@article {9848, title = {Regression of castrate-recurrent prostate cancer by a small-molecule inhibitor of the amino-terminus domain of the androgen receptor}, journal = {Cancer cell}, volume = {17}, year = {2010}, note = {MEDLINE AN 2010506539(Journal; Article; (JOURNAL ARTICLE); (RESEARCH SUPPORT, NON-U.S. GOV{\textquoteright}T); (RESEARCH SUPPORT, U.S. GOV{\textquoteright}T, NON-P.H.S.))}, month = {2010///}, pages = {535 - 46}, abstract = {Castration-recurrent prostate cancer (CRPC) is suspected to depend on androgen receptor (AR). The AF-1 region in the amino-terminal domain (NTD) of AR contains most, if not all, of the transcriptional activity. Here we identify EPI-001, a small molecule that blocked transactivation of the NTD and was specific for inhibition of AR without attenuating transcriptional activities of related steroid receptors. EPI-001 interacted with the AF-1 region, inhibited protein-protein interactions with AR, and reduced AR interaction with androgen-response elements on target genes. Importantly, EPI-001 blocked androgen-induced proliferation and caused cytoreduction of CRPC in xenografts dependent on AR for growth and survival without causing toxicity.[on SciFinder (R)]}, isbn = {1878-3686}, author = {Andersen, R. J. and Mawji,Nasrin R. and Wang,Jun and Wang,Gang and Haile,Simon and Myung,Jae-Kyung and Watt,Kate and Tam,Teresa and Yang,Yu Chi and Banuelos,Carmen A. and Williams,David E. and McEwan,Iain J. and Wang,Yuzhou and Sadar,Marianne D.} }