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 signaling and neural tube closure defects.
Sign Up to like & getrecommendations! Published in 2017 at "Birth defects research"
DOI: 10.1002/bdra.23567
Abstract: Disruption of the normal mechanisms that mediate neural tube closure can result in neural tube defects (NTDs) with devastating consequences in affected patients. With the advent of next-generation sequencing, we are increasingly detecting mutations in… read more here.
Keywords: tube; protein coupled; neural tube; tube closure ... See more keywords
Activation processes in ligand‐activated G protein‐coupled receptors: A case study of the adenosine A2A receptor
Sign Up to like & getrecommendations! Published in 2017 at "BioEssays"
DOI: 10.1002/bies.201700072
Abstract: Here we review concepts related to an ensemble description of G‐protein‐coupled receptors (GPCRs). The ensemble is characterized by both inactive and active states, whose equilibrium populations and exchange rates depend sensitively on ligand, environment, and… read more here.
Keywords: protein; protein coupled; coupled receptors; activation ... See more keywords
Targeting G Protein‐Coupled Receptors with Magnetic Carbon Nanotubes: The Case of the A3 Adenosine Receptor
Sign Up to like & getrecommendations! Published in 2020 at "ChemMedChem"
DOI: 10.1002/cmdc.202000466
Abstract: The A3 adenosine receptor (AR) is a G protein‐coupled receptor (GPCR) overexpressed in the membrane of specific cancer cells. Thus, the development of nanosystems targeting this receptor could be a strategy to both treat and… read more here.
Keywords: adenosine receptor; carbon nanotubes; protein coupled; cancer ... See more keywords
Shuttling of Peptide‐Drug Conjugates by G Protein‐Coupled Receptors Is Significantly Improved by Pulsed Application
Sign Up to like & getrecommendations! Published in 2020 at "Chemmedchem"
DOI: 10.1002/cmdc.202000490
Abstract: G protein‐coupled receptors (GPCRs) can be used to shuttle peptide‐drug conjugates into cells. But, for efficient therapy, a high concentration of cargo needs to be delivered. To explore this, we studied the pharmacologically interesting neuropeptide… read more here.
Keywords: pulsed application; peptide drug; drug; application ... 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
The orphan G protein‐coupled receptor GPR149 is a negative regulator of myelination and remyelination
Sign Up to like & getrecommendations! Published in 2022 at "Glia"
DOI: 10.1002/glia.24233
Abstract: Myelin sheath, formed by oligodendrocytes (OLs) in the central nervous system (CNS) and Schwann cells in periphery, plays a critical role in supporting neuronal functions. OLs, differentiated from oligodendrocyte precursor cells (OPCs), are important for… read more here.
Keywords: orphan protein; remyelination; gpr149; myelination ... See more keywords
Therapeutic Potential of G Protein‐Coupled Receptors Against Nonalcoholic Steatohepatitis
Sign Up to like & getrecommendations! Published in 2021 at "Hepatology"
DOI: 10.1002/hep.31852
Abstract: Nonalcoholic steatohepatitis (NASH), the advanced stage of nonalcoholic fatty liver disease (NAFLD), affects approximately 6% of the population worldwide and is strongly associated with cardiometabolic disorders, placing subjects at a sharply increased risk of end-stage… read more here.
Keywords: protein coupled; therapeutic potential; coupled receptors; nonalcoholic steatohepatitis ... See more keywords
G protein‐coupled estrogen receptor‐1 enhances excitatory synaptic responses in the entorhinal cortex
Sign Up to like & getrecommendations! Published in 2021 at "Hippocampus"
DOI: 10.1002/hipo.23383
Abstract: Activation of estrogen receptors is thought to modulate cognitive function in the hippocampus, prefrontal cortex, and striatum by affecting both excitatory and inhibitory synaptic transmission. The entorhinal cortex is a major source of cortical sensory… read more here.
Keywords: entorhinal cortex; cortex; coupled estrogen; synaptic transmission ... 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
Two neuroendocrine G protein‐coupled receptor molecules, somatostatin and melatonin: Physiology of signal transduction and therapeutic perspectives
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Cellular Physiology"
DOI: 10.1002/jcp.30062
Abstract: Recent studies have shown that G protein‐coupled receptors (GPCRs), the largest signal‐conveying receptor family, are targets for mutations occurring frequently in different cancer types. GPCR alterations associated with cancer development represent significant challenges for the… read more here.
Keywords: protein coupled; physiology; somatostatin melatonin; cancer ... See more keywords