Targeting G protein coupled receptor-related pathways as emerging molecular therapies

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β-Arrestins and Cell Signaling

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Uncovering Molecular Mechanisms Involved in Activation of G Protein-Coupled Receptors

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Enhanced Morphine Analgesia in Mice Lacking β-Arrestin 2

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An Akt/β-Arrestin 2/PP2A Signaling Complex Mediates Dopaminergic Neurotransmission and Behavior

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Seven-transmembrane-spanning receptors and heart function

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Signal Transduction Mechanisms Mediating the Physiological and Pathophysiological Actions of Angiotensin II in Vascular Smooth Muscle Cells

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μ-Opioid receptor desensitization by β-arrestin-2 determines morphine tolerance but not dependence

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Teaching old receptors new tricks: biasing seven-transmembrane receptors

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Cellular Regulation of RGS Proteins: Modulators and Integrators of G Protein Signaling

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Role of βγ Subunits of G Proteins in Targeting the β-Adrenergic Receptor Kinase to Membrane-Bound Receptors

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Putative Mammalian Taste Receptors

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Insights into G Protein Structure, Function, and Regulation

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Metabotropic glutamate receptors: From the workbench to the bedside

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Protein kinase cascades in the regulation of cardiac hypertrophy

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β-Arrestin-biased ligands at seven-transmembrane receptors

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A unique mechanism of β-blocker action: Carvedilol stimulates β-arrestin signaling

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A novel phosphoinositide 3 kinase activity in myeloid-derived cells is activated by G protein βγ subunits

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Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery

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Neuropharmacological Mechanisms of Nerve Agent-induced Seizure and Neuropathology 1 1The animals used in studies performed in, or sponsored by, this Institute were handled in accordance with the principles stated in the Guide for the Care and Use of Laboratory Animals, proposed by the Committee on Care and Use of Laboratory Animals of the Institute of Laboratory Animal Resources, National Research Council, DHHA, National Institute of Health Publication #85–23, 1985, and the Animal Welfare Act of 1966, as amended. The opinions, or assertions contained herein are the private views of the authors, and are not to be construed as reflecting the views of the Department of the Army or the Department of Defense.

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Therapeutic potential of β-arrestin- and G protein-biased agonists

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New Concepts in Drug Discovery: Collateral Efficacy and Permissive Antagonism

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Third Generation Antipsychotic Drugs: Partial Agonism or Receptor Functional Selectivity?

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β-Blockers alprenolol and carvedilol stimulate β-arrestin-mediated EGFR transactivation

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Signaling by internalized G-protein-coupled receptors

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Toll-like receptor-4 (TLR4) signaling augments chemokine-induced neutrophil migration by modulating cell surface expression of chemokine receptors

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β-Arrestin-biased Agonism at the β2-Adrenergic Receptor

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Desensitization, internalization, and signaling functions of β-arrestins demonstrated by RNA interference

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Learned helplessness in the rat: improvements in validity and reliability

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Small Molecule Disruption of G Protein βγ Subunit Signaling Inhibits Neutrophil Chemotaxis and Inflammation

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Differential Targeting of Gßγ-Subunit Signaling with Small Molecules

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IUPHAR-DB: the IUPHAR database of G protein-coupled receptors and ion channels

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Uncovering G protein-coupled receptor kinase-5 as a histone deacetylase kinase in the nucleus of cardiomyocytes

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The G protein-coupled receptor subset of the rat genome

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Enhanced Rewarding Properties of Morphine, but not Cocaine, in βarrestin-2 Knock-Out Mice

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GPCR functional selectivity has therapeutic impact

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β-Arrestin1 Knockout Mice Appear Normal but Demonstrate Altered Cardiac Responses to β-Adrenergic Stimulation

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Global phosphorylation analysis of β-arrestin–mediated signaling downstream of a seven transmembrane receptor (7TMR)

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Aripiprazole has Functionally Selective Actions at Dopamine D2 Receptor-Mediated Signaling Pathways

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The Origins of Diversity and Specificity in G Protein-Coupled Receptor Signaling

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Selective Activation of Postsynaptic 5-HT1A Receptors Induces Rapid Antidepressant Response

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How do you treat motor complications in Parkinson's disease: medicine, surgery, or both?

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Regulation of Constitutive Cargo Transport from the trans-Golgi Network to Plasma Membrane by Golgi-localized G Protein βγ Subunits

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Interactions between the human sweet-sensing T1R2–T1R3 receptor and sweeteners detected by saturation transfer difference NMR spectroscopy

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Analyzing Schizophrenia by DNA Microarrays

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Oxidative Stress Decreases G Protein-Coupled Receptor Kinase 2 in Lymphocytes via a Calpain-Dependent Mechanism

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Gβγ Signaling Promotes Breast Cancer Cell Migration and Invasion

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SIGNAL TRANSDUCTION IN ENVIRONMENTAL NEUROTOXICITY

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Gene expression profiles of the rat brain both immediately and 3 months following acute sarin exposure

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Gene Expression Profiling of Rat Hippocampus Following Exposure to the Acetylcholinesterase Inhibitor Soman

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Signaling requirements for translocation of P-Rex1, a key Rac2 exchange factor involved in chemoattractant-stimulated human neutrophil function

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Post-receptorial mechanisms underlie functional disregulation of β2-adrenergic receptors in lymphocytes from Multiple Sclerosis patients

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5-HT1A receptor-mediated inhibition of long-term potentiation in rat visual cortex

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Toxic Effects of Sarin in Rats at Three Months Following Single or Repeated Low-Level Inhalation Exposure

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Genome Wide Gene Expression Studies in Mood Disorders

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The Human Gonadotropin Releasing Hormone Type I Receptor Is a Functional Intracellular GPCR Expressed on the Nuclear Membrane

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Drosophila, a genetic model system to study cocaine-related behaviors: A review with focus on LIM-only proteins

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The organophosphate sarin, at low concentrations, inhibits the evoked release of GABA in rat hippocampal slices.

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Regulation of Smoothened by Drosophila G-protein-coupled receptor kinases

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Lipoic acid stimulates cAMP production in T lymphocytes and NK cells

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Lipoic acid stimulates cAMP production via the EP2 and EP4 prostanoid receptors and inhibits IFN gamma synthesis and cellular cytotoxicity in NK cells

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Learning and memory in 5-HT1A-receptor mutant mice

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Regulation of GRK 2 and 6, β-arrestin-2 and associated proteins in the prefrontal cortex of drug-free and antidepressant drug-treated subjects with major depression

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Reorganization of the actin cytoskeleton upon G-protein coupled receptor signaling

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Modulation of voluntary ethanol consumption by beta‐arrestin 2

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A role for G protein‐coupled receptor kinase 2 in mechanical allodynia

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Opportunities for therapeutic antibodies directed at G-protein-coupled receptors

Hutchings, C. J., Koglin, M., Olson, W. C., & Marshall, F. H. (2017) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2017.91 · Cited by 198 · see citing works

ONC201 and imipridones: Anti-cancer compounds with clinical efficacy

Prabhu, V. V., Morrow, S. N., Kawakibi, A. R., Zhou, L., Ralff, M. D., Ray, J., Jhaveri, A., Ferrarini, I., Lee, Y., Parker, C., et al. (2020) · Neoplasia · doi:10.1016/j.neo.2020.09.005 · Cited by 179 · see citing works

APOE*E2 allele delays age of onset in PSEN1 E280A Alzheimer’s disease

Vélez, J. I., Lopera, F., Sepulveda-Falla, D., Patel, H. R., Johar, A. S., Chuah, A., Tobón, C., Rivera, D., Villegas, A., Cai, Y., et al. (2016) · Molecular Psychiatry · doi:10.1038/mp.2015.177 · Cited by 111 · see citing works

Importance of GPCR-Mediated Microglial Activation in Alzheimer’s Disease

Haque, M. E., Kim, I., Jakaria, M., Akther, M., & Choi, D. (2018) · Frontiers in Cellular Neuroscience · doi:10.3389/fncel.2018.00258 · Cited by 55 · see citing works

Molecular assembly of rhodopsin with G protein-coupled receptor kinases

He, Y., Gao, X., Goswami, D., Hou, L., Pal, K., Yin, Y., Zhao, G., Ernst, O. P., Griffin, P. R., Melcher, K., et al. (2017) · Cell Research · doi:10.1038/cr.2017.72 · Cited by 52 · see citing works

Therapeutic Perspectives on the Modulation of G-Protein Coupled Estrogen Receptor, GPER, Function

Rouhimoghadam, M., Lu, A. S., Salem, A. K., & Filardo, E. J. (2020) · Frontiers in Endocrinology · doi:10.3389/fendo.2020.591217 · Cited by 49 · see citing works

Regulation of G Protein βγ Signaling

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GPR88 in A2AR Neurons Enhances Anxiety-Like Behaviors

Meirsman, A. C., Robé, A., d’Exaerde, A. D. K., & Kieffer, B. L. (2016) · eNeuro · doi:10.1523/eneuro.0202-16.2016 · Cited by 40 · see citing works

Cell cultures in drug development: Applications, challenges and limitations

Ghanemi, A. (2014) · Saudi Pharmaceutical Journal · doi:10.1016/j.jsps.2014.04.002 · Cited by 39 · see citing works

Endothelial progenitor cells: Exploring the pleiotropic effects of statins

Sandhu, K., Mamas, M. A., & Butler, R. (2017) · World Journal of Cardiology · doi:10.4330/wjc.v9.i1.1 · Cited by 34 · see citing works

Activation and Allosteric Modulation of Human μ Opioid Receptor in Molecular Dynamics

Bartuzi, D., Kaczor, A. A., & Matosiuk, D. (2015) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.5b00280 · Cited by 33 · see citing works

The signaling proteins GPR158 and RGS7 modulate excitability of L2/3 pyramidal neurons and control A-type potassium channel in the prelimbic cortex

Song, C., Orlandi, C., Sutton, L. P., & Martemyanov, K. A. (2019) · Journal of Biological Chemistry · doi:10.1074/jbc.ra119.007533 · Cited by 30 · see citing works

G-protein coupled receptors as therapeutic targets for neurodegenerative and cerebrovascular diseases

Guerram, M., Zhang, L., & Jiang, Z. (2016) · Neurochemistry International · doi:10.1016/j.neuint.2016.09.005 · Cited by 32 · see citing works

Shorter and sturdier bridges between traditional Chinese medicines and modern pharmacology

Ghanemi, A., & Boubertakh, B. (2014) · Saudi Pharmaceutical Journal · doi:10.1016/j.jsps.2014.02.010 · Cited by 28 · see citing works

Artificial Intelligence and the detection of pediatric concussion using epigenomic analysis

Bahado-Singh, R. O., Vishweswaraiah, S., Er, A., Aydas, B., Türkoğlu, O., Taşkın, B. D., Duman, M., Yılmaz, D., & Radhakrishna, U. (2019) · Brain Research · doi:10.1016/j.brainres.2019.146510 · Cited by 27 · see citing works

M3 muscarinic receptor activation reduces hepatocyte lipid accumulation via CaMKKβ/AMPK pathway

Jadeja, R. N., Chu, X., Wood, C., Bartoli, M., & Khurana, S. (2019) · Biochemical Pharmacology · doi:10.1016/j.bcp.2019.08.015 · Cited by 24 · see citing works

Dopaminergic gene methylation is associated with cognitive performance in a childhood monozygotic twin study

Lewis, C. R., Henderson-Smith, A., Breitenstein, R. S., Sowards, H., Piras, I. S., Huentelman, M. J., Doane, L. D., & Lemery‐Chalfant, K. (2019) · Epigenetics · doi:10.1080/15592294.2019.1583032 · Cited by 22 · see citing works

Is mapping borders between pharmacology and toxicology a necessity?

Ghanemi, A. (2014) · Saudi Pharmaceutical Journal · doi:10.1016/j.jsps.2014.03.001 · Cited by 21 · see citing works

Mutations modifying sporadic Alzheimer’s disease age of onset

Vélez, J. I., Lopera, F., Patel, H. R., Johar, A. S., Cai, Y., Rivera, D., Tobón, C., Villegas, A., Sepulveda‐Falla, D., Lehmann, S. G., et al. (2016) · American Journal of Medical Genetics Part B: Neuropsychiatric Genetics · doi:10.1002/ajmg.b.32493 · Cited by 19 · see citing works

Elements toward novel therapeutic targeting of the adrenergic system

Ghanemi, A., & Hu, X. (2014) · Neuropeptides · doi:10.1016/j.npep.2014.11.003 · Cited by 19 · see citing works

In silicostructure prediction, molecular docking and dynamic simulation studies on G Protein-Coupled Receptor 116: a novel insight into breast cancer therapy

Indiraleka, M., Rajendran, K., Dhanaraj, P., & Vallinayagam, S. (2020) · Journal of Biomolecular Structure and Dynamics · doi:10.1080/07391102.2020.1783365 · Cited by 16 · see citing works

CXCL16/CXCR6 Axis in Adipocytes Differentiated from Human Adipose Derived Mesenchymal Stem Cells Regulates Macrophage Polarization

Lee, S., Lee, Y., Choi, I., Kim, M., & Sung, J. (2021) · Cells · doi:10.3390/cells10123410 · Cited by 14 · see citing works

Presymptomatic change in microRNAs modulates Tau pathology

Sharma, S., Khadimallah, I., Corya, A. W., Ali, Y., Rao, X., Liu, Y., & Lu, H. (2018) · Scientific Reports · doi:10.1038/s41598-018-27527-6 · Cited by 9 · see citing works

Diet Impact on Obesity beyond Calories and Trefoil Factor Family 2 (TFF2) as an Illustration: Metabolic Implications and Potential Applications

Ghanemi, A., Yoshioka, M., & St‐Amand, J. (2021) · Biomolecules · doi:10.3390/biom11121830 · Cited by 9 · see citing works

Targeting the orexinergic system: Mainly but not only for sleep-wakefulness therapies

Ghanemi, A., & Hu, X. (2014) · Alexandria Journal of Medicine · doi:10.1016/j.ajme.2014.07.002 · Cited by 8 · see citing works

Bioactivity-guided synthesis of tropine derivatives as new agonists for melatonin receptors

Yin, X., Geng, C., Huang, X., Chen, H., Ma, Y., Chen, X., Sun, C., Yang, T., Zhou, J., Zhang, X., et al. (2016) · RSC Advances · doi:10.1039/c6ra06748d · Cited by 7 · see citing works

Trace Amines in Neuropsychiatric Disorders

Sherwani, S. I., & Khan, H. A. (2016) · Elsevier eBooks · doi:10.1016/b978-0-12-803603-7.00018-5 · Cited by 7 · see citing works

An epigenome-wide association analysis of cardiac autonomic responses among a population of welders

Zhang, J., Liu, Z., Umukoro, P. E., Cavallari, J. M., Fang, S. C., Weisskopf, M. G., Lin, X., Mittleman, M. A., & Christiani, D. C. (2017) · Epigenetics · doi:10.1080/15592294.2016.1270486 · Cited by 7 · see citing works

WITHDRAWN: How to map the bridges between zoology and pharmacology?

Ghanemi, A. (2015) · The Journal of Basic and Applied Zoology · doi:10.1016/j.jobaz.2014.12.003 · Cited by 5 · see citing works

Regulation of CXCR6 Expression on Adipocytes and Osteoblasts Differentiated from Human Adipose Tissue-Derived Mesenchymal Stem Cells

Lee, S., Lee, Y., Shin, M. K., & Sung, J. (2020) · Stem Cells International · doi:10.1155/2020/8870133 · Cited by 5 · see citing works

For dentists and doctors: The neglected concepts about the factors influencing the effects of drugs

Ghanemi, A. (2015) · The Saudi Dental Journal · doi:10.1016/j.sdentj.2015.05.001 · Cited by 5 · see citing works

How to map the bridges between zoology and pharmacology?

Ghanemi, A. (2015) · The Journal of Basic and Applied Zoology · doi:10.1016/s2090-9896(16)00021-7 · Cited by 4 · see citing works

Unraveling the RKIP–YY1 axis: immune crosstalk in the pathogenesis of metabolic disorders

Alzaïd, F., Arefanian, H., Bahman, F., Albeloushi, S., Alhamar, G., Mohammad, A., Hasan, A., Madhoun, A. S. A., Ahmad, R., & Al‐Mulla, F. (2025) · Frontiers in Immunology · doi:10.3389/fimmu.2025.1675699 · Cited by 3 · see citing works

Are we in Need of Dividing Zoology into Two Fields?

Ghanemi, A. (2014) · Journal of Dairy Veterinary & Animal Research · doi:10.15406/jdvar.2014.01.00001 · Cited by 3 · see citing works

How can we Imagine the Future of Anti-Tumors Therapies?

Ghanemi, A. (2014) · Journal of Neurology & Stroke · doi:10.15406/jnsk.2014.01.00038 · Cited by 3 · see citing works

Membrane Receptors and Signal Transduction Pathway

Wardhan, R., & Mudgal, P. (2017) · Springer eBooks · doi:10.1007/978-981-10-7101-0_9 · Cited by 3 · see citing works

Nutraceutical regulations of G-protein coupled receptors in neurological, cardiovascular and endocrine disorders: a review

Adeoye, B. O., Akano, O. P., Awojebe, D. R., Ogunbiyi, B. T., Adeoye, A. D., Ukangwa, N. A., Elizabeth, O. A., Olosunde, O. A., & Oyebanji, A. H. (2025) · Phytochemistry Reviews · doi:10.1007/s11101-025-10184-9 · Cited by 1 · see citing works

An Allosteric Assay for Identifying Ligands Binding to β 2 Adrenergic Receptor by Surface-Enhanced Raman Scattering (SERS)-Active Nanoparticles

Wang, Y., Lu, N., Wu, P., Chu, Y., Xing, Y., Wang, J., & Zhao, X. (2026) · Analytical Chemistry · doi:10.1021/acs.analchem.5c07045 · Cited by 1 · see citing works

Selecting Species for Pharmaceutical and Medical Research

Ghanemi, A. (2014) · MOJ Cell Science & Report · doi:10.15406/mojcsr.2014.01.00016 · Cited by 1 · see citing works

Scientific Research in the Developing Countries: The Challenges We Need to Overcome

Ghanemi, A. (2014) · MOJ Proteomics & Bioinformatics · doi:10.15406/mojpb.2014.01.00017 · Cited by 1 · see citing works

The role of Raf kinase inhibitory protein in inflammation

Shenouda, S., Bosso, M., Ahmad, R., & Al-Mulla, F. (2020) · Elsevier eBooks · doi:10.1016/b978-0-12-819612-0.00016-x · Cited by 1 · see citing works

Docking Methodologies and Recent Advances

Kumar, A., Goyal, R., & Jain, S. (2016) · IGI Global eBooks · doi:10.4018/978-1-5225-0549-5.ch031 · Cited by 1 · see citing works

Association of TAS2R16 gene (rs860170, rs978739, rs1357949) polymorphisms and TAS2R16 serum levels in patients with age-related macular degeneration

Inokaityte, I., Gedvilaitė, G., & Liutkevičienė, R. (2023) · Ophthalmic Genetics · doi:10.1080/13816810.2023.2291681 · Cited by 1 · see citing works

Unifying the Common Concepts Shared by Neurodegenerative Diseases

Ghanemi, A. (2015) · Journal of Neurology & Stroke · doi:10.15406/jnsk.2015.02.00065 · Cited by 1 · see citing works

Roles of Endothelial Motilin Receptor and Its Signal Transduction Pathway in Motilin-Induced Left Gastric Artery Relaxation in Dogs

Li, H., Yang, L., Jin, Y. H., & Jin, C. (2021) · Frontiers in Physiology · doi:10.3389/fphys.2021.770430 · Cited by 1 · see citing works

Modelling Parkinson’s Disease Pre-Clinically: A Novel Virus-Fibril Inducible Mouse Model Exploring Disease Characteristics and Therapeutic Intervention via Metabotropic Glutamate Receptor 5 Negative Allosteric Modulation

Bureau, S. C. (2022) · doi:10.22215/etd/2022-14889 · Cited by 1 · see citing works

Neuropharmacognosy as an emerging multidisciplinary science

Ghanemi, A., & Boubertakh, B. (2014) · Indonesian Journal of Electrical Engineering and Computer Science

Towards More Implications of Biochemistry in Neuroscience

Ghanemi, A. (2015) · Journal of Neurology & Stroke · doi:10.15406/jnsk.2015.02.00059

Therapeutic Perspectives beyond the Pathogenic Properties of the Microbes

Ghanemi, A. (2014) · MOJ Immunology · doi:10.15406/moji.2014.01.00030

Neuropsychology of Cell Cultures?

Ghanemi, A. (2015) · Journal of Neurology & Stroke · doi:10.15406/jnsk.2015.03.00097

Docking Methodologies and Recent Advances

Kumar, A., Goyal, R., & Jain, S. (2016) · Advances in medical technologies and clinical practice book series · doi:10.4018/978-1-5225-0115-2.ch012

Spotlight on Neuroimmunology: Illustrations from Neurodegenerative Diseases

Ghanemi, A., & Boubertakh, B. (2017) · International Journal of Public Health Science (IJPHS) · doi:10.11591/.v6i2.6645

Synthèse de nouveaux conjugués fluorocarbonés pour augmenter la stabilité métabolique de peptides thérapeutiques ciblant les récepteurs couplés aux protéines G : application aux peptides apeline et spexine, étude mécanistique et évaluation biologique.

Ramanoudjame, S. M. (2020) · theses.fr (ABES) · doi:10.70675/9aaefdefz6dafz4974za324zc779e3d0df04

Advances in the molecular understanding of G protein-coupled receptors and their future therapeutic opportunities

Obot, D. N., Udom, G. J., Udoh, A. E., Onyeukwu, N. J., Olusola, A. J., Udoh, I. M., Umana, I. K., Yemitan, O. K., & Okokon, J. E. (2021) · Future Journal of Pharmaceutical Sciences · doi:10.1186/s43094-021-00341-0 · Cited by 3 · see citing works

Advances in the molecular level understanding of G-protein coupled receptor

Roy, A. (2022) · Progress in molecular biology and translational science · doi:10.1016/bs.pmbts.2022.07.013 · Cited by 1 · see citing works

G protein-coupled receptors in health and disease

Tao, Y. (2009) · Academic Press eBooks · Cited by 1 · see citing works

G Protein-Coupled Receptors in Cell Signaling Transduction

Beer‐Hammer, S., & Liebscher, I. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms25010291 · Cited by 2 · see citing works

Target Molecular Pharmacology

Wang, D. (2026) · Springer eBooks · doi:10.1007/978-981-92-5166-7_9