The Role of Target Binding Kinetics in Drug Discovery
Dong Ming Guo, Laura H. Heitman, Adriaan P. IJzerman
Abstract
Dong Ming Guo, Laura H. Heitman, Adriaan P. IJzerman
Abstract
Traditionally structure-activity/affinity relationships (SAR) have dominated research in medicinal chemistry. However, structure-kinetics relationships (SKR) can be very informative too. In this viewpoint we explore the molecular determinants of binding kinetics and discuss challenges for future binding kinetics studies. A scheme for future kinetics-directed drug design and discovery is also proposed.
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Traditionally structure-activity/affinity relationships (SAR) have dominated research in medicinal chemistry. However, structure-kinetics relationships (SKR) can be very informative too. In this viewpoint we explore the molecular determinants of binding kinetics and discuss challenges for future binding kinetics studies. A scheme for future kinetics-directed drug design and discovery is also proposed.
Key concepts: Kinetics, Receptor–ligand kinetics, Drug discovery, Computational biology, Chemistry, Enzyme kinetics, Drug, Biophysics