Prof. Kay Ahn, Janssen Research and Development

Enzymology continues to play a pivotal role in drug discovery.  I will discuss the drug discovery projects below where development of a detailed understanding of the mechanism of enzyme inhibition was critical in driving the structure-activity relationship data, determining target engagement, understanding pharmacokinetic-pharmacodynamic relationships, and selecting clinical candidates.  I will also present an example showing how developing the “right” assay was essential to intelligently determine the fate of the project.

1. Fatty acid amide hydrolase (FAAH) inhibitor  

2. Sirt1 activator 

3. Diacylglycerol acyltransferase 2 inhibitor