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Development of Toxoplasma gondii calcium-dependent protein kinase 1 (TgCDPK1) inhibitors with potent anti-toxoplasma activity. 2012
Steven M Johnson, and
Ryan C Murphy, and
Jennifer A Geiger, and
Amy E DeRocher, and
Zhongsheng Zhang, and
Kayode K Ojo, and
Eric T Larson, and
B Gayani K Perera, and
Edward J Dale, and
Panqing He, and
Molly C Reid, and
Anna M W Fox, and
Natascha R Mueller, and
Ethan A Merritt, and
Erkang Fan, and
Marilyn Parsons, and
Wesley C Van Voorhis, and
Dustin J Maly
Department of Chemistry, University of Washington, Seattle, Washington, USA.
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.
Related Publications
Steven M Johnson, and
Ryan C Murphy, and
Jennifer A Geiger, and
Amy E DeRocher, and
Zhongsheng Zhang, and
Kayode K Ojo, and
Eric T Larson, and
B Gayani K Perera, and
Edward J Dale, and
Panqing He, and
Molly C Reid, and
Anna M W Fox, and
Natascha R Mueller, and
Ethan A Merritt, and
Erkang Fan, and
Marilyn Parsons, and
Wesley C Van Voorhis, and
Dustin J Maly
May 2010,
Nature structural & molecular biology,
Steven M Johnson, and
Ryan C Murphy, and
Jennifer A Geiger, and
Amy E DeRocher, and
Zhongsheng Zhang, and
Kayode K Ojo, and
Eric T Larson, and
B Gayani K Perera, and
Edward J Dale, and
Panqing He, and
Molly C Reid, and
Anna M W Fox, and
Natascha R Mueller, and
Ethan A Merritt, and
Erkang Fan, and
Marilyn Parsons, and
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Dustin J Maly
November 2015,
European journal of medicinal chemistry,
Steven M Johnson, and
Ryan C Murphy, and
Jennifer A Geiger, and
Amy E DeRocher, and
Zhongsheng Zhang, and
Kayode K Ojo, and
Eric T Larson, and
B Gayani K Perera, and
Edward J Dale, and
Panqing He, and
Molly C Reid, and
Anna M W Fox, and
Natascha R Mueller, and
Ethan A Merritt, and
Erkang Fan, and
Marilyn Parsons, and
Wesley C Van Voorhis, and
Dustin J Maly
September 2014,
BMC infectious diseases,
Steven M Johnson, and
Ryan C Murphy, and
Jennifer A Geiger, and
Amy E DeRocher, and
Zhongsheng Zhang, and
Kayode K Ojo, and
Eric T Larson, and
B Gayani K Perera, and
Edward J Dale, and
Panqing He, and
Molly C Reid, and
Anna M W Fox, and
Natascha R Mueller, and
Ethan A Merritt, and
Erkang Fan, and
Marilyn Parsons, and
Wesley C Van Voorhis, and
Dustin J Maly
August 2012,
Bioorganic & medicinal chemistry letters,
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Ryan C Murphy, and
Jennifer A Geiger, and
Amy E DeRocher, and
Zhongsheng Zhang, and
Kayode K Ojo, and
Eric T Larson, and
B Gayani K Perera, and
Edward J Dale, and
Panqing He, and
Molly C Reid, and
Anna M W Fox, and
Natascha R Mueller, and
Ethan A Merritt, and
Erkang Fan, and
Marilyn Parsons, and
Wesley C Van Voorhis, and
Dustin J Maly
June 2007,
Parasite (Paris, France),
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Jennifer A Geiger, and
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Edward J Dale, and
Panqing He, and
Molly C Reid, and
Anna M W Fox, and
Natascha R Mueller, and
Ethan A Merritt, and
Erkang Fan, and
Marilyn Parsons, and
Wesley C Van Voorhis, and
Dustin J Maly
April 2013,
Journal of medicinal chemistry,
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Jennifer A Geiger, and
Amy E DeRocher, and
Zhongsheng Zhang, and
Kayode K Ojo, and
Eric T Larson, and
B Gayani K Perera, and
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Panqing He, and
Molly C Reid, and
Anna M W Fox, and
Natascha R Mueller, and
Ethan A Merritt, and
Erkang Fan, and
Marilyn Parsons, and
Wesley C Van Voorhis, and
Dustin J Maly
July 2016,
Parasites & vectors,
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Ryan C Murphy, and
Jennifer A Geiger, and
Amy E DeRocher, and
Zhongsheng Zhang, and
Kayode K Ojo, and
Eric T Larson, and
B Gayani K Perera, and
Edward J Dale, and
Panqing He, and
Molly C Reid, and
Anna M W Fox, and
Natascha R Mueller, and
Ethan A Merritt, and
Erkang Fan, and
Marilyn Parsons, and
Wesley C Van Voorhis, and
Dustin J Maly
July 2016,
Journal of medicinal chemistry,
Steven M Johnson, and
Ryan C Murphy, and
Jennifer A Geiger, and
Amy E DeRocher, and
Zhongsheng Zhang, and
Kayode K Ojo, and
Eric T Larson, and
B Gayani K Perera, and
Edward J Dale, and
Panqing He, and
Molly C Reid, and
Anna M W Fox, and
Natascha R Mueller, and
Ethan A Merritt, and
Erkang Fan, and
Marilyn Parsons, and
Wesley C Van Voorhis, and
Dustin J Maly
October 2010,
ACS medicinal chemistry letters,
Steven M Johnson, and
Ryan C Murphy, and
Jennifer A Geiger, and
Amy E DeRocher, and
Zhongsheng Zhang, and
Kayode K Ojo, and
Eric T Larson, and
B Gayani K Perera, and
Edward J Dale, and
Panqing He, and
Molly C Reid, and
Anna M W Fox, and
Natascha R Mueller, and
Ethan A Merritt, and
Erkang Fan, and
Marilyn Parsons, and
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Dustin J Maly
June 2018,
Antimicrobial agents and chemotherapy,
