The neuroprotective activity of GPE tripeptide analogues does not correlate with glutamate receptor binding affinity

The influence of several modifications on the GPE tripeptide structure upon the binding to GluRs and on their neuroprotective effects has been studied. The results indicated that the prevention of neuronal death showed by GPE and some analogues is not directly related to their affinity at glutamate...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-07, Vol.16 (13), p.3396-3400
Hauptverfasser:	Alonso De Diego, Sergio A., Gutiérrez-Rodríguez, Marta, Pérez de Vega, M. Jesús, González-Muñiz, Rosario, Herranz, Rosario, Martín-Martínez, Mercedes, Cenarruzabeitia, Edurne, Frechilla, Diana, Río, Joaquín Del, Jimeno, M. Luisa, García-López, M. Teresa
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Binding, Competitive Biological and medical sciences Cell Death - drug effects Dose-Response Relationship, Drug Excitatory Amino Acid Antagonists - toxicity Glutamate receptors binding Glutamatergic system (aspartate and other excitatory aminoacids) GPE Hippocampus - cytology Hippocampus - drug effects Medical sciences Molecular Structure Neurons - drug effects Neurons - metabolism Neuropharmacology Neuroprotection Neuroprotective agent Neuroprotective Agents - chemical synthesis Neuroprotective Agents - chemistry Neuroprotective Agents - pharmacology Neurotransmitters. Neurotransmission. Receptors Oligopeptides - chemical synthesis Oligopeptides - chemistry Oligopeptides - pharmacology Peptidomimetics Pharmacology. Drug treatments Protein Binding Rats Receptors, Glutamate - drug effects Receptors, Glutamate - metabolism Stereoisomerism Structure-Activity Relationship Tripeptides
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Zusammenfassung:	The influence of several modifications on the GPE tripeptide structure upon the binding to GluRs and on their neuroprotective effects has been studied. The results indicated that the prevention of neuronal death showed by GPE and some analogues is not directly related to their affinity at glutamate receptors.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.04.033