Literature DB >> 19889539

Fragment-based discovery of selective inhibitors of the Mycobacterium tuberculosis protein tyrosine phosphatase PtpA.

Katherine A Rawls1, P Therese Lang, Jun Takeuchi, Shinichi Imamura, Tyler D Baguley, Christoph Grundner, Tom Alber, Jonathan A Ellman.   

Abstract

The development of low muM inhibitors of the Mycobacterium tuberculosis phosphatase PtpA is reported. The most potent of these inhibitors (K(i)=1.4+/-0.3 microM) was found to be selective when tested against a panel of human tyrosine and dual-specificity phosphatases (11-fold vs the highly homologous HCPtpA, and >70-fold vs all others tested). Modeling the inhibitor-PtpA complexes explained the structure-activity relationships observed in vitro and revealed further possibilities for compound development.

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Year:  2009        PMID： 19889539      PMCID： PMC2801607          DOI： 10.1016/j.bmcl.2009.10.090

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


  29 in total

1.  Crystal structure of low-molecular-weight protein tyrosine phosphatase from Mycobacterium tuberculosis at 1.9-A resolution.

Authors:  Chaithanya Madhurantakam; Eerappa Rajakumara; Pooja Anjali Mazumdar; Baisakhee Saha; Devrani Mitra; Harald G Wiker; Rajan Sankaranarayanan; Amit Kumar Das
Journal:  J Bacteriol       Date:  2005-03       Impact factor: 3.490

Review 2.  Screening in a spirit haunted world.

Authors:  Brian K Shoichet
Journal:  Drug Discov Today       Date:  2006-07       Impact factor: 7.851

3.  Multiple ligand-binding properties of the lipocalin member chicken alpha1-acid glycoprotein studied by circular dichroism and electronic absorption spectroscopy: the essential role of the conserved tryptophan residue.

Authors:  Ferenc Zsila; Hisami Matsunaga; Zsolt Bikádi; Jun Haginaka
Journal:  Biochim Biophys Acta       Date:  2006-05-09

4.  Rapid identification of potent nonpeptidic serine protease inhibitors.

Authors:  Cleo M Salisbury; Jonathan A Ellman
Journal:  Chembiochem       Date:  2006-07       Impact factor: 3.164

5.  Methylxanthine drugs are chitinase inhibitors: investigation of inhibition and binding modes.

Authors:  Francesco V Rao; Ole A Andersen; Kalpit A Vora; Julie A Demartino; Daan M F van Aalten
Journal:  Chem Biol       Date:  2005-09

6.  Identification of selective, nonpeptidic nitrile inhibitors of cathepsin s using the substrate activity screening method.

Authors:  Andrew W Patterson; Warren J L Wood; Michael Hornsby; Scott Lesley; Glen Spraggon; Jonathan A Ellman
Journal:  J Med Chem       Date:  2006-10-19       Impact factor: 7.446

7.  The drug binding site of human alpha1-acid glycoprotein: insight from induced circular dichroism and electronic absorption spectra.

Authors:  Ferenc Zsila; Yasunori Iwao
Journal:  Biochim Biophys Acta       Date:  2007-01-28

8.  Substrate activity screening: a fragment-based method for the rapid identification of nonpeptidic protease inhibitors.

Authors:  Warren J L Wood; Andrew W Patterson; Hiroyuki Tsuruoka; Rishi K Jain; Jonathan A Ellman
Journal:  J Am Chem Soc       Date:  2005-11-09       Impact factor: 15.419

9.  Screening-based discovery and structural dissection of a novel family 18 chitinase inhibitor.

Authors:  Alexander W Schüttelkopf; Ole A Andersen; Francesco V Rao; Matthew Allwood; Clare Lloyd; Ian M Eggleston; Daan M F van Aalten
Journal:  J Biol Chem       Date:  2006-07-14       Impact factor: 5.157

Review 10.  PTP1B as a drug target: recent developments in PTP1B inhibitor discovery.

Authors:  Sheng Zhang; Zhong-Yin Zhang
Journal:  Drug Discov Today       Date:  2007-04-06       Impact factor: 7.851
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  11 in total

Review 1.  Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.

Authors:  Roland E Dolle; Bertrand Le Bourdonnec; Karin Worm; Guillermo A Morales; Craig J Thomas; Wei Zhang
Journal:  J Comb Chem       Date:  2010-10-05

Review 2.  Small molecule tools for functional interrogation of protein tyrosine phosphatases.

Authors:  Rongjun He; Li-Fan Zeng; Yantao He; Sheng Zhang; Zhong-Yin Zhang
Journal:  FEBS J       Date:  2012-08-16       Impact factor: 5.542

3.  Mycobacterial Protein Tyrosine Phosphatases A and B Inhibitors Augment the Bactericidal Activity of the Standard Anti-tuberculosis Regimen.

Authors:  Noton K Dutta; Rongjun He; Michael L Pinn; Yantao He; Francis Burrows; Zhong-Yin Zhang; Petros C Karakousis
Journal:  ACS Infect Dis       Date:  2015-12-24       Impact factor: 5.084

4.  Identification of multiple structurally distinct, nonpeptidic small molecule inhibitors of protein arginine deiminase 3 using a substrate-based fragment method.

Authors:  Haya Jamali; Hasan A Khan; Joseph R Stringer; Somenath Chowdhury; Jonathan A Ellman
Journal:  J Am Chem Soc       Date:  2015-03-05       Impact factor: 15.419

Review 5.  Mycobacterium tuberculosis Serine/Threonine Protein Kinases.

Authors:  Sladjana Prisic; Robert N Husson
Journal:  Microbiol Spectr       Date:  2014-10

6.  Substrate-based fragment identification for the development of selective, nonpeptidic inhibitors of striatal-enriched protein tyrosine phosphatase.

Authors:  Tyler D Baguley; Hai-Chao Xu; Manavi Chatterjee; Angus C Nairn; Paul J Lombroso; Jonathan A Ellman
Journal:  J Med Chem       Date:  2013-10-01       Impact factor: 7.446

7.  Substrate deconstruction and the nonadditivity of enzyme recognition.

Authors:  Sarah Barelier; Jennifer A Cummings; Alissa M Rauwerdink; Daniel S Hitchcock; Jeremiah D Farelli; Steven C Almo; Frank M Raushel; Karen N Allen; Brian K Shoichet
Journal:  J Am Chem Soc       Date:  2014-05-12       Impact factor: 15.419

8.  Glutathione-Responsive Selenosulfide Prodrugs as a Platform Strategy for Potent and Selective Mechanism-Based Inhibition of Protein Tyrosine Phosphatases.

Authors:  Caroline Chandra Tjin; Kate D Otley; Tyler D Baguley; Pradeep Kurup; Jian Xu; Angus C Nairn; Paul J Lombroso; Jonathan A Ellman
Journal:  ACS Cent Sci       Date:  2017-12-06       Impact factor: 14.553

9.  The antibiotic Furvina® targets the P-site of 30S ribosomal subunits and inhibits translation initiation displaying start codon bias.

Authors:  Attilio Fabbretti; Letizia Brandi; Dezemona Petrelli; Cynthia L Pon; Nilo R Castañedo; Ricardo Medina; Claudio O Gualerzi
Journal:  Nucleic Acids Res       Date:  2012-08-31       Impact factor: 16.971

10.  Druggability analysis and classification of protein tyrosine phosphatase active sites.

Authors:  Mohammad A Ghattas; Noor Raslan; Asil Sadeq; Mohammad Al Sorkhy; Noor Atatreh
Journal:  Drug Des Devel Ther       Date:  2016-09-30       Impact factor: 4.162
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