ArticleJournal of diabetes investigation2015
Peptide modulators of alpha-glucosidase.
Article in Journal of diabetes investigation, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
7 citing papers in PubMed, 27 citations in OpenAlex.
- Molecular Networking-Based Metabolome, In Vitro Antidiabetic and Anti-Inflammatory Effects ofMetabolites · 2024Article
- An Update on Dipeptidyl Peptidase-IV Inhibiting Peptides.Current protein & peptide science · 2024Review
- UPLC-ESI-QTOF-MS Profiling of Phenolic Compounds fromMolecules (Basel, Switzerland) · 2022Article
- Protection against Oxidative Stress and Metabolic Alterations by Synthetic Peptides Derived fromAntioxidants (Basel, Switzerland) · 2022Article
- Antidiabetic bio-peptides of soft and hard wheat glutens.Food chemistry. Molecular sciences · 2022Article
- Alpha Glucosidase Inhibitory Activities of Plants with Focus on Common Vegetables.Plants (Basel, Switzerland) · 2019Review
- High-Throughput Approaches in Carbohydrate-Active Enzymology: Glycosidase and Glycosyl Transferase Inhibitors, Evolution, and Discovery.Angewandte Chemie (International ed. in English) · 2019Review
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
AIMS/
introductionAcute glucose fluctuations during the postprandial period pose great risk for cardiovascular complications and thus represent an important therapeutic approach in type 2 diabetes. In the present study, screening of peptide libraries was used to select peptides with an affinity towards mammalian intestinal alpha-glucosidase as potential leads in antidiabetic agent development. MATERIALS AND
methodsThree phage-displayed peptide libraries were used in independent selections with different elution strategies to isolate target-binding peptides. Selected peptides displayed on phage were tested to compete for an enzyme-binding site with known competitive inhibitors, acarbose and voglibose. The four best performing peptides were synthesized. Their binding to the mammalian alpha-glucosidase and their effect on enzyme activity were evaluated.
resultsTwo linear and two cyclic heptapeptides with high affinity towards intestinal alpha-glucosidase were selected. Phage-displayed as well as synthetic peptides bind into or to the vicinity of the active site on the enzyme. Both cyclic peptides inhibited enzyme activity, whereas both linear peptides increased enzyme activity.
conclusionsAlthough natural substrates of glycosidase are polysaccharides, in the present study we successfully isolated novel peptide modulators of alpha-glucosidase. Modulatory activity of selected peptides could be further optimized through peptidomimetic design. They represent promising leads for development of efficient alpha-glucosidase inhibitors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.