Last update 01 Nov 2024

Orphan GPCR

Last update 01 Nov 2024

Basic Info

Synonyms-

Introduction-

Drugs associated with Orphan GPCR

NBG-050

Target

Orphan GPCR

Mechanism

Orphan GPCR agonists

Active Org.

NB Health Laboratory Co. Ltd.

Originator Org.

NB Health Laboratory Co. Ltd.

Active Indication

Stroke

Inactive Indication-

Drug Highest PhaseDiscovery

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with Orphan GPCR

100 Translational Medicine associated with Orphan GPCR

0 Patents (Medical) associated with Orphan GPCR

Literatures (Medical) associated with Orphan GPCR

01 Jul 2024·British Journal of Pharmacology

Molecular insights into orphan G protein‐coupled receptors relevant to schizophrenia

Review

Author: Stewart, Gregory D ; Lu, Yao ; Hatzipantelis, Cassandra J ; Langmead, Christopher J

AbstractSchizophrenia remains a sizable socio‐economic burden that continues to be treated with therapeutics based on 70‐year old science. All currently approved therapeutics primarily target the dopamine D2 receptor to achieve their efficacy. Whilst dopaminergic dysregulation is a key feature in this disorder, the targeting of dopaminergic machinery has yielded limited efficacy and an appreciable side effect burden. Over the recent decades, numerous drugs that engage non‐dopaminergic G protein‐coupled receptors (GPCRs) have yielded a promise of efficacy without the deleterious side effect profile, yet none have successfully completed clinical studies and progressed to the market. More recently, there has been increased attention around non‐dopaminergic GPCR‐targeting drugs, which demonstrated efficacy in some schizophrenia symptom domains. This provides renewed hope that effective schizophrenia treatment may lie outside of the dopaminergic space. Despite the potential for muscarinic receptor‐ (and other well‐characterised GPCR families) targeting drugs to treat schizophrenia, they are often plagued with complications such as lack of receptor subtype selectivity and peripheral on‐target side effects. Orphan GPCR studies have opened a new avenue of exploration with many demonstrating schizophrenia‐relevant mechanisms and a favourable expression profile, thus offering potential for novel drug development. This review discusses centrally expressed orphan GPCRs: GPR3, GPR6, GPR12, GPR52, GPR85, GPR88 and GPR139 and their relationship to schizophrenia. We review their expression, signalling mechanisms and cellular function, in conjunction with small molecule development and structural insights. We seek to provide a snapshot of the growing evidence and development potential of new classes of schizophrenia therapeutics.LINKED ARTICLESThis article is part of a themed issue Therapeutic Targeting of G Protein‐Coupled Receptors: hot topics from the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists 2021 Virtual Annual Scientific Meeting. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v181.14/issuetoc

05 Mar 2024·Biochemistry

Lipid-Dependent Activation of the Orphan G Protein-Coupled Receptor, GPR3

Article

Author: Sexton, Patrick M. ; Bumbak, Fabian ; Russell, Isabella C. ; Wootten, Denise ; Venugopal, Hariprasad ; Leeming, Michael G. ; McNeill, Samantha M. ; Christopoulos, George ; Flocco, Maria M. ; Zhang, Xin ; Belousoff, Matthew J. ; Josephs, Tracy M.

The class A orphan G protein-coupled receptor (GPCR), GPR3, has been implicated in a variety of conditions, including Alzheimer's and premature ovarian failure. GPR3 constitutively couples with Gαs, resulting in the production of cAMP in cells. While tool compounds and several putative endogenous ligands have emerged for the receptor, its endogenous ligand, if it exists, remains a mystery. As novel potential drug targets, the structures of orphan GPCRs have been of increasing interest, revealing distinct modes of activation, including autoactivation, presence of constitutively activating mutations, or via cryptic ligands. Here, we present a cryo-electron microscopy (cryo-EM) structure of the orphan GPCR, GPR3 in complex with DNGαs and Gβ₁γ₂. The structure revealed clear density for a lipid-like ligand that bound within an extended hydrophobic groove, suggesting that the observed "constitutive activity" was likely due to activation via a lipid that may be ubiquitously present. Analysis of conformational variance within the cryo-EM data set revealed twisting motions of the GPR3 transmembrane helices that appeared coordinated with changes in the lipid-like density. We propose a mechanism for the binding of a lipid to its putative orthosteric binding pocket linked to the GPR3 dynamics.

01 Dec 2023·European Journal of Pharmacology

Research progress on the role of orphan receptor GPR139 in neuropsychiatric behaviours

Review

Author: Zhang, Rumin ; Chen, Jing

The study of orphan G protein-coupled receptors (GPCRs) holds much promise for increasing our understanding of neuropsychiatric diseases and for the development of new therapeutic strategies for these diseases. GPR139 is an orphan GPCR expressed in the central nervous system, especially in areas of the brain that control movement, motivation, and reward, and those that regulate neuropsychiatric behaviour. This review provides information about the discovery, tissue expression, signal transduction pathways, and physiological functions of GPR139, as well as how GPR139 interacts with other GPCRs, which form heteromeric complexes that affect their pharmacology and function. We also discuss the utility and therapeutic potential of ligands that target GPR139, including the pharmacological properties of reported agonists and antagonists. Finally, we highlight the pathologic role of GPR139 in neuropsychiatric behaviour and its potential as a therapeutic target in neuropsychiatric disorders.

News (Medical) associated with Orphan GPCR

05 Jul 2023

·www.prnewswire.com

Global G-Protein Coupled Receptors (GPCRs) Strategic Business Report 2023: CRISPR Holds Potential to Speed up GPCR-based Drug Discovery

DUBLIN, July 5, 2023 /PRNewswire/ -- The "G-Protein Coupled Receptors (GPCRs): Global Strategic Business Report" report has been added to ResearchAndMarkets.com's offering. The global market for G-Protein Coupled Receptors (GPCRs) estimated at US$2.9 Billion in the year 2022, is projected to reach a revised size of US$4.7 Billion by 2030, growing at a CAGR of 6.1% over the analysis period 2022-2030. Cell Lines, one of the segments analyzed in the report, is projected to record a 6% CAGR and reach US$1.8 Billion by the end of the analysis period. Taking into account the ongoing post pandemic recovery, growth in the Detection Kits segment is readjusted to a revised 6.7% CAGR for the next 8-year period. The U.S. Market is Estimated at $1.1 Billion, While China is Forecast to Grow at 8.9% CAGR The G-Protein Coupled Receptors (GPCRs) market in the U.S. is estimated at US$1.1 Billion in the year 2022. China, the world's second largest economy, is forecast to reach a projected market size of US$416.9 Million by the year 2030 trailing a CAGR of 8.9% over the analysis period 2022 to 2030. Among the other noteworthy geographic markets are Japan and Canada, each forecast to grow at 5.3% and 6.1% respectively over the 2022-2030 period. Within Europe, Germany is forecast to grow at approximately 5.8% CAGR. Select Competitors (Total 52 Featured) - Abcam plc Addex Pharmaceuticals Ltd. Arena Pharmaceuticals Inc. Becton-Dickinson and Company Eurofins DiscoverX Corporation HD Biosciences Co., Ltd Merck KGaA Perkin Elmer Inc Promega Corporation QIAGEN N.V. Thermo Fisher Scientific, Inc. Key Topics Covered: I. METHODOLOGY II. EXECUTIVE SUMMARY 1. MARKET OVERVIEW Impact of Covid-19 and a Looming Global Recession Influencer Market Insights World Market Trajectories G-Protein Coupled Receptors (GPCRs) - Global Key Competitors Percentage Market Share in 2022 (E) Competitive Market Presence - Strong/Active/Niche/Trivial for Players Worldwide in 2022 (E) GPCR: An Introduction Important Role of GPCRs in Drug Discovery Popular Types of GPCRs of Therapeutic Interest Classification of GPCRs Orphan GPCRs: A Promising Area for Drug Discovery GPCR Signaling Pathways Physiological Roles Performed by GPCRs Outlook Geographic Market Analysis Challenges Competition Recent Market Activity World Brands 2. FOCUS ON SELECT PLAYERS 3. MARKET TRENDS & DRIVERS Therapeutic Potential of GPCRs Gains Wide Recognition Allosteric Modulators and Implication of Allostery in Drug Discovery GPCRs Registered as Targets for Approved Drugs with EMBL-CHEMBL, IUPHAR, and The DrugBank GPCRs Registered as Targets for Approved Drugs with EMBL-CHEMBL GPCRs Registered as Targets for Approved Drugs with International Union of Basic and Clinical Pharmacology (IUPHAR) GPCRs Registered as Targets for Approved Drugs with The DrugBank FDA Approved GPCR Targeting Drugs (Excl. Diagnostic Agents) for the Period 2015-2019 Hurdles Faced. Developments in Structural Biology and Receptor Pharmacology Offer Novel Opportunities to GPCR Drug Discovery In Silico Approaches Underway for GPCR Drug Screening Microfluidic Cell Technology Holds Potential Pipeline GPCR Drug Candidates Widen Prospects Select GPCR Small Molecule Drugs in Active Clinical Development GPCR Ligands (Agonist) in Phase III Clinical Development GPCR Ligands (Antagonist) in Phase III Clinical Development New Indications to Aid Growth CRISPR Holds Potential to Speed Up GPCR-based Drug Discovery GPCR-targeted Drugs and Role in Cancer Treatment Select FDA Approved Drugs and Antibodies against Various Cancer Types Potential GPCR targets for Cancer Treatment Anti GPCRs Drugs and Antibodies under Clinical Trials Rising Incidence of Cancer to Drive Drives Opportunities Global Cancer Incidence: Number of New Cancer Cases in Million for the Years 2018, 2020, 2025, 2030, 2035 and 2040 Global Number of New Cancer Cases and Cancer-related Deaths by Cancer Site for 2018 GPCRs Evolve as Important targets for developing novel therapeutics for Neurodegerative Disorders Number of Individuals Suffering from Alzheimer's in the US: 2020 and 2025 Global Aging Population Statistics for the 65+ Age Group in Million by Geographic Region for the Years 2019, 2025, 2035 and 2050 GPCRs: An Important Target for Cardiovascular Drugs Fatalities by Heart Conditions - Estimated Percentage Breakdown for Cardiovascular Disease, Ischemic Heart Disease, Stroke, and Others GPCR Screening and Targeting Technologies 4. GLOBAL MARKET PERSPECTIVE III. MARKET ANALYSIS IV. COMPETITION For more information about this report visit About ResearchAndMarkets.com ResearchAndMarkets.com is the world's leading source for international market research reports and market data. We provide you with the latest data on international and regional markets, key industries, the top companies, new products and the latest trends. Media Contact: Research and Markets Laura Wood, Senior Manager [email protected] For E.S.T Office Hours Call +1-917-300-0470 For U.S./CAN Toll Free Call +1-800-526-8630 For GMT Office Hours Call +353-1-416-8900 U.S. Fax: 646-607-1904 Fax (outside U.S.): +353-1-481-1716 Logo: SOURCE Research and Markets

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Orphan GPCR

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