Bridged peptide macrocycles as ligands for PDZ domain proteins

  • Udugamasooriya G
  • Saro D
  • Spaller M
  • 18


    Mendeley users who have this article in their library.
  • 30


    Citations of this 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.

Get free article suggestions today

Mendeley saves you time finding and organizing research

Sign up here
Already have an account ?Sign in

Find this document

Get full text


  • Gomika Udugamasooriya

  • Dorina Saro

  • Mark R. Spaller

Cite this document

Choose a citation style from the tabs below

Save time finding and organizing research with Mendeley

Sign up for free