NCIt definition : An orally bioavailable androgen receptor (AR) antagonist, with potential antineoplastic
activity. Upon oral administration, AR antagonist TRC253 specifically binds to both
wild-type and certain mutant forms of AR, thereby preventing androgen-induced receptor
activation and facilitating the formation of inactive complexes that cannot translocate
to the nucleus. This prevents binding to and transcription of AR-responsive genes,
inhibits the expression of genes that regulate prostate cancer cell proliferation,
and may lead to an inhibition of growth of tumor cells in which AR is overexpressed
and/or mutated. AR is often overexpressed and/or mutated in prostate cancers and plays
a key role in proliferation, survival and chemoresistance of tumor cells.;
UNII : GNG9GQ9Y27;
Molecule name : TRC 253; TRC-253; JNJ 63576253; JNJ-63576253;