Bioorganic & Medicinal Chemistry Letters 2005-05-02

Analogues of the neuroprotective tripeptide Gly-Pro-Glu (GPE): synthesis and structure-activity relationships.

Sergio A Alonso De Diego, Pilar Muñoz, Rosario González-Muñiz, Rosario Herranz, Mercedes Martín-Martínez, Edurne Cenarruzabeitia, Diana Frechilla, Joaquín Del Río, M Luisa Jimeno, M Teresa García-López

Index: Bioorg. Med. Chem. Lett. 15 , 2279-83, (2005)

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Abstract

A series of GPE analogues, including modifications at the Pro and/or Glu residues, was prepared and evaluated for their NMDA binding and neuroprotective effects. Main results suggest that the pyrrolidine ring puckering of the Pro residue plays a key role in the biological responses, while the preference for cis or trans rotamers around the Gly-Pro peptide bond is not important.