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  • An overview, advantages and therapeutic potential of non-peptide positive allosteric modulators of glucagon-like peptide-1 receptor [Elektronski vir]
    Smelcerović, Andrija ...
    Due to uncomfortable injection regimens of peptidic agonists of glucagon-like peptide 1 receptor (GLP-1R), orally available non-peptide positive allosteric modulators (PAMs) of GLP-1 receptors are ... foreseen as the possible future mainstream therapy of diabetes type 2. In this article we review current GLP-1R PAMs. Based on the effectiveness and in silico predicted physico-chemical properties, pharmacokinetics and toxicity, possible candidates for further development as oral drugs were selected. Our suggestion is that GLP-1R PAMs might be used per os alone or in combination with dipeptidyl peptidase-4 (DPP-4) inhibitors, which could offer an optimal treatment option next to metformin monotherapy in diabetes mellitus type 2, or in a wider spectrum of indications. Quercetin acts as GLP-1R PAM and DPP-4 inhibitor, and therefore might be considered as a pioneer agent with dual mechanism of action in terms of GLP-1R positive allosteric modulation and DPP-4 inhibition for potentiating GLP-1 dependent effects.
    Source: ChemMedChem. - ISSN 1860-7187 (Vol. 14, iss. 5, 2019, str. 514-521)
    Type of material - e-article
    Publish date - 2019
    Language - english
    COBISS.SI-ID - 4658033

    Link(s):

    https://onlinelibrary.wiley.com/doi/pdf/10.1002/cmdc.201800699
    DOI

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