Event Information

Erin Hopper (Duke University)
High Throughput Screening Applications of SUPREX
Abstract:
The identification of novel ligands that bind disease-related proteins has far-reaching applications in both diagnostics and therapeutics. The number of compounds that can be synthesized or purified from natural sources, however, far exceeds our current ability to rigorously test them one by one. The discovery of new ligands for a protein relies on the ability to rapidly screen large libraries of compounds using high-throughput techniques. Current high throughput screening assays for protein-ligand binding have been relatively successful, but most have significant drawbacks, such as requirements for separation, compound labeling, and development of a new assay for every protein system. Current assays are also difficult or impossible to multiplex. Recently, a new mass spectrometry-based screening technique was reported in which separation, labeling, and new assay development are not required. This technique relies on the ability of SUPREX to rapidly detect thermodynamic changes upon ligand binding. In this study, we demonstrate the feasibility of this technique for the screening of an 880-member compound library. Using a series of three screenings, we were able to identify three ligands for the protein target Cyclophilin A with a screening rate of 3 min/ligand.

Preliminary Examination

Thursday, April 6, 2006, 10:30am
Student Exams Seminar