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How Ligands Illuminate GPCR Molecular Pharmacology
Open accessAbstract
G protein-coupled receptors (GPCRs), which are modulated by a variety of endogenous and synthetic ligands, represent the largest family of druggable targets in the human genome. Recent structural and molecular studies have both transformed and expanded classical concepts of receptor pharmacology and have begun to illuminate the distinct mechanisms by which structurally, chemically, and functionally diverse ligands modulate GPCR function. These molecular insights into ligand engagement and action have enabled new computational methods and accelerated the discovery of novel ligands and tool compounds, especially for understudied and orphan GPCRs. These advances promise to streamline the development of GPCR-targeted medications.
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“Slightly more than half of the non-olfactory GPCRs have annotated drugs and small molecules targeting them53,54,61; see also TABLE 1.”
From Unexplored therapeutic opportunities in the human genome (2018) · cites this paper as [53]
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“A recent analysis indicates, however, that a handful of GPCRs — mainly biogenic amine, muscarinic and opioid receptors — represent the most abundantly targeted receptors for FDA-approved medications53,54.”
From Unexplored therapeutic opportunities in the human genome (2018) · cites this paper as [53]
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“Alterations in GPCR signalling are implicated in the pathogenesis and treatment of neuropsychiatric55, immunological56, gastrointestinal57,58, cardiac59, renal, hormonal, infectious60 and many other disorders53,54.”
From Unexplored therapeutic opportunities in the human genome (2018) · cites this paper as [53]
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“GPCRs represent the largest family of druggable targets in the human genome9, with between 20% and 30% of approved drugs acting on them53,54.”
From Unexplored therapeutic opportunities in the human genome (2018) · cites this paper as [53]
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“GPCRs are membrane-bound, cell-surface receptors that transduce signals via interactions with heterotrimeric G proteins, arrestins and other cellular transducers53,54.”
From Unexplored therapeutic opportunities in the human genome (2018) · cites this paper as [53]
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“For covalent inhibitors, one of their chief advantages is potentially more durable inhibition at the PPI site leading to improved pharmacology in vivo [117, 118].”
From The design and development of covalent protein-protein interaction inhibitors for cancer treatment (2020) · cites this paper as [118]
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“The creation of small drug-like molecules that are G protein-coupled receptor (GPCR) agonists has now become of great importance due to their physiological significance [1].”
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Self-citationRecent Advances in the Development of Experimental Therapeutics for Levodopa-Induced Dyskinesia
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Optimizing the Expression of Human Dopamine Receptors in Escherichia coli
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“G protein-coupled receptors (GPCRs) are intensely studied drug targets since they regulate many physiological processes [1].”
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“Different ligands, such as hormones, photons, ions, proteins (chemokines), neurotransmitters, metabolites, and naturally produced synthetic agonists or antagonists determine the GPCRs’ functions [1].”
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Genetic and Epigenetic Modulation of Gene Expression by CRISPR‐dCas Systems
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Fragment-based approaches in GPCR-targeted drug discovery
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Class A GPCRs use the membrane potential to increase their sensitivity and selectivityPreprint
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“transmembrane (TM) helices surrounding a relatively polar core [1-4] (Fig.”
BackgroundThe Rag1-/- Mouse: Establishing Links between Obesity and Prostate Cancer
Maugham, M. (2019) · Queensland University of Technology · doi:10.5204/thesis.eprints.126971
Computer-Aided Design of Ligands at Multiple Protein Targets for Multifactorial Diseases
Kalash, L. N. (2018) · Apollo (University of Cambridge) · doi:10.17863/cam.38293
LIGAND DISCOVERY AND FUNCTIONAL CHARACTERIZATION OF MRGPRX FAMILY ORPHAN GPCRS
Lansu, K. (2020) · Carolina Digital Repository (University of North Carolina at Chapel Hill) · doi:10.17615/p9r4-re19
Activation Mechanism of Prostanoid Receptors —X-ray Crystallography of EP3 Receptor—
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Peptide/Receptor Evolution Explains the Lipolytic Function of the Neuropeptide TLQP-21Preprint
Sahu, B. S., Han, R., Cero, C., Razzoli, M., Rodriguez, P. J., Nguyen, M. E., Piaggi, P., Pavličev, M., Muglia, L. J., Mahata, S. K., et al. (2019) · SSRN Electronic Journal · doi:10.2139/ssrn.3341735
Structural Biological Study Based on Spectroscopic Analysis of Cone Pigment
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Prevalent mouse phenotypes in the unexplored druggable genomePreprint
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Metadata
- Authors
- Wacker, D., Stevens, R. C., & Roth, B. L.
- Affiliations
- University of North Carolina at Chapel Hill (US)
- University of Southern California (US)
- Corresponding author
- Roth, Bryan L.
- Venue
- Cell
- Publisher
- Elsevier BV
- Published
- 2017-07
- Volume
- 170
- Issue
- 3
- Pages
- 414-427
- ISSN
- 0092-8674 (ISSN-L)
- PMC
- PMC5560499
- OpenAlex
- W2741191097
- Cited by
- 560
- References
- 115
- Citations by year
- 2026: 33 · 2025: 46 · 2024: 56 · 2023: 51 · 2022: 68 · 2021: 75 · 2020: 73 · 2019: 75 · 2018: 70 · 2017: 12
- FWCI
- 5.94
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- Locations
- Cell (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Carolina Digital Repository (University of North Carolina at Chapel Hill) (submittedVersion)
- UNC Libraries
- Funders
- National Institute of Health (RO1MH112205, UO1MH104974, U19MH82441, PO1DA035764)
- Michael Hooker Distinguished Professorship
- 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 › Pharmacology, Toxicology and Pharmaceutics › Drug Discovery › Computational Drug Discovery Methods
- Keywords
- G protein-coupled receptors, GPCR pharmacology, ligand binding, ligand-receptor interactions, orphan G protein-coupled receptor, tool compounds, computational drug discovery, GPCR structure
- MeSH terms
- Animals, Humans, Ligands, Models, Molecular, Signal Transduction, Receptors, G-Protein-Coupled, Drug Discovery, Molecular Targeted Therapy
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