NSAID gels and COX-2 selectivity in topical pain killers

Research from Bing Xu’s lab, published in November in Journal of the American Chemical Society, has recently been featured in C&E News. The Xu lab researchers, including Chemistry grad students Jiayang Li, Yi Kuang, Yuan Gao, Xuewen Du and Junfeng Shi, synthesized hydrogels by synthetically coupling small D-amino acid peptides to naproxen (a non-steroidal antiinflammatory drug – NSAID). This was done with the idea of forming gels that can be used for topical pain treatment.

Studies on the compounds formed showed that not only are gels formed, but the D-peptide conjugates of naproxen showed better selectivity towards COX-2 (the therapeutic target) compared to COX-1 (a source of side effects) than naproxen alone or an L-peptide conjugate. Clinical applications are still far away, but this finding opens exciting new avenues for research.

Li J, Kuang Y, Gao Y, Du X, Shi J, Xu B. d-Amino Acids Boost the Selectivity and Confer Supramolecular Hydrogels of a Nonsteroidal Anti-Inflammatory Drug (NSAID). J Am Chem Soc. 2012.