ArticleBiochemical pharmacology2010
Activation of distinct P2Y receptor subtypes stimulates insulin secretion in MIN6 mouse pancreatic beta cells.
Article in Biochemical pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 36 citations in OpenAlex.
- The purinergic signalling and inflammation in the pathogenesis and progression of diabetes: key factors and therapeutic targets.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2022Review
- Article
- Potential Therapeutic Targeting Neurotransmitter Receptors in Diabetes.Frontiers in endocrinology · 2022Review
- Purinergic signaling in diabetes and metabolism.Biochemical pharmacology · 2021Review
- The regulatory G protein signaling complex, Gβ5-R7, promotes glucose- and extracellular signal-stimulated insulin secretion.The Journal of biological chemistry · 2020Article
- The P2X7 receptor and pannexin-1 are involved in glucose-induced autocrine regulation in β-cells.Scientific reports · 2018Article
- Signals in the pancreatic islet microenvironment influence β-cell proliferation.Diabetes, obesity & metabolism · 2017Review
- Thymidine 5'-O-monophosphorothioate induces HeLa cell migration by activation of the P2Y6 receptor.Purinergic signalling · 2016Article
- Important roles of P2Y receptors in the inflammation and cancer of digestive system.Oncotarget · 2016Review
- Purinergic signalling in endocrine organs.Purinergic signalling · 2014Review
- Purinergic signalling and diabetes.Purinergic signalling · 2013Review
- Minireview: Novel aspects of M3 muscarinic receptor signaling in pancreatic β-cells.Molecular endocrinology (Baltimore, Md.) · 2013Review
- 4-Alkyloxyimino-cytosine nucleotides: tethering approaches to molecular probes for the P2YMedChemComm · 2013Article
- AMP-activated protein kinase as regulator of P2Y(6) receptor-induced insulin secretion in mouse pancreatic β-cells.Biochemical pharmacology · 2013Article
- Spinophilin as a novel regulator of M3 muscarinic receptor-mediated insulin release in vitro and in vivo.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2012Article
- Molecular Structure of P2Y Receptors: Mutagenesis, Modeling, and Chemical Probes.Wiley interdisciplinary reviews. Membrane transport and signaling · 2012Article
- Virtual screening leads to the discovery of novel non-nucleotide P2Y₁ receptor antagonists.Bioorganic & medicinal chemistry · 2012Article
- G protein-coupled adenosine (P1) and P2Y receptors: ligand design and receptor interactions.Purinergic signalling · 2012Review
- Pyrimidine ribonucleotides with enhanced selectivity as P2Y(6) receptor agonists: novel 4-alkyloxyimino, (S)-methanocarba, and 5'-triphosphate gamma-ester modifications.Journal of medicinal chemistry · 2010Article
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
Extracellular nucleotides and their receptor antagonists have therapeutic potential in disorders such as inflammation, brain disorders, and cardiovascular diseases. Pancreatic beta cells express several purinergic receptors, and reported nucleotide effects on insulin secretion are contradictory. We studied the effect of P2Y receptors on insulin secretion and cell death in MIN6, mouse pancreatic beta cells. Expression of P2Y(1) and P2Y(6) receptors was revealed by total mRNA analysis using RT-PCR. MIN6 cells were stimulated in the presence of 16.7 mM glucose with or without P2Y(1) and P2Y(6) agonists, 2-MeSADP and Up(3)U, respectively. Both the agonists increased insulin secretion with EC(50) values of 44.6+/-7.0 nM and 30.7+/-12.7 nM respectively. The insulin secretion by P2Y(1) and P2Y(6) agonists was blocked by their selective antagonists MRS2179 and MRS2578, respectively. Binding of the selective P2Y(1) receptor antagonist radioligand [125I]MRS2500 in MIN6 cell membranes was saturable (K(D) 4.74+/-0.47 nM), and known P2Y(1) ligands competed with high affinities. Inflammation and glucose toxicity lead to pancreatic beta cell death in diabetes. Flow cytometric analysis revealed that Up(3)U but not 2-MeSADP protected MIN6 cells against TNF-alpha induced apoptosis. Overall, the results demonstrate that selective stimulation of P2Y(1) and P2Y(6) receptors increases insulin secretion that accompanies intracellular calcium release, suggesting potential application of P2Y receptor ligands in the treatment of diabetes.
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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 Socratic graph.