Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor.

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Ishioka T, Tanatani A, Nagasawa K, Hashimoto Y

Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor.

Bioorg Med Chem Lett. 2003 Aug 18;13(16):2655-8.

PubMed ID

12873487 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Flutamide	Androgen receptor	Ki (nM)	1300	N/A	N/A	Details