2. Academic Validation
  3. Benzoylbenzimidazole-based selective inhibitors targeting Cryptosporidium parvum and Toxoplasma gondii calcium-dependent protein kinase-1

Benzoylbenzimidazole-based selective inhibitors targeting Cryptosporidium parvum and Toxoplasma gondii calcium-dependent protein kinase-1

  • Bioorg Med Chem Lett. 2012 Aug 15;22(16):5264-7. doi: 10.1016/j.bmcl.2012.06.050.
Zhongsheng Zhang 1,  Kayode K Ojo,  Steven M Johnson,  Eric T Larson,  Penqing He,  Jennifer A Geiger,  Alejandro Castellanos-Gonzalez,  A Clinton White Jr,  Marilyn Parsons,  Ethan A Merritt,  Dustin J Maly,  Christophe L M J Verlinde,  Wesley C Van Voorhis,  Erkang Fan
Affiliations

Affiliation

  • 1 Department of Biochemistry, University of Washington, Seattle, WA 98195, USA.
PMID: 22795629 DOI: 10.1016/j.bmcl.2012.06.050
Abstract

Calcium-dependent protein kinase-1 (CDPK1) from Cryptosporidium parvum (CpCDPK1) and Toxoplasma gondii (TgCDPK1) have become attractive targets for discovering selective inhibitors to combat infections caused by these protozoa. We used structure-based design to improve a series of benzoylbenzimidazole-based compounds in terms of solubility, selectivity, and potency against CpCDPK1 and TgCDPK1. The best inhibitors show inhibitory potencies below 50 nM and selectivity well above 200-fold over two human kinases with small gatekeeper residues.

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