ArticleAssay and drug development technologies2011
Exchange protein directly activated by cyclic AMP isoform 2 is not a direct target of sulfonylurea drugs.
Article in Assay and drug development technologies, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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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.
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Who cites it
17 citing papers in PubMed, 32 citations in OpenAlex.
- Live Cell Monitoring of Phosphodiesterase Inhibition by Sulfonylurea Drugs.Biomolecules · 2024Article
- Noncanonical Regulation of cAMP-Dependent Insulin Secretion and Its Implications in Type 2 Diabetes.Comprehensive Physiology · 2023Article
- Review
- Selective small-molecule EPAC activators.Biochemical Society transactions · 2019Review
- β-Cell-intrinsic β-arrestin 1 signaling enhances sulfonylurea-induced insulin secretion.The Journal of clinical investigation · 2019Article
- Intracellular cAMP Sensor EPAC: Physiology, Pathophysiology, and Therapeutics Development.Physiological reviews · 2018Review
- The Potential of a Novel Class of EPAC-Selective Agonists to Combat Cardiovascular Inflammation.Journal of cardiovascular development and disease · 2017Review
- The role of Epac in the heart.Cellular and molecular life sciences : CMLS · 2017Review
- Review
- The future of EPAC-targeted therapies: agonism versus antagonism.Trends in pharmacological sciences · 2015Review
- Structure-guided design of selective Epac1 and Epac2 agonists.PLoS biology · 2015Article
- Activators of PKA and Epac distinctly influence insulin secretion and cytosolic Ca2+ in female mouse islets stimulated by glucose and tolbutamide.Endocrinology · 2014Article
- Recent advances in the discovery of small molecules targeting exchange proteins directly activated by cAMP (EPAC).Journal of medicinal chemistry · 2014Review
- Cyclic AMP dynamics in the pancreatic β-cell.Upsala journal of medical sciences · 2012Review
- Regulation of the inflammatory response of vascular endothelial cells by EPAC1.British journal of pharmacology · 2012Review
- Channeling dysglycemia: ion-channel variations perturbing glucose homeostasis.Trends in endocrinology and metabolism: TEM · 2012Review
- Mechanism of intracellular cAMP sensor Epac2 activation: cAMP-induced conformational changes identified by amide hydrogen/deuterium exchange mass spectrometry (DXMS).The Journal of biological chemistry · 2011Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
It has been reported by Zhang et al. that antidiabetic sulfonylurea drugs promote insulin secretion by directly binding to exchange protein directly activated by cyclic AMP isoform 2 (Epac2) and activating its down-stream effector Rap1. However, a critical link for an unambiguous validation of a direct interaction between Epac2 and sulfonylurea using purified individual components is missing. Our in vitro analyses using purified full-length Epac2 and Rap1 suggest that sulfonylureas are not able to directly bind to Epac2, nor are they capable of triggering Epac2-dependent Rap1 activation.
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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.