ReviewBritish journal of pharmacology2018
The current state of GPCR-based drug discovery to treat metabolic disease.
Review in British journal of pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed.
- Leptin and G-protein coupled receptor (GPCR) signaling: Therapeutic potential in obesity.The Journal of biological chemistry · 2025Review
- Discovery of novel and selective GPR17 antagonists as pharmacological tools for developing new therapeutic strategies in diabetes and obesity.European journal of medicinal chemistry · 2025Article
- Integrated cytomembrane proteomics identifies EpCAM/MGST1 as therapeutic targets in metastatic laryngeal carcinoma.Frontiers in genetics · 2025Article
- Pyridine Derivatives: A Comprehensive Review of Their Potential as Anti-Diabetic Agents.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2025Review
- High Doses of Exogenous Glucagon Stimulate Insulin Secretion and Reduce Insulin Clearance in Healthy Humans.Diabetes · 2024 · on this mapArticle
- Hepatic GRK2 is dispensable for glucose homeostasis and other key metabolic parameters in mice.Molecular metabolism · 2024Article
- Article
- Alcohol-Related Liver Disease: An Overview on Pathophysiology, Diagnosis and Therapeutic Perspectives.Biomedicines · 2022Review
- Orphan GPR26 Counteracts Early Phases of Hyperglycemia-Mediated Monocyte Activation and Is Suppressed in Diabetic Patients.Biomedicines · 2022Article
- Drug-Targeted Genomes: Mutability of Ion Channels and GPCRs.Biomedicines · 2022Article
- Cholesterol-dependent endocytosis of GPCRs: implications in pathophysiology and therapeutics.Biophysical reviews · 2021Review
- Integrated Multi-Class Classification and Prediction of GPCR Allosteric Modulators by Machine Learning Intelligence.Biomolecules · 2021Article
- Structural Characterization of Receptor-Receptor Interactions in the Allosteric Modulation of G Protein-Coupled Receptor (GPCR) Dimers.International journal of molecular sciences · 2021Review
- Regulatory roles of G-protein coupled receptors in adipose tissue metabolism and their therapeutic potential.Archives of pharmacal research · 2021Review
- Multiscale Molecular Modeling in G Protein-Coupled Receptor (GPCR)-Ligand Studies.Biomolecules · 2020Review
- Characterizing Interhelical Interactions of G-Protein Coupled Receptors with the Fragment Molecular Orbital Method.Journal of chemical theory and computation · 2020Article
- An activator of G protein-coupled receptor and MEK1/2-ERK1/2 signaling inhibits HIV-1 replication by altering viral RNA processing.PLoS pathogens · 2020Article
- F2r negatively regulates osteoclastogenesis through inhibiting the Akt and NFκB signaling pathways.International journal of biological sciences · 2020Article
- The current state of GPCR-based drug discovery to treat metabolic disease.British journal of pharmacology · 2018Review
- Molecular pharmacology of GPCRs.British journal of pharmacology · 2018Article
Corrections and comments
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Authors and funding
4 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
One approach of modern drug discovery is to identify agents that enhance or diminish signal transduction cascades in various cell types and tissues by modulating the activity of GPCRs. This strategy has resulted in the development of new medicines to treat many conditions, including cardiovascular disease, psychiatric disorders, HIV/AIDS, certain forms of cancer and Type 2 diabetes mellitus (T2DM). These successes justify further pursuit of GPCRs as disease targets and provide key learning that should help guide identifying future therapeutic agents. This report reviews the current landscape of GPCR drug discovery with emphasis on efforts aimed at developing new molecules for treating T2DM and obesity. We analyse historical efforts to generate GPCR-based drugs to treat metabolic disease in terms of causal factors leading to success and failure in this endeavour. LINKED ARTICLES: This article is part of a themed section on Molecular Pharmacology of GPCRs. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v175.21/issuetoc.
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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.