| Literature DB >> 24900293 |
Dramane Lainé1, Michael Palovich1, Brent McCleland1, Emilie Petitjean1, Isabelle Delhom1, Haibo Xie1, Jianghe Deng1, Guoliang Lin1, Roderick Davis1, Anais Jolit1, Neysa Nevins1, Baoguang Zhao1, Jim Villa1, Jessica Schneck1, Patrick McDevitt1, Robert Midgett1, Casey Kmett1, Sandra Umbrecht1, Brian Peck1, Alicia Bacon Davis1, David Bettoun1.
Abstract
The discovery of potent and selective cyanamide-based inhibitors of the cysteine protease cathepsin C is detailed. Optimization of the template with regard to plasma stability led to the identification of compound 17, a potent cathepsin C inhibitor with excellent selectivity over other cathepsins and potent in vivo activity in a cigarette smoke mouse model.Entities:
Keywords: Cathepsin C inhibitors; cigarette smoke; cyanamides; potent; selective
Year: 2010 PMID: 24900293 PMCID: PMC4018094 DOI: 10.1021/ml100212k
Source DB: PubMed Journal: ACS Med Chem Lett ISSN: 1948-5875 Impact factor: 4.345