The DOI matches its Crossref record; 139 of the 139 references it cites were found in a registry or an index.
Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders
Open accessAbstract
Despite G-protein-coupled receptors (GPCRs) being among the most fruitful targets for marketed drugs, intense discovery efforts for several GPCR subtypes have failed to deliver selective drug candidates. Historically, drug discovery programmes for GPCR ligands have been dominated by efforts to develop agonists and antagonists that act at orthosteric sites for endogenous ligands. However, in recent years, there have been tremendous advances in the discovery of novel ligands for GPCRs that act at allosteric sites to regulate receptor function. These compounds provide high selectivity, novel modes of efficacy and may lead to novel therapeutic agents for the treatment of multiple psychiatric and neurological human disorders.
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“G protein-coupled receptors (GPCRs) play essential roles in human physiology and are a major target for many pharmaceuticals on the market.295”
From Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials (2023) · cites this paper as [295]
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Molecular Dynamics Simulation for All
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Metadata
- Authors
- Jeffrey Conn, P., Christopoulos, A., & Lindsley, C. W.
- Affiliations
- Monash University (AU)
- Vanderbilt University (US)
- Venue
- Nature Reviews Drug Discovery
- Published
- 2009-01
- Volume
- 8
- Issue
- 1
- Pages
- 41-54
- ISSN
- 1474-1776 (ISSN-L)
- 1474-1784
- PMC
- PMC2907734
- OpenAlex
- W2003736358
- Cited by
- 1,063
- References
- 139
- Citations by year
- 2026: 30 · 2025: 46 · 2024: 37 · 2023: 25 · 2022: 48 · 2021: 51 · 2020: 44 · 2019: 58 · 2018: 57 · 2017: 68 · 2016: 64 · 2015: 67 · 2014: 69 · 2013: 80 · 2012: 75
- FWCI
- 6.60
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Nature Reviews Drug Discovery (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Institute of Mental Health (R01MH073676, R01MH074953, R01MH062646)
- National Institute on Drug Abuse (R01DA023926)
- National Institute of Neurological Disorders and Stroke (R01NS031373)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
- Keywords
- G protein-coupled receptors, allosteric modulators, allosteric site, orthosteric ligands, mental illness, neurological disorders, CNS drug discovery, receptor selectivity, novel therapeutic agents
- MeSH terms
- Allosteric Regulation, Animals, Central Nervous System Diseases, Drug Evaluation, Preclinical, Humans, Ligands, Drug Design, Receptors, G-Protein-Coupled
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