Literature DB >> 8807047

Antimalarial effects of vinyl sulfone cysteine proteinase inhibitors.

P J Rosenthal1, J E Olson, G K Lee, J T Palmer, J L Klaus, D Rasnick.   

Abstract

We evaluated the antimalarial effects of vinyl sulfone cysteine proteinase inhibitors. A number of vinyl sulfones strongly inhibited falcipain, a Plasmodium falciparum cysteine proteinase that is a critical hemoglobinase. In studies of cultured parasites, nanomolar concentrations of three vinyl sulfones inhibited parasite hemoglobin degradation, metabolic activity, and development. The antimalarial effects correlated with the inhibition of falcipain. Our results suggest that vinyl sulfones or related cysteine proteinase inhibitors may have promise as antimalarial agents.

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Year:  1996        PMID： 8807047      PMCID： PMC163380     

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  15 in total

1.  Localization and characterization of hemoglobin-degrading aspartic proteinases from the malarial parasite Plasmodium falciparum.

Authors:  D L vander Jagt; L A Hunsaker; N M Campos; J V Scaletti
Journal:  Biochim Biophys Acta       Date:  1992-08-21

2.  Plasmodium falciparum: inhibitors of lysosomal cysteine proteinases inhibit a trophozoite proteinase and block parasite development.

Authors:  P J Rosenthal; J H McKerrow; D Rasnick; J H Leech
Journal:  Mol Biochem Parasitol       Date:  1989-06-15       Impact factor: 1.759

Review 3.  Disease problems in the Third World.

Authors:  J A Walsh
Journal:  Ann N Y Acad Sci       Date:  1989       Impact factor: 5.691

4.  A malarial cysteine proteinase is necessary for hemoglobin degradation by Plasmodium falciparum.

Authors:  P J Rosenthal; J H McKerrow; M Aikawa; H Nagasawa; J H Leech
Journal:  J Clin Invest       Date:  1988-11       Impact factor: 14.808

5.  Antimalarial effects of peptide inhibitors of a Plasmodium falciparum cysteine proteinase.

Authors:  P J Rosenthal; W S Wollish; J T Palmer; D Rasnick
Journal:  J Clin Invest       Date:  1991-11       Impact factor: 14.808

6.  Inhibition of a Plasmodium vinckei cysteine proteinase cures murine malaria.

Authors:  P J Rosenthal; G K Lee; R E Smith
Journal:  J Clin Invest       Date:  1993-03       Impact factor: 14.808

7.  Structure-based inhibitor design by using protein models for the development of antiparasitic agents.

Authors:  C S Ring; E Sun; J H McKerrow; G K Lee; P J Rosenthal; I D Kuntz; F E Cohen
Journal:  Proc Natl Acad Sci U S A       Date:  1993-04-15       Impact factor: 11.205

8.  In vitro antimalarial activity of chalcones and their derivatives.

Authors:  R Li; G L Kenyon; F E Cohen; X Chen; B Gong; J N Dominguez; E Davidson; G Kurzban; R E Miller; E O Nuzum
Journal:  J Med Chem       Date:  1995-12-22       Impact factor: 7.446

9.  Synchronization of Plasmodium falciparum erythrocytic stages in culture.

Authors:  C Lambros; J P Vanderberg
Journal:  J Parasitol       Date:  1979-06       Impact factor: 1.276

10.  Hemoglobin degradation in the human malaria pathogen Plasmodium falciparum: a catabolic pathway initiated by a specific aspartic protease.

Authors:  D E Goldberg; A F Slater; R Beavis; B Chait; A Cerami; G B Henderson
Journal:  J Exp Med       Date:  1991-04-01       Impact factor: 14.307
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  36 in total

1.  Comparison of efficacies of cysteine protease inhibitors against five strains of Plasmodium falciparum.

Authors:  A Singh; P J Rosenthal
Journal:  Antimicrob Agents Chemother       Date:  2001-03       Impact factor: 5.191

2.  Probing the structure of falcipain-3, a cysteine protease from Plasmodium falciparum: comparative protein modeling and docking studies.

Authors:  Yogesh A Sabnis; Prashant V Desai; Philip J Rosenthal; Mitchell A Avery
Journal:  Protein Sci       Date:  2003-03       Impact factor: 6.725

3.  Expression and alteration of the S2 subsite of the Leishmania major cathepsin B-like cysteine protease.

Authors:  V J Chan; P M Selzer; J H McKerrow; J A Sakanari
Journal:  Biochem J       Date:  1999-05-15       Impact factor: 3.857

4.  Plasmodium falciparum cysteine protease falcipain-1 is not essential in erythrocytic stage malaria parasites.

Authors:  Puran S Sijwali; Kentaro Kato; Karl B Seydel; Jiri Gut; Julie Lehman; Michael Klemba; Daniel E Goldberg; Louis H Miller; Philip J Rosenthal
Journal:  Proc Natl Acad Sci U S A       Date:  2004-05-27       Impact factor: 11.205

5.  Substrate mapping and inhibitor profiling of falcipain-2, falcipain-3 and berghepain-2: implications for peptidase anti-malarial drug discovery.

Authors:  Manoj K Ramjee; Nicholas S Flinn; Tracy P Pemberton; Martin Quibell; Yikang Wang; John P Watts
Journal:  Biochem J       Date:  2006-10-01       Impact factor: 3.857

6.  Antimalarial synergy of cysteine and aspartic protease inhibitors.

Authors:  A Semenov; J E Olson; P J Rosenthal
Journal:  Antimicrob Agents Chemother       Date:  1998-09       Impact factor: 5.191

7.  Non-canonical maturation of two papain-family proteases in Toxoplasma gondii.

Authors:  Zhicheng Dou; Isabelle Coppens; Vern B Carruthers
Journal:  J Biol Chem       Date:  2012-12-18       Impact factor: 5.157

8.  Antimalarial activity of thiosemicarbazones and purine derived nitriles.

Authors:  Jeremy P Mallari; Wendyam A Guiguemde; R Kiplin Guy
Journal:  Bioorg Med Chem Lett       Date:  2009-05-05       Impact factor: 2.823

9.  Vinyl sulfones as antiparasitic agents and a structural basis for drug design.

Authors:  Iain D Kerr; Ji H Lee; Christopher J Farady; Rachael Marion; Mathias Rickert; Mohammed Sajid; Kailash C Pandey; Conor R Caffrey; Jennifer Legac; Elizabeth Hansell; James H McKerrow; Charles S Craik; Philip J Rosenthal; Linda S Brinen
Journal:  J Biol Chem       Date:  2009-07-20       Impact factor: 5.157

10.  Hemoglobin cleavage site-specificity of the Plasmodium falciparum cysteine proteases falcipain-2 and falcipain-3.

Authors:  Shoba Subramanian; Markus Hardt; Youngchool Choe; Richard K Niles; Eric B Johansen; Jennifer Legac; Jiri Gut; Iain D Kerr; Charles S Craik; Philip J Rosenthal
Journal:  PLoS One       Date:  2009-04-09       Impact factor: 3.240
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