Bridged peptide macrocycles as ligands for PDZ domain proteins |
| |
Authors: | Udugamasooriya Gomika Saro Dorina Spaller Mark R |
| |
Affiliation: | Department of Chemistry, Wayne State University, Detroit, Michigan 48202, USA. |
| |
Abstract: | [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. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|