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Article: Genetic variants, haplotype determination, and function of novel alleles of

Zhang, Li-Qun / Li, Xin-Yue / Chen, Lian-Guo / Chen, Zhe / Xu, Ren-Ai / Qian, Jian-Chang / Zhou, Xiao-Yang / Dai, Da-Peng / Hu, Guo-Xin / Cai, Jian-Ping

Heliyon

2024 Volume 10, Issue 7, Page(s) e28952

Abstract: Amino acid variants in protein may result in deleterious effects on enzymatic activity. In this study we investigate the DNA variants on activity ... ...

Abstract	Amino acid variants in protein may result in deleterious effects on enzymatic activity. In this study we investigate the DNA variants on activity of
Language	English
Publishing date	2024-03-30
Publishing country	England
Document type	Journal Article
ZDB-ID	2835763-2
ISSN	2405-8440
ISSN	2405-8440
DOI	10.1016/j.heliyon.2024.e28952
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Article ; Online: The effect of Resveratrol on the pharmacokinetic profile of tofacitinib and the underlying mechanism.

Ye, Zhize / Hu, Jinyu / Wang, Jing / Liu, Ya-Nan / Hu, Guo-Xin / Xu, Ren-Ai

Chemico-biological interactions

2023 Volume 374, Page(s) 110398

Abstract: The purpose of this study was to (i) investigate the effect of CYP3A4 variants on tofacitinib metabolism, and (ii) investigate the interaction of tofacitinib with resveratrol and its underlying mechanisms. The concentration of M9, the main metabolite of ... ...

Abstract	The purpose of this study was to (i) investigate the effect of CYP3A4 variants on tofacitinib metabolism, and (ii) investigate the interaction of tofacitinib with resveratrol and its underlying mechanisms. The concentration of M9, the main metabolite of tofacitinib, was determined by ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS). The results showed that the clearance rate of CYP3A4.18 variant was significantly decreased compared with CYP3A4.1, and the CYP3A4.28 variant was changed, but not statistically significant. In addition, the potential interaction of resveratrol with tofacitinib was determined based on rat liver microsomes (RLM), human liver microsomes (HLM), and CYP3A4 response systems. Resveratrol has an IC
MeSH term(s)	Rats ; Humans ; Animals ; Resveratrol/pharmacology ; Chromatography, Liquid ; Rats, Sprague-Dawley ; Cytochrome P-450 CYP3A/metabolism ; Tandem Mass Spectrometry/methods ; Microsomes, Liver/metabolism ; Chromatography, High Pressure Liquid/methods
Chemical Substances	Resveratrol (Q369O8926L) ; tofacitinib (87LA6FU830) ; Cytochrome P-450 CYP3A (EC 1.14.14.1)
Language	English
Publishing date	2023-02-09
Publishing country	Ireland
Document type	Journal Article
ZDB-ID	218799-1
ISSN	1872-7786 ; 0009-2797
ISSN (online)	1872-7786
ISSN	0009-2797
DOI	10.1016/j.cbi.2023.110398
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Zs.A 686: Show issues

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Article ; Online: Han Chinese specific cytochrome P450 polymorphisms and their impact on the metabolism of anti-hypertensive drugs with adrenoreceptor blocking properties.

Qian, Jian-Chang / Cai, Jian-Ping / Hu, Guo-Xin

Expert opinion on drug metabolism & toxicology

2021 Volume 17, Issue 6, Page(s) 707–716

Abstract: ... ...

Abstract	Introduction
MeSH term(s)	Adrenergic Antagonists/pharmacokinetics ; Adrenergic Antagonists/pharmacology ; Antihypertensive Agents/pharmacokinetics ; Antihypertensive Agents/pharmacology ; Asian Continental Ancestry Group/genetics ; Cytochrome P-450 Enzyme System/genetics ; Genotype ; Humans ; Polymorphism, Genetic
Chemical Substances	Adrenergic Antagonists ; Antihypertensive Agents ; Cytochrome P-450 Enzyme System (9035-51-2)
Language	English
Publishing date	2021-05-03
Publishing country	England
Document type	Journal Article ; Review
ZDB-ID	2214462-6
ISSN	1744-7607 ; 1742-5255
ISSN (online)	1744-7607
ISSN	1742-5255
DOI	10.1080/17425255.2021.1921147
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Article: Molecular Cloning, Characterization, and Expression of a Receptor for Activated Protein Kinase C1 (RACK1) Gene in

Cai, Yuefeng / Hu, Jie / Guo, Yepeng / Shen, Xin

Biology

2024 Volume 13, Issue 3

Abstract: The receptor for activated protein kinase C1 (RACK1) belongs to the typical WD repeat family, which is extremely conservative and important in multiple signal transduction pathways related to growth and development that coordinate the intracellular role ... ...

Abstract	The receptor for activated protein kinase C1 (RACK1) belongs to the typical WD repeat family, which is extremely conservative and important in multiple signal transduction pathways related to growth and development that coordinate the intracellular role of various life activities. As a novel protein with versatile functions, it was found in a variety of organisms. In a previous study, we identified the RACK1 sequence of white shrimp from transcriptome data. In this study, we employed specialized bioinformatics software to conduct an in-depth analysis of
Language	English
Publishing date	2024-03-08
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2661517-4
ISSN	2079-7737
ISSN	2079-7737
DOI	10.3390/biology13030174
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Article ; Online: Inhibitory effects of the main metabolites of Apatinib on CYP450 isozymes in human and rat liver microsomes.

Pang, Ni-Hong / Xu, Ren-Ai / Chen, Lian-Guo / Chen, Zhe / Hu, Guo-Xin / Zhang, Bo-Wen

Toxicology in vitro : an international journal published in association with BIBRA

2023 Volume 95, Page(s) 105739

Abstract: Purpose: The inhibitory effect of Apatinib on cytochrome P450 (CYP450) enzymes has been studied. However, it is unknown whether the inhibition is related to the major metabolites, M1-1, M1-2 and M1-6.: Methods: A 5-in-1 cocktail system composed of ... ...

Abstract	Purpose: The inhibitory effect of Apatinib on cytochrome P450 (CYP450) enzymes has been studied. However, it is unknown whether the inhibition is related to the major metabolites, M1-1, M1-2 and M1-6. Methods: A 5-in-1 cocktail system composed of CYP2B6/Cyp2b1, CYP2C9/Cyp2c11, CYP2E1/Cyp2e1, CYP2D6/Cyp2d1 and CYP3A/Cyp3a2 was used in this study. Firstly, the effects of APA and its main metabolites on the activities of HLMs, RLMs and recombinant isoforms were examined. The reaction mixture included HLMs, RLMs or recombinant isoforms (CYP3A4.1, CYP2D6.1, CYP2D6.10 or CYP2C9.1), analyte (APA, M1-1, M1-2 or M1-6), probe substrates. The reactions were pre-incubated for 5 min at 37 °C, followed by the addition of NAPDH to initiate the reactions, which continued for 40 min. Secondly, IC Results: Under the influence of M1-6, the activity of CYP2B6, 2C9, 2E1 and 3A4/5 was increased to 193.92%, 210.82%, 235.67% and 380.12% respectively; the activity of CYP2D6 was reduced to 92.61%. The inhibitory effects of M1-1 on CYP3A4/5 in HLMs and on Cyp2d1 in RLMs, as well as the effect of M1-2 on CYP3A in HLMs, were determined to be noncompetitive inhibition, with the K Conclusions: M1-1 and M1-2 exhibited inhibition for several CYP450 isozymes, especially CYP2B6, 2C9, 2D6 and 3A4/5. This observation may uncover potential drug-drug interactions and provide valuable insights for the clinical application of APA.
MeSH term(s)	Humans ; Rats ; Animals ; Microsomes, Liver/metabolism ; Cytochrome P-450 CYP3A/metabolism ; Cytochrome P-450 CYP2D6/metabolism ; Cytochrome P-450 CYP2D6/pharmacology ; Cytochrome P-450 CYP2E1/metabolism ; Isoenzymes/metabolism ; Cytochrome P-450 CYP2C9/metabolism ; Cytochrome P-450 CYP2B6/metabolism ; NADP/metabolism ; Cytochrome P-450 Enzyme System/metabolism ; Pyridines
Chemical Substances	Cytochrome P-450 CYP3A (EC 1.14.14.1) ; Cytochrome P-450 CYP2D6 (EC 1.14.14.1) ; apatinib (5S371K6132) ; Cytochrome P-450 CYP2E1 (EC 1.14.13.-) ; Isoenzymes ; Cytochrome P-450 CYP2C9 (EC 1.14.13.-) ; Cytochrome P-450 CYP2B6 (EC 1.14.14.1) ; NADP (53-59-8) ; Cytochrome P-450 Enzyme System (9035-51-2) ; Pyridines
Language	English
Publishing date	2023-12-01
Publishing country	England
Document type	Journal Article
ZDB-ID	639064-x
ISSN	1879-3177 ; 0887-2333
ISSN (online)	1879-3177
ISSN	0887-2333
DOI	10.1016/j.tiv.2023.105739
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Zs.A 2223: Show issues

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Article ; Online: A pilot study on the expression of circadian clock genes in the alveolar bone of mice with periodontitis.

Guo, Wu-Shuang / Deng, Xin / Yang, Man-Xin / Hu, Tian / Li, Xing-Han

Chronobiology international

2024 Volume 41, Issue 2, Page(s) 193–200

Abstract: This study aimed to investigate the expression of circadian clock genes in mouse alveolar bone, and the possible reasons for these changes. Fifty C57 mice were orally inoculated ... ...

Abstract	This study aimed to investigate the expression of circadian clock genes in mouse alveolar bone, and the possible reasons for these changes. Fifty C57 mice were orally inoculated with
MeSH term(s)	Mice ; Animals ; Circadian Clocks/genetics ; Circadian Rhythm/genetics ; Pilot Projects ; X-Ray Microtomography ; ARNTL Transcription Factors/genetics ; RNA, Messenger/metabolism ; Periodontitis/genetics ; CLOCK Proteins/genetics
Chemical Substances	ARNTL Transcription Factors ; RNA, Messenger ; CLOCK Proteins (EC 2.3.1.48)
Language	English
Publishing date	2024-01-26
Publishing country	England
Document type	Journal Article
ZDB-ID	998996-1
ISSN	1525-6073 ; 0742-0528
ISSN (online)	1525-6073
ISSN	0742-0528
DOI	10.1080/07420528.2024.2305212
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Article: Effects of CYP2C19 variants on the metabolism of tapentadol

Xu, Ren-Ai / Fang, Ping / Ye, Zhize / Han, Mingming / Cai, Jian-Ping / Hu, Guo-Xin

Iranian journal of basic medical sciences

2022 Volume 25, Issue 5, Page(s) 659–663

Abstract: Objectives: This study aims to evaluate the catalytic activities of 31 CYP2C19 alleles and their effects on the metabolism of tapentadol : Materials and methods: Insect microsomes expressing the CYP2C19 alleles were incubated with 50-1250 μM ... ...

Abstract	Objectives: This study aims to evaluate the catalytic activities of 31 CYP2C19 alleles and their effects on the metabolism of tapentadol Materials and methods: Insect microsomes expressing the CYP2C19 alleles were incubated with 50-1250 μM tapentadol for 40 min at 37 °C and terminated by cooling to -80 °C, immediately. Tapentadol and N-desmethyl tapentadol were analyzed by a UPLC-MS/MS system. The kinetic parameters Km, Vmax, and intrinsic clearance (Vmax/Km) of N-desmethyl tapentadol were determined. Results: As a result, the intrinsic clearance (V Conclusion: As the first study of all aforementioned alleles for tapentadol metabolism, the comprehensive data
Language	English
Publishing date	2022-06-21
Publishing country	Iran
Document type	Journal Article
ZDB-ID	2500485-2
ISSN	2008-3874 ; 2008-3866
ISSN (online)	2008-3874
ISSN	2008-3866
DOI	10.22038/IJBMS.2022.56996.12710
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Article ; Online: Effect of apatinib on the pharmacokinetics of tramadol and O-desmethyltramadol in rats.

Bao, Su-Su / Tang, Peng-Fei / Gao, Nan-Yong / Xiao, Zhong-Xiang / Qian, Jian-Chang / Zheng, Long / Hu, Guo-Xin / Xu, Huan-Hai

PeerJ

2023 Volume 11, Page(s) e16051

Abstract: Since the combination of anticancer drugs and opioids is very common, apatinib and tramadol are likely to be used in combination clinically. This study evaluated the effects of apatinib on the pharmacokinetics of tramadol and its main metabolite O- ... ...

Abstract	Since the combination of anticancer drugs and opioids is very common, apatinib and tramadol are likely to be used in combination clinically. This study evaluated the effects of apatinib on the pharmacokinetics of tramadol and its main metabolite O-desmethyltramadol in Sprague-Dawley (SD) rats and the inhibitory effects of apatinib on tramadol in rat liver microsomes (RLMs), human liver microsomes (HLMs) and recombinant human CYP2D6.1. The samples were determined by ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). The
MeSH term(s)	Humans ; Rats ; Animals ; Tramadol/pharmacology ; Chromatography, Liquid ; Cytochrome P-450 CYP2D6 ; Rats, Sprague-Dawley ; Tandem Mass Spectrometry ; Microsomes, Liver
Chemical Substances	O-demethyltramadol (2WA8F50C3F) ; Tramadol (39J1LGJ30J) ; apatinib (5S371K6132) ; Cytochrome P-450 CYP2D6 (EC 1.14.14.1)
Language	English
Publishing date	2023-09-11
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2703241-3
ISSN	2167-8359 ; 2167-8359
ISSN (online)	2167-8359
ISSN	2167-8359
DOI	10.7717/peerj.16051
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Article ; Online: Effects of drug-drug interactions and CYP3A4 variants on alectinib metabolism.

Liu, Ya-Nan / Chen, Jie / Wang, Jing / Li, Qingqing / Hu, Guo-Xin / Cai, Jian-Ping / Lin, Guanyang / Xu, Ren-Ai

Archives of toxicology

2023 Volume 97, Issue 8, Page(s) 2133–2142

Abstract: In this study, the effects of 17 CYP3A4 variants and drug-drug interactions (DDI) with its mechanism on alectinib metabolism were investigated. In vitro incubation systems of rat liver microsomes (RLM), human liver microsomes (HLM) and recombinant human ... ...

Abstract	In this study, the effects of 17 CYP3A4 variants and drug-drug interactions (DDI) with its mechanism on alectinib metabolism were investigated. In vitro incubation systems of rat liver microsomes (RLM), human liver microsomes (HLM) and recombinant human CYP3A4 variants were established. The formers were used to screen potential drugs that inhibited alectinib metabolism and study the underlying mechanism, and the latter was used to determine the dynamic characteristics of CYP3A4 variants. Alectinib and its main metabolite M4 were quantitatively determined by ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS). The results showed that compared with CYP3A4.1, only CYP3A4.29 showed higher catalytic activity, while the catalytic activity of CYP3A4.4, .7, .8, .12, .14, .16, .17, .18, .19, .20, .23, and .24 decreased significantly. Among them, the catalytic activity of CYP3A4.20 is the lowest, only 2.63% of that of CYP3A4.1. Based on the RLM incubation system in vitro, 81 drugs that may be combined with alectinib were screened, among which 18 drugs had an inhibition rate higher than 80%. In addition, nicardipine had an inhibition rate of 95.09% with a half-maximum inhibitory concentration (IC
MeSH term(s)	Rats ; Humans ; Animals ; Cytochrome P-450 CYP3A/genetics ; Cytochrome P-450 CYP3A/metabolism ; Cytochrome P-450 Enzyme System/metabolism ; Chromatography, Liquid ; Rats, Sprague-Dawley ; Nicardipine/metabolism ; Nicardipine/pharmacology ; Chromatography, High Pressure Liquid/methods ; Tandem Mass Spectrometry ; Drug Interactions ; Microsomes, Liver/metabolism
Chemical Substances	Cytochrome P-450 CYP3A (EC 1.14.14.1) ; alectinib (LIJ4CT1Z3Y) ; Cytochrome P-450 Enzyme System (9035-51-2) ; Nicardipine (CZ5312222S) ; CYP3A4 protein, human (EC 1.14.14.55)
Language	English
Publishing date	2023-05-20
Publishing country	Germany
Document type	Journal Article
ZDB-ID	124992-7
ISSN	1432-0738 ; 0340-5761
ISSN (online)	1432-0738
ISSN	0340-5761
DOI	10.1007/s00204-023-03524-1
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Uf I Zs.90: Show issues

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Article ; Online: Exploration of the reaction mechanism of the LaFeO

Feng, Yuchuan / Hu, Xiude / Guo, Xin / Wang, Nana

Physical chemistry chemical physics : PCCP

2023 Volume 25, Issue 18, Page(s) 13033–13040

Abstract: The CO conversion is expected to be controllable for chemical-looping steam methane reforming. Herein, density functional theory (DFT) calculations were employed to systematically explore the detailed reaction mechanism of CO conversion over the ... ...

Abstract	The CO conversion is expected to be controllable for chemical-looping steam methane reforming. Herein, density functional theory (DFT) calculations were employed to systematically explore the detailed reaction mechanism of CO conversion over the LaFeO
Language	English
Publishing date	2023-05-10
Publishing country	England
Document type	Journal Article
ZDB-ID	1476244-4
ISSN	1463-9084 ; 1463-9076
ISSN (online)	1463-9084
ISSN	1463-9076
DOI	10.1039/d2cp05795f
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