These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Unexpected binding orientation of bulky-B-ring anti-androgens and implications for future drug targets.
    Author: Duke CB, Jones A, Bohl CE, Dalton JT, Miller DD.
    Journal: J Med Chem; 2011 Jun 09; 54(11):3973-6. PubMed ID: 21506597.
    Abstract:
    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.
    [Abstract] [Full Text] [Related] [New Search]