Sebastian J Krug, Qingzhong Hu, Rolf W Hartmann
Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C2.3, 66123 Saarbrücken, Germany.
The Journal of steroid biochemistry and molecular biology 2013 MarA screening of structurally different steroid hormone synthesis inhibitors was performed in order to find a starting point for the development of a new inhibitor of the bifunctional steroidogenic enzyme CYP17A1. Emphasis was placed on determination of selectivity between the two catalytic steps, namely 17α-hydroxylase and C(17,20)-lyase. For that purpose a new inhibition assay has been developed. Hits identified within this novel assay demonstrated selective inhibition of CYP17A1 lyase activity, and thus mark the basis for the development of selective C(17,20)-lyase inhibitors for the treatment of prostate cancer. Copyright © 2012 Elsevier Ltd. All rights reserved.
Sebastian J Krug, Qingzhong Hu, Rolf W Hartmann. Hits identified in library screening demonstrate selective CYP17A1 lyase inhibition. The Journal of steroid biochemistry and molecular biology. 2013 Mar;134:75-9
PMID: 23142656
View Full Text