NMR solution structure of a peptide from the mdm-2 binding domain of the p53 protein that is selectively cytotoxic to cancer cells

Biochemistry. 2004 Feb 24;43(7):1854-61. doi: 10.1021/bi035718g.

Abstract

We have recently found that a peptide from the mdm-2 binding domain of the p53 protein induced rapid membranolytic necrosis of a variety of different human cancer cell lines. To determine the role of solution structure in this peptide's selective and rapid tumor membrane disruptive behavior, we have performed two-dimensional NMR on a 32-residue sequence called PNC-27, in both an aqueous cytosolic-like and a mixed organic membrane-mimetic solution environment. In an aqueous milieu, PNC-27 contains three alpha-helical domains connected by loop structures, forming an S shape, and another similar structure with less helical structure. In a solution environment simulating a membrane, the helical domains found in water increase in length, forming three classes of structures, all of which form a U-shaped helix-coil-helix ensemble. In both solvent systems, this peptide forms amphipathic structures such that its hydrophobic residues coalesce on one face while the polar residues aggregate on the opposite face. The ability to form these unique structures in these two solution environments may allow the PNC-27 peptide to selectively and rapidly disrupt cancer cell membranes.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Motifs
  • Amino Acid Sequence
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / toxicity*
  • Cell Line, Tumor
  • Cell Membrane / chemistry
  • Cell Membrane / metabolism
  • Crystallography, X-Ray
  • Humans
  • Molecular Sequence Data
  • Nuclear Magnetic Resonance, Biomolecular / methods
  • Nuclear Proteins / metabolism*
  • Peptide Fragments / chemistry*
  • Peptide Fragments / metabolism
  • Peptide Fragments / toxicity*
  • Protein Binding
  • Protein Conformation
  • Protein Structure, Secondary
  • Protein Structure, Tertiary
  • Proto-Oncogene Proteins / metabolism*
  • Proto-Oncogene Proteins c-mdm2
  • Solvents
  • Tumor Suppressor Protein p53 / chemistry*
  • Tumor Suppressor Protein p53 / metabolism
  • Tumor Suppressor Protein p53 / toxicity*
  • Water

Substances

  • Antineoplastic Agents
  • Nuclear Proteins
  • Peptide Fragments
  • Proto-Oncogene Proteins
  • Solvents
  • Tumor Suppressor Protein p53
  • Water
  • MDM2 protein, human
  • Proto-Oncogene Proteins c-mdm2

Associated data

  • PDB/1Q2F
  • PDB/1Q2I