[HTML][HTML] Crystal structure of the T877A human androgen receptor ligand-binding domain complexed to cyproterone acetate provides insight for ligand-induced …
Cyproterone acetate (CPA) is a steroidal antiandrogen used clinically in the treatment of
prostate cancer. Compared with steroidal agonists for the androgen receptor (AR)(eg
dihydrotestosterone, R1881), CPA is bulkier in structure and therefore seemingly
incompatible with the binding pockets observed in currently available x-ray crystal structures
of the AR ligand-binding domain (LBD). We solved the x-ray crystal structure of the human
AR LBD bound to CPA at 1.8 Å in the T877A variant, a mutation known to increase the …
prostate cancer. Compared with steroidal agonists for the androgen receptor (AR)(eg
dihydrotestosterone, R1881), CPA is bulkier in structure and therefore seemingly
incompatible with the binding pockets observed in currently available x-ray crystal structures
of the AR ligand-binding domain (LBD). We solved the x-ray crystal structure of the human
AR LBD bound to CPA at 1.8 Å in the T877A variant, a mutation known to increase the …