Description:
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