New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
A suitable solid-phase approach, based on Fmoc/(t)Bu 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.
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
Casabona
Diego
D
Cativiela
Carlos
C
González-Muñiz
Rosario
R
Herranz
Rosario
R
Cenarruzabeitia
Edurne
E
Frechilla
Diana
D
Del Río
Joaquín
J
Jimeno
M Luisa
ML
García-López
M Teresa
MT
D000595:Amino Acid Sequence; D000818:Animals; D002478:Cells, Cultured; D006624:Hippocampus / Q000187:drug effects; D015394:Molecular Structure; D016202:N-Methylaspartate / Q000633:toxicity; D018696:Neuroprotective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D017470:Receptors, Glutamate / Q000378:metabolism; D013329:Structure-Activity Relationship; D014320:Triphenylmethyl Compounds / Q000737:chemistry
D018696:Neuroprotective Agents; D010455:Peptides; D017470:Receptors, Glutamate; D014320:Triphenylmethyl Compounds; D016202:N-Methylaspartate