Partial agonism improves the anti-hyperglycaemic efficacy of an oxyntomodulin-derived GLP-1R/GCGR co-agonist
Sign Up to like & getrecommendations! Published in 2021 at "Molecular Metabolism"
DOI: 10.1016/j.molmet.2021.101242
Abstract: Objective Glucagon-like peptide-1 and glucagon receptor (GLP-1R/GCGR) co-agonism can maximise weight loss and improve glycaemic control in type 2 diabetes and obesity. In this study, we investigated the cellular and metabolic effects of modulating the… read more here.
Keywords: glp gcgr; arrestin recruitment; weight loss; efficacy ... See more keywords
Arrestin recruitment and signaling by G protein-coupled receptor heteromers
Sign Up to like & getrecommendations! Published in 2019 at "Neuropharmacology"
DOI: 10.1016/j.neuropharm.2018.11.010
Abstract: G protein-coupled receptors (GPCR) have a long history of being considered a prime target for drug development to treat a plethora of diseases and disorders. In fact in 1827, the first approved therapeutic in the… read more here.
Keywords: protein; recruitment signaling; receptor heteromers; arrestin recruitment ... See more keywords
Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over β-Arrestin 2 Recruitment) Within the Melanocortin Receptors.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00238
Abstract: Understanding the functional relevance of G protein-coupled receptor (GPCR) homodimerization has been limited by the insufficient tools to assess asymmetric signaling occurring within dimers comprised of the same receptor type. We present unmatched bivalent ligands… read more here.
Keywords: arrestin recruitment; allosteric signaling; unmatched bivalent; receptor ... See more keywords
The Role of Orthosteric Building Blocks of Bitopic Ligands for Muscarinic M1 Receptors
Sign Up to like & getrecommendations! Published in 2020 at "ACS Omega"
DOI: 10.1021/acsomega.0c04220
Abstract: The muscarinic M1 acetylcholine receptor is an important drug target for the treatment of various neurological disorders. Designing M1 receptor-selective drugs has proven challenging, mainly due to the high conservation of the acetylcholine binding site… read more here.
Keywords: receptor; bitopic ligands; arrestin recruitment;
Dopamine-induced arrestin recruitment and desensitization of the dopamine D4 receptor is regulated by G protein-coupled receptor kinase-2
Sign Up to like & getrecommendations! Published in 2023 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2023.1087171
Abstract: The dopamine D4 receptor (D4R) is expressed in the retina, prefrontal cortex, and autonomic nervous system and has been implicated in attention deficit hyperactivity disorder (ADHD), substance use disorders, and erectile dysfunction. D4R has also… read more here.
Keywords: desensitization; dopamine receptor; dopamine; d4r ... See more keywords
Improved Split TEV GPCR β-arrestin-2 Recruitment Assays via Systematic Analysis of Signal Peptide and β-arrestin Binding Motif Variants
Sign Up to like & getrecommendations! Published in 2022 at "Biosensors"
DOI: 10.3390/bios13010048
Abstract: G protein-coupled receptors (GPCRs) are major disease-relevant drug targets; robust monitoring of their activities upon drug treatment is key to drug discovery. The split TEV cell-based assay technique monitors the interaction of an activated GPCR… read more here.
Keywords: gpcr arrestin; split tev; arrestin recruitment; tev ... See more keywords
New Insights into Arrestin Recruitment to GPCRs
Sign Up to like & getrecommendations! Published in 2020 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms21144949
Abstract: G protein-coupled receptors (GPCRs) are cellular master regulators that translate extracellular stimuli such as light, small molecules or peptides into a cellular response. Upon ligand binding, they bind intracellular proteins such as G proteins or… read more here.
Keywords: new insights; insights arrestin; recruitment gpcrs; arrestin recruitment ... See more keywords