Event
Chemical Society Seminar: Dr. Xianshu Yang - Directly identifying novel lead compounds from chemical mixtures using an affinity selection mass spectrometry platform
Thursday, March 23, 2017 13:00to14:15
Maass Chemistry Building
Room 10, 801 rue Sherbrooke Ouest, Montreal, QC, H3A 0B8, CA
High throughput screening of large libraries of complex molecules is the most common starting point of drug discovery. The identified small molecule “hits” are then further investigated with the targets of interest using various techniques, including binding affinity and in vitro biological activity. In this presentation, we will discuss a novel platform-ALIS*, an Affinity Selection–Mass Spectrometry (AS-MS) platform for the discovery and characterization of protein–ligand interactions. ALIS takes advantage of the high sensitivity and selectivity inherent to MS, directly identifying compounds interacting with a target protein from chemical mixtures, such as combinatorial libraries, natural product extracts, and lead/drug metabolite mixture etc. ALIS affinity ranking techniques identify higher affinity compounds in the mixture and minimize the need for synthesis and purification resources for the most interesting ligands. ALIS platform has delivered thousands of novel hits for corporate projects at Merck, Schering-Plough, Pfizer, Aventis and other major pharmaceutical industries, and several of these programs were advanced to clinical trials.
Recent publications: 1) J. Med. Chem. 2016, 59, 1818 and 2017, 60, 1-3. 2) PNAS 2017, 114 (3), E297