ArticlePloS one2008
Boc5, a non-peptidic glucagon-like Peptide-1 receptor agonist, invokes sustained glycemic control and weight loss in diabetic mice.
Article in PloS one, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 46 citations in OpenAlex.
- Short-term administration of the GLP-1 analog liraglutide decreases circulating leptin and increases GIP levels and these changes are associated with alterations in CNS responses to food cues: A randomized, placebo-controlled, crossover study.Metabolism: clinical and experimental · 2016Trial
- Small-Molecule GLP-1 Receptor Agonists: A Promising Pharmacological Approach.Medicina (Kaunas, Lithuania) · 2025Review
- The Discovery and Development of Glucagon-Like Peptide-1 Receptor Agonists.Current medicinal chemistry · 2024Review
- Structural basis of peptidomimetic agonism revealed by small- molecule GLP-1R agonists Boc5 and WB4-24.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Non-peptide agonists and positive allosteric modulators of glucagon-like peptide-1 receptors: Alternative approaches for treatment of Type 2 diabetes.British journal of pharmacology · 2022Review
- DeepCPI: A Deep Learning-based Framework for Large-scale in silico Drug Screening.Genomics, proteomics & bioinformatics · 2019Article
- Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic Successes.Pharmacological reviews · 2016Review
- Landmark studies on the glucagon subfamily of GPCRs: from small molecule modulators to a crystal structure.Acta pharmacologica Sinica · 2015Review
- The class B G-protein-coupled GLP-1 receptor: an important target for the treatment of type-2 diabetes mellitus.International journal of obesity supplements · 2014Review
- Regulation of glucose homeostasis by GLP-1.Progress in molecular biology and translational science · 2014Review
- Clinical application of glucagon-like Peptide 1 receptor agonists for the treatment of type 2 diabetes mellitus.Endocrinology and metabolism (Seoul, Korea) · 2013Review
- The structure and function of the glucagon-like peptide-1 receptor and its ligands.British journal of pharmacology · 2012Review
- A continued saga of Boc5, the first non-peptidic glucagon-like peptide-1 receptor agonist with in vivo activities.Acta pharmacologica Sinica · 2012Review
- Reversal of obesity and insulin resistance by a non-peptidic glucagon-like peptide-1 receptor agonist in diet-induced obese mice.PloS one · 2010Article
- Non-peptidic glucose-like peptide-1 receptor agonists: aftermath of a serendipitous discovery.Acta pharmacologica Sinica · 2010Article
Corrections and comments
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Authors and funding
11 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundOur recent discovery of the substituted cyclobutane Boc5, one of the first non-peptidic agonists at glucagon-like peptide-1 receptors, offers the potential of combining oral availability with full agonism capable of eliciting antidiabetic and antiobesity effects. The present study was aimed at determining the in vivo pharmacologic properties of Boc5 in both normal and diabetic mice following chronic administration, with emphasis on glycemic control and weight loss. METHODOLOGY/PRINCIPAL
findingsC57BL/6J and db/db mice were treated daily with Boc5 for 4 weeks and a range of pharmacologic parameters, including hemoglobin A1c, intraperitoneal glucose tolerance, insulin tolerance, fasting insulin and leptin levels, food intake, body weight and fat mass, were assessed before and after the treatment. Effects on food intake, gastric emptying, and insulinogenic index were also investigated in animals acutely administered with Boc5. Boc5 (3 mg) was able to induce a durable restoration of glycemic control (normalization of both hemoglobin A1c and intraperitoneal glucose tolerance) in db/db mice, following 4 weeks of daily administration. As with peptidic glucagon-like peptide-1 receptor agonists, its glycemic benefit and weight (fat) loss were associated with dose-dependent effects that included reduction in food intake, slowing of gastric emptying (both of which reduce nutrient-drive at beta-cells), stimulation of insulin secretion (which was glucose-dependent), and elevation in insulin sensitivity. There was little effect on normal mice treated in the same manner. CONCLUSIONS/SIGNIFICANCE: Our findings suggest that Boc5 is the only non-peptidic molecule reported thus far to simultaneously activate this spectrum of antidiabetic effects.
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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.