| Unexpected Binding Orientation of Bulky-B-Ring Anti-Androgens and Implications for Future Drug Targets. | |
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MedLine Citation:
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PMID: 21506597 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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Several new androgen receptor antagonists were synthesized and found to have varying activities across typically anti-androgen resistant mutants (Thr877→Ala and Trp741→Leu) and markedly improved potency over previously reported pan-antagonists. X-ray crystallography of a new anti-androgen in an androgen receptor mutant (Thr877→Ala) shows that the receptor can accommodate the added bulk presented by phenyl to naphthyl substitution, casting doubt on previous reports of predicted binding orientation and the causes of antagonism in bulky-B-ring antagonists. |
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Authors:
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Charles B Duke; Amanda Jones; Casey E Bohl; James T Dalton; Duane D Miller |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-4-20 |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: - ISSN: 1520-4804 ISO Abbreviation: - Publication Date: 2011 Apr |
Date Detail:
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Created Date: 2011-4-21 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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