| Literature DB >> 22320388 |
Steven M Johnson1, Ryan C Murphy, Jennifer A Geiger, Amy E DeRocher, Zhongsheng Zhang, Kayode K Ojo, Eric T Larson, B Gayani K Perera, Edward J Dale, Panqing He, Molly C Reid, Anna M W Fox, Natascha R Mueller, Ethan A Merritt, Erkang Fan, Marilyn Parsons, Wesley C Van Voorhis, Dustin J Maly.
Abstract
Toxoplasmosis is a disease of prominent health concern that is caused by the protozoan parasite Toxoplasma gondii. Proliferation of T. gondii is dependent on its ability to invade host cells, which is mediated in part by calcium-dependent protein kinase 1 (CDPK1). We have developed ATP competitive inhibitors of TgCDPK1 that block invasion of parasites into host cells, preventing their proliferation. The presence of a unique glycine gatekeeper residue in TgCDPK1 permits selective inhibition of the parasite enzyme over human kinases. These potent TgCDPK1 inhibitors do not inhibit the growth of human cell lines and represent promising candidates as toxoplasmosis therapeutics.Entities:
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Year: 2012 PMID： 22320388 PMCID： PMC3306180 DOI： 10.1021/jm201713h
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446