Hits identified in library screening demonstrate selective CYP17A1 lyase inhibition.

Krug, Sebastian J; Hu, Qingzhong; Hartmann, Rolf W

dc.contributor.author	Krug, Sebastian J
dc.contributor.author	Hu, Qingzhong
dc.contributor.author	Hartmann, Rolf W
dc.date.accessioned	2013-08-14T14:20:01Z
dc.date.available	2013-08-14T14:20:01Z
dc.date.issued	2013-03
dc.identifier.citation	Hits identified in library screening demonstrate selective CYP17A1 lyase inhibition. 2013, 134:75-9 J. Steroid Biochem. Mol. Biol.	en_GB
dc.identifier.issn	1879-1220
dc.identifier.pmid	23142656
dc.identifier.doi	10.1016/j.jsbmb.2012.10.019
dc.identifier.uri	http://hdl.handle.net/10033/298252
dc.description.abstract	A 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.
dc.language.iso	en	en
dc.rights	Archived with thanks to The Journal of steroid biochemistry and molecular biology	en_GB
dc.subject.mesh	Enzyme Inhibitors	en_GB
dc.subject.mesh	Humans	en_GB
dc.subject.mesh	Inhibitory Concentration 50	en_GB
dc.subject.mesh	Male	en_GB
dc.subject.mesh	Prostatic Neoplasms	en_GB
dc.subject.mesh	Small Molecule Libraries	en_GB
dc.subject.mesh	Steroid 17-alpha-Hydroxylase	en_GB
dc.title	Hits identified in library screening demonstrate selective CYP17A1 lyase inhibition.	en
dc.type	Article	en
dc.contributor.department	Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C2.3, 66123 Saarbrücken, Germany.	en_GB
dc.identifier.journal	The Journal of steroid biochemistry and molecular biology	en_GB
refterms.dateFOA	2018-06-12T23:39:19Z
html.description.abstract	A 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.