C3aR Antagonists

Princeton University Invention # 10-2571

Using a novel computation framework, researchers at Princeton University and the University of California, Riverside, have identified potent antagonists of the C3a receptor (C3aR). Inhibition of binding of C3a to C3aR is an excellent target for drug design against autoimmune and inflammatory diseases involving under-regulated complement system activation. These peptides have been tested experimentally using Chem-1 C3aR stable cells and calcium mobilization assays. The most potent peptide showed reduction of C3a full response to 5% at 0.1mM concentration and possesses an IC₅₀    of 21mM.

In addition to offering potential peptides for therapeutic use, this computational framework is a promising addition to drug discovery computational methods as it allows for combinatorial screening of numerous compounds prior to selection for experimental testing. Additionally  the computations framework can be used to identify new sequence templates which can be subsequently used in experimental combinatorial design, such as with phage-display random peptide screening libraries to reduce the combinatorial challenge.

Princeton is currently seeking commercial partners for the further development and commercialization of this opportunity. Patent protection is pending.

 For more information on Princeton University invention # 10-2571 please contact:

                        Laurie Tzodikov

                        Office of Technology Licensing and Intellectual Property

                        Princeton University

                        4 New South Building

                        Princeton, NJ 08544-0036

                        (609) 258-7256

                        tzodikov@princeton.edu