Ontology highlight
ABSTRACT:
SUBMITTER: Conner KP
PROVIDER: S-EPMC4437715 | biostudies-literature | 2015 Feb
REPOSITORIES: biostudies-literature
Conner Kip P KP Cruce Alex A AA Krzyaniak Matthew D MD Schimpf Alina M AM Frank Daniel J DJ Frank Daniel J DJ Ortiz de Montellano Paul P Atkins William M WM Bowman Michael K MK
Biochemistry 20150129 5
Azoles and pyridines are commonly incorporated into small molecule inhibitor scaffolds that target cytochromes P450 (CYPs) as a strategy to increase drug binding affinity, impart isoform-dependent selectivity, and improve metabolic stability. Optical absorbance spectra of the CYP-inhibitor complex are widely used to infer whether these inhibitors are ligated directly to the heme iron as catalytically inert, low-spin (type II) complexes. Here, we show that the low-spin complex between a drug-meta ...[more]