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.
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Profile of Trofinetide in the Treatment of Rett Syndrome: Design, Development and Potential Place in Therapy.
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Scientific Institute IRCCS Eugenio Medea, Bosisio Parini, LC, Italy.
Trofinetide is a first-in-class pharmacological treatment proposed for patients with Rett Syndrome. It is a long half-life derivative of glycine-proline-glutamate, the tripeptide normally excided from Insulin-like Growth Factor 1 upon degradation. Due to containing glutamate and glycine in its structure, trofinetide is thought to act through NMDA receptor modulation, thus providing a normalization of neuronal activity and survival.
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J Clin Med
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Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Northern Border University, Rafha 91911, Saudi Arabia.
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Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN, USA; Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, TN, USA; Vanderbilt Kennedy Center, Vanderbilt University Medical Center, Nashville, TN, USA; Vanderbilt Brain Institute, Vanderbilt University School of Medicine, Nashville, TN, USA; Vanderbilt Institute of Chemical Biology, Vanderbilt University School of Medicine, Nashville, TN, USA. Electronic address:
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Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.
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The tripeptide H-Gly-Pro-Glu-OH (GPE) and its analogs began to take much interest from scientists for developing effective novel molecules in the treatment of several disorders including Alzheimer's disease, Parkinson's disease, and stroke. The peptidomimetics of GPEs exerted significant biological properties involving anti-inflammatory, antiapoptotic, and anticancer properties. The assessments of their hematological toxicity potentials are critically required for their possible usage in further preclinical and clinical trials against a wide range of pathological conditions.
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