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 |
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creator | 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 |
description | 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. |
doi_str_mv | 10.1016/j.bmcl.2006.04.033 |
format | Article |
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Jesús ; González-Muñiz, Rosario ; Herranz, Rosario ; Martín-Martínez, Mercedes ; Cenarruzabeitia, Edurne ; Frechilla, Diana ; Río, Joaquín Del ; Jimeno, M. Luisa ; García-López, M. Teresa</creator><creatorcontrib>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</creatorcontrib><description>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.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2006.04.033</identifier><identifier>PMID: 16650992</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>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. 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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.</description><subject>Animals</subject><subject>Binding, Competitive</subject><subject>Biological and medical sciences</subject><subject>Cell Death - drug effects</subject><subject>Dose-Response Relationship, Drug</subject><subject>Excitatory Amino Acid Antagonists - toxicity</subject><subject>Glutamate receptors binding</subject><subject>Glutamatergic system (aspartate and other excitatory aminoacids)</subject><subject>GPE</subject><subject>Hippocampus - cytology</subject><subject>Hippocampus - drug effects</subject><subject>Medical sciences</subject><subject>Molecular Structure</subject><subject>Neurons - drug effects</subject><subject>Neurons - metabolism</subject><subject>Neuropharmacology</subject><subject>Neuroprotection</subject><subject>Neuroprotective agent</subject><subject>Neuroprotective Agents - chemical synthesis</subject><subject>Neuroprotective Agents - chemistry</subject><subject>Neuroprotective Agents - pharmacology</subject><subject>Neurotransmitters. 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Drug treatments</subject><subject>Protein Binding</subject><subject>Rats</subject><subject>Receptors, Glutamate - drug effects</subject><subject>Receptors, Glutamate - metabolism</subject><subject>Stereoisomerism</subject><subject>Structure-Activity Relationship</subject><subject>Tripeptides</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2006</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1v1DAQhi0EokvhD3BAvsAtYezY-ZC4oKoUpEpwKBI3y7HHW6-SeLGdVv33ONqVeuPike3nHc08hLxnUDNg7edDPc5mqjlAW4OooWlekB0TragaAfIl2cHQQtUP4s8FeZPSAYAJEOI1uWBtK2EY-I7ku3ukC64xHGPIaLJ_QKq34vMTDY7e_LqmOfojHrO35WvRU9ivmKgN5VhCpibEiJPOSB99vqf7ac163q4RTUmFSEe_WL_sqXbOL6XvW_LK6Snhu3O9JL-_Xd9dfa9uf978uPp6WxnBZK7QybaXXTOaUXLHJLTMaDP0lvHOYc-NkX1THmRvO9bxfuzk0AvreNMYg1Y0l-TTqW_Z7W-ZOavZJ4PTpBcMa1KsxLoBZAH5CTQxpBTRqWP0s45PioHaXKuD2lyrzbUCoYrrEvpw7r6OM9rnyFluAT6eAZ2MnlzUi_Hpmet6AM427suJw-LiwWNUyXhcygq-KMzKBv-_Of4Bt8CfcA</recordid><startdate>20060701</startdate><enddate>20060701</enddate><creator>Alonso De Diego, Sergio A.</creator><creator>Gutiérrez-Rodríguez, Marta</creator><creator>Pérez de Vega, M. 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Jesús ; González-Muñiz, Rosario ; Herranz, Rosario ; Martín-Martínez, Mercedes ; Cenarruzabeitia, Edurne ; Frechilla, Diana ; Río, Joaquín Del ; Jimeno, M. Luisa ; García-López, M. 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subjects | 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 |
title | The neuroprotective activity of GPE tripeptide analogues does not correlate with glutamate receptor binding affinity |
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