Literature DB >> 12133721

Recent advances in the synthesis, design and selection of cysteine protease inhibitors.

Alejandro Alvarez Hernandez1, William R Roush.   

Abstract

Inhibition of cysteine proteases is emerging as an important strategy for the treatment of a variety of human diseases. Intense efforts involving structure-based inhibitor design have been directed toward several cysteine proteases, including cathepsin K, calpain, human rhinovirus 3C protease and several parasitic cysteine protease targets. Other successful recent efforts have involved combinatorial synthesis and screening for identification of new inhibitor templates.

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Year:  2002        PMID: 12133721     DOI: 10.1016/s1367-5931(02)00345-9

Source DB:  PubMed          Journal:  Curr Opin Chem Biol        ISSN: 1367-5931            Impact factor:   8.822


  14 in total

1.  Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype.

Authors:  Michael C Myers; Parag P Shah; Mary Pat Beavers; Andrew D Napper; Scott L Diamond; Amos B Smith; Donna M Huryn
Journal:  Bioorg Med Chem Lett       Date:  2008-05-01       Impact factor: 2.823

2.  Synthesis of macrocyclic trypanosomal cysteine protease inhibitors.

Authors:  Yen Ting Chen; Ricardo Lira; Elizabeth Hansell; James H McKerrow; William R Roush
Journal:  Bioorg Med Chem Lett       Date:  2008-06-10       Impact factor: 2.823

3.  Vital role of the calpain-calpastatin system for placental-integrity-dependent embryonic survival.

Authors:  Jiro Takano; Naomi Mihira; Ryo Fujioka; Emi Hosoki; Athar H Chishti; Takaomi C Saido
Journal:  Mol Cell Biol       Date:  2011-07-26       Impact factor: 4.272

4.  Design, synthesis and biological evaluation of a library of thiocarbazates and their activity as cysteine protease inhibitors.

Authors:  Zhuqing Liu; Michael C Myers; Parag P Shah; Mary Pat Beavers; Phillip A Benedetti; Scott L Diamond; Amos B Smith; Donna M Huryn
Journal:  Comb Chem High Throughput Screen       Date:  2010-05       Impact factor: 1.339

5.  In vitro and in vivo studies of the trypanocidal properties of WRR-483 against Trypanosoma cruzi.

Authors:  Yen Ting Chen; Linda S Brinen; Iain D Kerr; Elizabeth Hansell; Patricia S Doyle; James H McKerrow; William R Roush
Journal:  PLoS Negl Trop Dis       Date:  2010-09-14

6.  The deubiquitinase USP28 controls intestinal homeostasis and promotes colorectal cancer.

Authors:  Markus E Diefenbacher; Nikita Popov; Sophia M Blake; Christina Schülein-Völk; Emma Nye; Bradley Spencer-Dene; Laura A Jaenicke; Martin Eilers; Axel Behrens
Journal:  J Clin Invest       Date:  2014-06-24       Impact factor: 14.808

7.  Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor.

Authors:  Michael C Myers; Parag P Shah; Scott L Diamond; Donna M Huryn; Amos B Smith
Journal:  Bioorg Med Chem Lett       Date:  2007-11-01       Impact factor: 2.823

8.  Identification and characterization of 3-substituted pyrazolyl esters as alternate substrates for cathepsin B: the confounding effects of DTT and cysteine in biological assays.

Authors:  Michael C Myers; Andrew D Napper; Nuzhat Motlekar; Parag P Shah; Chun-Hao Chiu; Mary Pat Beavers; Scott L Diamond; Donna M Huryn; Amos B Smith
Journal:  Bioorg Med Chem Lett       Date:  2007-07-05       Impact factor: 2.823

Review 9.  The identification, characterization and optimization of small molecule probes of cysteine proteases: experiences of the Penn Center for Molecular Discovery with cathepsin B and cathepsin L.

Authors:  Donna M Huryn; Amos B Smith
Journal:  Curr Top Med Chem       Date:  2009       Impact factor: 3.295

10.  A highly potent and selective caspase 1 inhibitor that utilizes a key 3-cyanopropanoic acid moiety.

Authors:  Matthew B Boxer; Amy M Quinn; Min Shen; Ajit Jadhav; William Leister; Anton Simeonov; Douglas S Auld; Craig J Thomas
Journal:  ChemMedChem       Date:  2010-05-03       Impact factor: 3.466

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