Hits identified in library screening demonstrate selective CYP17A1 lyase inhibition.
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. |