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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-articlePublish date - 2019Language - englishCOBISS.SI-ID - 4658033
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Smelcerović, Andrija | |
Lazarević, Jelena, kemik | |
Tomović, Katarina | |
Anastasijevic, Marija | |
Jukič, Marko | 32587 |
Kocić, Gordana | |
Anderluh, Marko | 21456 |
Source: Personal bibliographies
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