Ask about this productRelated genes to: GPR27 Blocking Peptide
- Gene:
- GPR27 NIH gene
- Name:
- G protein-coupled receptor 27
- Previous symbol:
- -
- Synonyms:
- SREB1
- Chromosome:
- 3p13
- Locus Type:
- gene with protein product
- Date approved:
- 1997-02-05
- Date modifiied:
- 2016-10-05
Related products to: GPR27 Blocking Peptide
Related articles to: GPR27 Blocking Peptide
- In this review, we, on behalf of the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology, describe criteria for assessing the evidence for pairing receptors with endogenous/physiological ligands for formal receptor deorphanization. This process is illustrated through consideration of the class A G protein-coupled receptors (GPCRs) not yet formally paired with an endogenous/physiological ligand by the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology. Of the 67 orphan class A GPCRs considered, 25 class A GPCRs have no identified endogenous agonists, although 5 (GPR21, GPR27, GPR52, GPR85, and GPR88) have synthetic ligands that have the potential to be used as tools for uncovering physiological roles and further pharmacological properties of these receptors. Surprisingly, 6 orphan GPCRs (GPR135, GPR152, GPR153, MRGPRF, MRGPRG, and MRGPRX3) have no clear pharmacology or phenotype reported following genetic disruption. Thirty-two orphan GPCRs have been paired with at least 1 endogenous agonist (mainly lipids and their derivatives, peptides, and other metabolites), but further characterization is required from the scientific community to validate these results. We identify 10 orphan class A GPCRs for which there are plausible grounds for considering deorphanization: GPR4 (protons), GPR15 (GPR15L), GPR31 (12S-hydroxyeicosatetraenoic acid), GPR39 (zinc divalent ions, Zn), GPR65 (protons), GPR68 (protons), GPR132 (9-hydroxyoctadecadienoic acid), GPR183 (7α,25-dihydroxycholesterol), MRGPRD (β-alanine), and MRGPRX1 (bovine adrenal medulla peptide 8-22). The issue of nomenclature for these 10 GPCRs will be considered by further subcommittees of the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology. We hope this review will prompt further investigations into these members of the currently most widely clinically exploited protein superfamily. SIGNIFICANCE STATEMENT: The use of systematic, rational nomenclature for drug targets provides a framework to ensure consistent identification and rapid recognition. Given that G protein-coupled receptors have fundamental physiological roles and are widespread targets of drugs in current clinical use, we hope the target summary and deorphanization criteria provided here will prompt renewed efforts to investigate these orphan receptors as regulators of physiology and as opportunities for future therapeutic exploitation. - Source: PubMed
Publication date: 2026/05/08
Alexander Stephen P HBennett Kirstie ABrown Andrew JGlass MichelleGloriam David EHanson JulienInsel Paul AKelly EamonnLangmead Christopher JMartemyanov Kirill ANeubig Rick ROffermanns StefanRosenkilde Mette MSchulte GunnarSmith Nicola JWu HuixianFaccenda ElenaHarding Simon DDavenport Anthony P - This study explored the prognostic role of GPR27 and its predictive value to platinum-based therapy in ovarian cancer. - Source: PubMed
Publication date: 2025/04/24
Peng XiulanCai YahongTang BingZhang MingtaoWang Xia - Super-conserved Receptors Expressed in Brain (SREB) are a highly conserved family of orphan G protein-coupled receptors that consist of three members in most vertebrates: SREB1 (GPR27), SREB2 (GPR85), and SREB3 (GPR173). Each receptor is associated with diverse physiological processes and expressed in both ovaries and testes, but reproductive functions are only beginning to be understood. In addition, some fishes gained a novel fourth gene, SREB3B, which may have unique functions. The purpose of this study was to conduct a spatial and quantitative analysis of SREBs in the gonads of pufferfish (Dichotomyctere nigroviridis), which expresses all four genes. Multiplex RNAscope and absolute qPCR were used to assess gene expression patterns in both ovaries and testes. Expression was detected in early ovaries and dominated by sreb1 (approximately 2500 copies/ng RNA vs. 300 or less for others), with notable expression of all receptors in primary oocytes, granulosa cells, and small numbers of extra-follicular cells. Within primary oocytes, sreb1 and sreb3b exhibited diffuse patterns that may indicate early functions, while sreb2 and sreb3a were granular and may reflect stored mRNA. Early testicular development was dominated by sreb1 and sreb2 (∼5000 copies/ng RNA) in spermatogonia. These patterns were somewhat reduced in late testes (∼1000-2600 copies/ng RNA), but sreb3b exhibited a novel spatial pattern (∼380 copies/ng RNA) within spermatogenic cysts. These results highlight diverse roles for the SREB family, and sreb3b is hypothesized to have unique roles in fish reproduction. - Source: PubMed
Publication date: 2024/11/12
Breton Timothy SOliveira Maria EduardaChillemi TrulyHarriman WilliamKorasadowicz JoannaSaverese EmeBourget EmmaMurray Casey AMartyniuk Christopher JDiMaggio Matthew A - Glioma is a highly aggressive type of brain tumor, and its prognosis is still poor despite recent progress in treatment strategies. G protein-coupled receptor 27 (GPR27) is a member of the G protein-coupled receptor family and has been reported to be involved in various cellular processes, including tumor progression. Nevertheless, the clinical potential and tumor-related role of GPR27 in glioma remain unknown. Here we aimed to explore the function and role of GPR27 in gliomas. - Source: PubMed
Publication date: 2024/04/15
Cai ChangchengHu LiboWu KeLiu Yinggang - The orphan G protein-coupled receptor GPR27 appears to play a role in insulin production, secretion, lipid metabolism, neuronal plasticity, and l-lactate homeostasis. However, investigations on the function of GPR27 are impaired by the lack of potent and efficacious agonists. We describe herein the development of di- and trisubstituted benzamide derivatives -, -, and -, which display GPR27-specific activity in a β-arrestin 2 recruitment-based assay. Highlighted compounds are PT-91 (: pEC 6.15; 100%) and (pEC 6.56; 99%). A putative binding mode was revealed by the docking studies of and with a GPR27 homology model. The novel active compounds exhibited no GPR27-mediated activation of G proteins, indicating that the receptor may possess an atypical profile. Compound displays high metabolic stability and brain exposure in mice. Thus, represents a novel tool to investigate the elusive pharmacology of GPR27 and assess its potential as a drug target. - Source: PubMed
Publication date: 2023/12/07
Pillaiyar ThanigaimalaiWozniak MonikaAbboud DayanaRasch AlexanderLiebing Aenne-DorotheaPoso AnttiKronenberger ThalesStäubert ClaudiaLaufer Stefan AHanson Julien