Design, synthesis, and activity of small molecule inhibitors of the TNFα/TNFR interaction

CHED 267

Jessica M. Davis, jmdavis@mail.fairfield.edu and Christopher Pace. Department of Chemistry, Fairfield University, 1073 North Benson Rd, Fairfield, CT 06824
The overexpression of the cytokine tumor necrosis factor-α (TNFα), has been linked to inflammation in Crohn's disease and has proven to be a viable therapeutic target. Our work focuses on the rational design and synthesis of small-molecule mimetics of the TNF receptor (TNFR). Using in silico modeling, we have designed a guanine-based scaffold that mimics the residues of TNFR involved in binding to TNFα. The synthesis and activity of these small molecule mimetics will be presented.