G protein‐coupled receptor binding and pharmacological evaluation of indole‐derived thiourea compounds
Sign Up to like & getrecommendations! Published in 2019 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.201900218
Abstract: Four 2‐(1H‐indol‐3‐yl)ethylthiourea derivatives were prepared by condensation of 2‐(1H‐indol‐3‐yl)ethanamine with the corresponding aryl/alkylisothiocyanates in a medium‐polarity solvent. Their structures were confirmed by spectral techniques, and the molecular structure of 3 was determined by X‐ray crystal… read more here.
Keywords: binding pharmacological; pharmacological evaluation; protein coupled; coupled receptor ... See more keywords
G protein‐coupled receptor 37‐like 1 modulates astrocyte glutamate transporters and neuronal NMDA receptors and is neuroprotective in ischemia
Sign Up to like & getrecommendations! Published in 2018 at "Glia"
DOI: 10.1002/glia.23198
Abstract: We show that the G protein‐coupled receptor GPR37‐like 1 (GPR37L1) is expressed in most astrocytes and some oligodendrocyte precursors in the mouse central nervous system. This contrasts with GPR37, which is mainly in mature oligodendrocytes.… read more here.
Keywords: astrocyte glutamate; protein coupled; coupled receptor; glutamate transporters ... See more keywords
G‐protein‐coupled receptor kinase 2 safeguards epithelial phenotype in head and neck squamous cell carcinomas
Sign Up to like & getrecommendations! Published in 2019 at "International Journal of Cancer"
DOI: 10.1002/ijc.32838
Abstract: Head and neck squamous cell carcinoma (HNSCC) arises from the mucosal lining of the upper aerodigestive tract and display few treatment options in advanced stages. Despite increased knowledge of HNSCC molecular biology, the identification of… read more here.
Keywords: neck squamous; squamous cell; protein coupled; hnscc ... See more keywords
Time-Resolved FRET-Based Assays to Characterize G Protein-Coupled Receptor Hetero-oligomer Pharmacology.
Sign Up to like & getrecommendations! Published in 2019 at "Methods in molecular biology"
DOI: 10.1007/978-1-4939-9121-1_8
Abstract: Although G protein-coupled receptor (GPCR) oligomerization is a matter of debate, it has been shown that the nature of the GPCR partners within the oligomers can influence the pharmacological properties of the receptors. Therefore, finding… read more here.
Keywords: protein coupled; pharmacology; time resolved; coupled receptor ... See more keywords
On the G Protein-Coupled Receptor Neuromodulation of the Claustrum
Sign Up to like & getrecommendations! Published in 2019 at "Neurochemical Research"
DOI: 10.1007/s11064-019-02822-4
Abstract: G protein-coupled receptors modulate the synaptic glutamate and GABA transmission of the claustrum. The work focused on the transmitter–receptor relationships in the claustral catecholamine system and receptor–receptor interactions between kappa opioid receptors (KOR) and SomatostatinR2… read more here.
Keywords: transmission; protein coupled; coupled receptor; receptor ... See more keywords
Discovery of endogenous inverse agonists for G protein-coupled receptor 6.
Sign Up to like & getrecommendations! Published in 2019 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2019.12.004
Abstract: The orphan G protein-coupled receptor 6 (GPR6) is highly expressed in the striatum and has been linked to multiple striatal pathologies. The identification of endogenous ligands and their mechanisms of action at GPR6 will help… read more here.
Keywords: endogenous inverse; inverse agonists; dopamine; protein coupled ... See more keywords
G protein‐coupled receptor 39 plays an anti‐inflammatory role by enhancing IL‐10 production from macrophages under inflammatory conditions
Sign Up to like & getrecommendations! Published in 2018 at "European Journal of Pharmacology"
DOI: 10.1016/j.ejphar.2018.07.045
Abstract: ABSTRACT The possible role of G protein‐coupled receptor 39 (GPR39) in inflammation was examined in macrophages. Gpr39 expression increased in thioglycollate‐induced peritoneal macrophages. TC‐G 1008, a G protein‐coupled receptor 39 agonist, enhanced interleukin (IL)‐10 production… read more here.
Keywords: protein coupled; coupled receptor; production; anti inflammatory ... See more keywords
G-protein coupled receptor 55 agonists increase insulin secretion through inositol trisphosphate-mediated calcium release in pancreatic β-cells.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of pharmacology"
DOI: 10.1016/j.ejphar.2019.04.050
Abstract: G-protein coupled receptor 55 (GPR55) is an orphan G-protein coupled receptor, which is activated by endocannabinoids and lipid transmitters. Recently, GPR55 was shown to play a role in glucose and energy homeostasis, and insulin secretion… read more here.
Keywords: protein coupled; insulin secretion; secretion; coupled receptor ... See more keywords
A Nonsynonymous Change in Adhesion G Protein–Coupled Receptor L3 Associated With Risk for Equine Degenerative Myeloencephalopathy in the Caspian Horse
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Equine Veterinary Science"
DOI: 10.1016/j.jevs.2018.08.010
Abstract: Abstract Equine degenerative myeloencephalopathy (EDM), a neurological disease of young horses, causes progressive development of symmetric ataxia predominantly in the pelvic limbs. Equine degenerative myeloencephalopathy is likely inherited and with no known treatment affected horses… read more here.
Keywords: protein coupled; adhesion protein; coupled receptor; degenerative myeloencephalopathy ... See more keywords
Impact of G protein-coupled receptor heteromers in endocrine systems
Sign Up to like & getrecommendations! Published in 2017 at "Molecular and Cellular Endocrinology"
DOI: 10.1016/j.mce.2017.01.030
Abstract: The fine-tuning of endocrine homeostasis is regulated by dynamic receptor mediated processes. The superfamily of G protein-coupled receptors (GPCRs) have diverse roles in the modulation of all endocrine axes, thus understanding the mechanisms underpinning their… read more here.
Keywords: impact protein; receptor heteromers; heteromers endocrine; protein coupled ... See more keywords
Allosteric interactions via the orthosteric ligand binding sites in a constitutive G-protein-coupled receptor homodimer.
Sign Up to like & getrecommendations! Published in 2020 at "Pharmacological research"
DOI: 10.1016/j.phrs.2020.105116
Abstract: I interpret some recent data to indicate that co-operative effects take place between the (identical) orthosteric binding sites in a G-protein-coupled receptor dimer. In the current study, the reasonability of this concept was tested by… read more here.
Keywords: protein coupled; coupled receptor; binding sites; receptor ... See more keywords