Results 91 to 100 of about 6,551 (208)

Profiling of HCAR1 signalling reveals Gαi/o and Gαs activation without β‐arrestin recruitment and the discovery of an allosteric agonist

British Journal of Pharmacology, Volume 183, Issue 10, Page 2219-2235, May 2026.
Abstract Background and Purpose Lactate, historically viewed as a metabolic by‐product, has emerged as a signalling molecule via the G protein–coupled receptor Hydroxycarboxylic Acid Receptor 1 (HCAR1). The receptor is primarily expressed in adipocytes but also found in various other tissues.
Simon Lind, Shane C. Wright, Emilia Gvozdenovic, Kristina Nilsson, Kenneth L. Granberg, Michel Bouvier, Linda C. Johansson   +6 more
wiley   +1 more source

GRK2-mediated AKT activation controls cell cycle progression and G2 checkpoint in a p53-dependent manner

Cell cycle checkpoints, activated by stressful events, halt the cell cycle progression, and prevent the transmission of damaged DNA. These checkpoints prompt cell repair but also trigger cell death if damage persists.
Delgado-Arévalo, Cristina, González-Muñoz, Teresa, Penela, Petronila, Lafarga, Vanesa, Rivas, Verónica, Albitre, Ángela, Mayor, Federico   +6 more
core   +1 more source

Hepatic GRK2 is dispensable for glucose homeostasis and other key metabolic parameters in mice

Molecular Metabolism
Objective: G-protein-coupled receptor (GPCR) kinases (GRKs) abrogate GPCR signaling by promoting receptor desensitization and internalization. Accumulating evidence suggests that GRK2 represents an important regulator of GPCR-mediated effects on systemic
Antwi-Boasiako Oteng, Srinivas Pittala, Andrea Kliewer, Yishu Qiu, Jürgen Wess   +4 more
doaj   +1 more source

GRK2 expression is enhanced in neutrophils during acute malaria.

, 2013
Neutrophils isolated from P. vivax-infected patients (closed circles; n = 11) or healthy donors (closed circles; n = 12) were stained for GRK2 and mean fluorescence intensity (MFI) of GRK2 was quantified (A).
Ricardo T. Gazzinelli (164680), Silvia Cellone Trevelin (318226), Mauro Shugiro Tada (318232), Dhelio Batista Pereira (318235), Pedro Augusto Carvalho Costa (133954), Lis Ribeiro do Valle Antonelli (318240), Bruno Coelho Rocha (318228), Douglas Taylor Golenbock (318237), Humberto Doriguêtto Gravina (318230), Fernando Queiroz Cunha (318227), Fabiana Maria de Souza Leoratti (318225)   +10 more
core   +1 more source

Extracellular signal-regulated kinases control expression of G protein-coupled receptor kinase 2 (GRK2) [PDF]

, 2002
G protein-coupled receptor kinase 2 (GRK2) phosphorylates G protein-coupled receptors resulting in uncoupling from G proteins. Receptors modulate GRK2 expression, however the mechanistic basis for this effect is largely unknown.
Lerche Hansen, Jakob, Stig Haunsø, Sheikh, Søren P, Theilade, Juliane, Juliane Theilade, Søren P Sheikh, Haunsø, Stig, Jakob Lerche Hansen   +7 more
core   +1 more source

The Role of Mitochondrial GRK2 in the Pathogenesis and Progression of Heart Failure

, 2022
Rationale: G protein-coupled receptor (GPCR) kinases (GRKs) are important regulators of cardiac function whose primary role is the phosphorylation of GPCRs and attenuation of downstream signaling, and GRK2 is upregulated after cardiac stress, injury ...
Ferrero, Kimberly, 0000-0001-9711-7683
core   +1 more source

Development of Inflammatory Immune Response-Related Drugs Based on G Protein-Coupled Receptor Kinase 2

Cellular Physiology and Biochemistry, 2018
G protein-coupled receptor kinase 2 (GRK2), as a vital Ser/Thr kinase, is an important regulatory protein in the inflammatory immune response (IIR) by maintaining the balance between the function of inflammatory immune cells and non-conventional ...
Chenchen Han, Yifan Li, Yang Wang, Dongqian Cui, Tingting Luo, Yuwen Zhang, Yang Ma, Wei  Wei   +7 more
doaj   +1 more source

Unveiling the Role of GRK2: From Immune Regulation to Cancer Therapeutics

Mediators of Inflammation
G protein-coupled receptors (GPCRs) represent humans’ most prominent family of membrane proteins. In contrast, G protein-coupled receptor kinases (GRKs) play a pivotal role in the rapid desensitization of GPCRs.
Xizhuang Gao, Dehuai Jing, Yaowen Zhang, Fengqin Zhu, Yonghong Yang, Guangxi Zhou   +5 more
doaj   +1 more source

Early intervention of baicalin suppresses obesity-induced adipose tissue fibrotic remodeling through Interfering NF-κB/HIF-1ɑ/GRK2 Signaling Pathway

Phytomedicine Plus
Obesity-induced adipose tissue (AT) fibrosis is difficult to reverse, indicating the importance of early intervention. G protein-coupled receptor kinase 2 (GRK2) is a potential regulator of energy metabolism.
Ying Zeng, Wenting Li, Tingting Ma, Honglei Zhang, Jiaxing Xu, Kang Liu   +5 more
doaj   +1 more source

Cell-Type Specific GRK2 Interactomes: Pathophysiological Implications [PDF]

, 2018
G protein-coupled receptor kinase 2 (GRK2) is emerging as a key hub in cell signaling cascades. In addition to modulating activated G protein-coupled receptors, GRK2 can phosphorylate and/or functionally interact with a complex network of cellular ...
Penela Márquez, Petronila, Nogués Vera, Laura, Reglero Gómez, Clara, Mayor Menéndez, Federico, Vila Bedmar, Rocio, Murga Montesinos, Cristina, Lucas, Elisa, Cruces Sande, Marta, Rivas Guerrero, Verónica   +8 more
core   +1 more source