Description of Invention: The inventions described herein are antimalarial small molecule inhibitors of the plasmodial surface anion channel (PSAC), an essential nutrient acquisition ion channel expressed on human erythrocytes infected with malaria parasites. These inhibitors were discovered by high-throughput screening of chemical libraries and analysis of their ability to kill malaria parasites in culture. Two separate classes of inhibitors were found to work synergistically in combination against PSAC and killed malaria cultures at markedly lower concentrations than separately. These inhibitors have high affinity and specificity for PSAC and have acceptable cytotoxicity profiles. Preliminary in vivo testing of these compounds in a mouse malaria model is currently ongoing.
Applications: Treatment of malarial infections
Novel drug treatment for malarial infections
Synergistic effect of these compounds on PSAC
Development Status: In vitro and in vivo data can be provided upon request.
M Kang, G Lisk, S Hollingworth, SM Baylor, SA Desai. Malaria parasites are rapidly killed by dantrolene derivatives specific for the plasmodial surface anion channel. Mol. Pharmacol. 2005 Jul;68(1):34-40. [ PubMed abs ]
SA Desai, SM Bezrukov, J Zimmerberg. A voltage-dependent channel involved in nutrient uptake by red blood cells infected with the malaria parasite. Nature. 2000 Aug 31;406(6799):1001-1005. [ PubMed abs ]
Licensing Status: Available for licensing.
Collaborative Research Opportunity: The NIAID Office of Technology Development is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize antimalarial drugs that target PSAC or other parasite-specific transporters. Please contact Dana Hsu at 301-496-2644 for more information.
Portfolios: Infectious Diseases Infectious Diseases - Therapeutics In-vivo Data In-vitro Data
For Additional Information Please Contact: Kevin Chang Ph.D. NIH Office of Technology Transfer 6011 Executive Blvd. Suite 325, Rockville, MD 20852 United States Email: firstname.lastname@example.org Phone: 301-435-5018 Fax: 301-402-0220