenz (difference: 34.54 cells/muL), and similar to other core agents. dolutegravir 51-54 CD4 molecule Homo sapiens 0-3 31146698-11 2019 DTG was more likely to result in patients achieving VS (probability: 94-100%), and a greater CD4+ count increase (probability: 53-100%) versus other core agents, including INSTIs (probability: 94-97% and 53-93%, respectively). dolutegravir 0-3 CD4 molecule Homo sapiens 93-96 31167838-12 2019 Dolutegravir and other HIV integrase inhibitor drugs were evaluated in vitro for inhibition of the major folate transport pathways: proton-coupled folate transporter, reduced folate carrier, and folate receptor alpha-mediated endocytosis. dolutegravir 0-12 solute carrier family 46 member 1 Homo sapiens 132-165 31217351-12 2019 These findings indicate that EVG and DLG use is associated with slow proliferation and impaired respiration with underlying mitochondrial dysfunction, resulting in overall decreased cellular function in CD4+ T cells. dolutegravir 37-40 CD4 molecule Homo sapiens 203-206 30934067-15 2019 Conclusion: Although NTD risks may be higher with dolutegravir than efavirenz, dolutegravir will lead to many fewer deaths among women, as well as fewer overall HIV transmissions. dolutegravir 50-62 fuzzy planar cell polarity protein Homo sapiens 21-24 30975760-5 2019 Remarkably, the Env compensatory mutants can also rescue a replication-delayed integrase (IN) mutant, and exhibit reduced sensitivity to the IN inhibitor Dolutegravir (DTG), demonstrating that they confer a global replication advantage. dolutegravir 154-166 endogenous retrovirus group K member 20 Homo sapiens 16-19 30804050-7 2019 The kinetic data from expression systems suggested the major enzymes in each tissue: hepatic UGT1A9 > UGT1A1 (dolutegravir and raltegravir) and UGT1A1 (cabotegravir), intestinal UGT1A3 > UGT1A8 > UGT1A1 (dolutegravir) and UGT1A8 > UGT1A1 (raltegravir), and renal UGT1A9 (dolutegravir and raltegravir). dolutegravir 113-125 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 93-99 30804050-7 2019 The kinetic data from expression systems suggested the major enzymes in each tissue: hepatic UGT1A9 > UGT1A1 (dolutegravir and raltegravir) and UGT1A1 (cabotegravir), intestinal UGT1A3 > UGT1A8 > UGT1A1 (dolutegravir) and UGT1A8 > UGT1A1 (raltegravir), and renal UGT1A9 (dolutegravir and raltegravir). dolutegravir 113-125 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 105-111 30975760-5 2019 Remarkably, the Env compensatory mutants can also rescue a replication-delayed integrase (IN) mutant, and exhibit reduced sensitivity to the IN inhibitor Dolutegravir (DTG), demonstrating that they confer a global replication advantage. dolutegravir 168-171 endogenous retrovirus group K member 20 Homo sapiens 16-19 30975760-6 2019 In addition, confirming the ability of Env mutants to confer escape from DTG, we performed de novo selection for DTG resistance and observed resistance mutations in Env. dolutegravir 73-76 endogenous retrovirus group K member 20 Homo sapiens 39-42 30975760-6 2019 In addition, confirming the ability of Env mutants to confer escape from DTG, we performed de novo selection for DTG resistance and observed resistance mutations in Env. dolutegravir 113-116 endogenous retrovirus group K member 20 Homo sapiens 39-42 29603882-8 2018 RESULTS: Compared to SOC, DTG improved 5-year survival from 76.7% to 83.0%, increased life expectancy from 22.0 to 24.8 years (14.0 to 15.5 years, discounted), averted 13,000 transmitted HIV infections over 5 years, increased discounted lifetime care costs from $3040 to $3240, and resulted in a lifetime ICER of $130/YLS, less than 10% of India"s per capita GDP in 2015. dolutegravir 26-29 cAMP responsive element modulator Homo sapiens 305-309 30561642-2 2019 We hypothesized that increasing dolutegravir trough concentrations (Ctrough) and/or polymorphism in the SLC22A2 gene, encoding the organic cation transporter-2 (OCT2), which is involved in monoamine clearance in the CNS and is inhibited by dolutegravir, might be associated with NPs. dolutegravir 32-44 solute carrier family 22 member 2 Homo sapiens 104-111 30561642-2 2019 We hypothesized that increasing dolutegravir trough concentrations (Ctrough) and/or polymorphism in the SLC22A2 gene, encoding the organic cation transporter-2 (OCT2), which is involved in monoamine clearance in the CNS and is inhibited by dolutegravir, might be associated with NPs. dolutegravir 32-44 solute carrier family 22 member 2 Homo sapiens 131-159 30561642-2 2019 We hypothesized that increasing dolutegravir trough concentrations (Ctrough) and/or polymorphism in the SLC22A2 gene, encoding the organic cation transporter-2 (OCT2), which is involved in monoamine clearance in the CNS and is inhibited by dolutegravir, might be associated with NPs. dolutegravir 32-44 solute carrier family 22 member 2 Homo sapiens 161-165 30561642-2 2019 We hypothesized that increasing dolutegravir trough concentrations (Ctrough) and/or polymorphism in the SLC22A2 gene, encoding the organic cation transporter-2 (OCT2), which is involved in monoamine clearance in the CNS and is inhibited by dolutegravir, might be associated with NPs. dolutegravir 240-252 solute carrier family 22 member 2 Homo sapiens 104-111 30561642-2 2019 We hypothesized that increasing dolutegravir trough concentrations (Ctrough) and/or polymorphism in the SLC22A2 gene, encoding the organic cation transporter-2 (OCT2), which is involved in monoamine clearance in the CNS and is inhibited by dolutegravir, might be associated with NPs. dolutegravir 240-252 solute carrier family 22 member 2 Homo sapiens 131-159 30561642-2 2019 We hypothesized that increasing dolutegravir trough concentrations (Ctrough) and/or polymorphism in the SLC22A2 gene, encoding the organic cation transporter-2 (OCT2), which is involved in monoamine clearance in the CNS and is inhibited by dolutegravir, might be associated with NPs. dolutegravir 240-252 solute carrier family 22 member 2 Homo sapiens 161-165 30561642-11 2019 CONCLUSIONS: A variant of the OCT2-encoding gene, in addition to or in synergy with higher dolutegravir Ctrough, is associated with a set of NPs observed during dolutegravir therapy. dolutegravir 91-103 solute carrier family 22 member 2 Homo sapiens 30-34 30561642-11 2019 CONCLUSIONS: A variant of the OCT2-encoding gene, in addition to or in synergy with higher dolutegravir Ctrough, is associated with a set of NPs observed during dolutegravir therapy. dolutegravir 161-173 solute carrier family 22 member 2 Homo sapiens 30-34 30541077-7 2019 Dolutegravir AUC0- GMR (90% CI) was 1.16 (1.00-1.34) with elbasvir and grazoprevir. dolutegravir 0-12 colony stimulating factor 2 receptor subunit alpha Homo sapiens 20-23 30541077-9 2019 The grazoprevir AUC0-24 GMR (90% CI) was 0.89 (0.72-1.09) with raltegravir and 0.81 (0.67-0.97) with dolutegravir. dolutegravir 101-113 colony stimulating factor 2 receptor subunit alpha Homo sapiens 24-27 30342022-7 2018 In summary, the current study uncovered the CYP1A1 and 1B1-mediated metabolic pathways of DTG. dolutegravir 90-93 cytochrome P450, family 1, subfamily a, polypeptide 1 Mus musculus 44-58 30342022-8 2018 These data suggest that persons with HIV infection receiving DTG should be cautious to cigarettes, and drugs, or exposure to environmental chemicals that induce CYP1A1 and 1B1. dolutegravir 61-64 cytochrome P450, family 1, subfamily a, polypeptide 1 Mus musculus 161-175 30443021-4 2018 TMEM97 KO resulted in a complete loss of binding of [125I]RHM-4 and a significant reduction in binding of [3H]DTG. dolutegravir 110-113 transmembrane protein 97 Homo sapiens 0-6 30081493-11 2018 Regression of DTG curves from thermal analysis showed improvement of thermal stability with the increase of PCL and PE. dolutegravir 14-17 PHD finger protein 1 Homo sapiens 108-118 29688533-0 2018 Plasma cystatin C as a marker for estimated glomerular filtration rate assessment in HIV-1-infected patients treated with dolutegravir-based ART. dolutegravir 122-134 cystatin C Homo sapiens 7-17 29688533-2 2018 Serum cystatin C is a non-organic cation transporter-2-dependent marker, possibly enabling glomerular filtration rate (GFR) estimation under dolutegravir. dolutegravir 141-153 cystatin C Homo sapiens 6-16 29150412-12 2018 CONCLUSIONS: eGFRcys provided the most precise estimate and most closely approximate Cin in HIV-1-infected Japanese patients with suppressed viremia treated with dolutegravir. dolutegravir 162-174 pyridoxal phosphatase Homo sapiens 85-88 30541118-0 2019 Improvement in insulin sensitivity and serum leptin concentration after the switch from a ritonavir-boosted PI to raltegravir or dolutegravir in non-diabetic HIV-infected patients. dolutegravir 129-141 insulin Homo sapiens 15-22 30541118-0 2019 Improvement in insulin sensitivity and serum leptin concentration after the switch from a ritonavir-boosted PI to raltegravir or dolutegravir in non-diabetic HIV-infected patients. dolutegravir 129-141 leptin Homo sapiens 45-51 30541118-8 2019 CONCLUSIONS: In HIV-positive subjects on suppressive cART, the switch from a PI/r to raltegravir or dolutegravir led to a significant and comparable reduction in both HOMA index and serum leptin level, reflecting a similar and significant improvement in insulin sensitivity. dolutegravir 100-112 leptin Homo sapiens 188-194 30541118-8 2019 CONCLUSIONS: In HIV-positive subjects on suppressive cART, the switch from a PI/r to raltegravir or dolutegravir led to a significant and comparable reduction in both HOMA index and serum leptin level, reflecting a similar and significant improvement in insulin sensitivity. dolutegravir 100-112 insulin Homo sapiens 254-261 30559742-7 2018 All identified DTGs were found to directly or indirectly inhibit IFN-gamma production or Th1 differentiation. dolutegravir 15-19 interferon gamma Homo sapiens 65-74 30559742-8 2018 We hypothesize that the absolute need for DTG to control potentially lethal IFN-gamma PRG activity leads to T. cruzi persistence and establishment of chronic infection. dolutegravir 42-45 interferon gamma Homo sapiens 76-85 30342022-0 2018 CYP1A1 and 1B1-mediated metabolic pathways of dolutegravir, an HIV integrase inhibitor. dolutegravir 46-58 cytochrome P450, family 1, subfamily a, polypeptide 1 Mus musculus 0-14 30342022-5 2018 CYP1A1 and 1B1 were also identified as the major enzymes contributing to the formation of M1 (an N-dealkylated metabolite of DTG) and M5 (an aldehyde). dolutegravir 125-128 cytochrome P450, family 1, subfamily a, polypeptide 1 Mus musculus 0-14 29285709-7 2018 In the DTG, after IWT, the methylation increased at 4/6 sites in the promoter region of the NFKB2 gene in the whole blood (all, P < 0.04), with an 18% increase in the average methylation of the 6 sites (P = 0.035). dolutegravir 7-10 nuclear factor kappa B subunit 2 Homo sapiens 92-97 30252923-0 2018 Glomerular filtration rate estimated by cystatin C formulas in HIV-1 patients treated with dolutegravir, rilpivirine or cobicistat. dolutegravir 91-103 cystatin C Homo sapiens 40-50 29957545-1 2018 BACKGROUND: Dolutegravir (DTG) is a next-generation HIV integrase inhibitor (INI) with an increased genetic barrier to resistance with respect to raltegravir (RAL) or elvitegravir (EVG). dolutegravir 12-24 PHD finger protein 5A Homo sapiens 77-80 29957545-1 2018 BACKGROUND: Dolutegravir (DTG) is a next-generation HIV integrase inhibitor (INI) with an increased genetic barrier to resistance with respect to raltegravir (RAL) or elvitegravir (EVG). dolutegravir 26-29 PHD finger protein 5A Homo sapiens 77-80 29617822-11 2018 Changes in the 3"-PPT point to a new dolutegravir resistance mechanism in vivo. dolutegravir 37-49 tachykinin precursor 1 Homo sapiens 18-21 29688533-13 2018 Use of cystatin C may enable better understanding of plasma creatinine fluctuations after dolutegravir initiation, particularly in high-risk renal patients. dolutegravir 90-102 cystatin C Homo sapiens 7-17 29698323-0 2018 Does simplification to dolutegravir-based dual regimens impact on the CD4+/CD8+ T-cell ratio? dolutegravir 23-35 CD4 molecule Homo sapiens 70-73 29698323-0 2018 Does simplification to dolutegravir-based dual regimens impact on the CD4+/CD8+ T-cell ratio? dolutegravir 23-35 CD8a molecule Homo sapiens 75-78 29558972-8 2018 Within 4-8 weeks after DTG treatment onset, a complete viral suppression and a concomitant increase of CD4+ cell count was observed. dolutegravir 23-26 CD4 molecule Homo sapiens 103-106 29603882-9 2018 DTG maintained an ICER below 50% of India"s per capita GDP as long as the annual three-drug regimen cost was <=$180/year. dolutegravir 0-3 cAMP responsive element modulator Homo sapiens 18-22 28838281-0 2018 Utility of estimated glomerular filtration rate based on cystatin C in patients receiving combination antiretroviral therapy including dolutegravir. dolutegravir 135-147 cystatin C Homo sapiens 57-67 28741965-8 2018 The cost per QALY gained (ICER) for DTG compared to EFV was $6,939. dolutegravir 36-39 cAMP responsive element modulator Homo sapiens 26-30 28379313-9 2017 Analysis by 2D-DIGE indicated a significant decrease in two phosphorylated spots of cardiac troponin I (cTnI) in the DTG animals compared to NTG and Tm54. dolutegravir 117-120 troponin I, cardiac 3 Mus musculus 84-102 28649847-0 2017 Short Communication: The Clinical Value of Cystatin C as a Marker of Renal Function in HIV Patients Receiving Dolutegravir. dolutegravir 110-122 cystatin C Homo sapiens 43-53 28649847-9 2017 In HIV patients receiving DTG, measurement of serum cystatin C as an alternative renal function test might be clinically valuable because it is not affected by DTG administration. dolutegravir 26-29 cystatin C Homo sapiens 52-62 28915895-0 2017 Impact of UGT1A1 gene polymorphisms on plasma dolutegravir trough concentrations and neuropsychiatric adverse events in Japanese individuals infected with HIV-1. dolutegravir 46-58 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 10-16 28915895-1 2017 BACKGROUND: Dolutegravir (DTG) is metabolized mainly by uridine diphosphate (UDP)-glucuronosyltransferase 1A1 (UGT1A1), and partly by cytochrome P450 3A (CYP3A). dolutegravir 12-24 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 56-109 28915895-1 2017 BACKGROUND: Dolutegravir (DTG) is metabolized mainly by uridine diphosphate (UDP)-glucuronosyltransferase 1A1 (UGT1A1), and partly by cytochrome P450 3A (CYP3A). dolutegravir 12-24 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 111-117 28915895-1 2017 BACKGROUND: Dolutegravir (DTG) is metabolized mainly by uridine diphosphate (UDP)-glucuronosyltransferase 1A1 (UGT1A1), and partly by cytochrome P450 3A (CYP3A). dolutegravir 12-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 134-152 28915895-1 2017 BACKGROUND: Dolutegravir (DTG) is metabolized mainly by uridine diphosphate (UDP)-glucuronosyltransferase 1A1 (UGT1A1), and partly by cytochrome P450 3A (CYP3A). dolutegravir 12-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 154-159 28915895-1 2017 BACKGROUND: Dolutegravir (DTG) is metabolized mainly by uridine diphosphate (UDP)-glucuronosyltransferase 1A1 (UGT1A1), and partly by cytochrome P450 3A (CYP3A). dolutegravir 26-29 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 56-109 28915895-1 2017 BACKGROUND: Dolutegravir (DTG) is metabolized mainly by uridine diphosphate (UDP)-glucuronosyltransferase 1A1 (UGT1A1), and partly by cytochrome P450 3A (CYP3A). dolutegravir 26-29 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 111-117 28915895-1 2017 BACKGROUND: Dolutegravir (DTG) is metabolized mainly by uridine diphosphate (UDP)-glucuronosyltransferase 1A1 (UGT1A1), and partly by cytochrome P450 3A (CYP3A). dolutegravir 26-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 134-152 28915895-1 2017 BACKGROUND: Dolutegravir (DTG) is metabolized mainly by uridine diphosphate (UDP)-glucuronosyltransferase 1A1 (UGT1A1), and partly by cytochrome P450 3A (CYP3A). dolutegravir 26-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 154-159 28915895-10 2017 Multivariate analysis revealed that carrying one or two UGT1A1*6 gene polymorphisms, one UGT1A1*28 polymorphism, and age of < 40 years were independent factors associated with high DTG trough concentrations. dolutegravir 184-187 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 56-62 28915895-10 2017 Multivariate analysis revealed that carrying one or two UGT1A1*6 gene polymorphisms, one UGT1A1*28 polymorphism, and age of < 40 years were independent factors associated with high DTG trough concentrations. dolutegravir 184-187 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 89-95 28915895-13 2017 CONCLUSION: In addition to younger age, carrying UGT1A1*6 and/or UGT1A1*28 was demonstrated to be a factor associated with high DTG trough concentrations. dolutegravir 128-131 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 49-55 28915895-13 2017 CONCLUSION: In addition to younger age, carrying UGT1A1*6 and/or UGT1A1*28 was demonstrated to be a factor associated with high DTG trough concentrations. dolutegravir 128-131 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 65-71 28858994-0 2017 High plasma concentrations of dolutegravir in patients with ABCG2 genetic variants. dolutegravir 30-42 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 60-65 28858994-2 2017 Dolutegravir was identified recently as a substrate of both ABCB1 and ABCG2. dolutegravir 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 60-65 28858994-2 2017 Dolutegravir was identified recently as a substrate of both ABCB1 and ABCG2. dolutegravir 0-12 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 70-75 28858994-3 2017 This study aimed to determine the relations between single-nucleotide polymorphisms of ABCB1 and ABCG2 genes and plasma dolutegravir concentrations. dolutegravir 120-132 ATP binding cassette subfamily B member 1 Homo sapiens 87-92 28858994-3 2017 This study aimed to determine the relations between single-nucleotide polymorphisms of ABCB1 and ABCG2 genes and plasma dolutegravir concentrations. dolutegravir 120-132 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 97-102 28858994-9 2017 In contrast, the mean peak plasma concentration of dolutegravir was significantly higher in the genotypes of ABCG2 421 AA (5002 ng/ml, n=3) compared with the genotypes of ABCG2 421 CC (2569 ng/ml, n=22) and ABCG2 421 CA (2479 ng/ml, n=17) (P=0.0005). dolutegravir 51-63 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 109-114 28858994-10 2017 The speculated peak level of plasma dolutegravir concentration was significantly higher in ABCG2 genetic variant holders, probably, at least in part, because of low expression levels of efflux transporters in the intestines associated with these genetic variants. dolutegravir 36-48 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 91-96 28379313-9 2017 Analysis by 2D-DIGE indicated a significant decrease in two phosphorylated spots of cardiac troponin I (cTnI) in the DTG animals compared to NTG and Tm54. dolutegravir 117-120 troponin I, cardiac 3 Mus musculus 104-108 27999010-3 2017 Patients and methods: A prospective observational study in HIV/HCV-coinfected patients with liver cirrhosis on ART with dolutegravir plus rilpivirine and treated with simeprevir plus sofosbuvir (+-ribavirin) was conducted. dolutegravir 120-132 artemin Homo sapiens 111-114 28584127-7 2017 RNA sequencing demonstrated in doxycycline-treated dTg-211 cortices overrepresentation of synaptic activity, Ca2+ transmembrane transport, TGFBR2 signaling, and cholinergic synapse pathways. dolutegravir 51-54 transforming growth factor, beta receptor II Mus musculus 139-145 28007569-6 2017 Furthermore, isothermal titration calorimetry was conducted to examine if DTG and PB28, two structurally distinct nanomolar affinity sigma-2 ligands, bind to purified PGRMC1 proteins that have recently been revealed to form both apo-monomeric and heme-mediated dimeric forms. dolutegravir 74-77 progesterone receptor membrane component 1 Homo sapiens 167-173 28007569-7 2017 While no binding to apo-PGRMC1 monomer was detected, a micromolar affinity to heme-mediated dimerized PGRMC1 was demonstrated in DTG but not in PB28. dolutegravir 129-132 progesterone receptor membrane component 1 Homo sapiens 102-108 26974526-1 2016 BACKGROUND: Dolutegravir is an integrase strand transfer inhibitor (INSTI) licensed for use in HIV-1 infection and is an inhibitor of organic cation transporter 2 (OCT2). dolutegravir 12-24 solute carrier family 22 member 2 Homo sapiens 164-168 26974526-2 2016 This study assessed the effect of dolutegravir on the pharmacokinetics of metformin, an OCT2 substrate. dolutegravir 34-46 solute carrier family 22 member 2 Homo sapiens 88-92 26974526-12 2016 CONCLUSIONS: Dolutegravir significantly increased metformin plasma exposure, which can be partially explained by OCT2 inhibition. dolutegravir 13-25 solute carrier family 22 member 2 Homo sapiens 113-117 26365498-0 2015 Missing CD4+ cell response in randomized clinical trials of maraviroc and dolutegravir. dolutegravir 74-86 CD4 molecule Homo sapiens 8-11 27442249-8 2016 RESULTS: A 48 hours exposure of human erythrocytes to dolutegravir significantly increased the percentage of annexin-V-binding cells (>= 4.8 microM), significantly increased hemolysis (19.1 microM), but did not significantly modify forward scatter. dolutegravir 54-66 annexin A5 Homo sapiens 109-118 27442249-10 2016 The effect of dolutegravir on annexin-V-binding was significantly blunted by removal of extracellular Ca2+, but was not significantly modified by protein kinase C inhibitor staurosporine (1 microM), p38 kinase inhibitor SB203580 (2 microM), casein kinase inhibitor D4476 (10 microM) or pancaspase inhibitor zVAD (10 microM). dolutegravir 14-26 annexin A5 Homo sapiens 30-39 27442249-10 2016 The effect of dolutegravir on annexin-V-binding was significantly blunted by removal of extracellular Ca2+, but was not significantly modified by protein kinase C inhibitor staurosporine (1 microM), p38 kinase inhibitor SB203580 (2 microM), casein kinase inhibitor D4476 (10 microM) or pancaspase inhibitor zVAD (10 microM). dolutegravir 14-26 PDLIM1 interacting kinase 1 like Homo sapiens 241-254 26898568-1 2016 PURPOSE: Dolutegravir (DTG) is primarily metabolized by UGT1A1 with CYP3A as a minor route. dolutegravir 9-21 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 56-62 26898568-1 2016 PURPOSE: Dolutegravir (DTG) is primarily metabolized by UGT1A1 with CYP3A as a minor route. dolutegravir 9-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-73 26898568-1 2016 PURPOSE: Dolutegravir (DTG) is primarily metabolized by UGT1A1 with CYP3A as a minor route. dolutegravir 23-26 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 56-62 26898568-1 2016 PURPOSE: Dolutegravir (DTG) is primarily metabolized by UGT1A1 with CYP3A as a minor route. dolutegravir 23-26 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-73 25394090-3 2014 In vitro, DTG inhibits organic cation transporter 2 (OCT2) and multidrug and toxin extrusion transporter 1 (MATE 1) which are known to be involved in the disposition of metformin. dolutegravir 10-13 solute carrier family 22 member 2 Homo sapiens 23-51 26071720-2 2015 The pressure coefficients of the glass transition temperature (dT(g)/dp) for itraconazole and ketoconazole were determined to be equal to 183 and 228 K/GPa, respectively. dolutegravir 63-68 glycophorin A (MNS blood group) Homo sapiens 152-155 26229068-9 2015 Kidney injury molecule-1 tissue expression in raltegravir and dolutegravir groups was nonsignificantly elevated compared to control (1.2-fold compared to control). dolutegravir 62-74 hepatitis A virus cellular receptor 1 Mus musculus 0-24 25849829-0 2015 Dolutegravir inhibits HIV-1 Env evolution in primary human cells. dolutegravir 0-12 Envelope surface glycoprotein gp160, precursor Human immunodeficiency virus 1 28-31 25849829-4 2015 METHODS: Here, we tested this hypothesis by measuring the genetic and amino-acid diversity of Env/gp160 from two HIV-1 primary isolates that were grown in the presence of increasing concentrations of DTG or RAL over the course of 38-55 weeks. dolutegravir 200-203 Envelope surface glycoprotein gp160, precursor Human immunodeficiency virus 1 94-97 25858605-4 2015 Dolutegravir is metabolized by UGT1A1 and, to a lesser extent, by CYP3A4, without being an inducer or inhibitor of the usual metabolic systems. dolutegravir 0-12 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 31-37 25858605-4 2015 Dolutegravir is metabolized by UGT1A1 and, to a lesser extent, by CYP3A4, without being an inducer or inhibitor of the usual metabolic systems. dolutegravir 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-72 25858605-10 2015 Dolutegravir can reduce renal tubule secretion of substances excreted via OCT2, with a slight initial increase in creatinine, with no risk of renal toxicity. dolutegravir 0-12 POU class 2 homeobox 2 Homo sapiens 74-78 25845873-3 2015 From the interaction between atazanavir and DTG via CYP3A4 and UGT1A1 and placental efflux transporter inhibition and considering the infant"s probable enzymatic immaturity, the DTG elimination half-life was estimated to be 4-fold longer in neonates than in adults. dolutegravir 44-47 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-58 25845873-3 2015 From the interaction between atazanavir and DTG via CYP3A4 and UGT1A1 and placental efflux transporter inhibition and considering the infant"s probable enzymatic immaturity, the DTG elimination half-life was estimated to be 4-fold longer in neonates than in adults. dolutegravir 44-47 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 63-69 25397494-1 2014 INTRODUCTION: The most recently approved antiretroviral, the integrase inhibitor dolutegravir (DTG), is described to be a very potent drug with a unique resistance profile, but a certain degree of cross-resistance to RAL or EVG induced drug resistance, which is mediated mainly by integrase mutations at positions 140 and 148. dolutegravir 81-93 RAS like proto-oncogene A Homo sapiens 217-220 25397494-1 2014 INTRODUCTION: The most recently approved antiretroviral, the integrase inhibitor dolutegravir (DTG), is described to be a very potent drug with a unique resistance profile, but a certain degree of cross-resistance to RAL or EVG induced drug resistance, which is mediated mainly by integrase mutations at positions 140 and 148. dolutegravir 95-98 RAS like proto-oncogene A Homo sapiens 217-220 25397500-0 2014 Use of dolutegravir in two INI-experienced patients with multiclass resistance resulted in excellent virological and immunological responses. dolutegravir 7-19 PHD finger protein 5A Homo sapiens 27-30 25733917-4 2015 As a substrate of CYP 3A4, dolutegravir is affected by rifampin, efavirenz, tipranavir/ritonavir, fosamprenavir/ritonavir, and dose increase is required. dolutegravir 27-39 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 18-25 25733917-5 2015 Dolutegravir inhibits the organic cation transporter 2, resulting in decreased creatinine clearance with no apparent decrease in renal function. dolutegravir 0-12 solute carrier family 22 member 2 Homo sapiens 26-54 25924475-5 2015 Comparing the two INIs as the "anchor" for HAART, DTG exhibited an equivalent CI to that of RAL on wild type HIV-1 replication; but a greater synergy than RAL on INI-resistant HIV-1 replication. dolutegravir 50-53 PHD finger protein 5A Homo sapiens 18-21 25394090-3 2014 In vitro, DTG inhibits organic cation transporter 2 (OCT2) and multidrug and toxin extrusion transporter 1 (MATE 1) which are known to be involved in the disposition of metformin. dolutegravir 10-13 solute carrier family 22 member 2 Homo sapiens 53-57 25394090-3 2014 In vitro, DTG inhibits organic cation transporter 2 (OCT2) and multidrug and toxin extrusion transporter 1 (MATE 1) which are known to be involved in the disposition of metformin. dolutegravir 10-13 solute carrier family 47 member 1 Homo sapiens 63-106 25394090-3 2014 In vitro, DTG inhibits organic cation transporter 2 (OCT2) and multidrug and toxin extrusion transporter 1 (MATE 1) which are known to be involved in the disposition of metformin. dolutegravir 10-13 solute carrier family 47 member 1 Homo sapiens 108-114 24446523-1 2014 BACKGROUND: The pilot phase IIb VIKING study suggested that dolutegravir (DTG), a human immunodeficiency virus (HIV) integrase inhibitor (INI), would be efficacious in INI-resistant patients at the 50 mg twice daily (BID) dose. dolutegravir 60-72 BH3 interacting domain death agonist Homo sapiens 217-220 25188312-7 2014 Adjusting for the effect of NRTI backbone, treatment with DTG resulted in significantly higher odds of virologic suppression (HIV RNA<50 copies/mL) and increase in CD4+ cells/microL versus ATV/r, DRV/r, EFV, LPV/r, and RPV. dolutegravir 58-61 CD4 molecule Homo sapiens 167-170 24446523-1 2014 BACKGROUND: The pilot phase IIb VIKING study suggested that dolutegravir (DTG), a human immunodeficiency virus (HIV) integrase inhibitor (INI), would be efficacious in INI-resistant patients at the 50 mg twice daily (BID) dose. dolutegravir 74-77 BH3 interacting domain death agonist Homo sapiens 217-220 24446523-7 2014 DTG 50 mg BID had a low (3%) discontinuation rate due to adverse events, similar to INI-naive subjects receiving DTG 50 mg once daily. dolutegravir 0-3 BH3 interacting domain death agonist Homo sapiens 10-13 24446523-8 2014 CONCLUSIONS: DTG 50 mg BID-based therapy was effective in this highly treatment-experienced population with INI-resistant virus. dolutegravir 13-16 BH3 interacting domain death agonist Homo sapiens 23-26 24891452-5 2014 Both sigma1R agonists, (+)pentazocine (PTZ) and DTG [1,3-di-(2-tolyl)guanidine], dose dependently inhibited calcium current (ICa) with Ba(2+) as charge carrier in control sensory neurons. dolutegravir 48-51 sigma non-opioid intracellular receptor 1 Rattus norvegicus 5-12 24096683-1 2014 PURPOSE: Dolutegravir (DTG), an unboosted HIV integrase inhibitor (INI), is metabolized by UGT1A1 and to a minor extent by CYP3A. dolutegravir 9-21 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 91-97 24646860-8 2014 Trimethoprim potently inhibited MATE2-K, whereas dolutegravir preferentially inhibited OCT2. dolutegravir 49-61 POU class 2 homeobox 2 Homo sapiens 87-91 25102336-7 2014 Rilpivirine and dolutegravir block the uptake of creatinine from the blood, inhibiting organic cation transporter 2, and cobicistat interacts with the efflux inhibiting multidrug and toxin extrusion protein 1. dolutegravir 16-28 solute carrier family 22 member 2 Homo sapiens 87-115 24096683-1 2014 PURPOSE: Dolutegravir (DTG), an unboosted HIV integrase inhibitor (INI), is metabolized by UGT1A1 and to a minor extent by CYP3A. dolutegravir 9-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 123-128 24096683-1 2014 PURPOSE: Dolutegravir (DTG), an unboosted HIV integrase inhibitor (INI), is metabolized by UGT1A1 and to a minor extent by CYP3A. dolutegravir 23-26 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 91-97 24096683-1 2014 PURPOSE: Dolutegravir (DTG), an unboosted HIV integrase inhibitor (INI), is metabolized by UGT1A1 and to a minor extent by CYP3A. dolutegravir 23-26 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 123-128 24096683-9 2014 DTG mean exposure was lower in subjects with severe renal impairment compared to healthy, matched subjects: AUC(0- ) and Cmax were 40 % and 23 % lower, while mean DTG-Gluc was increased. dolutegravir 0-3 glucosylceramidase beta 3 (gene/pseudogene) Homo sapiens 167-171 24096683-9 2014 DTG mean exposure was lower in subjects with severe renal impairment compared to healthy, matched subjects: AUC(0- ) and Cmax were 40 % and 23 % lower, while mean DTG-Gluc was increased. dolutegravir 163-166 glucosylceramidase beta 3 (gene/pseudogene) Homo sapiens 167-171 24096683-11 2014 CONCLUSIONS: The modest reductions in mean PK exposures for DTG and increases for DTG-Gluc in the severe renal impairment group are not considered clinically significant. dolutegravir 82-85 glucosylceramidase beta 3 (gene/pseudogene) Homo sapiens 86-90 24329186-0 2014 Evaluation of the effect of UGT1A1 polymorphisms on dolutegravir pharmacokinetics. dolutegravir 52-64 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 28-34 24329186-1 2014 AIM: To evaluate potential pharmacogenetic effects of UGT1A1 polymorphisms on the pharmacokinetics (PK) of dolutegravir (Tivicay ; ViiV Healthcare, NC, USA), an HIV-1 integrase inhibitor. dolutegravir 107-119 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 54-60 24329186-4 2014 CONCLUSION: Increased dolutegravir exposure in carriers of UGT1A1 reduced function polymorphisms is not clinically significant based on accumulated safety data so dose adjustment in these individuals is not required. dolutegravir 22-34 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 59-65 23111447-11 2013 treatment was done, and the proportion of large A-fiber neurons expressing TRPV1 increased in dTg capsaicin-treated mice. dolutegravir 94-97 transient receptor potential cation channel, subfamily V, member 1 Mus musculus 75-80 23824675-11 2013 Dolutegravir"s major and minor metabolic pathways are uridine diphosphate glucuronosyltransferase 1A1 and cytochrome P450 (CYP)-3A4, respectively, and it neither induces nor inhibits CYP isoenzymes. dolutegravir 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 106-131 23132334-3 2013 DTG is a substrate for the efflux transporters P-glycoprotein (Pgp) and human breast cancer resistance protein (BCRP). dolutegravir 0-3 ATP binding cassette subfamily B member 1 Homo sapiens 47-61 23132334-3 2013 DTG is a substrate for the efflux transporters P-glycoprotein (Pgp) and human breast cancer resistance protein (BCRP). dolutegravir 0-3 ATP binding cassette subfamily B member 1 Homo sapiens 63-66 23132334-3 2013 DTG is a substrate for the efflux transporters P-glycoprotein (Pgp) and human breast cancer resistance protein (BCRP). dolutegravir 0-3 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 78-110 23132334-3 2013 DTG is a substrate for the efflux transporters P-glycoprotein (Pgp) and human breast cancer resistance protein (BCRP). dolutegravir 0-3 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 112-116 23132334-5 2013 UDP-glucuronosyltransferase (UGT) 1A1 is the main enzyme responsible for the metabolism of DTG in vivo, with cytochrome P450 (P450) 3A4 being a notable pathway and UGT1A3 and UGT1A9 being only minor pathways. dolutegravir 91-94 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 0-37 23132334-5 2013 UDP-glucuronosyltransferase (UGT) 1A1 is the main enzyme responsible for the metabolism of DTG in vivo, with cytochrome P450 (P450) 3A4 being a notable pathway and UGT1A3 and UGT1A9 being only minor pathways. dolutegravir 91-94 UDP glucuronosyltransferase family 1 member A3 Homo sapiens 164-170 23132334-5 2013 UDP-glucuronosyltransferase (UGT) 1A1 is the main enzyme responsible for the metabolism of DTG in vivo, with cytochrome P450 (P450) 3A4 being a notable pathway and UGT1A3 and UGT1A9 being only minor pathways. dolutegravir 91-94 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 175-181 23132334-8 2013 DTG does inhibit the renal OCT2 (IC(50) = 1.9 muM) transporter, which provides a mechanistic basis for the mild increases in serum creatinine observed in clinical studies. dolutegravir 0-3 POU class 2 homeobox 2 Homo sapiens 27-31 22802950-7 2012 However, the inhibitory effect of transgenic RGS2 on G(q/11)-mediated PLCbeta activation differed between ventricles and atria: (i) in sham-operated dTG mice the magnitude of the inhibitory effect was less pronounced in ventricles than in atria, and (ii) after TAC, negative regulation of G(q/11) signaling was absent in ventricles but fully preserved in atria. dolutegravir 149-152 regulator of G-protein signaling 2 Mus musculus 45-49 23195954-2 2013 We demonstrate unknown facets of calnuc, which is a serine protease in which Ser-378 of GXSXG motif, Asp-328 of DTG motif, and His-339 form the "catalytic triad," locating the enzyme active site in the C-terminal region. dolutegravir 112-115 nucleobindin 1 Homo sapiens 33-39 23195954-2 2013 We demonstrate unknown facets of calnuc, which is a serine protease in which Ser-378 of GXSXG motif, Asp-328 of DTG motif, and His-339 form the "catalytic triad," locating the enzyme active site in the C-terminal region. dolutegravir 112-115 coagulation factor II, thrombin Homo sapiens 52-67 23899439-2 2013 A Phase I open-label pharmacokinetic (PK) study was performed to describe first dose (PK1) and steady-state (PK2) PKs of the integrase inhibitor dolutegravir (DTG) in blood plasma (BP), cervicovaginal fluid (CVF), cervical tissue (CT) and vaginal tissue (VT) in HIV type-1-negative women. dolutegravir 145-157 prokineticin 1 Homo sapiens 86-89 23899439-2 2013 A Phase I open-label pharmacokinetic (PK) study was performed to describe first dose (PK1) and steady-state (PK2) PKs of the integrase inhibitor dolutegravir (DTG) in blood plasma (BP), cervicovaginal fluid (CVF), cervical tissue (CT) and vaginal tissue (VT) in HIV type-1-negative women. dolutegravir 145-157 prokineticin 2 Homo sapiens 109-112 23899439-11 2013 Accumulation of DTG from PK1 to PK2 occurred in BP, CT and VT, but only marginally in CVF. dolutegravir 16-19 prokineticin 1 Homo sapiens 25-28 23899439-11 2013 Accumulation of DTG from PK1 to PK2 occurred in BP, CT and VT, but only marginally in CVF. dolutegravir 16-19 prokineticin 2 Homo sapiens 32-35 23899439-14 2013 At PK2, DTG accumulated to a greater extent in tissue than in BP or CVF, suggesting increased tissue affinity. dolutegravir 8-11 prokineticin 2 Homo sapiens 3-6 20950794-6 2011 DTG-induced stimulation of DA was antagonized by the nonselective sigma(1/2)-receptor antagonist BD 1008 (10 mg/kg intraperitoneal [IP]) and the preferential sigma2-receptor antagonist SN 79 (1-3 mg/kg IP), but not by the preferential sigma1-receptor antagonist, BD 1063 (10-30 mg/kg IP). dolutegravir 0-3 sigma non-opioid intracellular receptor 1 Rattus norvegicus 235-250 21381981-3 2011 S/GSK1349572 represents a new INI in current development. dolutegravir 2-12 PHD finger protein 5A Homo sapiens 30-33 21381981-10 2011 EXPERT OPINION: S/GSK1349572 represents a new, unboosted, once-daily INI in development with distinct pharmacokinetics and resistance profile, which has showed promising potency and tolerability in the first clinical studies. dolutegravir 18-28 PHD finger protein 5A Homo sapiens 9-12 22101373-11 2011 Global phase III clinical trials of dolutegravir (DTG), a second generation INI, are currently in progress. dolutegravir 36-48 PHD finger protein 5A Homo sapiens 76-79 22101373-11 2011 Global phase III clinical trials of dolutegravir (DTG), a second generation INI, are currently in progress. dolutegravir 50-53 PHD finger protein 5A Homo sapiens 76-79 19787680-10 2009 Taking ITA haplotype as reference, multivariate regression analysis confirmed the negative (ITG), and positive (DCG, DTG, DCA and DTA) association of specific ACE haplotypes with DN, after adjusting for potential nephropathy-linked covariates. dolutegravir 117-120 angiotensin I converting enzyme Homo sapiens 159-162 21157032-0 2011 17alpha-estradiol attenuates neuron loss in ovariectomized Dtg AbetaPP/PS1 mice. dolutegravir 59-62 presenilin 1 Mus musculus 71-74 18474109-2 2008 PS1 is regarded as an atypical aspartyl protease harboring two essential aspartic acids in the context of the sequence D257LV and D385FI, respectively, rather than the typical DTG...DTG catalytic motif of classical aspartyl proteases. dolutegravir 176-179 presenilin 1 Homo sapiens 0-3 19699265-0 2009 Caloric restriction attenuates amyloid deposition in middle-aged dtg APP/PS1 mice. dolutegravir 65-68 amyloid beta (A4) precursor protein Mus musculus 69-76 19699265-6 2009 These findings support the view that CR could be a potentially effective, non-pharmacology strategy for reducing relatively heavy Abeta deposition in older adult dtg APP/PS1 mice, and possibly afford similar protection against the onset and progression of AD in older adult humans. dolutegravir 162-165 amyloid beta (A4) precursor protein Mus musculus 166-173 20032576-4 2009 RESULTS: The correlation between percent changes of WC (%dWC) and BMI (%dBMI) were both statistically significantly correlated with percent changes in LDL-C (%dLDL), HDL-C (%dHDL), and TG (%dTG) except that between %dWC and %dHDL in women. dolutegravir 190-193 component of oligomeric golgi complex 2 Homo sapiens 151-156 18563934-6 2008 Site-directed mutagenesis of the DTG motif of ValG to DCD altered its preferences for metal ion binding, but did not seem to affect its substrate specificity. dolutegravir 33-36 dermcidin Homo sapiens 54-57 18474109-2 2008 PS1 is regarded as an atypical aspartyl protease harboring two essential aspartic acids in the context of the sequence D257LV and D385FI, respectively, rather than the typical DTG...DTG catalytic motif of classical aspartyl proteases. dolutegravir 182-185 presenilin 1 Homo sapiens 0-3 18474109-3 2008 In the present studies, we introduced the sequence DTG in PS1 at and around the catalytic D257 and D385 residues to generate three PS1 mutants: D257TG, D385TG, and the double-mutant D257TG/D385TG. dolutegravir 51-54 presenilin 1 Homo sapiens 58-61 18474109-3 2008 In the present studies, we introduced the sequence DTG in PS1 at and around the catalytic D257 and D385 residues to generate three PS1 mutants: D257TG, D385TG, and the double-mutant D257TG/D385TG. dolutegravir 51-54 presenilin 1 Homo sapiens 131-134 12204120-1 2002 Cathepsin E, an intracellular aspartic proteinase of the pepsin family, is composed of two homologous domains, each containing the catalytic Asp residue in a consensus DTG motif. dolutegravir 168-171 cathepsin E Homo sapiens 0-11 18195469-4 2007 The effect of DTG and 8-OH-DPAT co-administration was partly counteracted by WAY 100635 (0.1 mg/kg) as well as by BD 1047 (3 mg/kg), a 5-HT(1A) and sigma(1) receptor antagonists, respectively, suggesting the involvement of both receptor types in the anti-immobility effect in rats. dolutegravir 14-17 5-hydroxytryptamine receptor 1A Rattus norvegicus 135-142 18195469-4 2007 The effect of DTG and 8-OH-DPAT co-administration was partly counteracted by WAY 100635 (0.1 mg/kg) as well as by BD 1047 (3 mg/kg), a 5-HT(1A) and sigma(1) receptor antagonists, respectively, suggesting the involvement of both receptor types in the anti-immobility effect in rats. dolutegravir 14-17 sigma non-opioid intracellular receptor 1 Rattus norvegicus 148-165 11714775-4 2001 We have previously shown that, in these DTg mice, most peripheral CD8 T cells express one TCRbeta chain associated with two TCRalpha chains, as in one-third of the mature T cells from normal mice. dolutegravir 40-43 T cell receptor beta chain Mus musculus 90-97 11714775-4 2001 We have previously shown that, in these DTg mice, most peripheral CD8 T cells express one TCRbeta chain associated with two TCRalpha chains, as in one-third of the mature T cells from normal mice. dolutegravir 40-43 T cell receptor alpha chain Mus musculus 124-132 10834092-4 2000 sigma 1-Receptor agonists (DTG, N-allyl-normetazocine, (+)-3-PPP, (-)-3-PPP) had proarrhythmic effect after systemic administration. dolutegravir 27-30 sigma non-opioid intracellular receptor 1 Rattus norvegicus 0-16