Mechanistic Enzymology Short Course

Special

Enzymology provides a vital link between chemistry and biology and understanding the role of enzymes and how to modulate their activity remains a key focus for drug discovery. Fortunately, the language used to describe enzyme reactions is the chemical language of thermodynamics and kinetics, which facilitates the chemist’s ability to become fluent and so enriches the opportunity to design effective new medicines.

This short course will provide a brief introduction to the kinetics and thermodynamics of ligand binding, an overview of different enzyme inhibition mechanisms, as well as an illustration of the analysis of time-dependent inhibition.

Exploiting the information gained from such detailed mechanistic studies on enzymes with and without inhibitors allows the identification and evaluation of diverse compounds with favourable physicochemical properties, facilitates an understanding of detailed structure-activity relationships and provides the knowledge required to optimise leads towards differentiated candidate drugs.

This course is provided by AZ Discovery Sciences.

To start at 11.30am to allow a general introduction to ligand binding and enzyme catalysis, followed by a networking lunch.

The core afternoon sessions will start at 1.30pm and comprise around 3 hours to cover inhibition mechanisms and time-dependency, together with some real-life worked examples.

One half day session