PMID-sentid Pub_year Sent_text comp_official_name comp_offset protein_name organism prot_offset 33387482-3 2021 Treatment of HepaRG cells with 3-deazaadenosine, an inhibitor of RNA methylation, significantly increased UGT1A1, UGT1A3, UGT1A4, UGT1A9, UGT2B7, UGT2B10, and UGT2B15 mRNA levels (1.3- to 2.6-fold). 3-deazaadenosine 31-47 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 146-153 35062878-4 2022 UGT2B10 is a phase II drug metabolizing enzyme involved in the N-glucuronidation of tertiary amine containing drugs. Nitrogen 63-64 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 0-7 35062878-4 2022 UGT2B10 is a phase II drug metabolizing enzyme involved in the N-glucuronidation of tertiary amine containing drugs. tertiary amine 84-98 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 0-7 35062878-10 2022 RESULTS: Four potential ligands for UGT2B10 namely acetaminophen, lorazepam, mycophenolic acid and voriconazole n-oxide intermediate were identified. Acetaminophen 51-64 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 36-43 35062878-10 2022 RESULTS: Four potential ligands for UGT2B10 namely acetaminophen, lorazepam, mycophenolic acid and voriconazole n-oxide intermediate were identified. Lorazepam 66-75 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 36-43 35062878-10 2022 RESULTS: Four potential ligands for UGT2B10 namely acetaminophen, lorazepam, mycophenolic acid and voriconazole n-oxide intermediate were identified. Mycophenolic Acid 77-94 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 36-43 35062878-10 2022 RESULTS: Four potential ligands for UGT2B10 namely acetaminophen, lorazepam, mycophenolic acid and voriconazole n-oxide intermediate were identified. Voriconazole N-Oxide 99-119 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 36-43 35062878-11 2022 Other metabolites of voriconazole satisfied the criteria of being possible ligands of UGT2B10. Voriconazole 21-33 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 86-93 33741369-4 2021 Following screening a variety of phenolic compound(s), we have found that methylophiopogonanone A (MOA) can be readily O-glucuronidated by all tested human UGTs, including the typical N-glucuronidating enzymes UGT1A4 and UGT2B10. methylophiopogonanone 74-95 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 221-228 30049229-0 2018 Highly selective N-glucuronidation of four piperazine-containing drugs by UDP-glucuronosyltransferase 2B10. Nitrogen 17-18 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 74-106 31839590-7 2020 Of these, dothiepin, cidoxepin, cyclobenzaprine, azatadine, cyproheptadine, bifonazole, and asenapine were indicated to be selective UGT2B10 substrates which have not previously been described. Dothiepin 10-19 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 133-140 31839590-7 2020 Of these, dothiepin, cidoxepin, cyclobenzaprine, azatadine, cyproheptadine, bifonazole, and asenapine were indicated to be selective UGT2B10 substrates which have not previously been described. doxepin 21-30 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 133-140 31839590-7 2020 Of these, dothiepin, cidoxepin, cyclobenzaprine, azatadine, cyproheptadine, bifonazole, and asenapine were indicated to be selective UGT2B10 substrates which have not previously been described. cyclobenzaprine 32-47 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 133-140 31839590-7 2020 Of these, dothiepin, cidoxepin, cyclobenzaprine, azatadine, cyproheptadine, bifonazole, and asenapine were indicated to be selective UGT2B10 substrates which have not previously been described. azatadine 49-58 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 133-140 31839590-7 2020 Of these, dothiepin, cidoxepin, cyclobenzaprine, azatadine, cyproheptadine, bifonazole, and asenapine were indicated to be selective UGT2B10 substrates which have not previously been described. Cyproheptadine 60-74 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 133-140 31839590-7 2020 Of these, dothiepin, cidoxepin, cyclobenzaprine, azatadine, cyproheptadine, bifonazole, and asenapine were indicated to be selective UGT2B10 substrates which have not previously been described. bifonazole 76-86 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 133-140 31839590-7 2020 Of these, dothiepin, cidoxepin, cyclobenzaprine, azatadine, cyproheptadine, bifonazole, and asenapine were indicated to be selective UGT2B10 substrates which have not previously been described. asenapine 92-101 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 133-140 33109037-2 2020 CYP2C8 and UGT2B10 are metabolic enzymes, which may be involved in the metabolism of desloratadine. desloratadine 85-98 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 11-18 31699808-4 2020 Where cytochrome P450 (P450) was responsible for the metabolism in rats with a low Michaelis constant, human-specific UDP-glucuronosyltransferase 2B10- and 1A4-mediated N-glucuronidation was identified as the leading contributor to metabolism in humans with a high V max capacity. Nitrogen 169-170 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 118-159 31554697-0 2019 Potential Regulation of UGT2B10 and UGT2B7 by miR-485-5p in Human Liver. mir-485-5p 46-56 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 31554697-9 2019 UGT2B10 and UGT2B7 activities were probed using nicotine and 3"-azido-3"-deoxythymidine, respectively, and significant decreases in glucuronidation activity were observed for both substrates in HuH-7 and Hep3B cells upon overexpression of miR-485-5p mimic. Nicotine 48-56 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 0-7 31554697-9 2019 UGT2B10 and UGT2B7 activities were probed using nicotine and 3"-azido-3"-deoxythymidine, respectively, and significant decreases in glucuronidation activity were observed for both substrates in HuH-7 and Hep3B cells upon overexpression of miR-485-5p mimic. Zidovudine 61-87 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 0-7 30049229-0 2018 Highly selective N-glucuronidation of four piperazine-containing drugs by UDP-glucuronosyltransferase 2B10. Piperazine 43-53 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 74-106 30049229-5 2018 Reaction phenotyping, chemical inhibition, and activity correlation analysis revealed that UGT2B10 was a high-affinity enzyme and mainly responsible for hepatic N-glucuronidation of all drugs except mianserin. Nitrogen 161-162 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 91-98 30049229-5 2018 Reaction phenotyping, chemical inhibition, and activity correlation analysis revealed that UGT2B10 was a high-affinity enzyme and mainly responsible for hepatic N-glucuronidation of all drugs except mianserin. Mianserin 199-208 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 91-98 30049229-6 2018 Both UGT1A4 and UGT2B10 were important contributors to mianserin N-glucuronidation. mianserin n 55-66 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 16-23 30049229-9 2018 CONCLUSIONS: UGT2B10 plays a critical role in N-glucuronidation of piperazine-containing drugs. Nitrogen 2-3 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 13-20 30049229-9 2018 CONCLUSIONS: UGT2B10 plays a critical role in N-glucuronidation of piperazine-containing drugs. Piperazine 67-77 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 13-20 29431853-1 2018 UGT2B10 is an important metabolism enzyme in human body and its substrates include multiple amine-containing compounds, especially nicotine, tamoxifen and multiple antidepressants. Amines 92-97 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 0-7 29691239-0 2018 Disposition of Mianserin and Cyclizine in UGT2B10-Overexpressing Human Embryonic Kidney 293 Cells: Identification of UGT2B10 as a Novel N-Glucosidation Enzyme and Breast Cancer Resistance Protein as an N-Glucoside Transporter. Mianserin 15-24 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 42-49 29691239-0 2018 Disposition of Mianserin and Cyclizine in UGT2B10-Overexpressing Human Embryonic Kidney 293 Cells: Identification of UGT2B10 as a Novel N-Glucosidation Enzyme and Breast Cancer Resistance Protein as an N-Glucoside Transporter. Mianserin 15-24 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 117-124 29691239-0 2018 Disposition of Mianserin and Cyclizine in UGT2B10-Overexpressing Human Embryonic Kidney 293 Cells: Identification of UGT2B10 as a Novel N-Glucosidation Enzyme and Breast Cancer Resistance Protein as an N-Glucoside Transporter. Cyclizine 29-38 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 117-124 29691239-2 2018 We aimed to investigate a potential role of UGT2B10 in N-glucosidation and to determine the transporters for the excretion of N-glucosides. Nitrogen 55-56 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 44-51 29691239-10 2018 In conclusion, UGT2B10 was for the first time identified as an N-glucosidation enzyme. Nitrogen 63-64 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 15-22 29431853-1 2018 UGT2B10 is an important metabolism enzyme in human body and its substrates include multiple amine-containing compounds, especially nicotine, tamoxifen and multiple antidepressants. Nicotine 131-139 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 0-7 29431853-1 2018 UGT2B10 is an important metabolism enzyme in human body and its substrates include multiple amine-containing compounds, especially nicotine, tamoxifen and multiple antidepressants. Tamoxifen 141-150 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 0-7 29158210-8 2018 The UGT2B10 phenotype ratio (nicotine glucuronide/nicotine) was higher at early and late pregnancy compared with postpartum (P = 0.07 and P < 0.05, respectively) and correlated with a second UGT2B10 phenotype ratio (cotinine glucuronide/cotinine) (all P < 0.001), suggesting UGT2B10 activity is induced during pregnancy. Cotinine 219-227 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 4-11 29438977-1 2018 The detoxification enzyme UDP-glucuronosyltransferase UGT2B10 is specialized in the N-linked glucuronidation of many drugs and xenobiotics. Nitrogen 84-85 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 54-61 29631575-7 2018 RESULTS: For cotinine levels, SNPs near UGT2B10 gene achieved genome-wide significance (i.e. P < 5 x 10- 8) with top SNP rs10023464, P = 1.27 x 10- 11. Cotinine 13-21 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 40-47 29158210-9 2018 In conclusion, pregnancy-induced increases in nicotine metabolism start by 12 weeks gestation and continue as pregnancy progresses most likely due to induction of CYP2A6 and UGT2B10, resulting in potential reductions in the effectiveness of nicotine replacement therapies and an increase in metabolism of other CYP2A6 and UGT2B10 substrates during pregnancy. Nicotine 46-54 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 174-181 29158210-9 2018 In conclusion, pregnancy-induced increases in nicotine metabolism start by 12 weeks gestation and continue as pregnancy progresses most likely due to induction of CYP2A6 and UGT2B10, resulting in potential reductions in the effectiveness of nicotine replacement therapies and an increase in metabolism of other CYP2A6 and UGT2B10 substrates during pregnancy. Nicotine 46-54 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 322-329 29158210-9 2018 In conclusion, pregnancy-induced increases in nicotine metabolism start by 12 weeks gestation and continue as pregnancy progresses most likely due to induction of CYP2A6 and UGT2B10, resulting in potential reductions in the effectiveness of nicotine replacement therapies and an increase in metabolism of other CYP2A6 and UGT2B10 substrates during pregnancy. Nicotine 241-249 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 174-181 28803208-0 2017 N-glucuronidation catalyzed by UGT1A4 and UGT2B10 in human liver microsomes: Assay optimization and substrate identification. Nitrogen 0-1 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 42-49 29158210-8 2018 The UGT2B10 phenotype ratio (nicotine glucuronide/nicotine) was higher at early and late pregnancy compared with postpartum (P = 0.07 and P < 0.05, respectively) and correlated with a second UGT2B10 phenotype ratio (cotinine glucuronide/cotinine) (all P < 0.001), suggesting UGT2B10 activity is induced during pregnancy. nicotine N-glucuronide 29-49 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 4-11 29158210-8 2018 The UGT2B10 phenotype ratio (nicotine glucuronide/nicotine) was higher at early and late pregnancy compared with postpartum (P = 0.07 and P < 0.05, respectively) and correlated with a second UGT2B10 phenotype ratio (cotinine glucuronide/cotinine) (all P < 0.001), suggesting UGT2B10 activity is induced during pregnancy. nicotine N-glucuronide 29-49 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 194-201 29158210-8 2018 The UGT2B10 phenotype ratio (nicotine glucuronide/nicotine) was higher at early and late pregnancy compared with postpartum (P = 0.07 and P < 0.05, respectively) and correlated with a second UGT2B10 phenotype ratio (cotinine glucuronide/cotinine) (all P < 0.001), suggesting UGT2B10 activity is induced during pregnancy. nicotine N-glucuronide 29-49 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 194-201 29158210-8 2018 The UGT2B10 phenotype ratio (nicotine glucuronide/nicotine) was higher at early and late pregnancy compared with postpartum (P = 0.07 and P < 0.05, respectively) and correlated with a second UGT2B10 phenotype ratio (cotinine glucuronide/cotinine) (all P < 0.001), suggesting UGT2B10 activity is induced during pregnancy. Nicotine 29-37 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 4-11 29158210-8 2018 The UGT2B10 phenotype ratio (nicotine glucuronide/nicotine) was higher at early and late pregnancy compared with postpartum (P = 0.07 and P < 0.05, respectively) and correlated with a second UGT2B10 phenotype ratio (cotinine glucuronide/cotinine) (all P < 0.001), suggesting UGT2B10 activity is induced during pregnancy. Nicotine 29-37 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 194-201 29158210-8 2018 The UGT2B10 phenotype ratio (nicotine glucuronide/nicotine) was higher at early and late pregnancy compared with postpartum (P = 0.07 and P < 0.05, respectively) and correlated with a second UGT2B10 phenotype ratio (cotinine glucuronide/cotinine) (all P < 0.001), suggesting UGT2B10 activity is induced during pregnancy. Nicotine 29-37 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 194-201 29158210-8 2018 The UGT2B10 phenotype ratio (nicotine glucuronide/nicotine) was higher at early and late pregnancy compared with postpartum (P = 0.07 and P < 0.05, respectively) and correlated with a second UGT2B10 phenotype ratio (cotinine glucuronide/cotinine) (all P < 0.001), suggesting UGT2B10 activity is induced during pregnancy. cotinine N-glucuronide 219-239 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 4-11 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. Nitrogen 63-64 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. Amines 98-104 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. asenapine 116-125 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. Loxapine 127-135 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. Clozapine 137-146 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. Chlorpromazine 148-162 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. Dothiepin 164-173 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. Doxepin 175-182 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. Mirtazapine 184-195 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. Mianserin 197-206 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. chlorcyclizine 208-222 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. Cyclizine 213-222 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. Promethazine 235-247 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. cyclobenzaprine 249-264 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. Imatinib Mesylate 266-274 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. retrorsine 276-286 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. Strychnine 288-298 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-6 2017 In addition, UGT1A4 and UGT2B10 were primarily responsible for N-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine, dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine, imatinib, retrorsine, strychnine and brucine. brucine 303-310 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28803208-8 2017 Also, UGT1A4- and UGT2B10-mediated N-glucuronidation might play significant roles in metabolism and detoxification of tertiary amines in humans. Nitrogen 35-36 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 18-25 28803208-8 2017 Also, UGT1A4- and UGT2B10-mediated N-glucuronidation might play significant roles in metabolism and detoxification of tertiary amines in humans. tertiary amines 118-133 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 18-25 28267333-1 2017 Little is known about transcriptional regulators of UDP-glucuronosyltransferase 2B10 (UGT2B10), an enzyme known to glucuronidate many chemicals and drugs such as nicotine and tricyclic antidepressants. Nicotine 162-170 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 52-84 28267333-1 2017 Little is known about transcriptional regulators of UDP-glucuronosyltransferase 2B10 (UGT2B10), an enzyme known to glucuronidate many chemicals and drugs such as nicotine and tricyclic antidepressants. Nicotine 162-170 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 86-93 28267333-2 2017 Here, we uncovered that UGT2B10 was transcriptionally regulated by farnesoid X receptor (FXR), the bile acid sensing nuclear receptor. Bile Acids and Salts 99-108 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 28267333-3 2017 GW4064 and chenodeoxycholic acid (two specific FXR agonists) treatment of HepG2 cells led to a significant increase in the mRNA level of UGT2B10. GW 4064 0-6 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 137-144 28267333-3 2017 GW4064 and chenodeoxycholic acid (two specific FXR agonists) treatment of HepG2 cells led to a significant increase in the mRNA level of UGT2B10. Chenodeoxycholic Acid 11-32 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 137-144 28267333-4 2017 The treated cells also showed enhanced glucuronidation activities toward amitriptyline (an UGT2B10 probe substrate). Amitriptyline 73-86 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 91-98 28803208-3 2017 However, the metabolic patterns of UGT1A4- and UGT2B10-mediated N-glucuronidation are not fully clear. Nitrogen 64-65 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 47-54 28803208-4 2017 In this study, we first optimized in vitro reaction conditions for N-glucuronidation by using specific substrates (i.e., trifluoperazine for UGT1A4, cotinine and amitriptyline for UGT2B10). Nitrogen 67-68 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 180-187 28803208-4 2017 In this study, we first optimized in vitro reaction conditions for N-glucuronidation by using specific substrates (i.e., trifluoperazine for UGT1A4, cotinine and amitriptyline for UGT2B10). Trifluoperazine 121-136 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 180-187 28803208-4 2017 In this study, we first optimized in vitro reaction conditions for N-glucuronidation by using specific substrates (i.e., trifluoperazine for UGT1A4, cotinine and amitriptyline for UGT2B10). Amitriptyline 162-175 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 180-187 27474751-8 2016 UGT2B4 activity against codeine and UGT2B10 activity against nicotine were significantly decreased in both HuH-7 and Hep3B cells (P < 0.001 and P = 0.0048, and P = 0.017 and P = 0.043, respectively) after overexpression of miR-216b-5p mimic. Nicotine 61-69 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 36-43 26669329-1 2016 Although there is evidence for an important role of UGT2B10 in the N-glucuronidation of drugs and other xenobiotics, the inhibitor selectivity of this enzyme is poorly understood. Nitrogen 67-68 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 52-59 26669329-2 2016 This study sought primarily to characterize the inhibition selectivity of UGT2B10 by UDP-glucuronosyltransferase (UGT) enzyme-selective inhibitors used for reaction phenotyping, and 34 antidepressant and antipsychotic drugs that contain an amine functional group. Amines 240-245 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 74-81 26669329-3 2016 Initial studies demonstrated that cotinine is a highly selective substrate of human liver microsomal UGT2B10. Cotinine 34-42 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 101-108 26669329-5 2016 Of the UGT enzyme-selective inhibitors employed for reaction phenotyping, only the UGT2B4/7 inhibitor fluconazole reduced recombinant UGT2B10 activity to an appreciable extent. Fluconazole 102-113 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 134-141 26669329-10 2016 values for amitriptyline, doxepin, and mianserin inhibition of human liver microsomal UGT2B10 were 0.61 +- 0.05, 0.95 +- 0.18, and 0.43 +- 0.01 microM. Amitriptyline 11-24 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 86-93 26669329-10 2016 values for amitriptyline, doxepin, and mianserin inhibition of human liver microsomal UGT2B10 were 0.61 +- 0.05, 0.95 +- 0.18, and 0.43 +- 0.01 microM. Doxepin 26-33 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 86-93 26669329-10 2016 values for amitriptyline, doxepin, and mianserin inhibition of human liver microsomal UGT2B10 were 0.61 +- 0.05, 0.95 +- 0.18, and 0.43 +- 0.01 microM. Mianserin 39-48 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 86-93 26833182-5 2016 This variant is in high linkage disequilibrium with a known functional variant in the UGT2B10 gene which is associated with reduced nicotine and cotinine glucuronidation activity, but intriguingly is not associated with nicotine intake. Nicotine 132-140 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 86-93 26833182-5 2016 This variant is in high linkage disequilibrium with a known functional variant in the UGT2B10 gene which is associated with reduced nicotine and cotinine glucuronidation activity, but intriguingly is not associated with nicotine intake. Cotinine 145-153 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 86-93 25595597-0 2015 A long-standing mystery solved: the formation of 3-hydroxydesloratadine is catalyzed by CYP2C8 but prior glucuronidation of desloratadine by UDP-glucuronosyltransferase 2B10 is an obligatory requirement. 3-hydroxydesloratadine 49-71 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 141-173 26135009-0 2015 Further Characterization of the Metabolism of Desloratadine and Its Cytochrome P450 and UDP-glucuronosyltransferase Inhibition Potential: Identification of Desloratadine as a Relatively Selective UGT2B10 Inhibitor. desloratadine 46-59 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 196-203 26135009-0 2015 Further Characterization of the Metabolism of Desloratadine and Its Cytochrome P450 and UDP-glucuronosyltransferase Inhibition Potential: Identification of Desloratadine as a Relatively Selective UGT2B10 Inhibitor. desloratadine 156-169 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 196-203 26135009-2 2015 Previously we reported that the formation of 3-hydroxydesloratadine, the major human metabolite of desloratadine, involves three sequential reactions, namely N-glucuronidation by UGT2B10 followed by 3-hydroxylation by CYP2C8 followed by deconjugation (rapid, nonenzymatic hydrolysis of the N-glucuronide). 3-hydroxydesloratadine 45-67 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 179-186 26135009-2 2015 Previously we reported that the formation of 3-hydroxydesloratadine, the major human metabolite of desloratadine, involves three sequential reactions, namely N-glucuronidation by UGT2B10 followed by 3-hydroxylation by CYP2C8 followed by deconjugation (rapid, nonenzymatic hydrolysis of the N-glucuronide). desloratadine 54-67 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 179-186 26135009-2 2015 Previously we reported that the formation of 3-hydroxydesloratadine, the major human metabolite of desloratadine, involves three sequential reactions, namely N-glucuronidation by UGT2B10 followed by 3-hydroxylation by CYP2C8 followed by deconjugation (rapid, nonenzymatic hydrolysis of the N-glucuronide). Nitrogen 158-159 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 179-186 26135009-6 2015 Assessment of UGT inhibition identified desloratadine as a potent and relatively selective competitive inhibitor of UGT2B10 (Ki value of 1.3 muM). desloratadine 40-53 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 116-123 26135009-7 2015 Chemical inhibition of UGT enzymes in HLM demonstrated that nicotine (UGT2B10 inhibitor) but not hecogenin (UGT1A4 inhibitor) completely inhibited the conversion of desloratadine (1 microM) to 3-hydroxydesloratadine in HLM fortified with both NADPH and UDP-glucuronic acid. Nicotine 60-68 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 70-77 26135009-7 2015 Chemical inhibition of UGT enzymes in HLM demonstrated that nicotine (UGT2B10 inhibitor) but not hecogenin (UGT1A4 inhibitor) completely inhibited the conversion of desloratadine (1 microM) to 3-hydroxydesloratadine in HLM fortified with both NADPH and UDP-glucuronic acid. desloratadine 165-178 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 70-77 26135009-7 2015 Chemical inhibition of UGT enzymes in HLM demonstrated that nicotine (UGT2B10 inhibitor) but not hecogenin (UGT1A4 inhibitor) completely inhibited the conversion of desloratadine (1 microM) to 3-hydroxydesloratadine in HLM fortified with both NADPH and UDP-glucuronic acid. 3-hydroxydesloratadine 193-215 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 70-77 26135009-8 2015 3-Hydroxydesloratadine formation correlated well with levomedetomidine glucuronidation (UGT2B10 marker activity) with a panel of individual CHH (r(2) = 0.72). Medetomidine 54-70 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 88-95 25595597-8 2015 Detailed mechanistic studies with sonicated or saponin-treated CHHs, human liver microsomes, and S9 fractions showed that both NADPH and UDP-glucuronic acid are required for 3-hydroxydesloratadine formation, and studies with recombinant UDP-glucuronosyltransferase (UGT) and P450 enzymes implicated the specific involvement of UGT2B10 in addition to CYP2C8. Saponins 47-54 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 327-334 25595597-8 2015 Detailed mechanistic studies with sonicated or saponin-treated CHHs, human liver microsomes, and S9 fractions showed that both NADPH and UDP-glucuronic acid are required for 3-hydroxydesloratadine formation, and studies with recombinant UDP-glucuronosyltransferase (UGT) and P450 enzymes implicated the specific involvement of UGT2B10 in addition to CYP2C8. NADP 127-132 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 327-334 25595597-9 2015 Overall, our results demonstrate for the first time that desloratadine glucuronidation by UGT2B10 followed by CYP2C8 oxidation and a deconjugation event are responsible for the formation of 3-hydroxydesloratadine. desloratadine 57-70 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 90-97 25595597-9 2015 Overall, our results demonstrate for the first time that desloratadine glucuronidation by UGT2B10 followed by CYP2C8 oxidation and a deconjugation event are responsible for the formation of 3-hydroxydesloratadine. 3-hydroxydesloratadine 190-212 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 90-97 25595597-0 2015 A long-standing mystery solved: the formation of 3-hydroxydesloratadine is catalyzed by CYP2C8 but prior glucuronidation of desloratadine by UDP-glucuronosyltransferase 2B10 is an obligatory requirement. desloratadine 58-71 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 141-173 25293881-11 2015 CONCLUSIONS: Genetic variation in UGT2B10 contributes significantly to nicotine and cotinine glucuronidation but not to nicotine dose. Nicotine 71-79 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 34-41 25503386-9 2015 Our results highlight the need to include UGT2B10 when screening the human UGTs for the enzymes involved in the glucuronidation of a new compound, particularly when there is a possibility of N-glucuronidation. Nitrogen 191-192 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 42-49 25293881-11 2015 CONCLUSIONS: Genetic variation in UGT2B10 contributes significantly to nicotine and cotinine glucuronidation but not to nicotine dose. Cotinine 84-92 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 34-41 25233931-2 2014 We report here on the proportion of nicotine metabolism by cytochrome P450 2A6-catalyzed C-oxidation, UDP-glucuronosyl transferase 2B10 (UGT2B10)-catalyzed N-glucuronidation and flavin monooxygenase 3-catalyzed N-oxidation in five ethnic/racial groups and the role of UGT2B10 genotype on the metabolic patterns observed. Nicotine 36-44 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 137-144 25233931-2 2014 We report here on the proportion of nicotine metabolism by cytochrome P450 2A6-catalyzed C-oxidation, UDP-glucuronosyl transferase 2B10 (UGT2B10)-catalyzed N-glucuronidation and flavin monooxygenase 3-catalyzed N-oxidation in five ethnic/racial groups and the role of UGT2B10 genotype on the metabolic patterns observed. Nicotine 36-44 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 102-135 25233931-2 2014 We report here on the proportion of nicotine metabolism by cytochrome P450 2A6-catalyzed C-oxidation, UDP-glucuronosyl transferase 2B10 (UGT2B10)-catalyzed N-glucuronidation and flavin monooxygenase 3-catalyzed N-oxidation in five ethnic/racial groups and the role of UGT2B10 genotype on the metabolic patterns observed. Nicotine 36-44 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 268-275 25233931-2 2014 We report here on the proportion of nicotine metabolism by cytochrome P450 2A6-catalyzed C-oxidation, UDP-glucuronosyl transferase 2B10 (UGT2B10)-catalyzed N-glucuronidation and flavin monooxygenase 3-catalyzed N-oxidation in five ethnic/racial groups and the role of UGT2B10 genotype on the metabolic patterns observed. Nitrogen 156-157 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 102-135 25233931-2 2014 We report here on the proportion of nicotine metabolism by cytochrome P450 2A6-catalyzed C-oxidation, UDP-glucuronosyl transferase 2B10 (UGT2B10)-catalyzed N-glucuronidation and flavin monooxygenase 3-catalyzed N-oxidation in five ethnic/racial groups and the role of UGT2B10 genotype on the metabolic patterns observed. Nitrogen 156-157 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 137-144 25233931-2 2014 We report here on the proportion of nicotine metabolism by cytochrome P450 2A6-catalyzed C-oxidation, UDP-glucuronosyl transferase 2B10 (UGT2B10)-catalyzed N-glucuronidation and flavin monooxygenase 3-catalyzed N-oxidation in five ethnic/racial groups and the role of UGT2B10 genotype on the metabolic patterns observed. Nitrogen 156-157 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 268-275 25233931-5 2014 The relationship of UGT2B10 genotype to nicotine metabolic pathways was determined for each group; geometric means were computed and adjusted for age, sex, creatinine, and body mass index. Nicotine 40-48 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 20-27 23936477-3 2013 The clearance of 3HC, which affects the NMR, occurs via renal excretion and metabolism by UGT2B17, and possibly UGT2B10, to 3HC-glucuronide. hydroxycotinine 17-20 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 112-119 24192532-0 2013 The contribution of common UGT2B10 and CYP2A6 alleles to variation in nicotine glucuronidation among European Americans. Nicotine 70-78 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 27-34 24192532-2 2013 UDP-glucuronosyltransferase-2B10 (UGT2B10) is the primary catalyst of nicotine glucuronidation. Nicotine 70-78 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 0-32 24192532-2 2013 UDP-glucuronosyltransferase-2B10 (UGT2B10) is the primary catalyst of nicotine glucuronidation. Nicotine 70-78 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 34-41 24192532-3 2013 MATERIALS AND METHODS: The conversion of deuterated (D2)-nicotine to D2-nicotine-glucuronide, D2-cotinine, D2-cotinine-glucuronide, and D2-trans-3"-hydroxycotinine were quantified in 188 European Americans, and the contribution of UGT2B10 genotype to variability in first-pass nicotine glucuronidation assessed, following a procedure previously applied to nicotine C-oxidation. deuterated (d2)-nicotine 41-65 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 231-238 24192532-3 2013 MATERIALS AND METHODS: The conversion of deuterated (D2)-nicotine to D2-nicotine-glucuronide, D2-cotinine, D2-cotinine-glucuronide, and D2-trans-3"-hydroxycotinine were quantified in 188 European Americans, and the contribution of UGT2B10 genotype to variability in first-pass nicotine glucuronidation assessed, following a procedure previously applied to nicotine C-oxidation. Nicotine 57-65 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 231-238 24192532-8 2013 CONCLUSION: CYP2A6 and UGT2B10 genotype explain 53% of the variance in oral nicotine glucuronidation in this sample. Nicotine 76-84 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 23-30 24192532-9 2013 CYP2A6 and UGT2B10 genetic variants are also significantly associated with undeuterated (D0) nicotine glucuronidation in individuals smoking ad libitum. Nicotine 93-101 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 11-18 23936477-3 2013 The clearance of 3HC, which affects the NMR, occurs via renal excretion and metabolism by UGT2B17, and possibly UGT2B10, to 3HC-glucuronide. 3hc-glucuronide 124-139 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 112-119 19786624-0 2010 Nicotine metabolism in African Americans and European Americans: variation in glucuronidation by ethnicity and UGT2B10 haplotype. Nicotine 0-8 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 111-118 23930678-6 2013 The formation of the various olanzapine metabolites is influenced by polymorphisms in the genes coding for CYP1A2, CYP1A expression regulator AHR, UGT1A4 and UGT2B10, as well as FMO3. Olanzapine 29-39 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 158-165 23611809-0 2013 Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Nitrogen 53-54 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 6-44 23611809-1 2013 Recent observations revealed that human UDP-glucuronosyltransferase (UGT) 2B10 catalyzes N-glucuronidation of amine-containing compounds. Nitrogen 89-90 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 40-78 23611809-1 2013 Recent observations revealed that human UDP-glucuronosyltransferase (UGT) 2B10 catalyzes N-glucuronidation of amine-containing compounds. Amines 110-115 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 40-78 23611809-4 2013 Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole, and midazolam. Nitrogen 58-59 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 18-25 23611809-4 2013 Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole, and midazolam. Amitriptyline 79-92 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 18-25 23611809-4 2013 Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole, and midazolam. Imipramine 94-104 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 18-25 23611809-4 2013 Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole, and midazolam. Ketotifen 106-115 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 18-25 23611809-4 2013 Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole, and midazolam. Pizotyline 117-126 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 18-25 23611809-4 2013 Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole, and midazolam. Olanzapine 128-138 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 18-25 23611809-4 2013 Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole, and midazolam. Diphenhydramine 140-155 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 18-25 23611809-4 2013 Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole, and midazolam. Tamoxifen 157-166 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 18-25 23611809-4 2013 Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole, and midazolam. Ketoconazole 168-180 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 18-25 23611809-4 2013 Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole, and midazolam. Midazolam 186-195 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 18-25 23611809-6 2013 UGT2B10 was inactive in the glucuronidation of desipramine, nortriptyline, carbamazepine, and afloqualone. Nortriptyline 60-73 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 0-7 23611809-6 2013 UGT2B10 was inactive in the glucuronidation of desipramine, nortriptyline, carbamazepine, and afloqualone. Carbamazepine 75-88 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 0-7 23611809-7 2013 This group of drugs contains secondary or primary amines, and these results suggest that UGT2B10 preferably conjugates tertiary amines. Amines 50-56 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 89-96 23611809-7 2013 This group of drugs contains secondary or primary amines, and these results suggest that UGT2B10 preferably conjugates tertiary amines. Amines 128-134 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 89-96 23611809-9 2013 Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher. Amitriptyline 73-86 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 61-68 23611809-9 2013 Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher. Imipramine 88-98 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 61-68 23611809-9 2013 Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher. Diphenhydramine 104-119 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 61-68 23611809-10 2013 These findings suggest that UGT2B10 plays a major role in the N-glucuronidation of these drugs at therapeutic concentrations. Nitrogen 62-63 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 28-35 23611809-12 2013 In conclusion, this study expands the understanding of the substrate specificity of UGT2B10, highlighting its preference for tertiary amines with higher affinities and clearance values than those of UGT1A4 and UGT1A3. Amines 134-140 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 84-91 22228205-0 2012 Glucuronidation of trans-3"-hydroxycotinine by UGT2B17 and UGT2B10. hydroxycotinine 19-43 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 59-66 22228205-7 2012 There was 91 (P<0.0001) and 39% (P<0.001) decreases in the 3HC-N-Gluc formation activities in HLM from participants with the UGT2B10 (*2/*2) and UGT2B10 (*1/*2) genotypes, respectively, compared with that of HLM from participants with the wild-type UGT2B10 (*1/*1) genotype. 3hc-n 65-70 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 131-138 22228205-7 2012 There was 91 (P<0.0001) and 39% (P<0.001) decreases in the 3HC-N-Gluc formation activities in HLM from participants with the UGT2B10 (*2/*2) and UGT2B10 (*1/*2) genotypes, respectively, compared with that of HLM from participants with the wild-type UGT2B10 (*1/*1) genotype. 3hc-n 65-70 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 151-158 22228205-7 2012 There was 91 (P<0.0001) and 39% (P<0.001) decreases in the 3HC-N-Gluc formation activities in HLM from participants with the UGT2B10 (*2/*2) and UGT2B10 (*1/*2) genotypes, respectively, compared with that of HLM from participants with the wild-type UGT2B10 (*1/*1) genotype. 3hc-n 65-70 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 151-158 20457141-3 2010 Surprisingly, UGT2B4 and UGT2B10 mRNA were found to be abundant in human liver suggesting an underestimated role of the liver in detoxification of their major substrates, bile acids and eicosanoids. Bile Acids and Salts 171-181 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 25-32 20457141-3 2010 Surprisingly, UGT2B4 and UGT2B10 mRNA were found to be abundant in human liver suggesting an underestimated role of the liver in detoxification of their major substrates, bile acids and eicosanoids. Eicosanoids 186-197 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 25-32 20133892-0 2010 Role of human UGT2B10 in N-glucuronidation of tricyclic antidepressants, amitriptyline, imipramine, clomipramine, and trimipramine. Nitrogen 25-26 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 14-21 20133892-0 2010 Role of human UGT2B10 in N-glucuronidation of tricyclic antidepressants, amitriptyline, imipramine, clomipramine, and trimipramine. Amitriptyline 73-86 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 14-21 20133892-0 2010 Role of human UGT2B10 in N-glucuronidation of tricyclic antidepressants, amitriptyline, imipramine, clomipramine, and trimipramine. Imipramine 88-98 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 14-21 20133892-0 2010 Role of human UGT2B10 in N-glucuronidation of tricyclic antidepressants, amitriptyline, imipramine, clomipramine, and trimipramine. Clomipramine 100-112 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 14-21 20133892-0 2010 Role of human UGT2B10 in N-glucuronidation of tricyclic antidepressants, amitriptyline, imipramine, clomipramine, and trimipramine. Trimipramine 118-130 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 14-21 20133892-1 2010 The role of human UDP glucuronosyltransferase (UGT) 2B10 in the N-glucuronidation of a number of tricyclic antidepressants was investigated and compared with that of UGT1A4 in both the Sf9 expressed system and human liver microsomes. Nitrogen 64-65 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 18-56 20133892-2 2010 The apparent K(m) (S(50)) values for the formation of quaternary N-glucuronides of amitriptyline, imipramine, clomipramine, and trimipramine were 2.60, 16.8, 14.4, and 11.2 microM in UGT2B10 and 448, 262, 112, and 258 microM in UGT1A4, respectively. n-glucuronides 65-79 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 183-190 20133892-2 2010 The apparent K(m) (S(50)) values for the formation of quaternary N-glucuronides of amitriptyline, imipramine, clomipramine, and trimipramine were 2.60, 16.8, 14.4, and 11.2 microM in UGT2B10 and 448, 262, 112, and 258 microM in UGT1A4, respectively. Amitriptyline 83-96 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 183-190 20133892-2 2010 The apparent K(m) (S(50)) values for the formation of quaternary N-glucuronides of amitriptyline, imipramine, clomipramine, and trimipramine were 2.60, 16.8, 14.4, and 11.2 microM in UGT2B10 and 448, 262, 112, and 258 microM in UGT1A4, respectively. Imipramine 98-108 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 183-190 20133892-2 2010 The apparent K(m) (S(50)) values for the formation of quaternary N-glucuronides of amitriptyline, imipramine, clomipramine, and trimipramine were 2.60, 16.8, 14.4, and 11.2 microM in UGT2B10 and 448, 262, 112, and 258 microM in UGT1A4, respectively. Clomipramine 110-122 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 183-190 20133892-2 2010 The apparent K(m) (S(50)) values for the formation of quaternary N-glucuronides of amitriptyline, imipramine, clomipramine, and trimipramine were 2.60, 16.8, 14.4, and 11.2 microM in UGT2B10 and 448, 262, 112, and 258 microM in UGT1A4, respectively. Trimipramine 128-140 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 183-190 20133892-3 2010 The kinetics of amitriptyline and imipramine glucuronidation in human liver microsomes exhibited a biphasic character, where the high- and low-affinity components were in good agreement with our results in expressed UGT2B10 and UGT1A4, respectively. Amitriptyline 16-29 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 216-223 20133892-3 2010 The kinetics of amitriptyline and imipramine glucuronidation in human liver microsomes exhibited a biphasic character, where the high- and low-affinity components were in good agreement with our results in expressed UGT2B10 and UGT1A4, respectively. Imipramine 34-44 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 216-223 20133892-5 2010 The in vitro clearances (CL(int) or CL(max)) were comparable between UGT2B10 and UGT1A4 for glucuronidation of imipramine, clomipramine, and trimipramine, whereas CL(int) of amitriptyline glucuronidation by UGT2B10 was more than 10-fold higher than that by UGT1A4. Imipramine 111-121 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 69-76 20133892-6 2010 Nicotine was found to selectively inhibit UGT2B10 but not UGT1A4 activity. Nicotine 0-8 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 42-49 23110092-8 2012 Treatment of WM3211 or metastatic melanoma cell lines with anti-cancer agents (including vemurafenib) induced expression of UGT2B7, UGT2B10 and UGT2B15 demonstrating that melanoma cells retain the ability to re-express these same three UGTs. Vemurafenib 89-100 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 132-139 21750471-9 2011 There was a 1.9-fold (P<0.003) decrease in the formation of both isomers of the olanzapine-10-N-glucuronide, a 2.7-fold (P<0.0001) decrease in olanzapine-4"-N-glucuronide formation, and a 2.1-fold (P=0.0002) decrease in the overall olanzapine glucuronide formation in HLM with at least one UGT2B10*2 allele. Olanzapine 10-N-glucuronide 83-110 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 296-303 21750471-9 2011 There was a 1.9-fold (P<0.003) decrease in the formation of both isomers of the olanzapine-10-N-glucuronide, a 2.7-fold (P<0.0001) decrease in olanzapine-4"-N-glucuronide formation, and a 2.1-fold (P=0.0002) decrease in the overall olanzapine glucuronide formation in HLM with at least one UGT2B10*2 allele. Olanzapine 83-93 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 296-303 21750471-9 2011 There was a 1.9-fold (P<0.003) decrease in the formation of both isomers of the olanzapine-10-N-glucuronide, a 2.7-fold (P<0.0001) decrease in olanzapine-4"-N-glucuronide formation, and a 2.1-fold (P=0.0002) decrease in the overall olanzapine glucuronide formation in HLM with at least one UGT2B10*2 allele. Glucuronides 99-110 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 296-303 21750471-10 2011 In regression analysis, the UGT1A4*3 (P<0.02) and UGT2B10*2 (P<0.002) alleles were significant predictors of the formation of all olanzapine glucuronide isomers. Olanzapine 10-N-glucuronide 136-158 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 53-60 21750471-12 2011 These data suggest that the UGT1A4*3 and UGT2B10*2 alleles contribute significantly to interindividual variability in olanzapine metabolism. Olanzapine 118-128 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 41-48 21434773-9 2011 The N-glucuronidation rates in humans are typically much higher than in animals, largely due to the activity of two enzymes, the extensively studied UGT1A4, and the more recently identified as a main player in N-glucuronidation, UGT2B10. Nitrogen 4-5 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 229-236 21434773-9 2011 The N-glucuronidation rates in humans are typically much higher than in animals, largely due to the activity of two enzymes, the extensively studied UGT1A4, and the more recently identified as a main player in N-glucuronidation, UGT2B10. Nitrogen 210-211 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 229-236 21434773-10 2011 We discuss both enzymes and review the findings that revealed the role of UGT2B10 in N-glucuronidation. Nitrogen 85-86 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 74-81 21497036-0 2011 Liquid chromatography-tandem mass spectrometry method for measurement of nicotine N-glucuronide: a marker for human UGT2B10 inhibition. nicotine N-glucuronide 73-95 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 116-123 21497036-1 2011 Nicotine is considered to be a specific substrate for UGT2B10, an isoform of human uridine diphosphate glucuronosyltransferase (UGT). Nicotine 0-8 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 54-61 21497036-9 2011 This established method was employed to evaluate the inhibitory effects of five target compounds including amitriptyline, hecogenin, imipramine, lamotrigine, and trifluoperazine on enzymatic activity of UGT2B10. Amitriptyline 107-120 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 203-210 21497036-9 2011 This established method was employed to evaluate the inhibitory effects of five target compounds including amitriptyline, hecogenin, imipramine, lamotrigine, and trifluoperazine on enzymatic activity of UGT2B10. hecogenin 122-131 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 203-210 21497036-9 2011 This established method was employed to evaluate the inhibitory effects of five target compounds including amitriptyline, hecogenin, imipramine, lamotrigine, and trifluoperazine on enzymatic activity of UGT2B10. Imipramine 133-143 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 203-210 21497036-9 2011 This established method was employed to evaluate the inhibitory effects of five target compounds including amitriptyline, hecogenin, imipramine, lamotrigine, and trifluoperazine on enzymatic activity of UGT2B10. Lamotrigine 145-156 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 203-210 21497036-9 2011 This established method was employed to evaluate the inhibitory effects of five target compounds including amitriptyline, hecogenin, imipramine, lamotrigine, and trifluoperazine on enzymatic activity of UGT2B10. Trifluoperazine 162-177 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 203-210 21497036-11 2011 Trifluoperazine was found to be a non-substrate inhibitor for human UGT2B10. Trifluoperazine 0-15 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 68-75 20876810-3 2010 In the present study, the relationship between the levels of urinary nicotine metabolites and functional polymorphisms in UGTs 2B10 and 2B17 was analyzed in urine specimens from 104 Caucasian smokers. Nicotine 69-77 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 122-140 20876810-6 2010 These data suggest that UGTs 2B10 and 2B17 play important roles in the glucuronidation of nicotine, cotinine, and 3HC and suggest that the UGT2B10 codon 67 SNP and the UGT2B17 gene deletion significantly reduce overall glucuronidation rates of nicotine and its major metabolites in smokers. Nicotine 90-98 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-42 20876810-6 2010 These data suggest that UGTs 2B10 and 2B17 play important roles in the glucuronidation of nicotine, cotinine, and 3HC and suggest that the UGT2B10 codon 67 SNP and the UGT2B17 gene deletion significantly reduce overall glucuronidation rates of nicotine and its major metabolites in smokers. Nicotine 90-98 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 139-146 20876810-6 2010 These data suggest that UGTs 2B10 and 2B17 play important roles in the glucuronidation of nicotine, cotinine, and 3HC and suggest that the UGT2B10 codon 67 SNP and the UGT2B17 gene deletion significantly reduce overall glucuronidation rates of nicotine and its major metabolites in smokers. Cotinine 100-108 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-42 20876810-6 2010 These data suggest that UGTs 2B10 and 2B17 play important roles in the glucuronidation of nicotine, cotinine, and 3HC and suggest that the UGT2B10 codon 67 SNP and the UGT2B17 gene deletion significantly reduce overall glucuronidation rates of nicotine and its major metabolites in smokers. Nicotine 244-252 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-42 20876810-6 2010 These data suggest that UGTs 2B10 and 2B17 play important roles in the glucuronidation of nicotine, cotinine, and 3HC and suggest that the UGT2B10 codon 67 SNP and the UGT2B17 gene deletion significantly reduce overall glucuronidation rates of nicotine and its major metabolites in smokers. Nicotine 244-252 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 139-146 19786624-5 2010 In a second study of smokers (n = 84), the relationship of a UGT2B10 haplotype linked with D67Y to nicotine and cotinine glucuronidation levels was determined. Nicotine 99-107 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 61-68 19786624-8 2010 In smokers with a UGT2B10 Tyr67 allele, glucuronide conjugation of nicotine and cotinine was decreased by 20% compared with smokers without this allele. Glucuronides 40-51 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 18-25 19786624-8 2010 In smokers with a UGT2B10 Tyr67 allele, glucuronide conjugation of nicotine and cotinine was decreased by 20% compared with smokers without this allele. Nicotine 67-75 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 18-25 19786624-8 2010 In smokers with a UGT2B10 Tyr67 allele, glucuronide conjugation of nicotine and cotinine was decreased by 20% compared with smokers without this allele. Cotinine 80-88 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 18-25 18502788-4 2008 However, H37 is not totally conserved, being replaced by either Pro or Leu in UGT1A4 and UGT2B10. Leucine 71-74 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 89-96 19487247-1 2009 An N-terminal domain histidine [corresponding to position 39 of UDP-glucuronosyltransferase (UGT) 1A1] is conserved in all UGT1A and UGT2B subfamily proteins except UGT1A4 (Pro-40) and UGT2B10 (Leu-34). Histidine 21-30 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 185-192 19487247-2 2009 Unlike most UGT1A and UGT2B xenobiotic-metabolizing enzymes, UGT1A4 and UGT2B10 lack the ability to glucuronidate 4-methylumbelliferone (4MU) and 1-naphthol (1NP), both planar phenols, and naproxen (a carboxylic acid). Hymecromone 114-135 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 72-79 19487247-2 2009 Unlike most UGT1A and UGT2B xenobiotic-metabolizing enzymes, UGT1A4 and UGT2B10 lack the ability to glucuronidate 4-methylumbelliferone (4MU) and 1-naphthol (1NP), both planar phenols, and naproxen (a carboxylic acid). Hymecromone 137-140 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 72-79 19487247-2 2009 Unlike most UGT1A and UGT2B xenobiotic-metabolizing enzymes, UGT1A4 and UGT2B10 lack the ability to glucuronidate 4-methylumbelliferone (4MU) and 1-naphthol (1NP), both planar phenols, and naproxen (a carboxylic acid). 1-naphthol 146-156 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 72-79 19487247-2 2009 Unlike most UGT1A and UGT2B xenobiotic-metabolizing enzymes, UGT1A4 and UGT2B10 lack the ability to glucuronidate 4-methylumbelliferone (4MU) and 1-naphthol (1NP), both planar phenols, and naproxen (a carboxylic acid). 1-naphthol 158-161 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 72-79 19487247-2 2009 Unlike most UGT1A and UGT2B xenobiotic-metabolizing enzymes, UGT1A4 and UGT2B10 lack the ability to glucuronidate 4-methylumbelliferone (4MU) and 1-naphthol (1NP), both planar phenols, and naproxen (a carboxylic acid). Phenols 176-183 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 72-79 19487247-2 2009 Unlike most UGT1A and UGT2B xenobiotic-metabolizing enzymes, UGT1A4 and UGT2B10 lack the ability to glucuronidate 4-methylumbelliferone (4MU) and 1-naphthol (1NP), both planar phenols, and naproxen (a carboxylic acid). Naproxen 189-197 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 72-79 19487247-2 2009 Unlike most UGT1A and UGT2B xenobiotic-metabolizing enzymes, UGT1A4 and UGT2B10 lack the ability to glucuronidate 4-methylumbelliferone (4MU) and 1-naphthol (1NP), both planar phenols, and naproxen (a carboxylic acid). Carboxylic Acids 201-216 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 72-79 19487247-5 2009 The conserved N-terminal domain histidine of UGT1A1, UGT1A6, UGT1A9, and UGT2B7 was mutated to proline and leucine 34 of UGT2B10 was substituted with histidine, and the capacity of the wild-type and mutant proteins to glucuronidate 4MU, 1NP, LTG, TFP, and naproxen was characterized. Histidine 32-41 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 121-128 19487247-5 2009 The conserved N-terminal domain histidine of UGT1A1, UGT1A6, UGT1A9, and UGT2B7 was mutated to proline and leucine 34 of UGT2B10 was substituted with histidine, and the capacity of the wild-type and mutant proteins to glucuronidate 4MU, 1NP, LTG, TFP, and naproxen was characterized. Proline 95-102 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 121-128 19487247-5 2009 The conserved N-terminal domain histidine of UGT1A1, UGT1A6, UGT1A9, and UGT2B7 was mutated to proline and leucine 34 of UGT2B10 was substituted with histidine, and the capacity of the wild-type and mutant proteins to glucuronidate 4MU, 1NP, LTG, TFP, and naproxen was characterized. Leucine 107-114 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 121-128 19487247-5 2009 The conserved N-terminal domain histidine of UGT1A1, UGT1A6, UGT1A9, and UGT2B7 was mutated to proline and leucine 34 of UGT2B10 was substituted with histidine, and the capacity of the wild-type and mutant proteins to glucuronidate 4MU, 1NP, LTG, TFP, and naproxen was characterized. Histidine 150-159 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 121-128 19487247-5 2009 The conserved N-terminal domain histidine of UGT1A1, UGT1A6, UGT1A9, and UGT2B7 was mutated to proline and leucine 34 of UGT2B10 was substituted with histidine, and the capacity of the wild-type and mutant proteins to glucuronidate 4MU, 1NP, LTG, TFP, and naproxen was characterized. glucuronidate 218-231 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 121-128 19487247-5 2009 The conserved N-terminal domain histidine of UGT1A1, UGT1A6, UGT1A9, and UGT2B7 was mutated to proline and leucine 34 of UGT2B10 was substituted with histidine, and the capacity of the wild-type and mutant proteins to glucuronidate 4MU, 1NP, LTG, TFP, and naproxen was characterized. Naproxen 256-264 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 121-128 18474681-0 2008 Regio- and stereospecific N-glucuronidation of medetomidine: the differences between UDP glucuronosyltransferase (UGT) 1A4 and UGT2B10 account for the complex kinetics of human liver microsomes. Nitrogen 26-27 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 127-134 18474681-0 2008 Regio- and stereospecific N-glucuronidation of medetomidine: the differences between UDP glucuronosyltransferase (UGT) 1A4 and UGT2B10 account for the complex kinetics of human liver microsomes. Medetomidine 47-59 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 127-134 17909004-0 2007 Glucuronidation of nicotine and cotinine by UGT2B10: loss of function by the UGT2B10 Codon 67 (Asp>Tyr) polymorphism. Nicotine 19-27 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 44-51 18238858-0 2008 Glucuronidation of tobacco-specific nitrosamines by UGT2B10. Nitrosamines 36-48 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 52-59 18238858-8 2008 These data suggest that UGT2B10 is likely the most active UGT isoform in human liver for the N-glucuronidation of TSNAs. Nitrogen 93-94 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 18300939-0 2008 Identification of a prevalent functional missense polymorphism in the UGT2B10 gene and its association with UGT2B10 inactivation against tobacco-specific nitrosamines. Nitrosamines 154-166 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 70-77 18300939-0 2008 Identification of a prevalent functional missense polymorphism in the UGT2B10 gene and its association with UGT2B10 inactivation against tobacco-specific nitrosamines. Nitrosamines 154-166 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 108-115 18300939-1 2008 OBJECTIVE: To study the potential association between UDP-glucuronosyltransferase (UGT)2B10 genotypes and [4-(methylnitrosamino)-1-(3-pyridyl)-1-butanol] NNAL-N-glucuronidation activity in human liver microsomes (HLM) and to identify potential functional polymorphisms. [4-(methylnitrosamino)-1-(3-pyridyl)-1-butanol] nnal-n-glucuronidation 106-176 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 83-91 18300939-2 2008 METHODS: A total of 77 subjects were genotyped for three UGT2B10 tagging single nucleotide polymorphisms NNAL-N-glucuronidation activity in HLM was determined by high-pressure liquid chromatography and analyzed by UGT2B10 haplotypes. nnal-n 105-111 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 57-64 18300939-6 2008 A novel polymorphism resulting in an aspartic acid to tyrosine amino acid change at codon 67 of the UGT2B10 complementary DNA was identified exclusively in subjects with a haplotype C. Unlike the high activity observed in microsomes from HEK293 cells over expressing the wild-type UGT2B10(67Asp) variant, microsomes from HEK293 cells over expressing the UGT2B10(67Tyr) variant exhibited minimal glucuronide formation activity against NNAL or other tobacco-specific nitrosamines tested in vitro. Glucuronides 395-406 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 100-107 18300939-6 2008 A novel polymorphism resulting in an aspartic acid to tyrosine amino acid change at codon 67 of the UGT2B10 complementary DNA was identified exclusively in subjects with a haplotype C. Unlike the high activity observed in microsomes from HEK293 cells over expressing the wild-type UGT2B10(67Asp) variant, microsomes from HEK293 cells over expressing the UGT2B10(67Tyr) variant exhibited minimal glucuronide formation activity against NNAL or other tobacco-specific nitrosamines tested in vitro. Nitrosamines 465-477 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 100-107 17909004-0 2007 Glucuronidation of nicotine and cotinine by UGT2B10: loss of function by the UGT2B10 Codon 67 (Asp>Tyr) polymorphism. Nicotine 19-27 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 77-84 17909004-0 2007 Glucuronidation of nicotine and cotinine by UGT2B10: loss of function by the UGT2B10 Codon 67 (Asp>Tyr) polymorphism. Cotinine 32-40 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 44-51 17909004-0 2007 Glucuronidation of nicotine and cotinine by UGT2B10: loss of function by the UGT2B10 Codon 67 (Asp>Tyr) polymorphism. Aspartic Acid 95-98 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 77-84 17909004-0 2007 Glucuronidation of nicotine and cotinine by UGT2B10: loss of function by the UGT2B10 Codon 67 (Asp>Tyr) polymorphism. Tyrosine 102-105 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 44-51 17909004-0 2007 Glucuronidation of nicotine and cotinine by UGT2B10: loss of function by the UGT2B10 Codon 67 (Asp>Tyr) polymorphism. Tyrosine 102-105 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 77-84 17909004-2 2007 Recent studies have shown that UGT2B10 is a major enzyme involved in the N-glucuronidation of several tobacco-specific nitrosamines. Nitrogen 73-74 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 31-38 17909004-2 2007 Recent studies have shown that UGT2B10 is a major enzyme involved in the N-glucuronidation of several tobacco-specific nitrosamines. Nitrosamines 119-131 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 31-38 17909004-3 2007 In the present study, microsomes of UGT2B10-overexpressing HEK293 cells exhibited high N-glucuronidation activity against both nicotine and cotinine with apparent KM"s that were 37- and 3-fold lower than that observed for microsomes of UGT1A4-overexpressing cells against nicotine and cotinine, respectively. Nitrogen 87-88 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 36-43 17909004-3 2007 In the present study, microsomes of UGT2B10-overexpressing HEK293 cells exhibited high N-glucuronidation activity against both nicotine and cotinine with apparent KM"s that were 37- and 3-fold lower than that observed for microsomes of UGT1A4-overexpressing cells against nicotine and cotinine, respectively. Nicotine 127-135 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 36-43 17909004-3 2007 In the present study, microsomes of UGT2B10-overexpressing HEK293 cells exhibited high N-glucuronidation activity against both nicotine and cotinine with apparent KM"s that were 37- and 3-fold lower than that observed for microsomes of UGT1A4-overexpressing cells against nicotine and cotinine, respectively. Cotinine 140-148 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 36-43 17909004-3 2007 In the present study, microsomes of UGT2B10-overexpressing HEK293 cells exhibited high N-glucuronidation activity against both nicotine and cotinine with apparent KM"s that were 37- and 3-fold lower than that observed for microsomes of UGT1A4-overexpressing cells against nicotine and cotinine, respectively. Nicotine 272-280 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 36-43 17909004-3 2007 In the present study, microsomes of UGT2B10-overexpressing HEK293 cells exhibited high N-glucuronidation activity against both nicotine and cotinine with apparent KM"s that were 37- and 3-fold lower than that observed for microsomes of UGT1A4-overexpressing cells against nicotine and cotinine, respectively. Cotinine 285-293 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 36-43 17909004-4 2007 The KM of microsomes from wild-type (WT) UGT2B10-overexpressing cells for nicotine and cotinine was similar to that observed for human liver microsomes (HLM) against both substrates. Nicotine 74-82 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 41-48 17909004-4 2007 The KM of microsomes from wild-type (WT) UGT2B10-overexpressing cells for nicotine and cotinine was similar to that observed for human liver microsomes (HLM) against both substrates. Cotinine 87-95 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 41-48 17909004-7 2007 These data suggest that UGT2B10 is the major hepatic enzyme involved in nicotine/cotinine glucuronidation and that the UGT2B10*2 variant significantly reduces nicotine- and cotinine-N-glucuronidation formation and plays an important role in nicotine metabolism and elimination. Nicotine 72-80 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 17909004-7 2007 These data suggest that UGT2B10 is the major hepatic enzyme involved in nicotine/cotinine glucuronidation and that the UGT2B10*2 variant significantly reduces nicotine- and cotinine-N-glucuronidation formation and plays an important role in nicotine metabolism and elimination. Nicotine 72-80 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 119-126 17909004-7 2007 These data suggest that UGT2B10 is the major hepatic enzyme involved in nicotine/cotinine glucuronidation and that the UGT2B10*2 variant significantly reduces nicotine- and cotinine-N-glucuronidation formation and plays an important role in nicotine metabolism and elimination. Cotinine 81-89 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 17909004-7 2007 These data suggest that UGT2B10 is the major hepatic enzyme involved in nicotine/cotinine glucuronidation and that the UGT2B10*2 variant significantly reduces nicotine- and cotinine-N-glucuronidation formation and plays an important role in nicotine metabolism and elimination. Cotinine 81-89 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 119-126 17909004-7 2007 These data suggest that UGT2B10 is the major hepatic enzyme involved in nicotine/cotinine glucuronidation and that the UGT2B10*2 variant significantly reduces nicotine- and cotinine-N-glucuronidation formation and plays an important role in nicotine metabolism and elimination. Nicotine 159-167 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 17909004-7 2007 These data suggest that UGT2B10 is the major hepatic enzyme involved in nicotine/cotinine glucuronidation and that the UGT2B10*2 variant significantly reduces nicotine- and cotinine-N-glucuronidation formation and plays an important role in nicotine metabolism and elimination. Nicotine 159-167 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 119-126 17909004-7 2007 These data suggest that UGT2B10 is the major hepatic enzyme involved in nicotine/cotinine glucuronidation and that the UGT2B10*2 variant significantly reduces nicotine- and cotinine-N-glucuronidation formation and plays an important role in nicotine metabolism and elimination. Cotinine 173-181 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 17909004-7 2007 These data suggest that UGT2B10 is the major hepatic enzyme involved in nicotine/cotinine glucuronidation and that the UGT2B10*2 variant significantly reduces nicotine- and cotinine-N-glucuronidation formation and plays an important role in nicotine metabolism and elimination. Cotinine 173-181 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 119-126 17909004-7 2007 These data suggest that UGT2B10 is the major hepatic enzyme involved in nicotine/cotinine glucuronidation and that the UGT2B10*2 variant significantly reduces nicotine- and cotinine-N-glucuronidation formation and plays an important role in nicotine metabolism and elimination. Nitrogen 182-183 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 17576790-2 2007 Using an improved analytical method, we have discovered that the human UDP-glucuronosyltransferase (UGT) 2B10, a liver enzyme previously unknown to conjugate nicotine or exhibit considerable activity toward any compound, plays a major role in nicotine inactivation by direct conjugation with glucuronic acid at the aromatic nitrogen atom. Nicotine 158-166 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 71-109 17576790-2 2007 Using an improved analytical method, we have discovered that the human UDP-glucuronosyltransferase (UGT) 2B10, a liver enzyme previously unknown to conjugate nicotine or exhibit considerable activity toward any compound, plays a major role in nicotine inactivation by direct conjugation with glucuronic acid at the aromatic nitrogen atom. Nicotine 243-251 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 71-109 17576790-2 2007 Using an improved analytical method, we have discovered that the human UDP-glucuronosyltransferase (UGT) 2B10, a liver enzyme previously unknown to conjugate nicotine or exhibit considerable activity toward any compound, plays a major role in nicotine inactivation by direct conjugation with glucuronic acid at the aromatic nitrogen atom. Glucuronic Acid 292-307 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 71-109 17576790-2 2007 Using an improved analytical method, we have discovered that the human UDP-glucuronosyltransferase (UGT) 2B10, a liver enzyme previously unknown to conjugate nicotine or exhibit considerable activity toward any compound, plays a major role in nicotine inactivation by direct conjugation with glucuronic acid at the aromatic nitrogen atom. Nitrogen 324-332 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 71-109 17576790-3 2007 The K(m) value of recombinant UGT2B10 for nicotine (0.29 mM) was similar to that determined for human liver microsomes (0.33 mM), whereas the K(m) value of UGT1A4 for nicotine was almost 10-fold greater (2.4 mM). Nicotine 42-50 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 30-37 17576790-4 2007 UGT2B10 was also more active than UGT1A4 in N-glucuronidation of cotinine (oxidative nicotine metabolite), whereas UGT2B7 exhibited only low nicotine glucuronidation activity and was essentially inactive toward cotinine. Nitrogen 44-45 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 0-7 17576790-4 2007 UGT2B10 was also more active than UGT1A4 in N-glucuronidation of cotinine (oxidative nicotine metabolite), whereas UGT2B7 exhibited only low nicotine glucuronidation activity and was essentially inactive toward cotinine. Cotinine 65-73 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 0-7 17576790-4 2007 UGT2B10 was also more active than UGT1A4 in N-glucuronidation of cotinine (oxidative nicotine metabolite), whereas UGT2B7 exhibited only low nicotine glucuronidation activity and was essentially inactive toward cotinine. Nicotine 85-93 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 0-7 17576790-4 2007 UGT2B10 was also more active than UGT1A4 in N-glucuronidation of cotinine (oxidative nicotine metabolite), whereas UGT2B7 exhibited only low nicotine glucuronidation activity and was essentially inactive toward cotinine. Cotinine 211-219 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 0-7 17576790-7 2007 These findings for UGT2B10 (but not for UGT1A4 and UGT2B7) were mirrored by human tissue activities because nicotine and cotinine glucuronidation rates in intestine microsomes were less than 0.1% that of human liver microsomes. Nicotine 108-116 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 19-26 17576790-7 2007 These findings for UGT2B10 (but not for UGT1A4 and UGT2B7) were mirrored by human tissue activities because nicotine and cotinine glucuronidation rates in intestine microsomes were less than 0.1% that of human liver microsomes. Cotinine 121-129 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 19-26 8674824-4 1995 Among these UGTs, UGT2B7 is specific for estriol and 3,4-catechol estrogens, UGT2B15 glucuronidates 17beta-hydroxy-C19 steroids while UGT2B10 has as yet an undescribed activity. Estriol 41-48 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 134-141 12639971-6 2003 Interestingly, UGT2B10 and UGT2B11, which are considered as orphan enzymes since no conjugation activity has so far been demonstrated with these enzymes, conjugated 12-HETE, 15-HETE, and 13-HODE. 12-Hete 165-172 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 15-22 12639971-6 2003 Interestingly, UGT2B10 and UGT2B11, which are considered as orphan enzymes since no conjugation activity has so far been demonstrated with these enzymes, conjugated 12-HETE, 15-HETE, and 13-HODE. 5-hydroxy-6,8,11,14-eicosatetraenoic acid 168-172 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 15-22 12639971-6 2003 Interestingly, UGT2B10 and UGT2B11, which are considered as orphan enzymes since no conjugation activity has so far been demonstrated with these enzymes, conjugated 12-HETE, 15-HETE, and 13-HODE. 13-hydroxy-9,11-octadecadienoic acid 190-194 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 15-22 17909004-7 2007 These data suggest that UGT2B10 is the major hepatic enzyme involved in nicotine/cotinine glucuronidation and that the UGT2B10*2 variant significantly reduces nicotine- and cotinine-N-glucuronidation formation and plays an important role in nicotine metabolism and elimination. Nitrogen 182-183 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 119-126 17909004-7 2007 These data suggest that UGT2B10 is the major hepatic enzyme involved in nicotine/cotinine glucuronidation and that the UGT2B10*2 variant significantly reduces nicotine- and cotinine-N-glucuronidation formation and plays an important role in nicotine metabolism and elimination. Nicotine 159-167 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 24-31 17909004-7 2007 These data suggest that UGT2B10 is the major hepatic enzyme involved in nicotine/cotinine glucuronidation and that the UGT2B10*2 variant significantly reduces nicotine- and cotinine-N-glucuronidation formation and plays an important role in nicotine metabolism and elimination. Nicotine 159-167 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 119-126 8269638-1 1993 The capacity of four cDNA-expressed human liver UDP-glucuronosyltransferases (UGT), UGT1*6, UGT2B7, UGT2B10 and UGT2B11, to glucuronidate hydroxylated metabolites of benzo[a]pyrene (B[a]P) and 2-acetylaminofluorene (AAF) has been investigated. glucuronidate 124-137 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 100-107 8269638-1 1993 The capacity of four cDNA-expressed human liver UDP-glucuronosyltransferases (UGT), UGT1*6, UGT2B7, UGT2B10 and UGT2B11, to glucuronidate hydroxylated metabolites of benzo[a]pyrene (B[a]P) and 2-acetylaminofluorene (AAF) has been investigated. Benzo(a)pyrene 166-180 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 100-107 8269638-1 1993 The capacity of four cDNA-expressed human liver UDP-glucuronosyltransferases (UGT), UGT1*6, UGT2B7, UGT2B10 and UGT2B11, to glucuronidate hydroxylated metabolites of benzo[a]pyrene (B[a]P) and 2-acetylaminofluorene (AAF) has been investigated. 2-Acetylaminofluorene 193-214 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 100-107 8269638-1 1993 The capacity of four cDNA-expressed human liver UDP-glucuronosyltransferases (UGT), UGT1*6, UGT2B7, UGT2B10 and UGT2B11, to glucuronidate hydroxylated metabolites of benzo[a]pyrene (B[a]P) and 2-acetylaminofluorene (AAF) has been investigated. 2-Acetylaminofluorene 216-219 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 100-107