Literature DB >> 19769357

Structure-guided development of selective TbcatB inhibitors.

Jeremy P Mallari1, Anang A Shelat, Aaron Kosinski, Conor R Caffrey, Michele Connelly, Fangyi Zhu, James H McKerrow, R Kiplin Guy.   

Abstract

The trypanosomal cathepsin TbcatB is essential for parasite survival and is an attractive therapeutic target. Herein we report the structure-guided development of TbcatB inhibitors with specificity relative to rhodesain and human cathepsins B and L. Inhibitors were tested for enzymatic activity, trypanocidal activity, and general cytotoxicity. These data chemically validate TbcatB as a drug target and demonstrate that it is possible to potently and selectively inhibit TbcatB relative to trypanosomal and human homologues.

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Year:  2009        PMID： 19769357      PMCID： PMC2762491          DOI： 10.1021/jm900908p

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  15 in total

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Authors:  Doron C Greenbaum; Zachary Mackey; Elizabeth Hansell; Patricia Doyle; Jiri Gut; Conor R Caffrey; Julia Lehrman; Philip J Rosenthal; James H McKerrow; Kelly Chibale
Journal:  J Med Chem       Date:  2004-06-03       Impact factor: 7.446

3.  External validation and prediction employing the predictive squared correlation coefficient test set activity mean vs training set activity mean.

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4.  VMD: visual molecular dynamics.

Authors:  W Humphrey; A Dalke; K Schulten
Journal:  J Mol Graph       Date:  1996-02

5.  Cathepsins B and D are dispensable for major histocompatibility complex class II-mediated antigen presentation.

Authors:  J Deussing; W Roth; P Saftig; C Peters; H L Ploegh; J A Villadangos
Journal:  Proc Natl Acad Sci U S A       Date:  1998-04-14       Impact factor: 11.205

6.  Trypanosoma brucei: killing of bloodstream forms in vitro and in vivo by the cysteine proteinase inhibitor Z-phe-ala-CHN2.

Authors:  S Scory; C R Caffrey; Y D Stierhof; A Ruppel; D Steverding
Journal:  Exp Parasitol       Date:  1999-04       Impact factor: 2.011

7.  Cysteine proteinase inhibitors kill cultured bloodstream forms of Trypanosoma brucei brucei.

Authors:  L Troeberg; R E Morty; R N Pike; J D Lonsdale-Eccles; J T Palmer; J H McKerrow; T H Coetzer
Journal:  Exp Parasitol       Date:  1999-04       Impact factor: 2.011

8.  Neuronal loss and brain atrophy in mice lacking cathepsins B and L.

Authors:  Ute Felbor; Benedikt Kessler; Walther Mothes; Hans H Goebel; Hidde L Ploegh; Roderick T Bronson; Bjorn R Olsen
Journal:  Proc Natl Acad Sci U S A       Date:  2002-06-04       Impact factor: 11.205

9.  A cathepsin B-like protease is required for host protein degradation in Trypanosoma brucei.

Authors:  Zachary B Mackey; Theresa C O'Brien; Doron C Greenbaum; Rebecca B Blank; James H McKerrow
Journal:  J Biol Chem       Date:  2004-08-23       Impact factor: 5.157

10.  RNA interference of Trypanosoma brucei cathepsin B and L affects disease progression in a mouse model.

Authors:  Maha-Hamadien Abdulla; Theresa O'Brien; Zachary B Mackey; Mohamed Sajid; Dennis J Grab; James H McKerrow
Journal:  PLoS Negl Trop Dis       Date:  2008-09-24
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  5 in total

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Journal:  Chem Rev       Date:  2014-11-03       Impact factor: 60.622

2.  Synthesis and biochemical evaluation of thiochromanone thiosemicarbazone analogues as inhibitors of cathepsin L.

Authors:  Jiangli Song; Lindsay M Jones; G D Kishore Kumar; Elizabeth S Conner; Liela Bayeh; Gustavo E Chavarria; Amanda K Charlton-Sevcik; Shen-En Chen; David J Chaplin; Mary Lynn Trawick; Kevin G Pinney
Journal:  ACS Med Chem Lett       Date:  2012-04-18       Impact factor: 4.345

3.  Assessing the trypanocidal potential of natural and semi-synthetic diketopiperazines from two deep water marine-derived fungi.

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Journal:  Bioorg Med Chem       Date:  2010-03-01       Impact factor: 3.641

4.  Crystal Structures of TbCatB and rhodesain, potential chemotherapeutic targets and major cysteine proteases of Trypanosoma brucei.

Authors:  Iain D Kerr; Peng Wu; Rachael Marion-Tsukamaki; Zachary B Mackey; Linda S Brinen
Journal:  PLoS Negl Trop Dis       Date:  2010-06-08

5.  Mining a cathepsin inhibitor library for new antiparasitic drug leads.

Authors:  Kenny K H Ang; Joseline Ratnam; Jiri Gut; Jennifer Legac; Elizabeth Hansell; Zachary B Mackey; Katarzyna M Skrzypczynska; Anjan Debnath; Juan C Engel; Philip J Rosenthal; James H McKerrow; Michelle R Arkin; Adam R Renslo
Journal:  PLoS Negl Trop Dis       Date:  2011-05-03
  5 in total

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