对具有突变雄激素受体的人前列腺肿瘤LNCaP细胞具有完全拮抗活性的抗雄激素药物。
Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor.
作者信息
Ishioka Toshiyasu, Tanatani Aya, Nagasawa Kazuo, Hashimoto Yuichi
机构信息
Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
出版信息
Bioorg Med Chem Lett. 2003 Aug 18;13(16):2655-8. doi: 10.1016/s0960-894x(03)00575-4.
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.
抗雄激素药物是基于抑制核雄激素受体螺旋12折叠的原理设计的。所制备的抗雄激素药物对具有T877A点突变核雄激素受体的人前列腺肿瘤LNCaP细胞表现出完全的拮抗活性，就目前所检测的情况而言，其他已知的抗雄激素药物，包括羟基氟他胺，对该细胞无活性或起雄激素激动剂的作用。
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