ArticleThe Journal of pharmacology and experimental therapeutics2020
Slow-, Tight-Binding Inhibition of CYP17A1 by Abiraterone Redefines Its Kinetic Selectivity and Dosing Regimen.
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Article in The Journal of pharmacology and experimental therapeutics, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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16citing papers in PubMed
2.3field-weighted citation impact, top 11% of its field
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Who cites it
16 citing papers in PubMed, 27 citations in OpenAlex.
- Trial
- Exploring the roles of cytochrome P450 enzymes and their inhibitors in cancers and non-neoplastic human diseases.Archives of pharmacal research · 2025Review
- Comparative effectiveness and safety of enzalutamide versus abiraterone in patients with metastatic castration-resistant prostate cancer: a nationwide registry-based cohort study from Taiwan.Journal of cancer research and clinical oncology · 2025Article
- Evaluation of exposure-response-safety relationship of model-informed low-dose 500 mg abiraterone acetate in prostate cancer patients.Cancer communications (London, England) · 2025Article
- Human Cytochrome P450 Cancer-Related Metabolic Activities and Gene Polymorphisms: A Review.Cells · 2024Review
- Cytochrome P450 Enzymes as Drug Targets in Human Disease.Drug metabolism and disposition: the biological fate of chemicals · 2024Review
- Efficacy of abiraterone combined with prednisone in castration-resistant prostate cancer and its impact on miR-221/222 expression.American journal of cancer research · 2024Article
- Steroid 17α-hydroxylase/17, 20-lyase (cytochrome P450 17A1).Methods in enzymology · 2023Article
- Synthesis and Preclinical Evaluation of Small-Molecule Prostate-Specific Membrane Antigen-Targeted Abiraterone Conjugate.Molecules (Basel, Switzerland) · 2022Article
- How Is CYP17A1 Activity Altered in Autism? A Pilot Study to Identify Potential Pharmacological Targets.Life (Basel, Switzerland) · 2022Article
- Inhibition of Cytochrome P450 Enzymes by Drugs-Molecular Basis and Practical Applications.Biomolecules & therapeutics · 2022Review
- Fully automated virtual screening pipeline of FDA-approved drugs using Caver Web.Computational and structural biotechnology journal · 2022Article
- Roles of cytochrome P450 enzymes in pharmacology and toxicology: Past, present, and future.Advances in pharmacology (San Diego, Calif.) · 2022Article
- Biotransformation of Abiraterone Into Five Characteristic Metabolites by the Rat Gut Microbiota and Liver Microsomes.Frontiers in oncology · 2022Article
- Steroidogenic cytochrome P450 17A1 structure and function.Molecular and cellular endocrinology · 2021Review
- Kinetics of cytochrome P450 3A4 inhibition by heterocyclic drugs defines a general sequential multistep binding process.The Journal of biological chemistryArticle
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Authors and funding
14 authors at 1 institution in 3 countries.
Eleanor Jing Yi CheongDepartment of Pharmacy, Faculty of Science (E.J.Y.C., R.W.Y.N., H.T.T., C.L.L.C., E.C.Y.C.) and Department of Biological Sciences (H.F.), National University of Singapore, Singapore, Singapore; Department of Clinical Pharmacology and Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia (P.C.N., J.O.M.); Bioinformatics Institute, Biotransformation Innovation Platform (BioTrans) (F.L.) and Bioinformatics Institute (H.F.), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore; Department of Surgery, National University Health System, Singapore, Singapore (E.C., K.E.); Department of Urology, National University Hospital, Singapore, Singapore (E.C., K.E.); Centre for Computational Biology, DUKE-NUS Medical School, Singapore, Singapore (H.F.); The University of Chicago, Chicago, Illinois (R.Z.S.); National Cancer Institute, Rockville, Maryland (C.J.P., W.D.F.); and National University Cancer Institute, Singapore (NCIS), NUH Medical Centre (NUHMC), Singapore, Singapore (E.C.Y.C.).
Pramod C NairDepartment of Pharmacy, Faculty of Science (E.J.Y.C., R.W.Y.N., H.T.T., C.L.L.C., E.C.Y.C.) and Department of Biological Sciences (H.F.), National University of Singapore, Singapore, Singapore; Department of Clinical Pharmacology and Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia (P.C.N., J.O.M.); Bioinformatics Institute, Biotransformation Innovation Platform (BioTrans) (F.L.) and Bioinformatics Institute (H.F.), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore; Department of Surgery, National University Health System, Singapore, Singapore (E.C., K.E.); Department of Urology, National University Hospital, Singapore, Singapore (E.C., K.E.); Centre for Computational Biology, DUKE-NUS Medical School, Singapore, Singapore (H.F.); The University of Chicago, Chicago, Illinois (R.Z.S.); National Cancer Institute, Rockville, Maryland (C.J.P., W.D.F.); and National University Cancer Institute, Singapore (NCIS), NUH Medical Centre (NUHMC), Singapore, Singapore (E.C.Y.C.).
Rebecca Wan Yi NeoDepartment of Pharmacy, Faculty of Science (E.J.Y.C., R.W.Y.N., H.T.T., C.L.L.C., E.C.Y.C.) and Department of Biological Sciences (H.F.), National University of Singapore, Singapore, Singapore; Department of Clinical Pharmacology and Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia (P.C.N., J.O.M.); Bioinformatics Institute, Biotransformation Innovation Platform (BioTrans) (F.L.) and Bioinformatics Institute (H.F.), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore; Department of Surgery, National University Health System, Singapore, Singapore (E.C., K.E.); Department of Urology, National University Hospital, Singapore, Singapore (E.C., K.E.); Centre for Computational Biology, DUKE-NUS Medical School, Singapore, Singapore (H.F.); The University of Chicago, Chicago, Illinois (R.Z.S.); National Cancer Institute, Rockville, Maryland (C.J.P., W.D.F.); and National University Cancer Institute, Singapore (NCIS), NUH Medical Centre (NUHMC), Singapore, Singapore (E.C.Y.C.).
Ho Thanh TuDepartment of Pharmacy, Faculty of Science (E.J.Y.C., R.W.Y.N., H.T.T., C.L.L.C., E.C.Y.C.) and Department of Biological Sciences (H.F.), National University of Singapore, Singapore, Singapore; Department of Clinical Pharmacology and Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia (P.C.N., J.O.M.); Bioinformatics Institute, Biotransformation Innovation Platform (BioTrans) (F.L.) and Bioinformatics Institute (H.F.), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore; Department of Surgery, National University Health System, Singapore, Singapore (E.C., K.E.); Department of Urology, National University Hospital, Singapore, Singapore (E.C., K.E.); Centre for Computational Biology, DUKE-NUS Medical School, Singapore, Singapore (H.F.); The University of Chicago, Chicago, Illinois (R.Z.S.); National Cancer Institute, Rockville, Maryland (C.J.P., W.D.F.); and National University Cancer Institute, Singapore (NCIS), NUH Medical Centre (NUHMC), Singapore, Singapore (E.C.Y.C.).
Fu LinDepartment of Pharmacy, Faculty of Science (E.J.Y.C., R.W.Y.N., H.T.T., C.L.L.C., E.C.Y.C.) and Department of Biological Sciences (H.F.), National University of Singapore, Singapore, Singapore; Department of Clinical Pharmacology and Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia (P.C.N., J.O.M.); Bioinformatics Institute, Biotransformation Innovation Platform (BioTrans) (F.L.) and Bioinformatics Institute (H.F.), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore; Department of Surgery, National University Health System, Singapore, Singapore (E.C., K.E.); Department of Urology, National University Hospital, Singapore, Singapore (E.C., K.E.); Centre for Computational Biology, DUKE-NUS Medical School, Singapore, Singapore (H.F.); The University of Chicago, Chicago, Illinois (R.Z.S.); National Cancer Institute, Rockville, Maryland (C.J.P., W.D.F.); and National University Cancer Institute, Singapore (NCIS), NUH Medical Centre (NUHMC), Singapore, Singapore (E.C.Y.C.).
Edmund ChiongDepartment of Pharmacy, Faculty of Science (E.J.Y.C., R.W.Y.N., H.T.T., C.L.L.C., E.C.Y.C.) and Department of Biological Sciences (H.F.), National University of Singapore, Singapore, Singapore; Department of Clinical Pharmacology and Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia (P.C.N., J.O.M.); Bioinformatics Institute, Biotransformation Innovation Platform (BioTrans) (F.L.) and Bioinformatics Institute (H.F.), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore; Department of Surgery, National University Health System, Singapore, Singapore (E.C., K.E.); Department of Urology, National University Hospital, Singapore, Singapore (E.C., K.E.); Centre for Computational Biology, DUKE-NUS Medical School, Singapore, Singapore (H.F.); The University of Chicago, Chicago, Illinois (R.Z.S.); National Cancer Institute, Rockville, Maryland (C.J.P., W.D.F.); and National University Cancer Institute, Singapore (NCIS), NUH Medical Centre (NUHMC), Singapore, Singapore (E.C.Y.C.).
Kesavan EsuvaranathanDepartment of Pharmacy, Faculty of Science (E.J.Y.C., R.W.Y.N., H.T.T., C.L.L.C., E.C.Y.C.) and Department of Biological Sciences (H.F.), National University of Singapore, Singapore, Singapore; Department of Clinical Pharmacology and Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia (P.C.N., J.O.M.); Bioinformatics Institute, Biotransformation Innovation Platform (BioTrans) (F.L.) and Bioinformatics Institute (H.F.), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore; Department of Surgery, National University Health System, Singapore, Singapore (E.C., K.E.); Department of Urology, National University Hospital, Singapore, Singapore (E.C., K.E.); Centre for Computational Biology, DUKE-NUS Medical School, Singapore, Singapore (H.F.); The University of Chicago, Chicago, Illinois (R.Z.S.); National Cancer Institute, Rockville, Maryland (C.J.P., W.D.F.); and National University Cancer Institute, Singapore (NCIS), NUH Medical Centre (NUHMC), Singapore, Singapore (E.C.Y.C.).
Hao FanDepartment of Pharmacy, Faculty of Science (E.J.Y.C., R.W.Y.N., H.T.T., C.L.L.C., E.C.Y.C.) and Department of Biological Sciences (H.F.), National University of Singapore, Singapore, Singapore; Department of Clinical Pharmacology and Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia (P.C.N., J.O.M.); Bioinformatics Institute, Biotransformation Innovation Platform (BioTrans) (F.L.) and Bioinformatics Institute (H.F.), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore; Department of Surgery, National University Health System, Singapore, Singapore (E.C., K.E.); Department of Urology, National University Hospital, Singapore, Singapore (E.C., K.E.); Centre for Computational Biology, DUKE-NUS Medical School, Singapore, Singapore (H.F.); The University of Chicago, Chicago, Illinois (R.Z.S.); National Cancer Institute, Rockville, Maryland (C.J.P., W.D.F.); and National University Cancer Institute, Singapore (NCIS), NUH Medical Centre (NUHMC), Singapore, Singapore (E.C.Y.C.).
Russell Z SzmulewitzDepartment of Pharmacy, Faculty of Science (E.J.Y.C., R.W.Y.N., H.T.T., C.L.L.C., E.C.Y.C.) and Department of Biological Sciences (H.F.), National University of Singapore, Singapore, Singapore; Department of Clinical Pharmacology and Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia (P.C.N., J.O.M.); Bioinformatics Institute, Biotransformation Innovation Platform (BioTrans) (F.L.) and Bioinformatics Institute (H.F.), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore; Department of Surgery, National University Health System, Singapore, Singapore (E.C., K.E.); Department of Urology, National University Hospital, Singapore, Singapore (E.C., K.E.); Centre for Computational Biology, DUKE-NUS Medical School, Singapore, Singapore (H.F.); The University of Chicago, Chicago, Illinois (R.Z.S.); National Cancer Institute, Rockville, Maryland (C.J.P., W.D.F.); and National University Cancer Institute, Singapore (NCIS), NUH Medical Centre (NUHMC), Singapore, Singapore (E.C.Y.C.).
Cody J PeerDepartment of Pharmacy, Faculty of Science (E.J.Y.C., R.W.Y.N., H.T.T., C.L.L.C., E.C.Y.C.) and Department of Biological Sciences (H.F.), National University of Singapore, Singapore, Singapore; Department of Clinical Pharmacology and Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia (P.C.N., J.O.M.); Bioinformatics Institute, Biotransformation Innovation Platform (BioTrans) (F.L.) and Bioinformatics Institute (H.F.), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore; Department of Surgery, National University Health System, Singapore, Singapore (E.C., K.E.); Department of Urology, National University Hospital, Singapore, Singapore (E.C., K.E.); Centre for Computational Biology, DUKE-NUS Medical School, Singapore, Singapore (H.F.); The University of Chicago, Chicago, Illinois (R.Z.S.); National Cancer Institute, Rockville, Maryland (C.J.P., W.D.F.); and National University Cancer Institute, Singapore (NCIS), NUH Medical Centre (NUHMC), Singapore, Singapore (E.C.Y.C.).
William D FiggDepartment of Pharmacy, Faculty of Science (E.J.Y.C., R.W.Y.N., H.T.T., C.L.L.C., E.C.Y.C.) and Department of Biological Sciences (H.F.), National University of Singapore, Singapore, Singapore; Department of Clinical Pharmacology and Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia (P.C.N., J.O.M.); Bioinformatics Institute, Biotransformation Innovation Platform (BioTrans) (F.L.) and Bioinformatics Institute (H.F.), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore; Department of Surgery, National University Health System, Singapore, Singapore (E.C., K.E.); Department of Urology, National University Hospital, Singapore, Singapore (E.C., K.E.); Centre for Computational Biology, DUKE-NUS Medical School, Singapore, Singapore (H.F.); The University of Chicago, Chicago, Illinois (R.Z.S.); National Cancer Institute, Rockville, Maryland (C.J.P., W.D.F.); and National University Cancer Institute, Singapore (NCIS), NUH Medical Centre (NUHMC), Singapore, Singapore (E.C.Y.C.).ORCID 0000-0003-2428-5613
Christina Li Lin ChaiDepartment of Pharmacy, Faculty of Science (E.J.Y.C., R.W.Y.N., H.T.T., C.L.L.C., E.C.Y.C.) and Department of Biological Sciences (H.F.), National University of Singapore, Singapore, Singapore; Department of Clinical Pharmacology and Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia (P.C.N., J.O.M.); Bioinformatics Institute, Biotransformation Innovation Platform (BioTrans) (F.L.) and Bioinformatics Institute (H.F.), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore; Department of Surgery, National University Health System, Singapore, Singapore (E.C., K.E.); Department of Urology, National University Hospital, Singapore, Singapore (E.C., K.E.); Centre for Computational Biology, DUKE-NUS Medical School, Singapore, Singapore (H.F.); The University of Chicago, Chicago, Illinois (R.Z.S.); National Cancer Institute, Rockville, Maryland (C.J.P., W.D.F.); and National University Cancer Institute, Singapore (NCIS), NUH Medical Centre (NUHMC), Singapore, Singapore (E.C.Y.C.).
John O MinersDepartment of Pharmacy, Faculty of Science (E.J.Y.C., R.W.Y.N., H.T.T., C.L.L.C., E.C.Y.C.) and Department of Biological Sciences (H.F.), National University of Singapore, Singapore, Singapore; Department of Clinical Pharmacology and Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia (P.C.N., J.O.M.); Bioinformatics Institute, Biotransformation Innovation Platform (BioTrans) (F.L.) and Bioinformatics Institute (H.F.), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore; Department of Surgery, National University Health System, Singapore, Singapore (E.C., K.E.); Department of Urology, National University Hospital, Singapore, Singapore (E.C., K.E.); Centre for Computational Biology, DUKE-NUS Medical School, Singapore, Singapore (H.F.); The University of Chicago, Chicago, Illinois (R.Z.S.); National Cancer Institute, Rockville, Maryland (C.J.P., W.D.F.); and National University Cancer Institute, Singapore (NCIS), NUH Medical Centre (NUHMC), Singapore, Singapore (E.C.Y.C.).
Eric Chun Yong ChanDepartment of Pharmacy, Faculty of Science (E.J.Y.C., R.W.Y.N., H.T.T., C.L.L.C., E.C.Y.C.) and Department of Biological Sciences (H.F.), National University of Singapore, Singapore, Singapore; Department of Clinical Pharmacology and Flinders Centre for Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia (P.C.N., J.O.M.); Bioinformatics Institute, Biotransformation Innovation Platform (BioTrans) (F.L.) and Bioinformatics Institute (H.F.), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore; Department of Surgery, National University Health System, Singapore, Singapore (E.C., K.E.); Department of Urology, National University Hospital, Singapore, Singapore (E.C., K.E.); Centre for Computational Biology, DUKE-NUS Medical School, Singapore, Singapore (H.F.); The University of Chicago, Chicago, Illinois (R.Z.S.); National Cancer Institute, Rockville, Maryland (C.J.P., W.D.F.); and National University Cancer Institute, Singapore (NCIS), NUH Medical Centre (NUHMC), Singapore, Singapore (E.C.Y.C.) phaccye@nus.edu.sg.ORCID 0000-0001-6107-9072
Agency for Science, Technology and Research · SG
Funding
Using Clinical Pharmacology Principles to Develop New Anticancer TherapiesZICSC006537 · NCI · DIVISION OF CLINICAL SCIENCES - NCI · PI FIGG, WILLIAM DOUGLAS · 2009 to 2025
$14.4MAbstract
Substantial evidence underscores the clinical efficacy of inhibiting CYP17A1-mediated androgen biosynthesis by abiraterone for treatment of prostate oncology. Previous structural analysis and in vitro assays revealed inconsistencies surrounding the nature and potency of CYP17A1 inhibition by abiraterone. Here, we establish that abiraterone is a slow-, tight-binding inhibitor of CYP17A1, with initial weak binding preceding the subsequent slow isomerization to a high-affinity CYP17A1-abiraterone complex. The in vitro inhibition constant of the final high-affinity CYP17A1-abiraterone complex (
Indexed as
AndrostenesCell Line, TumorDehydroepiandrosteroneEnzyme InhibitorsHumansKineticsMaleProstatic NeoplasmsSteroid 17-alpha-HydroxylaseSteroidsabirateroneAndrostenesCYP17A1 protein, humanDehydroepiandrosteroneEnzyme InhibitorsSteroid 17-alpha-HydroxylaseSteroids
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