Ontology highlight
ABSTRACT:
SUBMITTER: Yu W
PROVIDER: S-EPMC4454744 | biostudies-literature | 2015 Apr
REPOSITORIES: biostudies-literature
Yu Weixuan W Neckles Carla C Chang Andrew A Bommineni Gopal Reddy GR Spagnuolo Lauren L Zhang Zhuo Z Liu Nina N Lai Christina C Truglio James J Tonge Peter J PJ
Analytical biochemistry 20150214
The classical methods for quantifying drug-target residence time (tR) use loss or regain of enzyme activity in progress curve kinetic assays. However, such methods become imprecise at very long residence times, mitigating the use of alternative strategies. Using the NAD(P)H-dependent FabI enoyl-acyl carrier protein (enoyl-ACP) reductase as a model system, we developed a Penefsky column-based method for direct measurement of tR, where the off-rate of the drug was determined with radiolabeled [ade ...[more]