Results 211 to 220 of about 19,533 (266)
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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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Recent Developments in Androgen Receptor Antagonists
Archiv der Pharmazie, 2015The androgen receptor (AR), a ligand‐dependent transcription factor that regulates the expression of a series of downstream target genes after the binding of androgens, has been a target for the discovery of drugs used to treat prostate cancer. Prostate cancer always progresses to castration‐resistant prostate cancer after a period of androgen ...
Fansheng, Ran +5 more
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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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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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Androgen Receptor Antagonists (Antiandrogens) Structure-Activity Relationships
Current Medicinal Chemistry, 2000Prostate cancer, acne, seborrhea, hirsutism, and androgenic alopecia are well recognized to depend upon an excess or increased sensitivity to androgens or to be at least sensitive to androgens. It thus seems logical to use antiandrogens as therapeutic agents to prevent androgens from binding to the androgen receptor.
S M, Singh, S, Gauthier, F, Labrie
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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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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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