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, 2007 Androgens are essential for the development and maintenance of male sexual characteristics. They exert their effects through the androgen receptor, which is a member of the …
Marshall, K.; id_orcid
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Androgen antagonists in androgen target tissues
Pharmacology & Therapeutics, 1984Most antiandrogens appear to act by binding to the androgen receptor and competitively inhibiting the binding of testosterone and cihydrotestosterone to the receptor. Focusing on those compounds which appear to inhibit androgen receptor mediated responses this review discusses the chemistry of those antiandrogens which have been studied to the extent ...
D J, Tindall +3 more
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Bioorganic and Medicinal Chemistry Letters, 2007 The synthesis and in vivo SAR of N-benzyl, N-aceto, and N-ethylene ether derivatives of 2-(2,2,2-trifluoroethyl)-5,6-dichloro-benzimidazole as novel androgen receptor antagonists are described.
Tifanie Sbriscia +2 more
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Classification and Virtual Screening of Androgen Receptor Antagonists
Journal of Chemical Information and Modeling, 2010Computational tools, such as quantitative structure-activity relationship (QSAR), are highly useful as screening support for prioritization of substances of very high concern (SVHC). From the practical point of view, QSAR models should be effective to pick out more active rather than inactive compounds, expressed as sensitivity in classification works.
Jiazhong Li, Paola Gramatica
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Peptide Antagonist of the Androgen Receptor
Current Pharmaceutical Design, 2010Androgen receptor (AR) is a steroid hormone receptor that is activated by endogenous androgens, mainly testosterone and 5alpha-dihydrotestosterone (5alpha-DHT). AR is also an important drug target, and AR antagonists (antiandrogens) have been widely used for prostate cancer therapy.
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2010
Androgen receptor (AR) antagonists used clinically include steroidal (cyproterone acetate) and nonsteroidal antagonists (bicalutamide, flutamide, and nilutamide), with the latter nonsteroidal compounds being the only ones in general use in the United States. AR antagonists are used as single agents or in conjunction with surgical or medical castration (
Howard C. Shen +2 more
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Androgen receptor (AR) antagonists used clinically include steroidal (cyproterone acetate) and nonsteroidal antagonists (bicalutamide, flutamide, and nilutamide), with the latter nonsteroidal compounds being the only ones in general use in the United States. AR antagonists are used as single agents or in conjunction with surgical or medical castration (
Howard C. Shen +2 more
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Androgens and acne: perspectives on clascoterone, the first topical androgen receptor antagonist
Expert Opinion on Pharmacotherapy, 2021Introduction: Increased circulating androgens are key to the multifactorial pathogenesis of acne. Clascoterone is the first topical androgen antagonist developed to treat acne in both male and female patients and the first such agent to receive U.S. Food and Drug Administration (FDA) approval for treatment of acne.
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Advances in the computational development of androgen receptor antagonists
Drug Discovery Today, 2020The androgen receptor is a ligand-dependent transcriptional factor and an essential therapeutic target for prostate cancer. Competitive binding of antagonists to the androgen receptor can alleviate aberrant activation of the androgen receptor in prostate cancer.
Xueping Hu +7 more
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Antagonistic effect of androgen on prostatic cell death
The Prostate, 1984AbstractAndrogen, besides having the well‐established agonistic ability to stimulate prostate cell proliferation, also has an antagonistic ability to inhibit prostatic cell death. This statement is based upon the observations that 1) only 2.1% of the total prostatic cells die per day when serum testosterone level is sufficient for chronic maintenance ...
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Recent Androgen Receptor Antagonists in Prostate Cancer
Mini-Reviews in Medicinal Chemistry, 2014Androgen receptor has been shown to promote prostate cell growth and carcinogenesis of prostate cancer by up-regulating its target genes. Testosterone and dihydrotestosterone are two major hormones which bind to and activate androgen receptor. Targeting both the androgen receptor and the enzymes catalyzing the biosynthesis of testosterone and ...
Xufang, Lu +5 more
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