Journal
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 135, Issue 2, Pages 542-545Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ja310019x
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Funding
- Human Frontier Program (HFSP) [RGP 0056/2008]
- Brandeis University
- NIH [R01CA142746, P01 GM-62580]
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As systemically used therapeutics for treating acute or chronic pains or inflammations, nonsteroidal anti-inflammatory drugs (NSAIDs) also associate with the adverse gastrointestinal and renal effects and cardiovascular risks. Thus, it is beneficial to develop topical gels that selectively inhibit cyclooxygenase-2 (COX-2) for the management of local inflammation. In this work, we demonstrate that the covalent conjugation of D-amino acids to naproxen (i.e., a NSAID) not only affords supramolecular hydrogelators for the topical gels but also unexpectedly and significantly elevates the selectivity toward COX-2 about 20X at little expense of the activity of naproxen. This work illustrates a previously unexplored approach that employs D-amino acids for the development of functional molecules that have dual or multiple roles and exceptional biostability, which offers a new class of molecular hydrogels of therapeutic agents.
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