Literature DB >> 24592859

Cathepsin C inhibitors: property optimization and identification of a clinical candidate.

Mark Furber1, Anna-Karin Tiden, Philip Gardiner, Antonio Mete, Rhonan Ford, Ian Millichip, Linda Stein, Andrew Mather, Elizabeth Kinchin, Christopher Luckhurst, Simon Barber, Peter Cage, Hitesh Sanganee, Rupert Austin, Kamaldeep Chohan, Raj Beri, Bob Thong, Alan Wallace, Victor Oreffo, Ray Hutchinson, Steve Harper, Judit Debreczeni, Jason Breed, Lisa Wissler, Karl Edman.   

Abstract

A lead generation and optimization program delivered the highly selective and potent CatC inhibitor 10 as an in vivo tool compound and potential development candidate. Structural studies were undertaken to generate SAR understanding.

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Year:  2014        PMID： 24592859     DOI： 10.1021/jm401705g

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


  7 in total

1.  DPP1 Inhibitors: Exploring the Role of Water in the S2 Pocket of DPP1 with Substituted Pyrrolidines.

Authors:  Helena Käck; Kevin Doyle; Samantha J Hughes; Michael S Bodnarchuk; Hans Lönn; Amanda Van De Poël; Nicholas Palmer
Journal:  ACS Med Chem Lett       Date:  2019-07-15       Impact factor: 4.345

Review 2.  Cysteine proteases as therapeutic targets: does selectivity matter? A systematic review of calpain and cathepsin inhibitors.

Authors:  Marton Siklos; Manel BenAissa; Gregory R J Thatcher
Journal:  Acta Pharm Sin B       Date:  2015-09-26       Impact factor: 11.413

3.  Characterization of P. falciparum dipeptidyl aminopeptidase 3 specificity identifies differences in amino acid preferences between peptide-based substrates and covalent inhibitors.

Authors:  Laura E de Vries; Mateo I Sanchez; Katarzyna Groborz; Laurie Kuppens; Marcin Poreba; Christine Lehmann; Neysa Nevins; Chrislaine Withers-Martinez; David J Hirst; Fang Yuan; Shirin Arastu-Kapur; Martin Horn; Michael Mares; Matthew Bogyo; Marcin Drag; Edgar Deu
Journal:  FEBS J       Date:  2019-06-24       Impact factor: 5.542

4.  Identification of Plasmodium dipeptidyl aminopeptidase allosteric inhibitors by high throughput screening.

Authors:  Mateo I Sanchez; Laura E de Vries; Christine Lehmann; Jeong T Lee; Kenny K Ang; Christopher Wilson; Steven Chen; Michelle R Arkin; Matthew Bogyo; Edgar Deu
Journal:  PLoS One       Date:  2019-12-18       Impact factor: 3.240

5.  Proteome-wide Map of Targets of T790M-EGFR-Directed Covalent Inhibitors.

Authors:  Sherry Niessen; Melissa M Dix; Sabrina Barbas; Zachary E Potter; Shuyan Lu; Oleg Brodsky; Simon Planken; Douglas Behenna; Chau Almaden; Ketan S Gajiwala; Kevin Ryan; RoseAnn Ferre; Michael R Lazear; Matthew M Hayward; John C Kath; Benjamin F Cravatt
Journal:  Cell Chem Biol       Date:  2017-09-28       Impact factor: 8.116

6.  Neutrophil maturation rate determines the effects of dipeptidyl peptidase 1 inhibition on neutrophil serine protease activity.

Authors:  P Gardiner; C Wikell; S Clifton; J Shearer; A Benjamin; S A Peters
Journal:  Br J Pharmacol       Date:  2016-07-07       Impact factor: 8.739

Review 7.  Lung Protection by Cathepsin C Inhibition: A New Hope for COVID-19 and ARDS?

Authors:  Brice Korkmaz; Adam Lesner; Sylvain Marchand-Adam; Celia Moss; Dieter E Jenne
Journal:  J Med Chem       Date:  2020-08-07       Impact factor: 7.446
  7 in total

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