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
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
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
Allosteric modulation of G protein‐coupled receptors by amiloride and its derivatives. Perspectives for drug discovery?
Sign Up to like & getrecommendations! Published in 2019 at "Medicinal Research Reviews"
DOI: 10.1002/med.21633
Abstract: The function of G protein‐coupled receptors (GPCRs) can be modulated by compounds that bind to other sites than the endogenous orthosteric binding site, so‐called allosteric sites. Structure elucidation of a number of GPCRs has revealed… read more here.
Keywords: amiloride analogs; receptors amiloride; protein coupled; coupled receptors ... See more keywords
A robust antibody discovery platform for difficult‐to‐express G protein‐coupled receptors
Sign Up to like & getrecommendations! Published in 2022 at "Protein Science"
DOI: 10.1002/pro.4520
Abstract: G protein‐coupled receptors (GPCRs) are in the spotlight as drug targets due to the fact that multiple research results have verified the correlation between the activation of GPCRs and disease indications. This is because the… read more here.
Keywords: difficult express; coupled receptors; gpcrs; protein coupled ... See more keywords
Genetic variants of G‐protein coupled receptors associated with pubertal disorders
Sign Up to like & getrecommendations! Published in 2023 at "Reproductive Medicine and Biology"
DOI: 10.1002/rmb2.12515
Abstract: Abstract Background The human hypothalamic–pituitary‐gonadal (HPG) axis is the regulatory center for pubertal development. This axis involves six G‐protein coupled receptors (GPCRs) encoded by KISS1R, TACR3, PROKR2, GNRHR, LHCGR, and FSHR. Methods Previous studies have… read more here.
Keywords: hpg axis; protein coupled; pubertal disorders; coupled receptors ... See more keywords
Homology Modeling of Class A G-Protein-Coupled Receptors in the Age of the Structure Boom.
Sign Up to like & getrecommendations! Published in 2021 at "Methods in molecular biology"
DOI: 10.1007/978-1-0716-1468-6_5
Abstract: With 700 members, G protein-coupled receptors (GPCRs) of the rhodopsin family (class A) form the largest membrane receptor family in humans and are the target of about 30% of presently available pharmaceutical drugs. The recent… read more here.
Keywords: boom; protein coupled; coupled receptors; homology modeling ... See more keywords
Fragments of the second transmembrane helix of three G-protein-coupled receptors: comparative synthetic, structural and conformational studies
Sign Up to like & getrecommendations! Published in 2018 at "Amino Acids"
DOI: 10.1007/s00726-018-2662-z
Abstract: We compared the synthesis and structural/conformational details of the (66–97) segments of the second transmembrane helix of AT1, MAS and B2, all of which belong to the class of G-protein-coupled receptors (GPCR). Step-by-step monitoring of… read more here.
Keywords: second transmembrane; protein coupled; coupled receptors; transmembrane helix ... See more keywords
Function-related conformational dynamics of G protein–coupled receptors revealed by NMR
Sign Up to like & getrecommendations! Published in 2019 at "Biophysical Reviews"
DOI: 10.1007/s12551-019-00539-w
Abstract: G protein–coupled receptors (GPCRs) function as receptors for various neurotransmitters, hormones, cytokines, and metabolites. GPCR ligands impart differing degrees of signaling in the G protein and arrestin pathways, in phenomena called biased signaling, and each… read more here.
Keywords: biased signaling; conformational dynamics; protein coupled; coupled receptors ... See more keywords
Targeting G protein-coupled receptors in cancer therapy.
Sign Up to like & getrecommendations! Published in 2020 at "Advances in cancer research"
DOI: 10.1016/bs.acr.2019.11.002
Abstract: As basic research into GPCR signaling and its association with disease has come into fruition, greater clarity has emerged with regards to how these receptors may be amenable to therapeutic intervention. As a diverse group… read more here.
Keywords: research; targeting protein; protein coupled; receptors cancer ... See more keywords
Oligomerization of G protein-coupled receptors: Still doubted?
Sign Up to like & getrecommendations! Published in 2020 at "Progress in molecular biology and translational science"
DOI: 10.1016/bs.pmbts.2019.11.006
Abstract: Experimental data accumulated during the last 10 years strongly support the existence and functional significance of oligomerization of G protein-coupled receptors (GPCRs). In this essay, we discuss the unique biochemical properties of GPCR oligomers in… read more here.
Keywords: protein coupled; coupled receptors; gpcr oligomers; oligomerization protein ... See more keywords