The human orphan nuclear receptor tailless (TLX, NR2E1) is druggable. [PDF]
Nuclear receptors (NRs) are an important group of ligand-dependent transcriptional factors. Presently, no natural or synthetic ligand has been identified for a large group of orphan NRs.
Cindy Benod +9 more
doaj +1 more source
Transcriptional up-regulation of relaxin-3 by Nur77 attenuates β-adrenergic agonist-induced apoptosis in cardiomyocytes. [PDF]
The relaxin family peptides have been shown to exert several beneficial effects on the heart, including anti-apoptosis, anti-fibrosis, and anti-hypertrophy activity.
Cheng, Fang +10 more
core +1 more source
A universal ROR1 antibody‐engineered lipid nanoparticle (LNP) is constructed by sequential drug encapsulation and antibody conjugation. The LNP not only enables enhanced chemotherapeutic efficiency by targeting drug delivery and precise localization of deep‐seated tumors through NIR‐II fluorescence imaging, but also remodels immunosuppressive TME ...
Yeneng Dai +12 more
wiley +1 more source
The Histamine H4 Receptor: From Orphan to the Clinic
The histamine H4 receptor (H4R) was first noted as a sequence in genomic databases that had features of a G-protein coupled receptor. This putative receptor was found to bind histamine consistent with its homology to other histamine receptors and thus ...
Robin L. Thurmond
doaj +1 more source
The RNA-binding protein HuR contributes to neuroinflammation by promoting C-C chemokine receptor 6 (CCR6) expression on Th17 cells. [PDF]
In both multiple sclerosis and experimental autoimmune encephalomyelitis (EAE), the C-C chemokine receptor 6 (CCR6) is critical for pathogenic T helper 17 (Th17) cell migration to the central nervous system (CNS).
Atasoy, Ulus +6 more
core +2 more sources
Microglial GPR35 Ameliorates Epileptogenesis and Neuroinflammation via PDGFA Domain 2 Signaling
Activation of microglial G protein–coupled receptor 35 (GPR35) by L‐kynurenic acid (L‐Kyna) initiates a platelet‐derived growth factor A (PDGFA)–dependent phosphoinositide 3‐kinase–protein kinase B (PI3K–AKT) signaling cascade that dampens hippocampal neuroinflammation, thereby restraining epileptogenesis, lowering seizure susceptibility, and ...
Qi Wang +17 more
wiley +1 more source
PACAP-38 and PACAP(6–38) Degranulate Rat Meningeal Mast Cells via the Orphan MrgB3-Receptor
Infusion of pituitary adenylate cyclase activating peptide-38 (PACAP-38) provokes migraine attacks in migraineurs and headache in non-migraineurs. Adverse events like long-lasting flushing and heat sensation can be terminated with oral antihistamine ...
Sara Hougaard Pedersen +10 more
doaj +1 more source
Functional classification of G-Protein coupled receptors, based on their specific ligand coupling patterns [PDF]
Functional identification of G-Protein Coupled Receptors (GPCRs) is one of the current focus areas of pharmaceutical research. Although thousands of GPCR sequences are known, many of them re- main as orphan sequences (the activating ligand is unknown ...
Bakır, Burcu, Sezerman, Uğur
core +1 more source
Impaired endometrial receptivity contributes to the poor pregnancy outcomes in women with PCOS. The authors found that decreased endometrial IL‐22 levels and disrupted STAT3‐IGFBP5 signaling pathway contributed to impaired endometrial receptivity. Supplementation with IL‐22 or IGFBP5 exerts a protective effect on implantation failure in PCOS‐like mice,
Baoying Liao +13 more
wiley +1 more source
Mechanism of μ-opioid receptor inhibition by orphan GPR88
From the approximately 800 members of the G protein-coupled receptor (GPCR) family, more than 100 remain orphans (oGPCRs). There is evidence indicating that some oGPCRs may carry out a physiological role independently from endogenous ligands; this ...
Claudia Llinas del Torrent +7 more
doaj +1 more source

