Literature DB >> 33479608

Discovery of isoxazolyl-based inhibitors of Plasmodium falciparum cGMP-dependent protein kinase.

Shams Ul Mahmood1, Huimin Cheng1, Sreedhar R Tummalapalli1, Ramappa Chakrasali1, Rammohan R Yadav Bheemanaboina1, Tamara Kreiss1, Agnieska Chojnowski1, Tyler Eck1, John J Siekierka1, David P Rotella1.   

Abstract

The cGMP-dependent protein kinase in Plasmodium falciparum (PfPKG) plays multiple roles in the life cycle of the parasite. As a result, this enzyme is a potential target for new antimalarial agents. Existing inhbitors, while potent and active in malaria models are not optimal. This communication describes initial optimization of a structurally distinct class of PfPKG inhibitors. This journal is © The Royal Society of Chemistry 2020.

Entities:  

Year:  2019        PMID： 33479608      PMCID： PMC7536641          DOI： 10.1039/c9md00511k

Source DB:  PubMed          Journal:  RSC Med Chem        ISSN： 2632-8682


  12 in total

1.  Evaluation of Different Methods for Identification of Structural Alerts Using Chemical Ames Mutagenicity Data Set as a Benchmark.

Authors:  Hongbin Yang; Jie Li; Zengrui Wu; Weihua Li; Guixia Liu; Yun Tang
Journal:  Chem Res Toxicol       Date:  2017-05-23       Impact factor: 3.739

2.  Using 2D Structural Alerts to Define Chemical Categories for Molecular Initiating Events.

Authors:  Timothy E H Allen; Jonathan M Goodman; Steve Gutsell; Paul J Russell
Journal:  Toxicol Sci       Date:  2018-09-01       Impact factor: 4.849

3.  The malaria parasite cyclic GMP-dependent protein kinase plays a central role in blood-stage schizogony.

Authors:  Helen M Taylor; Louisa McRobert; Munira Grainger; Audrey Sicard; Anton R Dluzewski; Christine S Hopp; Anthony A Holder; David A Baker
Journal:  Eukaryot Cell       Date:  2009-11-13

4.  The role of a Brugia malayi p38 MAP kinase ortholog (Bm-MPK1) in parasite anti-oxidative stress responses.

Authors:  Akruti Patel; Agnieszka Nawrocka Chojnowski; Katie Gaskill; William De Martini; Ronald L Goldberg; John J Siekierka
Journal:  Mol Biochem Parasitol       Date:  2010-12-24       Impact factor: 1.759

5.  Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG).

Authors:  Denise J Tsagris; Kristian Birchall; Nathalie Bouloc; Jonathan M Large; Andy Merritt; Ela Smiljanic-Hurley; Mary Wheldon; Keith H Ansell; Catherine Kettleborough; David Whalley; Lindsay B Stewart; Paul W Bowyer; David A Baker; Simon A Osborne
Journal:  Bioorg Med Chem Lett       Date:  2018-08-27       Impact factor: 2.823

6.  Observing in real time the evolution of artemisinin resistance in Plasmodium falciparum.

Authors:  Carol Hopkins Sibley
Journal:  BMC Med       Date:  2015-03-31       Impact factor: 8.775

7.  A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission.

Authors:  David A Baker; Lindsay B Stewart; Jonathan M Large; Paul W Bowyer; Keith H Ansell; María B Jiménez-Díaz; Majida El Bakkouri; Kristian Birchall; Koen J Dechering; Nathalie S Bouloc; Peter J Coombs; David Whalley; Denise J Harding; Ela Smiljanic-Hurley; Mary C Wheldon; Eloise M Walker; Johannes T Dessens; María José Lafuente; Laura M Sanz; Francisco-Javier Gamo; Santiago B Ferrer; Raymond Hui; Teun Bousema; Iñigo Angulo-Barturén; Andy T Merritt; Simon L Croft; Winston E Gutteridge; Catherine A Kettleborough; Simon A Osborne
Journal:  Nat Commun       Date:  2017-09-05       Impact factor: 14.919

Review 8.  In Silico Prediction of Chemical Toxicity for Drug Design Using Machine Learning Methods and Structural Alerts.

Authors:  Hongbin Yang; Lixia Sun; Weihua Li; Guixia Liu; Yun Tang
Journal:  Front Chem       Date:  2018-02-20       Impact factor: 5.221

9.  High-throughput screening of the Plasmodium falciparum cGMP-dependent protein kinase identified a thiazole scaffold which kills erythrocytic and sexual stage parasites.

Authors:  Maria Penzo; Laura de Las Heras-Dueña; Lydia Mata-Cantero; Beatriz Diaz-Hernandez; Maria-Jesus Vazquez-Muñiz; Sonja Ghidelli-Disse; Gerard Drewes; Elena Fernandez-Alvaro; David A Baker
Journal:  Sci Rep       Date:  2019-05-07       Impact factor: 4.379

10.  Development of Chemical Entities Endowed with Potent Fast-Killing Properties against Plasmodium falciparum Malaria Parasites.

Authors:  Alexios N Matralis; Adnan Malik; Maria Penzo; Inmaculada Moreno; Maria J Almela; Isabel Camino; Benigno Crespo; Anas Saadeddin; Sonja Ghidelli-Disse; Lourdes Rueda; Felix Calderon; Simon A Osborne; Gerard Drewes; Markus Böesche; Elena Fernández-Álvaro; Jose Ignacio Martin Hernando; David A Baker
Journal:  J Med Chem       Date:  2019-10-14       Impact factor: 7.446
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  2 in total

1.  Discovery of Imidazole-Based Inhibitors of Plasmodium falciparum cGMP-Dependent Protein Kinase.

Authors:  Rammohan R Yadav Bheemanaboina; Mariana Laureano de Souza; Mariana Lozano Gonzalez; Shams Ul Mahmood; Tyler Eck; Tamara Kreiss; Samantha O Aylor; Alison Roth; Patricia Lee; Brandon S Pybus; Dennis J Colussi; Wayne E Childers; John Gordon; John J Siekierka; Purnima Bhanot; David P Rotella
Journal:  ACS Med Chem Lett       Date:  2021-11-15       Impact factor: 4.632

2.  Characterization of Competitive Inhibitors of Plasmodium falciparum cGMP-Dependent Protein Kinase.

Authors:  Tyler Eck; Mariana Laureano de Souza; Melvin Delvillar; Kutub Ashraf; Rammohan R Yadav Bheemanaboina; Ramappa Chakrasali; Tamara Kreiss; John J Siekierka; David P Rotella; Purnima Bhanot; Nina M Goodey
Journal:  Chembiochem       Date:  2022-02-23       Impact factor: 3.461
  2 in total

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