Bridged peptide macrocycles as ligands for PDZ domain proteins.

Journal Article (Journal Article)

[reaction: see text] Conformationally constrained side chain-bridged cyclic peptides were prepared using bis-carboxylic acid ring spacers. These macrocyles were designed to inhibit protein-protein interactions mediated by the third PDZ domain (PDZ3) of a mammalian neuronal protein, PSD-95. Isothermal titration calorimetry (ITC) experiments measured dissociation constants in the low micromolar range. For each compound, the change in entropy (TdeltaS) of binding either is comparable in magnitude to the enthalpy change (deltaH) or is the predominant driving force for association.

Full Text

Duke Authors

Cited Authors

  • Udugamasooriya, G; Saro, D; Spaller, MR

Published Date

  • March 2005

Published In

Volume / Issue

  • 7 / 7

Start / End Page

  • 1203 - 1206

PubMed ID

  • 15787467

Electronic International Standard Serial Number (EISSN)

  • 1523-7052

International Standard Serial Number (ISSN)

  • 1523-7060

Digital Object Identifier (DOI)

  • 10.1021/ol0475966


  • eng