Discovery and evaluation of a novel selective fluorescent substrate for CYP3A4 based on sulfoxidation characteristics

Chao-Hua Yan, Gui-Lin Wei, Zhuo-An Jin‡, Tian-Chi Lu, Xiao-dong Li, Ji-Cong Wu, Chun-Yang Yu, Li-Wei Zou and Ling Yang

Chem. Commun., 2025, 61, 8871
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A highly selective long-wavelength fluorescent probe for the detection of human carboxylesterase 2 and its biomedical applications

Lei Feng, Zhao-Ming Liu, Liang Xu, Xia Lv, Jing Ning, Jie Hou, Guang-Bo Ge, Jing-Nan Cui and Ling Yang

Chem. Commun., 2014, 50, 14519
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An optimized CYP3A4-activatable fluorogenic sensor for in situ functional imaging and multi-dimensional inhibitor assessment

Feng Zhang, Yufan Fan, Mei Luo, Jian Huang, Bei Zhao, Lin Chen, Guanghao Zhu, Yuan Xiong, Hong Lin, Chuting Xu, Xiaodi Yang, Tony D. James and Guangbo Ge

Chem. Sci., 2025, 16, 11386
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A highly selective marker reaction for measuring the activity of human carboxylesterase 1 in complex biological samples

Xia Lv, Dan-Dan Wang, Lei Feng, Ping Wang, Li-Wei Zou, Da-Cheng Hao, Jie Hou, Jing-Nan Cui, Guang-Bo Ge and Ling Yang

RSC Adv., 2016, 6, 4302
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Pyroglutamate aminopeptidase 1 may be an indicator of cellular inflammatory response as revealed using a sensitive long-wavelength fluorescent probe

Qiuyu Gong, Lihong Li, Xiaofeng Wu and Huimin Ma

Chem. Sci., 2016, 7, 4694
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A highly selective probe for UDP-glucuronosyltransferase 2B7 (UGT2B7) in human microsomes: isoform specificity, kinetic characterization, and applications

Xiang-Ge Tian, Chao Wang, Guang-Bo Ge, Jing Ning, Chun-Zhi Ai, James Y. Hong, Yong-Xv Cai, Xiao-Kui Huo, Jie Hou, Ke-Xin Liu, Hong-Zhi Sun and Xiao-Chi Ma

RSC Adv., 2015, 5, 5924
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Characterization of regio- and stereo-selective sulfation of bufadienolides: exploring the mechanism and providing insight into the structure–sulfation relationship by experimentation and molecular docking analysis

Jing Ning, Yonglei Cui, Chao Wang, Peipei Dong, Guangbo Ge, Xiangge Tian, Jie Hou, Xiaokui Huo, Baojing Zhang, Tonghui Ma and Xiaochi Ma

RSC Adv., 2016, 6, 5774
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A bioluminescent sensor for highly selective and sensitive detection of human carboxylesterase 1 in complex biological samples

Dan-Dan Wang, Qiang Jin, Li-Wei Zou, Jie Hou, Xia Lv, Wei Lei, Hai-Ling Cheng, Guang-Bo Ge and Ling Yang

Chem. Commun., 2016, 52, 3183
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A practical strategy to design and develop an isoform-specific fluorescent probe for a target enzyme: CYP1A1 as a case study

Zi-Ru Dai, Lei Feng, Qiang Jin, Hailing Cheng, Yan Li, Jing Ning, Yang Yu, Guang-Bo Ge, Jing-Nan Cui and Ling Yang

Chem. Sci., 2017, 8, 2795
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Biotransformation of alisol G by Penicillium janthinellum and the hCE2 inhibitory effects of its metabolites

Zhen-Peng Mai, Xiu-Lan Xin, Zheng Sun, Ning Zhang, Shan-Shan Huang, Chao Wang, Liang Chen, Ye Li, Xiao-Kui Huo and Guang-Jun Fan

Phytochemistry Letters, 2015, 13, 228
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Mechanism-based inactivation of CYP450 enzymes: a case study of lapatinib

Han Kiat Ho, James Chun Yip Chan, Klarissa D. Hardy and Eric Chun Yong Chan

Drug Metabolism Reviews, 2015, 47, 21
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Target Enzyme‐Activated Two‐Photon Fluorescent Probes: A Case Study of CYP3A4 Using a Two‐Dimensional Design Strategy

Jing Ning, Wei Wang, Guangbo Ge, Peng Chu, Feida Long, Yongliang Yang, Yulin Peng, Lei Feng, Xiaochi Ma and Tony D. James

Angew Chem Int Ed, 2019, 58, 9959
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Rationally Engineered CYP3A4 Fluorogenic Substrates for Functional Imaging Analysis and Drug–Drug Interaction Studies

Rong-Jing He, Zhen-Hao Tian, Jian Huang, Meng-Ru Sun, Feng Wei, Chun-Yu Li, Hai-Rong Zeng, Feng Zhang, Xiao-Qing Guan, Yan Feng, Xiang-Ming Meng, Hui Yang and Guang-Bo Ge

J. Med. Chem., 2023, 66, 6743
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In vitro phase I metabolism of gamabufotalin and arenobufagin: Reveal the effect of substituent group on metabolic stability

Yujie Feng, Chao Wang, Xiangge Tian, Xiaokui Huo, Lei Feng, Chengpeng Sun, Guangbo Ge, Ling Yang, Jing Ning and Xiaochi Ma

Fitoterapia, 2017, 121, 38
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Characterization of Phase I Metabolism of Resibufogenin and Evaluation of the Metabolic Effects on Its Antitumor Activity and Toxicity

Jing Ning, Zhen-Long Yu, Liang-Hai Hu, Chao Wang, Xiao-Kui Huo, Sa Deng, Jie Hou, Jing-Jing Wu, Guang-Bo Ge, Xiao-Chi Ma and Ling Yang

Drug Metabolism and Disposition, 2015, 43, 299
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Molecular probes for human cytochrome P450 enzymes: Recent progress and future perspectives

Jingjing Wu, Xiaoqing Guan, Ziru Dai, Rongjing He, Xinxin Ding, Ling Yang and Guangbo Ge

Coordination Chemistry Reviews, 2021, 427, 213600
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A highly selective near-infrared fluorescent probe for carboxylesterase 2 and its bioimaging applications in living cells and animals

Qiang Jin, Lei Feng, Dan-Dan Wang, Jing-Jing Wu, Jie Hou, Zi-Ru Dai, Shi-Guo Sun, Jia-Yue Wang, Guang-Bo Ge, Jing-Nan Cui and Ling Yang

Biosensors and Bioelectronics, 2016, 83, 193
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Unique Oxidative Metabolism of Bufalin Generates Two Reactive Metabolites That Strongly Inactivate Human Cytochrome P450 3A

Dongzhu Tu, Jing Ning, Liwei Zou, Ping Wang, Yani Zhang, Xiangge Tian, Feng Zhang, Jiang Zheng and Guangbo Ge

J. Med. Chem., 2022, 65, 4018
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Biotransformation of major flavonoid glycosides in herb epimedii by the fungus Cunninghamella blakesleana

XiuLan Xin, Guang-Jun Fan, Zheng Sun, Ning Zhang, Ye Li, Rong Lan, Liang Chen and PeiPei Dong

Journal of Molecular Catalysis B: Enzymatic, 2015, 122, 141
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A novel near-infrared fluorescent probe for sensitive detection of β-galactosidase in living cells

Jingtuo Zhang, Cong Li, Colina Dutta, Mingxi Fang, Shuwei Zhang, Ashutosh Tiwari, Thomas Werner, Fen-Tair Luo and Haiying Liu

Analytica Chimica Acta, 2017, 968, 97
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Real-Time Tracking the Synthesis and Degradation of Albumin in Complex Biological Systems with a near-Infrared Fluorescent Probe

Qiang Jin, Lei Feng, Shui-Jun Zhang, Dan-Dan Wang, Fang-Jun Wang, Yi Zhang, Jing-Nan Cui, Wen-Zhi Guo, Guang-Bo Ge and Ling Yang

Anal. Chem., 2017, 89, 9884
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Regioselective Glucuronidation of Andrographolide and Its Major Derivatives: Metabolite Identification, Isozyme Contribution, and Species Differences

Xiangge Tian, Sicheng Liang, Chao Wang, Baojian Wu, Guangbo Ge, Sa Deng, Kexin Liu, Ling Yang and Xiaochi Ma

AAPS J, 2015, 17, 156
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An Optimized Two‐Photon Fluorescent Probe for Biological Sensing and Imaging of Catechol‐O‐Methyltransferase

Ping Wang, Yang‐Liu Xia, Li‐Wei Zou, Xing‐Kai Qian, Tong‐Yi Dou, Qiang Jin, Shi‐Yang Li, Yang Yu, Dan‐Dan Wang, Qun Luo, Guang‐Bo Ge and Ling Yang

Chemistry A European J, 2017, 23, 10800
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A Practical and High-Affinity Fluorescent Probe for Uridine Diphosphate Glucuronosyltransferase 1A1: A Good Surrogate for Bilirubin

Xia Lv, Lei Feng, Chun-Zhi Ai, Jie Hou, Ping Wang, Li-Wei Zou, Jie Cheng, Guang-Bo Ge, Jing-Nan Cui and Ling Yang

J. Med. Chem., 2017, 60, 9664
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Metabolic Profile of 3-Acetyl-11-Keto-β-Boswellic Acid and 11-Keto-β-Boswellic Acid in Human Preparations In Vitro, Species Differences, and Bioactivity Variation

Yonglei Cui, Xiangge Tian, Jing Ning, Chao Wang, Zhenlong Yu, Yan Wang, Xiaokui Huo, Lingling Jin, Sa Deng, Baojing Zhang and Xiaochi Ma

AAPS J, 2016, 18, 1273
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Metabolites profiling of 10 bufadienolides in human liver microsomes and their cytotoxicity variation in HepG2 cell

Lingyu Han, Hongjie Wang, Nan Si, Wei Ren, Bo Gao, Yan Li, Jian Yang, Miao Xu, Haiyu Zhao and Baolin Bian

Anal Bioanal Chem, 2016, 408, 2485
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Cytochrome P450 3A Enzymes Are Key Contributors for Hepatic Metabolism of Bufotalin, a Natural Constitute in Chinese Medicine Chansu

Zi-Ru Dai, Jing Ning, Gui-Bo Sun, Ping Wang, Feng Zhang, Hong-Ying Ma, Li-Wei Zou, Jie Hou, Jing-Jing Wu, Guang-Bo Ge, Xiao-Bo Sun and Ling Yang

Front. Pharmacol., 2019, 10
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Biotransformation of resibufogenin by Actinomucor elegans and the cytotoxicity of the resulting metabolites

Yan Wang, Qingxi Yue, Xiaochi Ma, Ronggang Xi, Xiaokui Huo, Baojing Zhang, Xiaodong Ma, Chao Wang, Yan Tian, Meng Gao and Xiaobo Wang

Phytochemistry Letters, 2014, 9, 132
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Recent Advances in Molecular Fluorescent Probes for CYP450 Sensing and Imaging

Haiyan Li, Yang Sheng, Wei Li and Lin Yuan

Chemosensors, 2022, 10, 304
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The prenylated phenolic natural product isoglycycoumarin is a highly selective probe for human cytochrome P450 2A6

Qi Wang, Yi Kuang, Junbin He, Kai Li, Wei Song, Hongwei Jin, Xue Qiao and Min Ye

European Journal of Pharmaceutical Sciences, 2017, 109, 472
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Functional Imaging of CYP3A4 at Multiple Dimensions Using an AI‐Driven High Performance Fluorogenic Substrate

Feng Zhang, Lilin Song, Ruixuan Wang, Bei Zhao, Jian Huang, Luling Wu, Yufan Fan, Hong Lin, Zhengtao Jiang, Xiaodi Yang, Hairong Zeng, Xin Yang, Tony D. James and Guangbo Ge

Small, 2025, 21
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Gomisin A is a Novel Isoform-Specific Probe for the Selective Sensing of Human Cytochrome P450 3A4 in Liver Microsomes and Living Cells

Jing-Jing Wu, Guang-Bo Ge, Yu-Qi He, Ping Wang, Zi-Ru Dai, Jing Ning, Liang-Hai Hu and Ling Yang

AAPS J, 2016, 18, 134
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Chemical Probes for Human UDP‐Glucuronosyltransferases: A Comprehensive Review

Xia Lv, Jian‐Bin Zhang, Jie Hou, Tong‐Yi Dou, Guang‐Bo Ge, Wen‐Zhong Hu and Ling Yang

Biotechnology Journal, 2019, 14
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Solving the interactions of steroidal ligands with CYP3A4 using a grid-base template system

Takahiro Goto, Masahiro Tohkin and Yasushi Yamazoe

Drug Metabolism and Pharmacokinetics, 2019, 34, 351
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A patent review of CYP3A4 inhibitors (2018 – present)

Dong-Zhu Tu, Xue-Yan Hu, Jing-Xuan Lei, Shu-Yan Liu, Zhang-Ping Xiao, Ling Yang and Guang-Bo Ge

Expert Opinion on Therapeutic Patents, 2025, 35, 503
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A highly specific ratiometric two-photon fluorescent probe to detect dipeptidyl peptidase IV in plasma and living systems

Li-Wei Zou, Ping Wang, Xing-Kai Qian, Lei Feng, Yang Yu, Dan-Dan Wang, Qiang Jin, Jie Hou, Zhi-Hong Liu, Guang-Bo Ge and Ling Yang

Biosensors and Bioelectronics, 2017, 90, 283
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Microbial transformation of resibufogenin byCurvularia lunataAS 3.4381

Xiu-Lan Xin, Jiang-Hao Sun, Xiao-Bo Wang, Rong-Gang Xi, Gang Wang, Rong Lan, Dong-Hai Su, Hua Li, Xiao-Kui Huo and Chao Wang

Journal of Asian Natural Products Research, 2014, 16, 290
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Interspecies variation in phase I metabolism of bufalin in hepatic microsomes from mouse, rat, dog, minipig, monkey, and human

Jing Ning, Jie Hou, Ping Wang, Jing-Jing Wu, Zi-Ru Dai, Li-Wei Zou, Wei Li, Guang-Bo Ge, Xiao-Chi Ma and Ling Yang

Xenobiotica, 2015, 45, 954
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A Naturally Occurring Isoform-Specific Probe for Highly Selective and Sensitive Detection of Human Cytochrome P450 3A5

Jing-Jing Wu, Yun-Feng Cao, Liang Feng, Yu-Qi He, James Y. Hong, Tong-Yi Dou, Ping Wang, Da-Cheng Hao, Guang-Bo Ge and Ling Yang

J. Med. Chem., 2017, 60, 3804
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A Mechanism-Based Model for the Prediction of the Metabolic Sites of Steroids Mediated by Cytochrome P450 3A4

Zi-Ru Dai, Chun-Zhi Ai, Guang-Bo Ge, Yu-Qi He, Jing-Jing Wu, Jia-Yue Wang, Hui-Zi Man, Yan Jia and Ling Yang

IJMS, 2015, 16, 14677
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Rational Design of a Long-Wavelength Fluorescent Probe for Highly Selective Sensing of Carboxylesterase 1 in Living Systems

Zhenhao Tian, Lele Ding, Kun Li, Yunqing Song, Tongyi Dou, Jie Hou, Xiangge Tian, Lei Feng, Guangbo Ge and Jingnan Cui

Anal. Chem., 2019, 91, 5638
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A broad-spectrum substrate for the human UDP-glucuronosyltransferases and its use for investigating glucuronidation inhibitors

Qi-Hang Zhou, Wei-Wei Qin, Moshe Finel, Qing-Qing He, Dong-Zhu Tu, Chao-Ran Wang and Guang-Bo Ge

International Journal of Biological Macromolecules, 2021, 180, 252
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NNKcat: deep neural network to predict catalytic constants (Kcat) by integrating protein sequence and substrate structure with enhanced data imbalance handling

Jingchen Zhai, Xiguang Qi, Lianjin Cai, Yue Liu, Haocheng Tang, Lei Xie and Junmei Wang

Briefings in Bioinformatics, 2025, 26
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Biotransformation of resibufogenin by Actinomucor elegans

Li-Yan Mou, Xiu-Lan Xin, Liang Chen, Pei-Pei Dong, Rong Lan, Dong-Hai Su, Jian Huang, Jin-Hui Wang and Li-Bin Zhan

Journal of Asian Natural Products Research, 2014, 16, 623
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Identifying and applying a highly selective probe to simultaneously determine the O-glucuronidation activity of human UGT1A3 and UGT1A4

Li Jiang, Si-Cheng Liang, Chao Wang, Guang-Bo Ge, Xiao-Kui Huo, Xiao-Yi Qi, Sa Deng, Ke-Xin Liu and Xiao-Chi Ma

Sci Rep, 2015, 5
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A Dual Functional Probe for Assessing Human CYP450 3A5 and 3A Enzymes Bioactivities

Fei Yan, Yonglei Cui, Yue An, Jing Ning, Xinyu Zhao, Lei Feng, Xiaokui Huo, Chao Wang, Chuanzhu Lv, Xiaochi Ma and Xiangge Tian

Future Med. Chem., 2019, 11, 2891
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Activity-Independent Enzyme-Powered Amplification for Improving Signal Stability and Fidelity in Biosensing

Yibo Zhou, Shan Hu, Hong-Wen Liu, Xinyue Xiao, Weiju Chen, Sheng Yang, Huiqiu Shi, Zhengxuan Gu, Junbin Li, Ronghua Yang and Zhihe Qing

Chemical & Biomedical Imaging, 2024, 2, 304
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A Highly Selective Ratiometric Two-Photon Fluorescent Probe for Human Cytochrome P450 1A

Zi-Ru Dai, Guang-Bo Ge, Lei Feng, Jing Ning, Liang-Hai Hu, Qiang Jin, Dan-Dan Wang, Xia Lv, Tong-Yi Dou, Jing-Nan Cui and Ling Yang

J. Am. Chem. Soc., 2015, 137, 14488
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Photoacoustic nanoprobe for β-galactosidase activity detection and imaging in vivo

Qin Zeng, Yunxia Wu and Tao Zhang

J. Innov. Opt. Health Sci., 2019, 12
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Quantitative analysis of cytochrome P450 isoforms in human liver microsomes by the combination of proteomics and chemical probe-based assay

Xidong Liu, Lianghai Hu, Guangbo Ge, Bo Yang, Jing Ning, Shixin Sun, Ling Yang, Klaus Pors and Jingkai Gu

Proteomics, 2014, 14, 1943
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A novel substrate-inspired fluorescent probe to monitor native albumin in human plasma and living cells

Guang-Bo Ge, Lei Feng, Qiang Jin, Yi-Ru Wang, Zhao-Ming Liu, Xin-Yue Zhu, Ping Wang, Jie Hou, Jing-Nan Cui and Ling Yang

Analytica Chimica Acta, 2017, 989, 71
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Carboxylesterase-2-Selective Two-Photon Ratiometric Probe Reveals Decreased Carboxylesterase-2 Activity in Breast Cancer Cells

Sang Jun Park, Yun Ji Kim, Ji Su Kang, In Young Kim, Kyeong Sook Choi and Hwan Myung Kim

Anal. Chem., 2018, 90, 9465
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Recent progress in the discovery of natural inhibitors against human carboxylesterases

Dan-Dan Wang, Li-Wei Zou, Qiang Jin, Jie Hou, Guang-Bo Ge and Ling Yang

Fitoterapia, 2017, 117, 84
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A Two-Photon Ratiometric Fluorescent Probe for Imaging Carboxylesterase 2 in Living Cells and Tissues

Qiang Jin, Lei Feng, Dan-Dan Wang, Zi-Ru Dai, Ping Wang, Li-Wei Zou, Zhi-Hong Liu, Jia-Yue Wang, Yang Yu, Guang-Bo Ge, Jing-Nan Cui and Ling Yang

ACS Appl. Mater. Interfaces, 2015, 7, 28474
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Computational insights into the different catalytic activities of CYP3A4 and CYP3A5 toward schisantherin E

Yuhan Xue, Junhao Li, Zengrui Wu, Guixia Liu, Yun Tang and Weihua Li

Chem Biol Drug Des, 2019, 93, 854
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Characterization of CYP3A5 Selective Inhibitors for Reaction Phenotyping of Drug Candidates

Jie Chen, Lloyd Wei Tat Tang, Samantha Jordan, Makayla Harrison, Gabrielle M. Gualtieri, Ethan DaSilva, Danial Morris, Gary Bora, Ye Che and Li Di

AAPS J, 2024, 26
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Target Enzyme‐Activated Two‐Photon Fluorescent Probes: A Case Study of CYP3A4 Using a Two‐Dimensional Design Strategy

Jing Ning, Wei Wang, Guangbo Ge, Peng Chu, Feida Long, Yongliang Yang, Yulin Peng, Lei Feng, Xiaochi Ma and Tony D. James

Angewandte Chemie, 2019, 131, 10064
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ABSTRACTS FROM THE 10THINTERNATIONAL ISSX MEETING

Drug Metabolism Reviews, 2014, 45, 1
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Drug metabolism and disposition diversity of Ranunculales phytometabolites: a systems perspective

Da Cheng Hao and Ling Yang

Expert Opinion on Drug Metabolism & Toxicology, 2016, 12, 1047
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Herb-drug interaction between Styrax and warfarin: Molecular basis and mechanism

Feng Zhang, Jian Huang, Rong-Jing He, Lu Wang, Peng-Chao Huo, Xiao-Qing Guan, Sheng-Quan Fang, Yan-Wei Xiang, Shou-Ning Jia and Guang-Bo Ge

Phytomedicine, 2020, 77, 153287
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An Uncertainty-Guided Deep Learning Method Facilitates Rapid Screening of CYP3A4 Inhibitors

Ruixuan Wang, Zhikang Liu, Jiahao Gong, Qingping Zhou, Xiaoqing Guan and Guangbo Ge

J. Chem. Inf. Model., 2023, 63, 7699
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Metabolites analysis of 4 arenobufagin structure-related bufadienolides in human liver microsomes using UHPLC-ESI-Orbitrap mass

Lingyu Han, Nan Si, Bo Gao, Hongjie Wang, Yanyan Zhou, Jian Yang, Haiyu Zhao and Baolin Bian

International Journal of Mass Spectrometry, 2017, 422, 88
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Drug interaction study of flavonoids toward CYP3A4 and their quantitative structure activity relationship (QSAR) analysis for predicting potential effects

Yannan Li, Jing Ning, Yan Wang, Chao Wang, Chengpeng Sun, Xiaokui Huo, Zhenlong Yu, Lei Feng, Baojing Zhang, Xiangge Tian and Xiaochi Ma

Toxicology Letters, 2018, 294, 27
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Identification of the hydroxylated derivatives of bufalin: phase I metabolites in rats

Xiu-Lan Xin, Pei-Pei Dong, Xiao-Hong Sun, Sa Deng, Ning Zhang, Chao Wang, Xiao-Kui Huo, Ye Li, Rong Lan, Liang Chen and Guang-Jun Fan

Journal of Asian Natural Products Research, 2016, 18, 239
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Sensing carboxylesterase 1 in living systems by a practical and isoform-specific fluorescent probe

Lele Ding, Zhenhao Tian, Jie Hou, Tongyi Dou, Qiang Jin, Dandan Wang, Liwei Zou, Yadi Zhu, Yunqing Song, Jingnan Cui and Guangbo Ge

Chinese Chemical Letters, 2019, 30, 558
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