ArticleScientific reports2016
Synthetic small molecule GLP-1 secretagogues prepared by means of a three-component indole annulation strategy.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed.
- GLP-1 receptor agonist properties of a chimeric peptide derived by hybridization of Latrodectus αLatrotoxin and Heloderma Exendin-4.General and comparative endocrinology · 2025Article
- Review
- Enantioselective synthesis and selective functionalization of 4-aminotetrahydroquinolines as novel GLP-1 secretagogues.Chirality · 2022Article
- Incretin drugs in diabetic kidney disease: biological mechanisms and clinical evidence.Nature reviews. Nephrology · 2021Review
- Nucleophile-intercepted Beckmann fragmentation reactions.Chemical science · 2019Article
- Comparison of ELISA and HPLC-MS methods for the determination of exenatide in biological and biotechnology-based formulation matrices.Journal of pharmaceutical analysis · 2019Review
- Catechol estrogens stimulate insulin secretion in pancreatic β-cells via activation of the transient receptor potential A1 (TRPA1) channel.The Journal of biological chemistry · 2019Article
- Polygonum aviculare L. extract and quercetin attenuate contraction in airway smooth muscle.Scientific reports · 2018Article
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- Article
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10 authors.
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Abstract
Rational assembly of small molecule libraries for purposes of drug discovery requires an efficient approach in which the synthesis of bioactive compounds is enabled so that numerous structurally related compounds of a similar basic formulation can be derived. Here, we describe (4 + 3) and (3 + 2) indole annulation strategies that quickly generate complex indole heterocycle libraries that contain novel cyclohepta- and cyclopenta[b]indoles, respectively. Screening of one such library comprised of these indoles identifies JWU-A021 to be an especially potent stimulator of glucagon-like peptide-1 (GLP-1) secretion in vitro. Surprisingly, JWU-A021 is also a potent stimulator of Ca(2+) influx through TRPA1 cation channels (EC50 ca. 200 nM), thereby explaining its ability to stimulate GLP-1 release. Of additional importance, the available evidence indicates that JWU-A021 is one of the most potent non-electrophilic TRPA-1 channel agonists yet to be reported in the literature.
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