ArticleThe Journal of pharmacology and experimental therapeutics2018
A Combination of G Protein-Coupled Receptor Modulators Protects Photoreceptors from Degeneration.
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Article in The Journal of pharmacology and experimental therapeutics, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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21citing papers in PubMed
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21 citing papers in PubMed, 26 citations in OpenAlex.
- Altered Retinal Dopamine Homeostasis in Murine Models of Retinitis Pigmentosa.Journal of neurochemistry · 2026Article
- Cyclic nucleotide signaling as a drug target in retinitis pigmentosa.FEBS letters · 2025Review
- Retinal Proteome Profiling of Inherited Retinal Degeneration Across Three Different Mouse Models Suggests Common Drug Targets in Retinitis Pigmentosa.Molecular & cellular proteomics : MCP · 2024Article
- A combination treatment based on drug repurposing demonstrates mutation-agnostic efficacy in pre-clinical retinopathy models.Nature communications · 2024Article
- Distinct mouse models of Stargardt disease display differences in pharmacological targeting of ceramides and inflammatory responses.Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- CCR2-positive monocytes contribute to the pathogenesis of early diabetic retinopathy in mice.Diabetologia · 2023Article
- The Selective α1 Antagonist Tamsulosin Alters ECM Distributions and Cellular Metabolic Functions of ARPE 19 Cells in a Concentration-Dependent Manner.Bioengineering (Basel, Switzerland) · 2022Article
- VCP/p97 inhibitor CB-5083 modulates muscle pathology in a mouse model of VCP inclusion body myopathy.Journal of translational medicine · 2022Article
- The GPCR Antagonistic Drug CM-20 Stimulates Mitochondrial Activity in Human RPE Cells.The open biochemistry journal · 2022Article
- Comparison of effects of tamsulosin and silodosin on subfoveal choroidal thickness and pupil size diameters in patients with prostatic hyperplasia.International ophthalmology · 2021Article
- Regulation of Adrenergic, Serotonin, and Dopamine Receptors to Inhibit Diabetic Retinopathy: Monotherapies versus Combination Therapies.Molecular pharmacology · 2021Article
- Photoreceptor Cell Calcium Dysregulation and Calpain Activation Promote Pathogenic Photoreceptor Oxidative Stress and Inflammation in Prodromal Diabetic Retinopathy.The American journal of pathology · 2021Article
- A p97/Valosin-Containing Protein Inhibitor Drug CB-5083 Has a Potent but Reversible Off-Target Effect on Phosphodiesterase-6.The Journal of pharmacology and experimental therapeutics · 2021Article
- An inducible Cre mouse for studying roles of the RPE in retinal physiology and disease.JCI insight · 2021Article
- Sensory Transduction in Photoreceptors and Olfactory Sensory Neurons: Common Features and Distinct Characteristics.Frontiers in cellular neuroscience · 2021Review
- Article
- Successful induction of diabetes in mice demonstrates no gender difference in development of early diabetic retinopathy.PloS one · 2020Article
- Retinal Gene Distribution and Functionality Implicated in Inherited Retinal Degenerations Can Reveal Disease-Relevant Pathways for Pharmacologic Intervention.Pharmaceuticals (Basel, Switzerland) · 2019Article
- A Mixture of U.S. Food and Drug Administration-Approved Monoaminergic Drugs Protects the Retina From Light Damage in Diverse Models of Night Blindness.Investigative ophthalmology & visual science · 2019Article
- A novel small molecule chaperone of rod opsin and its potential therapy for retinal degeneration.Nature communications · 2018Article
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Authors and funding
11 authors at 3 institutions in 1 country.
Tivadar OrbanDepartment of Pharmacology, Cleveland Center for Membrane and Structural Biology, School of Medicine, Case Western Reserve University, Cleveland, Ohio (T.O., H.L., T.G., S.G., A.V., H.H.-T., T.S.K., P.D.K., K.P.); Research Service, Louis Stokes Cleveland Veterans Affairs Medical Center, Cleveland, Ohio (T.S.K., P.D.K.); and Polgenix Inc., Cleveland, Ohio (Z.D., W.S.).
Henri LeinonenDepartment of Pharmacology, Cleveland Center for Membrane and Structural Biology, School of Medicine, Case Western Reserve University, Cleveland, Ohio (T.O., H.L., T.G., S.G., A.V., H.H.-T., T.S.K., P.D.K., K.P.); Research Service, Louis Stokes Cleveland Veterans Affairs Medical Center, Cleveland, Ohio (T.S.K., P.D.K.); and Polgenix Inc., Cleveland, Ohio (Z.D., W.S.).
Tamar GetterDepartment of Pharmacology, Cleveland Center for Membrane and Structural Biology, School of Medicine, Case Western Reserve University, Cleveland, Ohio (T.O., H.L., T.G., S.G., A.V., H.H.-T., T.S.K., P.D.K., K.P.); Research Service, Louis Stokes Cleveland Veterans Affairs Medical Center, Cleveland, Ohio (T.S.K., P.D.K.); and Polgenix Inc., Cleveland, Ohio (Z.D., W.S.).
Zhiqian DongDepartment of Pharmacology, Cleveland Center for Membrane and Structural Biology, School of Medicine, Case Western Reserve University, Cleveland, Ohio (T.O., H.L., T.G., S.G., A.V., H.H.-T., T.S.K., P.D.K., K.P.); Research Service, Louis Stokes Cleveland Veterans Affairs Medical Center, Cleveland, Ohio (T.S.K., P.D.K.); and Polgenix Inc., Cleveland, Ohio (Z.D., W.S.).
Wenyu SunDepartment of Pharmacology, Cleveland Center for Membrane and Structural Biology, School of Medicine, Case Western Reserve University, Cleveland, Ohio (T.O., H.L., T.G., S.G., A.V., H.H.-T., T.S.K., P.D.K., K.P.); Research Service, Louis Stokes Cleveland Veterans Affairs Medical Center, Cleveland, Ohio (T.S.K., P.D.K.); and Polgenix Inc., Cleveland, Ohio (Z.D., W.S.).
Songqi GaoDepartment of Pharmacology, Cleveland Center for Membrane and Structural Biology, School of Medicine, Case Western Reserve University, Cleveland, Ohio (T.O., H.L., T.G., S.G., A.V., H.H.-T., T.S.K., P.D.K., K.P.); Research Service, Louis Stokes Cleveland Veterans Affairs Medical Center, Cleveland, Ohio (T.S.K., P.D.K.); and Polgenix Inc., Cleveland, Ohio (Z.D., W.S.).
Alexander VeenstraDepartment of Pharmacology, Cleveland Center for Membrane and Structural Biology, School of Medicine, Case Western Reserve University, Cleveland, Ohio (T.O., H.L., T.G., S.G., A.V., H.H.-T., T.S.K., P.D.K., K.P.); Research Service, Louis Stokes Cleveland Veterans Affairs Medical Center, Cleveland, Ohio (T.S.K., P.D.K.); and Polgenix Inc., Cleveland, Ohio (Z.D., W.S.).
Hossein Heidari-TorkabadiDepartment of Pharmacology, Cleveland Center for Membrane and Structural Biology, School of Medicine, Case Western Reserve University, Cleveland, Ohio (T.O., H.L., T.G., S.G., A.V., H.H.-T., T.S.K., P.D.K., K.P.); Research Service, Louis Stokes Cleveland Veterans Affairs Medical Center, Cleveland, Ohio (T.S.K., P.D.K.); and Polgenix Inc., Cleveland, Ohio (Z.D., W.S.).
Timothy S KernDepartment of Pharmacology, Cleveland Center for Membrane and Structural Biology, School of Medicine, Case Western Reserve University, Cleveland, Ohio (T.O., H.L., T.G., S.G., A.V., H.H.-T., T.S.K., P.D.K., K.P.); Research Service, Louis Stokes Cleveland Veterans Affairs Medical Center, Cleveland, Ohio (T.S.K., P.D.K.); and Polgenix Inc., Cleveland, Ohio (Z.D., W.S.).
Philip D KiserDepartment of Pharmacology, Cleveland Center for Membrane and Structural Biology, School of Medicine, Case Western Reserve University, Cleveland, Ohio (T.O., H.L., T.G., S.G., A.V., H.H.-T., T.S.K., P.D.K., K.P.); Research Service, Louis Stokes Cleveland Veterans Affairs Medical Center, Cleveland, Ohio (T.S.K., P.D.K.); and Polgenix Inc., Cleveland, Ohio (Z.D., W.S.).
Krzysztof PalczewskiDepartment of Pharmacology, Cleveland Center for Membrane and Structural Biology, School of Medicine, Case Western Reserve University, Cleveland, Ohio (T.O., H.L., T.G., S.G., A.V., H.H.-T., T.S.K., P.D.K., K.P.); Research Service, Louis Stokes Cleveland Veterans Affairs Medical Center, Cleveland, Ohio (T.S.K., P.D.K.); and Polgenix Inc., Cleveland, Ohio (Z.D., W.S.) kxp65@case.edu.
Case Western Reserve University · USPolgenix (United States) · USLouis Stokes Cleveland VA Medical Center · US
Funding
TISSUE CULTURE AND HYBRIDOMA MODULEP30EY011373 · NEI · CASE WESTERN RESERVE UNIVERSITY · PI Irina A Pikuleva · 1997 to 2026
$17.7MSTRUCTURAL STUDIES OF ARRESTINSR01EY009339 · NEI · UNIVERSITY OF WASHINGTON · PI KISER, PHILIP DAVID, PALCZEWSKI, KRZYSZTOF · 1992 to 2025
$16.0MNovel therapies to inhibit Diabetic RetinopathyR24EY024864 · NEI · UNIVERSITY OF CALIFORNIA-IRVINE · PI KERN, TIMOTHY S · 2015 to 2019
$8.1MUse of systems pharmacology to prevent rod and cone photoreceptor degenerationR24EY027283 · NEI · UNIVERSITY OF CALIFORNIA-IRVINE · PI PALCZEWSKI, KRZYSZTOF · 2017 to 2021
$7.9MRESOURCE/SERVICE CORE C - MOLECULAR INFORMATICS MODULEP30EY025585 · NEI · CLEVELAND CLINIC LERNER COM-CWRU · PI BELA ANAND-APTE · 2016 to 2026
$7.7MStudies on visual cycles and their relevance to age-related macular degenerationIK2BX002683 · VA · VETERANS HEALTH ADMINISTRATION · PI KISER, PHILIP DAVID · 2015 to 2019
–BLRD VA IK2 BX002683NEI NIH HHS P30 EY011373NEI NIH HHS P30 EY025585NEI NIH HHS R01 EY009339NEI NIH HHS R24 EY024864NEI NIH HHS R24 EY027283
Abstract
Degeneration of retinal photoreceptor cells can arise from environmental and/or genetic causes. Since photoreceptor cells, the retinal pigment epithelium (RPE), neurons, and glial cells of the retina are intimately associated, all cell types eventually are affected by retinal degenerative diseases. Such diseases often originate either in rod and/or cone photoreceptor cells or the RPE. Of these, cone cells located in the central retina are especially important for daily human activity. Here we describe the protection of cone cells by a combination therapy consisting of the G protein-coupled receptor modulators metoprolol, tamsulosin, and bromocriptine. These drugs were tested in
Indexed as
AnimalsDrug InteractionsGene Expression RegulationHumansMaleMiceReceptors, G-Protein-CoupledRetinal Cone Photoreceptor CellsRetinal DegenerationReceptors, G-Protein-Coupled
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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.