2.50
Hdl Handle:
http://hdl.handle.net/10033/298252
Title:
Hits identified in library screening demonstrate selective CYP17A1 lyase inhibition.
Authors:
Krug, Sebastian J; Hu, Qingzhong; Hartmann, Rolf W
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.
Affiliation:
Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C2.3, 66123 Saarbrücken, Germany.
Citation:
Hits identified in library screening demonstrate selective CYP17A1 lyase inhibition. 2013, 134:75-9 J. Steroid Biochem. Mol. Biol.
Journal:
The Journal of steroid biochemistry and molecular biology
Issue Date:
Mar-2013
URI:
http://hdl.handle.net/10033/298252
DOI:
10.1016/j.jsbmb.2012.10.019
PubMed ID:
23142656
Type:
Article
Language:
en
ISSN:
1879-1220
Appears in Collections:
publications of the department drug design and optimization (HIPS]DDOP)

Full metadata record

DC FieldValue Language
dc.contributor.authorKrug, Sebastian Jen_GB
dc.contributor.authorHu, Qingzhongen_GB
dc.contributor.authorHartmann, Rolf Wen_GB
dc.date.accessioned2013-08-14T14:20:01Z-
dc.date.available2013-08-14T14:20:01Z-
dc.date.issued2013-03-
dc.identifier.citationHits identified in library screening demonstrate selective CYP17A1 lyase inhibition. 2013, 134:75-9 J. Steroid Biochem. Mol. Biol.en_GB
dc.identifier.issn1879-1220-
dc.identifier.pmid23142656-
dc.identifier.doi10.1016/j.jsbmb.2012.10.019-
dc.identifier.urihttp://hdl.handle.net/10033/298252-
dc.description.abstractA 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.en_GB
dc.language.isoenen
dc.rightsArchived with thanks to The Journal of steroid biochemistry and molecular biologyen_GB
dc.subject.meshEnzyme Inhibitorsen_GB
dc.subject.meshHumansen_GB
dc.subject.meshInhibitory Concentration 50en_GB
dc.subject.meshMaleen_GB
dc.subject.meshProstatic Neoplasmsen_GB
dc.subject.meshSmall Molecule Librariesen_GB
dc.subject.meshSteroid 17-alpha-Hydroxylaseen_GB
dc.titleHits identified in library screening demonstrate selective CYP17A1 lyase inhibition.en
dc.typeArticleen
dc.contributor.departmentPharmaceutical and Medicinal Chemistry, Saarland University, Campus C2.3, 66123 Saarbrücken, Germany.en_GB
dc.identifier.journalThe Journal of steroid biochemistry and molecular biologyen_GB
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