Identification of very potent inhibitor of human aminopeptidase N (CD13)

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2497-9. doi: 10.1016/j.bmcl.2010.02.111. Epub 2010 Mar 4.

Abstract

In this Letter we describe broad comparision studies toward rat, pig, and human aminopeptidase N (CD13) orthologs using phosphinate inhibitors related in structure to hydroxamic acids. This SAR approach yielded a very potent inhibitor of human aminopeptidase N: alpha(1)-amino-3-phenylpropyl(alpha(2)-hydroxy-3-phenylpropyl)phosphinic acid with an IC(50)=60 nM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CD13 Antigens / antagonists & inhibitors*
  • Humans
  • Inhibitory Concentration 50
  • Protease Inhibitors / chemistry
  • Protease Inhibitors / pharmacology*

Substances

  • Protease Inhibitors
  • CD13 Antigens