Designed inhibitors of insulin-degrading enzyme regulate the catabolism and activity of insulin Academic Article uri icon

Overview

MeSH Major

  • Drug Design
  • Enzyme Inhibitors
  • Insulin
  • Insulysin

abstract

  • The inhibitors we describe are the first to potently and selectively inhibit IDE or indeed any member of this atypical zinc-metalloprotease superfamily. The distinctive structure of IDE's active site, and the mode of action of our inhibitors, suggests that it may be possible to develop inhibitors that cross-react minimally with conventional zinc-metalloproteases. Significantly, our results reveal that insulin signaling is normally regulated by IDE activity not only extracellularly but also within cells, supporting the longstanding view that IDE inhibitors could hold therapeutic value for the treatment of diabetes.

publication date

  • September 14, 2010

Research

keywords

  • Academic Article

Identity

Language

  • eng

PubMed Central ID

  • PMC2866327

Digital Object Identifier (DOI)

  • 10.1371/journal.pone.0010504

PubMed ID

  • 20498699

Additional Document Info

start page

  • e10504

volume

  • 5

number

  • 5