The Sound of Evolution
Bicalutamide
Mechanism of action:
Bicalutamide is a non-steroidal anti-androgen. Under normal conditions, testosterone and its metabolite dihydrotestosterone (DHT) bind to the androgen receptor, forming a complex that enters the nucleus and activates androgen-responsive genes, thereby promoting the proliferation and survival of prostate cells. Bicalutamide competitively antagonizes the androgen receptor, preventing formation of this complex and its entry into the nucleus, leading to reduced transcriptional activity of androgen-responsive genes, suppression of proliferation-related signaling, and effects on pathways related to cell survival and apoptosis.
Reference(s):
1. Wang LG et al. (1998). Androgen antagonistic effect of estramustine phosphate (EMP) metabolites on wild-type and mutated androgen receptor. Biochem Pharmacol.
2. Chang HC et al. (1999). Suppression of Delta(5)-androstenediol-induced androgen receptor transactivation by selective steroids in human prostate cancer cells. Proc Natl Acad Sci USA.