Sintokamides A to E, chlorinated peptides from the sponge Dysidea sp. that inhibit transactivation of the N-terminus of the androgen receptor in prostate cancer cells.
Castration recurrent prostate cancer is suggested to result from transactivation of the amino-terminus domain of the androgen receptor. Current therapies available target the C-terminus, ligand-binding domain of the androgen receptor and tend to fail presumably due to mutations such that these same antagonists become agonists. Here we identify sintokamides, never before described, that are the first small molecules known to selectively block transactivation of the N-terminus of the androgen receptor for potential development of a novel class of antagonists to the androgen receptor.
Full citation
Sadar MD, Williams DE, Mawji NR, Patrick BO, Wikanta T, Chasanah E, Irianto HE, Soest RV, Andersen RJ. 2008 Sintokamides A to E, chlorinated peptides from the sponge Dysidea sp. that inhibit transactivation of the N-terminus of the androgen receptor in prostate cancer cells. Org. Lett. 10(21):4947-4950. [Epub 2008 Oct 4.] PMID: 18834139 DOI: 10.1021/ol802021w
Further details of this publication can be found online at: