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

J Med Chem. 2014 Mar 27;57(6):2357-67. doi: 10.1021/jm401705g. Epub 2014 Mar 14.

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.

MeSH terms

  • Cathepsin C / antagonists & inhibitors*
  • Humans
  • Indicators and Reagents
  • Models, Molecular
  • Molecular Conformation
  • Protease Inhibitors / chemical synthesis*
  • Protease Inhibitors / pharmacology*
  • Recombinant Proteins / chemistry
  • Spectrometry, Fluorescence
  • Structure-Activity Relationship
  • Substrate Specificity
  • X-Ray Diffraction

Substances

  • Indicators and Reagents
  • Protease Inhibitors
  • Recombinant Proteins
  • Cathepsin C