Cor A. Berrevoets

TL;DR: In the LNCaP androgen receptor a single point mutation is discovered changing the sense of codon 868 (Thr to Ala) in the ligand binding domain, which influences both binding and the induction of gene expression by different steroids and antisteroids.

TL;DR: The mutated androgen receptor of LNCaP cells is a useful tool in the elucidation of different levels of action of steroids and antisteroids and the mutation directly affects both binding specificity and the induction of gene expression.

TL;DR: Recent evidence strongly supports a ligand dependent functional interaction between the ligand-binding domain and the NH2-terminal transactivating domain of the androgen receptor.

TL;DR: The present studies indicate that not all anti-androgens showed agonistic effects with the mutated receptor, and could not induce a release of heat-shock proteins and did not increase nuclear binding, but inhibited the transformation process induced by R1881.

TL;DR: A concept of hormone-dependent AR activation is proposed, which requires a functional, direct or indirect intramolecular interaction between the TAD and the LBD.