Embodiments of this invention include novel analogs of Glycyl-Prolyl-Glutamate (GPE) and compositions containing such analogs of GPE. Of these, certain analogs have modified proline residues. Other embodiments of this invention include uses of analogs of GPE to protect neural cells from degeneration and/or death in response to injury or disease. Disorders treatable with compounds and compositions of this invention include hypoxia/ischemia, toxic injury, and chronic neurodegenerative disorders including Parkinson's disease.
New Gly-Pro-Glu (GPE) analogues: Expedite solid-phase synthesis and biological activity
作者:Sergio A. Alonso De Diego、Marta Gutiérrez-Rodríguez、M. Jesús Pérez de Vega、Diego Casabona、Carlos Cativiela、Rosario González-Muñiz、Rosario Herranz、Edurne Cenarruzabeitia、Diana Frechilla、Joaquín Del Río、M. Luisa Jimeno、M. Teresa García-López
DOI:10.1016/j.bmcl.2005.11.040
日期:2006.3
A suitable solid-phase approach, based on Fmoc/Bu-t methodology and on the use of 2-chlorotrityl resin, allowed a rapid and efficient preparation of new GPE analogues. Most of the synthesized tripeptides displayed glutamate receptor binding affinity comparable to that of GPE, but only a few derivatives showed significant neuroprotective activity. (C) 2005 Elsevier Ltd. All rights reserved.