Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor.
Anti-androgens were designed based on the principle of inhibiting the folding of helix 12 of the nuclear androgen receptor. The prepared anti-androgens exhibited full antagonistic activity toward human prostate tumor LNCaP cells with T877A point-mutated nuclear androgen receptor, as far as examined, towards which other known anti-androgens, including hydroxyflutamide, are inactive or act as androgen agonists.
Ishioka
Toshiyasu
T
Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
Tanatani
Aya
A
Nagasawa
Kazuo
K
Hashimoto
Yuichi
Y
D000726:Androgen Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D001667:Binding, Competitive; D015195:Drug Design; D006801:Humans; D007555:Isoxazoles / Q000138:chemical synthesis / Q000494:pharmacology; D008297:Male; D015394:Molecular Structure; D017354:Point Mutation; D017430:Prostate-Specific Antigen / Q000032:analysis; D017510:Protein Folding; D011944:Receptors, Androgen / Q000096:biosynthesis / Q000187:drug effects* / Q000235:genetics; D013739:Testosterone; D014407:Tumor Cells, Cultured
D000726:Androgen Antagonists; D007555:Isoxazoles; D011944:Receptors, Androgen; D013739:Testosterone; D017430:Prostate-Specific Antigen