Results 101 to 110 of about 113,722 (335)

Astrocytic ET‐1 System Determines Microglia Phenotype Following Spinal Cord Injury

open access: yesAdvanced Science, EarlyView.
The study reveals that astrocytic ET‐1 system is solely activated by thrombin following SCI via RhoA/NF‐κB and MAPKs/NF‐κB signal pathway. The release of astrocytic ET‐1 drives microglia polarization toward M1 phenotype through YAP signaling via ETA and ETB receptors.
Bingqiang He   +11 more
wiley   +1 more source

Targeting Gi/o protein–coupled receptor signaling blocks HER2-induced breast cancer development and enhances HER2-targeted therapy

open access: yesJCI Insight, 2021
GPCRs are highly desirable drug targets for human disease. Although GPCR dysfunction drives development and progression of many tumors, including breast cancer (BC), targeting individual GPCRs has limited efficacy as a cancer therapy because numerous ...
Cancan Lyu   +5 more
doaj   +1 more source

Systematic analysis of primary sequence domain segments for the discrimination between class C GPCR subtypes [PDF]

open access: yes, 2018
G-protein-coupled receptors (GPCRs) are a large and diverse super-family of eukaryotic cell membrane proteins that play an important physiological role as transmitters of extracellular signal. In this paper, we investigate Class C, a member of this super-
Alquézar Mancho, René   +3 more
core   +2 more sources

TBXA2R gene variants associated with bleeding

open access: yesPlatelets, 2018
Platelet activity is regulated by a number of surface expressed G protein-coupled receptors (GPCRs) including the α isoform of the thromboxane receptor (TPα receptor). With the advance of genomic technologies, there has been a substantial increase in the
Stuart James Mundell, Andrew Mumford
doaj   +1 more source

Functional selectivity of GPCR-directed drug action through location bias. [PDF]

open access: yes, 2017
G-protein-coupled receptors (GPCRs) are increasingly recognized to operate from intracellular membranes as well as the plasma membrane. The β 2 -adrenergic GPCR can activate G s -linked cyclic AMP (G s -cAMP) signaling from endosomes.
Conti, Marco   +6 more
core   +3 more sources

Regulation of Chondrocyte Metabolism and Osteoarthritis Development by Sirt5 Through Protein Lysine Malonylation

open access: yesArthritis &Rheumatology, EarlyView.
Objective Chondrocytemetabolic dysfunction plays an important role in osteoarthritis (OA) development during aging and obesity. Protein posttranslational modifications (PTMs) have recently emerged as an important regulator of cellular metabolism. We aim to study one type of PTM, lysine malonylation (MaK), and its regulator sirtuin 5 (Sirt5) in OA ...
Huanhuan Liu   +11 more
wiley   +1 more source

Antibodies Against GPCR

open access: yesFrontiers in Bioscience, 2018
G-protein-coupled receptors (GPCRs) are the largest family of receptors in humans. GPCRs are seven-transmembrane receptors that are activated by the binding of a ligand to the extracellular domain. In addition to the endogenous ligands, auto-antibodies (aab) can also bind to the GPCRs.
Harald Heidecke, Carlotto Meyer
openaire   +2 more sources

Metal‐Mediated Protein Engineering within Live Cells

open access: yesChemistry – An Asian Journal, Volume 20, Issue 6, March 17, 2025.
This review discusses how metal ions can mediate protein modification within live cells. With its easy handling, rapid solubility, and ease of internalization within the cells, metal ions can be an excellent stimulus for many organic reactions needed within an intracellular medium, which can modify proteins and lead to applications in chemistry ...
Pritam Ghosh
wiley   +1 more source

Agonist and antagonist TRUPATH assays for G protein-coupled receptors

open access: yesSTAR Protocols, 2022
Summary: TRUPATH is a bioluminescence resonance energy transfer-based platform for quantifying G protein-coupled receptor activity via dissociation of heterotrimeric G protein biosensors.
Jeffrey F. DiBerto   +3 more
doaj  

GPCR heterodimerization in the reproductive system: functional regulation and implication for biodiversity

open access: yesFrontiers in Endocrinology, 2013
A G protein-coupled receptor (GPCR) functions not only as a monomer or homodimer but also as a heterodimer with another GPCR. GPCR heterodimerization results in the modulation of the molecular functions of the GPCR protomer, including ligand binding ...
Honoo eSatake   +4 more
doaj   +1 more source

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