A left-handed solution to peptide inhibition of the p53-MDM2 interaction

Angew Chem Int Ed Engl. 2010 May 10;49(21):3649-52. doi: 10.1002/anie.201000329.

Abstract

Throwing tumors a left hook punch: The oncoprotein MDM2 negatively regulates the activity and stability of the tumor suppressor protein p53, and is an important molecular target for anticancer therapy. Mirror image phage display identifies a high-affinity D-peptide ligand of MDM2 that can be developed into a potent and protease-resistant p53 activator with potential antitumor activity.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Drug Design
  • Enzyme Inhibitors / chemistry
  • Humans
  • Ligands
  • Molecular Sequence Data
  • Peptides / chemistry
  • Peptides / genetics
  • Peptides / pharmacology*
  • Proto-Oncogene Proteins c-mdm2 / antagonists & inhibitors*
  • Proto-Oncogene Proteins c-mdm2 / chemistry
  • Stereoisomerism

Substances

  • Enzyme Inhibitors
  • Ligands
  • Peptides
  • MDM2 protein, human
  • Proto-Oncogene Proteins c-mdm2

Associated data

  • PDB/3LNJ