Literature DB >> 21116453

Discovery of Potent and Selective Inhibitors of Calcium-Dependent Protein Kinase 1 (CDPK1) from C. parvum and T. gondii.

Ryan C Murphy1, Kayode K Ojo, Eric T Larson, Alejandro Castellanos-Gonzalez, B Gayani K Perera, Katelyn R Keyloun, Jessica E Kim, Janhavi G Bhandari, Natascha R Muller, Christophe L M J Verlinde, A Clinton White, Ethan A Merritt, Wesley C Van Voorhis, Dustin J Maly.   

Abstract

The protozoans Cryptosporidium parvum and Toxoplasma gondii are parasites of major health concern to humans. Both parasites contain a group of calcium-dependent protein kinases (CDPKs), which are found in plants and ciliates but not in humans or fungi. Here we describe a series of potent inhibitors that target CDPK1 in C. parvum (CpCDPK1) and T. gondii (TgCDPK1). These inhibitors are highly selective for CpCDPK1 and TgCDPK1 over the mammalian kinases SRC and ABL. Furthermore, they are able to block an early stage of C. parvum invasion of HCT-8 host cells, which is similar to their effects on T. gondii invasion of human fibroblasts.

Entities:  

Year:  2010        PMID： 21116453      PMCID： PMC2992447          DOI： 10.1021/ml100096t

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  15 in total

1.  Comparative genomic and phylogenetic analyses of calcium ATPases and calcium-regulated proteins in the apicomplexa.

Authors:  Kisaburo Nagamune; L David Sibley
Journal:  Mol Biol Evol       Date:  2006-06-02       Impact factor: 16.240

2.  Use of the kinase inhibitor analog 1NM-PP1 reveals a role for Toxoplasma gondii CDPK1 in the invasion step.

Authors:  Tatsuki Sugi; Kentaro Kato; Kyosuke Kobayashi; Shumpei Watanabe; Hitomi Kurokawa; Haiyan Gong; Kishor Pandey; Hitoshi Takemae; Hiroomi Akashi
Journal:  Eukaryot Cell       Date:  2010-02-19

3.  Design of allele-specific inhibitors to probe protein kinase signaling.

Authors:  A C Bishop; K Shah; Y Liu; L Witucki; C Kung; K M Shokat
Journal:  Curr Biol       Date:  1998-02-26       Impact factor: 10.834

4.  Toxoplasma gondii attachment to host cells is regulated by a calmodulin-like domain protein kinase.

Authors:  H Kieschnick; T Wakefield; C A Narducci; C Beckers
Journal:  J Biol Chem       Date:  2001-01-11       Impact factor: 5.157

5.  A chemical switch for inhibitor-sensitive alleles of any protein kinase.

Authors:  A C Bishop; J A Ubersax; D T Petsch; D P Matheos; N S Gray; J Blethrow; E Shimizu; J Z Tsien; P G Schultz; M D Rose; J L Wood; D O Morgan; K M Shokat
Journal:  Nature       Date:  2000-09-21       Impact factor: 49.962

6.  Apical organelle discharge by Cryptosporidium parvum is temperature, cytoskeleton, and intracellular calcium dependent and required for host cell invasion.

Authors:  Xian-Ming Chen; Steven P O'Hara; Bing Q Huang; Jeremy B Nelson; Jim Jung-Ching Lin; Guan Zhu; Honorine D Ward; Nicholas F LaRusso
Journal:  Infect Immun       Date:  2004-12       Impact factor: 3.441

7.  Closing the diarrhoea diagnostic gap in Indian children by the application of molecular techniques.

Authors:  S S R Ajjampur; P Rajendran; S Ramani; I Banerjee; B Monica; P Sankaran; V Rosario; R Arumugam; R Sarkar; H Ward; G Kang
Journal:  J Med Microbiol       Date:  2008-11       Impact factor: 2.472

8.  Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation.

Authors:  J H Hanke; J P Gardner; R L Dow; P S Changelian; W H Brissette; E J Weringer; B A Pollok; P A Connelly
Journal:  J Biol Chem       Date:  1996-01-12       Impact factor: 5.157

Review 9.  Calcium-dependent signaling and kinases in apicomplexan parasites.

Authors:  Oliver Billker; Sebastian Lourido; L David Sibley
Journal:  Cell Host Microbe       Date:  2009-06-18       Impact factor: 21.023

Review 10.  Protein kinases as targets for antimalarial intervention: Kinomics, structure-based design, transmission-blockade, and targeting host cell enzymes.

Authors:  Christian Doerig; Oliver Billker; David Pratt; Jane Endicott
Journal:  Biochim Biophys Acta       Date:  2005-10-06
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  70 in total

1.  Bumped kinase inhibitor 1294 treats established Toxoplasma gondii infection.

Authors:  J Stone Doggett; Kayode K Ojo; Erkang Fan; Dustin J Maly; Wesley C Van Voorhis
Journal:  Antimicrob Agents Chemother       Date:  2014-03-31       Impact factor: 5.191

2.  Validation of IMP dehydrogenase inhibitors in a mouse model of cryptosporidiosis.

Authors:  Suresh Kumar Gorla; Nina N McNair; Guangyi Yang; Song Gao; Ming Hu; Venkatakrishna R Jala; Bodduluri Haribabu; Boris Striepen; Gregory D Cuny; Jan R Mead; Lizbeth Hedstrom
Journal:  Antimicrob Agents Chemother       Date:  2013-12-23       Impact factor: 5.191

3.  A specific inhibitor of PfCDPK4 blocks malaria transmission: chemical-genetic validation.

Authors:  Kayode K Ojo; Richard T Eastman; Ramasubbarao Vidadala; Zhongsheng Zhang; Kasey L Rivas; Ryan Choi; Justin D Lutz; Molly C Reid; Anna M W Fox; Matthew A Hulverson; Mark Kennedy; Nina Isoherranen; Laura M Kim; Kenneth M Comess; Dale J Kempf; Christophe L M J Verlinde; Xin-Zhuan Su; Stefan H I Kappe; Dustin J Maly; Erkang Fan; Wesley C Van Voorhis
Journal:  J Infect Dis       Date:  2013-10-10       Impact factor: 5.226

Review 4.  Malaria medicines: a glass half full?

Authors:  Timothy N C Wells; Rob Hooft van Huijsduijnen; Wesley C Van Voorhis
Journal:  Nat Rev Drug Discov       Date:  2015-05-22       Impact factor: 84.694

Review 5.  Designing selective inhibitors for calcium-dependent protein kinases in apicomplexans.

Authors:  Raymond Hui; Majida El Bakkouri; L David Sibley
Journal:  Trends Pharmacol Sci       Date:  2015-05-20       Impact factor: 14.819

6.  Identification of Cryptosporidium parvum active chemical series by Repurposing the open access malaria box.

Authors:  Kovi Bessoff; Thomas Spangenberg; Jenna E Foderaro; Rajiv S Jumani; Gary E Ward; Christopher D Huston
Journal:  Antimicrob Agents Chemother       Date:  2014-02-24       Impact factor: 5.191

7.  Development of 5-Aminopyrazole-4-carboxamide-based Bumped-Kinase Inhibitors for Cryptosporidiosis Therapy.

Authors:  Wenlin Huang; Matthew A Hulverson; Ryan Choi; Samuel L M Arnold; Zhongsheng Zhang; Molly C McCloskey; Grant R Whitman; Robert C Hackman; Kasey L Rivas; Lynn K Barrett; Kayode K Ojo; Wesley C Van Voorhis; Erkang Fan
Journal:  J Med Chem       Date:  2019-03-15       Impact factor: 7.446

8.  A Novel Calcium-Dependent Kinase Inhibitor, Bumped Kinase Inhibitor 1517, Cures Cryptosporidiosis in Immunosuppressed Mice.

Authors:  Alejandro Castellanos-Gonzalez; Hayley Sparks; Samantha Nava; Wenlin Huang; Zhongsheng Zhang; Kasey Rivas; Matthew A Hulverson; Lynn K Barrett; Kayode K Ojo; Erkang Fan; Wesley C Van Voorhis; Arthur Clinton White
Journal:  J Infect Dis       Date:  2016-10-12       Impact factor: 5.226

9.  Multiple determinants for selective inhibition of apicomplexan calcium-dependent protein kinase CDPK1.

Authors:  Eric T Larson; Kayode K Ojo; Ryan C Murphy; Steven M Johnson; Zhongsheng Zhang; Jessica E Kim; David J Leibly; Anna M W Fox; Molly C Reid; Edward J Dale; B Gayani K Perera; Jae Kim; Stephen N Hewitt; Wim G J Hol; Christophe L M J Verlinde; Erkang Fan; Wesley C Van Voorhis; Dustin J Maly; Ethan A Merritt
Journal:  J Med Chem       Date:  2012-03-13       Impact factor: 7.446

10.  CDPKs of Cryptosporidium parvum--stage-specific expression in vitro.

Authors:  Manja Etzold; Matthias Lendner; Arwid Daugschies; Viktor Dyachenko
Journal:  Parasitol Res       Date:  2014-05-09       Impact factor: 2.289
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