ReviewActa pharmacologica Sinica2012
A continued saga of Boc5, the first non-peptidic glucagon-like peptide-1 receptor agonist with in vivo activities.
Review in Acta pharmacologica Sinica, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
13 citing papers in PubMed, 36 citations in OpenAlex.
- From Phytochemistry to Metabolic Regulation: The Insulin-Promoting Effects of Loureirin B Analogous to an Agonist of GLP-1 Receptor.International journal of molecular sciences · 2025Article
- Small-Molecule GLP-1 Receptor Agonists: A Promising Pharmacological Approach.Medicina (Kaunas, Lithuania) · 2025Review
- Synthesis of Bis(amino acids) Containing the Styryl-cyclobutane Core by Photosensitized [2+2]-Cross-cycloaddition of Allylidene-5(4International journal of molecular sciences · 2023Article
- 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
- Stereoselective, Ruthenium-Photocatalyzed Synthesis of 1,2-Diaminotruxinic Bis-amino Acids from 4-Arylidene-5(4The Journal of organic chemistry · 2022Article
- A quinoxaline-based compound ameliorates bone loss in ovariectomized mice.Experimental biology and medicine (Maywood, N.J.) · 2021Article
- 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
- Differential Requirement of the Extracellular Domain in Activation of Class B G Protein-coupled Receptors.The Journal of biological chemistry · 2016Article
- Landmark studies on the glucagon subfamily of GPCRs: from small molecule modulators to a crystal structure.Acta pharmacologica Sinica · 2015Review
- The non-peptide GLP-1 receptor agonist WB4-24 blocks inflammatory nociception by stimulating β-endorphin release from spinal microglia.British journal of pharmacology · 2015Article
- Clinical application of glucagon-like Peptide 1 receptor agonists for the treatment of type 2 diabetes mellitus.Endocrinology and metabolism (Seoul, Korea) · 2013Review
- A β-peptide agonist of the GLP-1 receptor, a class B GPCR.Organic letters · 2013Article
Corrections and comments
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Authors and funding
13 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Glucagon-like peptide-1 (GLP-1)-based therapy presents a promising option for treating type 2 diabetes. However, there are several limitations relative to the peptidic GLP-1 mimetics currently on the market or under development. This concern has led to a continued interest in the search for non-peptidic agonists for GLP-1 receptor (GLP-1R). Here, we briefly review the discovery, characterization and current status of a novel class of cyclobutane-derivative-based non-peptidic agonists for GLP-1R, including Boc5 and its newly discovered analogue WB4-24. Although the oral bioavailability of such compounds still poses great challenges, the progress made so far encourages us to identify a truly 'druggable' small molecule agonist for GLP-1R.
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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.