Results 221 to 230 of about 20,010 (263)
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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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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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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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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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Steroid derivatives as pure antagonists of the androgen receptor
The Journal of Steroid Biochemistry and Molecular Biology, 2012While the androgens of testicular origin (representing about 50% of total androgens in men over 50 years) can be completely eliminated by surgical or medical castration with GnRH (gonadotropin-releasing hormone) agonists or antagonists, the antiandrogens currently available as blockers of androgen binding to the androgen receptor (AR), namely ...
Sylvain, Gauthier +2 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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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 …
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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 …
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Flutamide as an Androgen Antagonist on Epididymal Function in the Rat*
Andrologia, 2009The purpose of this study was to investigate whether flutamide (alpha-alpha-alpha--Trifluro-2-methyl-4'-nitro-m-propionatoluidide), a nonsteroidal compound acts as an androgen antagonist at the level of the epididymis. For comparison, cyproterone acetate was also evaluated under identical experimental conditions. The levels of glycerylphosphorylcholine
J D, Dhar, S R, Srivastava, B S, Setty
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A Chemoenzymatic Synthesis of an Androgen Receptor Antagonist
Organic Process Research & Development, 2007A new scalable enzymatic resolution approach to both enantiomers of trans-2-hydroxycyclohexanecarbonitrile (9 and 11) was developed. Treatment of the racemic mixture (4) with succinic anhydride in the presence of Novozym 435 led to selective acylation of one enantiomer to the corresponding hemisuccinate, which was separated from the unreacted ...
Rajappa Vaidyanathan +2 more
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Assays to Measure Estrogen and Androgen Agonists and Antagonists
1998Substantial evidence has surfaced on the hormone-like effects of many xenobiotics in fish, wildlife and humans (Colborn et al., 1993). The endocrine and reproductive effects of xenobiotics are believed to be due to their 1) mimicking the effects of endogenous hormones such as estrogens and androgens, 2) antagonizing the effects of normal, endogenous ...
A M, Soto +6 more
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