Premium
Back Cover: Discovery and Biophysical Evaluation of First Low Nanomolar Hits Targeting CYP125 of M. tuberculosis (ChemMedChem 21/2016)
Author(s) -
Brengel Christian,
Thomann Andreas,
Schifrin Alexander,
Eberhard Jens,
Hartmann Rolf W.
Publication year - 2016
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201600532
Subject(s) - mycobacterium tuberculosis , surface plasmon resonance , drug discovery , cover (algebra) , chemistry , computational biology , biochemistry , tuberculosis , combinatorial chemistry , nanotechnology , biology , medicine , materials science , nanoparticle , mechanical engineering , pathology , engineering
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. on page 2385 in Issue 21, 2016 (DOI: 10.1002/cmdc.201600361).