Kinetic binding assays for the analysis of protein –ligand interactions

Publication date: October 2015 Source:Drug Discovery Today: Technologies, Volume 17 Author(s): Franz-Josef Meyer-Almes The importance of binding kinetics in terms of residence time and on-rate in drug discovery has been broadly accepted in the past few years. Furthermore, evidence has accumulated that the optimal binding mechanism of a drug to its target molecule is related to physiological efficacy as well as selectivity and thus drug safety. Homogeneous fluorescence-based binding assays have been shown to enable high throughput kinetics requiring only small amounts of protein and can be developed to elucidate even complex mechanisms of molecular recognition. A generalized approach is proposed that combines high quality kinetic and equilibrium data in an Integrated Global Fit analysis yielding the most probable binding mechanism. Graphical abstract
Source: Drug Discovery Today: Technologies - Category: Drugs & Pharmacology Source Type: research