Literature DB >> 20167486

Design and evaluation of Trypanosoma brucei metacaspase inhibitors.

Maya Berg1, Pieter Van der Veken, Jurgen Joossens, Venkatraj Muthusamy, Matthias Breugelmans, Catherine X Moss, Jana Rudolf, Paul Cos, Graham H Coombs, Louis Maes, Achiel Haemers, Jeremy C Mottram, Koen Augustyns.   

Abstract

Metacaspase (MCA) is an important enzyme in Trypanosoma brucei, absent from humans and differing significantly from the orthologous human caspases. Therefore MCA constitutes a new attractive drug target for antiparasitic chemotherapeutics, which needs further characterization to support the discovery of innovative drug candidates. A first series of inhibitors has been prepared on the basis of known substrate specificity and the predicted catalytic mechanism of the enzyme. In this Letter we present the first inhibitors of TbMCA2 with low micromolar enzymatic and antiparasitic activity in vitro combined with low cytotoxicity. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20167486      PMCID： PMC2845880          DOI： 10.1016/j.bmcl.2010.01.099

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


  20 in total

Review 1.  Programmed cell death in trypanosomatids and other unicellular organisms.

Authors:  Alain Debrabant; Nancy Lee; Sylvie Bertholet; Robert Duncan; Hira L Nakhasi
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2.  Identification of paracaspases and metacaspases: two ancient families of caspase-like proteins, one of which plays a key role in MALT lymphoma.

Authors:  A G Uren; K O'Rourke; L A Aravind; M T Pisabarro; S Seshagiri; E V Koonin; V M Dixit
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3.  Cell death in Leishmania induced by stress and differentiation: programmed cell death or necrosis?

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Journal:  Cell Death Differ       Date:  2002-10       Impact factor: 15.828

Review 4.  Programmed cell death in trypanosomatids: a way to maximize their biological fitness?

Authors:  Paul A Nguewa; Miguel A Fuertes; Basilio Valladares; Carlos Alonso; José M Pérez
Journal:  Trends Parasitol       Date:  2004-08

Review 5.  Clan CD cysteine peptidases of parasitic protozoa.

Authors:  Jeremy C Mottram; Matthew J Helms; Graham H Coombs; Mohammed Sajid
Journal:  Trends Parasitol       Date:  2003-04

6.  Data-mining approaches reveal hidden families of proteases in the genome of malaria parasite.

Authors:  Yimin Wu; Xiangyun Wang; Xia Liu; Yufeng Wang
Journal:  Genome Res       Date:  2003-04       Impact factor: 9.043

7.  Prostaglandin D2 induces programmed cell death in Trypanosoma brucei bloodstream form.

Authors:  K Figarella; M Rawer; N L Uzcategui; B K Kubata; K Lauber; F Madeo; S Wesselborg; M Duszenko
Journal:  Cell Death Differ       Date:  2005-04       Impact factor: 15.828

8.  Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone.

Authors:  Michael J Costanzo; Stephen C Yabut; Harold R Almond; Patricia Andrade-Gordon; Thomas W Corcoran; Lawrence De Garavilla; Jack A Kauffman; William M Abraham; Rosario Recacha; Debashish Chattopadhyay; Bruce E Maryanoff
Journal:  J Med Chem       Date:  2003-08-28       Impact factor: 7.446

9.  Anticoagulant and antithrombotic action of the synthetic thrombin inhibitor D-phenylalanyl-L-prolyl-L-arginine nitrile.

Authors:  B Kaiser; M Richter; J Hauptmann; F Markwardt
Journal:  Pharmazie       Date:  1991-02       Impact factor: 1.267

Review 10.  Development of protease inhibitors for protozoan infections.

Authors:  James H McKerrow; Philip J Rosenthal; Ryan Swenerton; Patricia Doyle
Journal:  Curr Opin Infect Dis       Date:  2008-12       Impact factor: 4.915
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  8 in total

1.  Antagonic activities of Trypanosoma cruzi metacaspases affect the balance between cell proliferation, death and differentiation.

Authors:  M Laverrière; J J Cazzulo; V E Alvarez
Journal:  Cell Death Differ       Date:  2012-03-09       Impact factor: 15.828

2.  Crystal structure of a Trypanosoma brucei metacaspase.

Authors:  Karen McLuskey; Jana Rudolf; William R Proto; Neil W Isaacs; Graham H Coombs; Catherine X Moss; Jeremy C Mottram
Journal:  Proc Natl Acad Sci U S A       Date:  2012-04-23       Impact factor: 11.205

3.  Screening and Identification of Metacaspase Inhibitors: Evaluation of Inhibition Mechanism and Trypanocidal Activity.

Authors:  Brian Pérez; León A Bouvier; Juan José Cazzulo; Fernán Agüero; Emir Salas-Sarduy; Vanina E Alvarez
Journal:  Antimicrob Agents Chemother       Date:  2021-02-17       Impact factor: 5.191

4.  α-ketoheterocycles as inhibitors of Leishmania mexicana cysteine protease CPB.

Authors:  Koen Steert; Maya Berg; Jeremy C Mottram; Gareth D Westrop; Graham H Coombs; Paul Cos; Louis Maes; Jurgen Joossens; Pieter Van der Veken; Achiel Haemers; Koen Augustyns
Journal:  ChemMedChem       Date:  2010-10-04       Impact factor: 3.466

5.  Apoptotic markers in protozoan parasites.

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Journal:  Parasit Vectors       Date:  2010-11-09       Impact factor: 3.876

Review 6.  Are protozoan metacaspases potential parasite killers?

Authors:  Benoît Meslin; Habib Zalila; Nicolas Fasel; Stephane Picot; Anne-Lise Bienvenu
Journal:  Parasit Vectors       Date:  2011-02-28       Impact factor: 3.876

7.  Identification and characterization of genes involved in leishmania pathogenesis: the potential for drug target selection.

Authors:  Robert Duncan; Sreenivas Gannavaram; Ranadhir Dey; Alain Debrabant; Ines Lakhal-Naouar; Hira L Nakhasi
Journal:  Mol Biol Int       Date:  2011-06-26

8.  Acyclic nucleoside phosphonates with adenine nucleobase inhibit Trypanosoma brucei adenine phosphoribosyltransferase in vitro.

Authors:  Eva Doleželová; Tomáš Klejch; Petr Špaček; Martina Slapničková; Luke Guddat; Dana Hocková; Alena Zíková
Journal:  Sci Rep       Date:  2021-06-25       Impact factor: 4.379
  8 in total

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