N,C-Capped dipeptides with selectivity for mycobacterial proteasome over human proteasomes: role of S3 and S1 binding pockets. Academic Article uri icon

Overview

abstract

  • We identified N,C-capped dipeptides that are selective for the Mycobacterium tuberculosis proteasome over human constitutive and immunoproteasomes. Differences in the S3 and S1 binding pockets appeared to account for the species selectivity. The inhibitors can penetrate mycobacteria and kill nonreplicating M. tuberculosis under nitrosative stress.

authors

  • Lin, Gang
  • Chidawanyika, Tamutenda
  • Tsu, Christopher
  • Warrier, Thulasi
  • Vaubourgeix, Julien
  • Blackburn, Christopher
  • Gigstad, Kenneth
  • Sintchak, Michael
  • Dick, Lawrence
  • Nathan, Carl F.

publication date

  • June 25, 2013

Research

keywords

  • Dipeptides
  • Mycobacterium tuberculosis
  • Proteasome Endopeptidase Complex

Identity

PubMed Central ID

  • PMC3773049

Scopus Document Identifier

  • 84880005002

Digital Object Identifier (DOI)

  • 10.1021/ja400021x

PubMed ID

  • 23782398

Additional Document Info

volume

  • 135

issue

  • 27