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 receptors.
Alonso De Diego
Sergio A
SA
Instituto de Química Médica Juan de la Cierva, 3, 28006 Madrid, Spain.
Gutiérrez-Rodríguez
Marta
M
Pérez de Vega
M Jesús
MJ
González-Muñiz
Rosario
R
Herranz
Rosario
R
Martín-Martínez
Mercedes
M
Cenarruzabeitia
Edurne
E
Frechilla
Diana
D
Del Río
Joaquín
J
Jimeno
M Luisa
ML
García-López
M Teresa
MT
D000818:Animals; D001667:Binding, Competitive; D016923:Cell Death / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D018691:Excitatory Amino Acid Antagonists / Q000633:toxicity; D006624:Hippocampus / Q000166:cytology / Q000187:drug effects; D015394:Molecular Structure; D009474:Neurons / Q000187:drug effects* / Q000378:metabolism; D018696:Neuroprotective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011485:Protein Binding; D051381:Rats; D017470:Receptors, Glutamate / Q000187:drug effects* / Q000378:metabolism*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D018691:Excitatory Amino Acid Antagonists; D018696:Neuroprotective Agents; D009842:Oligopeptides; D017470:Receptors, Glutamate; C062053:glycyl-prolyl-glutamic acid