Literature DB >> 23395653

Chemical probes of a trisubstituted pyrrole to identify its protein target(s) in Plasmodium sporozoites.

Tyrell Towle1, Isabell Chang, Isabel Chang, Robert J Kerns, Purnima Bhanot.   

Abstract

Malaria is a disease that has a major impact in many developing nations, especially on the African continent. There is a need to develop new therapeutics and prophylactic treatments against it. A trisubstituted pyrrole was recently found to inhibit infection of mammalian hepatocytes by Plasmodium sporozoites, but the target of this agent is not known. In this study trisubstituted pyrrole derivatives with different substituents on a piperidinyl nitrogen were prepared. We determined if modifications of the piperidinyl nitrogen would accommodate a drug-biotin linking strategy for affinity purification of the trisubstituted pyrrole's target protein(s).
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID: 23395653      PMCID: PMC5509439          DOI: 10.1016/j.bmcl.2013.01.010

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  Activity of a trisubstituted pyrrole in inhibiting sporozoite invasion and blocking malaria infection.

Authors:  Dhruv Panchal; Purnima Bhanot
Journal:  Antimicrob Agents Chemother       Date:  2010-07-19       Impact factor: 5.191

2.  Characterization of Plasmodium falciparum cGMP-dependent protein kinase (PfPKG): antiparasitic activity of a PKG inhibitor.

Authors:  Carmen A Diaz; John Allocco; Mary Ann Powles; Lai Yeung; Robert G K Donald; Jennifer W Anderson; Paul A Liberator
Journal:  Mol Biochem Parasitol       Date:  2005-11-17       Impact factor: 1.759

3.  Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.

Authors:  Olaf Kinzel; Laura Llauger-Bufi; Giovanna Pescatore; Michael Rowley; Carsten Schultz-Fademrecht; Edith Monteagudo; Massimiliano Fonsi; Odalys Gonzalez Paz; Fabrizio Fiore; Christian Steinkühler; Philip Jones
Journal:  J Med Chem       Date:  2009-06-11       Impact factor: 7.446

4.  Synthesis and SAR of 2,3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents.

Authors:  Tesfaye Biftu; Dennis Feng; Mitree Ponpipom; Narindar Girotra; Gui-Bai Liang; Xiaoxia Qian; Robert Bugianesi; Joseph Simeone; Linda Chang; Anne Gurnett; Paul Liberator; Paula Dulski; Penny Sue Leavitt; Tami Crumley; Andrew Misura; Terence Murphy; Sandra Rattray; Samantha Samaras; Tamas Tamas; John Mathew; Christine Brown; Don Thompson; Dennis Schmatz; Michael Fisher; Matthew Wyvratt
Journal:  Bioorg Med Chem Lett       Date:  2005-07-01       Impact factor: 2.823

5.  Role of Plasmodium berghei cGMP-dependent protein kinase in late liver stage development.

Authors:  Adebola Falae; Audrey Combe; Anburaj Amaladoss; Teresa Carvalho; Robert Menard; Purnima Bhanot
Journal:  J Biol Chem       Date:  2009-11-24       Impact factor: 5.157

6.  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
  6 in total

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