ArticleMolecules (Basel, Switzerland)2026
Novel Small Molecule GLP-1R Agonists Based on 1
Elena V Tolkacheva, Tagir L Salakhov, Alexandr Yu Saliev, Natalia D Lebedeva, Alisa M Krasnodubets, Eugene Y Smirnov, Sergey A Silonov, Konstantin V Balakin, Vladimir V Chernyshov, Roman A Ivanov
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In one paragraphArticle in Molecules (Basel, Switzerland), 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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5 · Who and what moneyAuthors and funding
10 authors.
Elena V TolkachevaMedicinal Biotechnology Department, Sirius University of Science and Technology, Olimpiyskiy Ave. 1, Sirius 354340, Krasnodar Region, Russia.ORCID 0009-0003-1039-5093 Tagir L SalakhovMedicinal Biotechnology Department, Sirius University of Science and Technology, Olimpiyskiy Ave. 1, Sirius 354340, Krasnodar Region, Russia.
Alexandr Yu SalievMedicinal Biotechnology Department, Sirius University of Science and Technology, Olimpiyskiy Ave. 1, Sirius 354340, Krasnodar Region, Russia.ORCID 0009-0000-6724-135X Natalia D LebedevaMedicinal Biotechnology Department, Sirius University of Science and Technology, Olimpiyskiy Ave. 1, Sirius 354340, Krasnodar Region, Russia.
Alisa M KrasnodubetsMedicinal Biotechnology Department, Sirius University of Science and Technology, Olimpiyskiy Ave. 1, Sirius 354340, Krasnodar Region, Russia.
Eugene Y SmirnovLaboratory of Structural Dynamics, Stability and Folding of Proteins, Institute of Cytology, Russian Academy of Sciences, Tikhoretsky Ave. 4, St. Petersburg 194064, Russia.ORCID 0000-0002-6047-5652 Sergey A SilonovLaboratory of Structural Dynamics, Stability and Folding of Proteins, Institute of Cytology, Russian Academy of Sciences, Tikhoretsky Ave. 4, St. Petersburg 194064, Russia.ORCID 0000-0001-8714-6659 Konstantin V BalakinInstitute of Future Biophysics, Institutsky Lane, 9, Dolgoprudny 141700, Moscow Region, Russia.ORCID 0000-0001-7611-0802 Vladimir V ChernyshovMedicinal Biotechnology Department, Sirius University of Science and Technology, Olimpiyskiy Ave. 1, Sirius 354340, Krasnodar Region, Russia.ORCID 0000-0003-1347-4398 Roman A IvanovMedicinal Biotechnology Department, Sirius University of Science and Technology, Olimpiyskiy Ave. 1, Sirius 354340, Krasnodar Region, Russia.ORCID 0000-0002-9573-4183 Funding
Ministry of Science and Higher Education of the Russian Federation 075-10-2025-017
6 · The paper itselfAbstract
Glucagon-like peptide-1 (GLP-1) is an incretin hormone secreted by intestinal endocrine L cells that activates the GLP-1 receptor (GLP-1R), leading to glucose-dependent insulin secretion and suppression of glucagon release. In recent years, GLP-1R agonists (GLP-1RAs) have become one of the leading therapeutic options for the treatment of type 2 diabetes mellitus; however, for a long time clinically approved GLP-1RAs were limited to peptide drugs unsuitable for oral administration. The discovery of the "first-in-class" small molecule agonist danuglipron in 2018 demonstrated the feasibility of orally available GLP-1RAs and stimulated the development of numerous danuglipron-like compounds, some of which showed increased efficacy over the prototype. In this study, we report the design and synthesis of novel GLP-1RAs based on a regioisomeric danuglipron scaffold, 1
Indexed as
BenzimidazolesGlucagon-Like Peptide-1 Receptor AgonistsHypoglycemic AgentsAnimalsCyclic AMPGlucagon-Like Peptide 1Glucagon-Like Peptide-1 ReceptorHumansStructure-Activity RelationshipBenzimidazolesCyclic AMPGlucagon-Like Peptide 1Glucagon-Like Peptide-1 ReceptorGlucagon-Like Peptide-1 Receptor AgonistsHypoglycemic Agents1H-benzo[d]imidazole-5-carboxylic acid derivativescAMP assayGLP-1RAs“next-in-class” agonistssmall moleculesT2DM
Identifiers
PMID41976172
PMCPMC13075017
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