Back Cover: Discovery and Biophysical Evaluation of First Low Nanomolar Hits Targeting CYP125 of M. tuberculosis (ChemMedChem 21/2016). (7th November 2016)

• Record Type: Journal Article
• Authors: Brengel, Christian; Thomann, Andreas; Schifrin, Alexander; Eberhard, Jens; Hartmann, Rolf W.
• Is Part Of: ChemMedChem. Volume 11:Number 21(2016)
• Page Start: 2466
• Page End: 2466
• Publication Date: 2016-11-07
• Subjects: anti-infectives -- biophysics -- inhibitors -- Mycobacterium tuberculosis -- screening; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201600532
• Languages: English
• ISSNs: 1860-7179

Abstract

Abstract : The back cover picture shows the applied screening strategy for the discovery of high affinity hits targeting CYP125, which is a P450 enzyme in Mycobacterium tuberculosis (Mtb). CYP125 plays an important role in cholesterol metabolism of Mtb and could therefore represent a promising novel target for the treatment of Mtb infections. The combined screening approach of surface plasmon resonance spectroscopy (SPR) and a heme coordination assay for a focused P450‐inhibitor library led to the identification of the first nanomolar hit targeting CYP125. More information can be found in the the Full Paper by Christian Brengel, Andreas Thomann, Rolf W. Hartmann et al. onpage 2385 in Issue 21, 2016 (DOI:10.1002/cmdc.201600361 ).