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  1. Article ; Online: Exploring structural determinants of neuroprotection bias on novel glypromate conjugates with bioactive amines.

    Silva-Reis, Sara C / Costa, Vera M / Correia da Silva, Daniela / Pereira, David M / Correia, Xavier Cruz / Costa-Almeida, Hugo F / García-Mera, Xerardo / Rodríguez-Borges, José E / Sampaio-Dias, Ivo E

    European journal of medicinal chemistry

    2024  Volume 267, Page(s) 116174

    Abstract: Neurodegenerative disorders of the central nervous system (CNS) such as Alzheimer's and Parkinson's diseases, afflict millions globally, posing a significant public health challenge. Despite extensive research, a critical hurdle in effectively treating ... ...

    Abstract Neurodegenerative disorders of the central nervous system (CNS) such as Alzheimer's and Parkinson's diseases, afflict millions globally, posing a significant public health challenge. Despite extensive research, a critical hurdle in effectively treating neurodegenerative diseases is the lack of neuroprotective drugs that can halt or reverse the underlying disease processes. In this work, we took advantage of the neuroprotective properties of the neuropeptide glycyl-l-prolyl-l-glutamic acid (Glypromate) for the development of new peptidomimetics using l-pipecolic acid as a proline surrogate and exploring their chemical conjugation with relevant active pharmaceutical ingredients (API) via a peptide bond. Together with prolyl-based Glypromate conjugates, a total of 36 conjugates were toxicologically and biologically evaluated. In this series, the results obtained showed that a constrained ring (l-proline) at the central position of the peptide motif accounts for enhanced toxicological profiles and biological effects using undifferentiated and differentiated human neuroblastoma SH-SY5Y cells. Additionally, it was shown that biased biological responses are API-dependent. Conjugation with (R)-1-aminoindane led to a 38-43% reduction of protein aggregation induced by Aβ
    MeSH term(s) Humans ; Neuroprotection ; Cell Line, Tumor ; Neuroblastoma/drug therapy ; Neuroprotective Agents/pharmacology ; Neuroprotective Agents/therapeutic use ; Oxidopamine/toxicity ; Oligopeptides/pharmacology ; Oligopeptides/therapeutic use ; Neurodegenerative Diseases ; Neuropeptides/pharmacology ; Apoptosis
    Chemical Substances glycyl-prolyl-glutamic acid (ZYK4RVV5LS) ; Neuroprotective Agents ; Oxidopamine (8HW4YBZ748) ; Oligopeptides ; Neuropeptides
    Language English
    Publishing date 2024-01-26
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2024.116174
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Concise Overview of Glypromate Neuropeptide Research: From Chemistry to Pharmacological Applications in Neurosciences.

    Silva-Reis, Sara C / Sampaio-Dias, Ivo E / Costa, Vera M / Correia, Xavier Cruz / Costa-Almeida, Hugo F / García-Mera, Xerardo / Rodríguez-Borges, José E

    ACS chemical neuroscience

    2023  Volume 14, Issue 4, Page(s) 554–572

    Abstract: Neurodegenerative diseases of the central nervous system (CNS) pose a serious health concern worldwide, with a particular incidence in developed countries as a result of life expectancy increase and the absence of restorative treatments. Presently, ... ...

    Abstract Neurodegenerative diseases of the central nervous system (CNS) pose a serious health concern worldwide, with a particular incidence in developed countries as a result of life expectancy increase and the absence of restorative treatments. Presently, treatments for these neurological conditions are focused on managing the symptoms and/or slowing down their progression. As so, the research on novel neuroprotective drugs is of high interest. Glypromate (glycyl-l-prolyl-l-glutamic acid, also known as GPE), an endogenous small peptide widespread in the brain, holds great promise to tackle neurodegenerative diseases such as Parkinson's, Alzheimer's, and Huntington's, s well as other CNS-related disorders like Rett and Down's syndromes. However, the limited pharmacokinetic properties of Glypromate hinder its clinical application. As such, intense research has been devoted to leveraging the pharmacokinetic profile of this neuropeptide. This review aims to offer an updated perspective on Glypromate research by exploring the vast array of chemical derivatizations of more than 100 analogs described in the literature over the past two decades. The collection and discussion of the most relevant structure-activity relationships will hopefully guide the discovery of new Glypromate-based neuroprotective drugs.
    MeSH term(s) Humans ; Neuroprotective Agents/therapeutic use ; Neuroprotective Agents/pharmacokinetics ; Neuropeptides ; Neurodegenerative Diseases/drug therapy ; Central Nervous System Diseases ; Neurosciences
    Chemical Substances glycyl-prolyl-glutamic acid (ZYK4RVV5LS) ; Neuroprotective Agents ; Neuropeptides
    Language English
    Publishing date 2023-02-03
    Publishing country United States
    Document type Journal Article ; Review ; Research Support, Non-U.S. Gov't
    ISSN 1948-7193
    ISSN (online) 1948-7193
    DOI 10.1021/acschemneuro.2c00675
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article: A Convenient On-Site Oxidation Strategy for the N-Hydroxylation of Melanostatin Neuropeptide Using Cope Elimination

    Sampaio-Dias, Ivo E. / Silva-Reis, Sara C. / Pires-Lima, Beatriz L. / Correia, Xavier Cruz / Costa-Almeida, Hugo F.

    Synthesis

    2021  Volume 54, Issue 08, Page(s) 2031–2036

    Abstract: A convenient synthetic protocol for the unprecedented N -hydroxylation of proline residue in Melanostatin (MIF-1) neuropeptide is reported. This methodology is grounded on the incorporation of N -(cyanoethyl)prolyl residue followed by on-site oxidation ...

    Abstract A convenient synthetic protocol for the unprecedented N -hydroxylation of proline residue in Melanostatin (MIF-1) neuropeptide is reported. This methodology is grounded on the incorporation of N -(cyanoethyl)prolyl residue followed by on-site oxidation by Cope elimination with m -chloroperbenzoic acid, exploring the unrecognized dual role of the cyanoethyl group as an effective N -protecting group under peptide synthesis conditions and as a suitable leaving group during the chemoselective on-site N -oxidation. Following this protocol N -hydroxy-MIF-1 is obtained in 78% global yield from N -(cyanoethyl)- l -proline. This synthetic approach opens a new avenue for access to N -hydroxylated Melanostatin analogues with direct application in neurochemistry and Parkinson’s research.
    Keywords Cope elimination ; Melanostatin ; Michael addition ; MIF-1 ; secondary hydroxylamines
    Language English
    Publishing date 2021-11-11
    Publisher Georg Thieme Verlag KG
    Publishing place Stuttgart ; New York
    Document type Article
    ZDB-ID 2033062-5
    ISSN 1437-210X ; 0039-7881
    ISSN (online) 1437-210X
    ISSN 0039-7881
    DOI 10.1055/a-1695-1095
    Database Thieme publisher's database

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