Results 171 to 180 of about 6,839 (207)

G protein-coupled receptor kinase 2 (GRK2) in migration and inflammation

Archives of Physiology and Biochemistry, 2008
G protein-coupled receptor kinase 2 (GRK2) is a key modulator of G protein-coupled receptors and other plasma membrane receptors stimulated by chemotactic messengers. On top of that, GRK2 has been reported to interact with a variety of signal transduction proteins related to cell migration such as MEK, Akt, PI3Kgamma or GIT.
Petronila, Penela, Cristina, Murga, Catalina, Ribas, Alicia, Salcedo, María, Jurado-Pueyo, Veronica, Rivas, Ivette, Aymerich, Federico, Mayor   +7 more
openaire   +2 more sources

A high-affinity peptide substrate for G protein-coupled receptor kinase 2 (GRK2)

Amino Acids, 2019
We synthesized a previously identified β-tubulin-derived G protein-coupled receptor kinase 2 (GKR2) peptide (GR-11-1; DEMEFTEAESNMN) and its amino-terminal extension (GR-11-1-N; GEGMDEMEFTEAESNMN) and carboxyl-terminal extension (GR-11-1-C; DEMEFTEAESNMNDLVSEYQ) peptides with the aim of finding a high-affinity peptide substrate for GRK2.
Daisuke Asai, Masaharu Murata, Riki Toita, Takahito Kawano, Hideki Nakashima, Jeong-Hun Kang   +5 more
openaire   +2 more sources

G protein-coupled receptor kinase 2 (GRK2) is a Rho-activated scaffold protein for the ERK MAP kinase cascade

Cellular Signalling, 2013
The G protein-coupled receptor kinases (GRKs) are best known for their role in phosphorylating and desensitising G protein-coupled receptors (GPCRs). The GRKs also regulate signalling downstream of other families of receptors and have a number of non-receptor substrates and binding partners.
Robinson, James D., Pitcher, Julie A.
exaly   +3 more sources

G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives

Journal of Medicinal Chemistry, 2016
G-protein-coupled receptor kinase 2 (GRK2) is a G-protein-coupled receptor kinase that is ubiquitously expressed in many tissues and regulates various intracellular mechanisms. The up- or down-regulation of GRK2 correlates with several pathological disorders.
GUCCIONE, MANUELA, ETTARI, Roberta, Taliani, Sabrina, Da Settimo, Federico, ZAPPALA', Maria, GRASSO, Silvana   +5 more
openaire   +4 more sources

Regulation of mGlu4 Metabotropic Glutamate Receptor Signaling by Type-2 G-Protein Coupled Receptor Kinase (GRK2)

Molecular Pharmacology, 2004
We examined the role of G-protein coupled receptor kinase-2 (GRK2) in the homologous desensitization of mGlu4 metabotropic glutamate receptors transiently expressed in human embryonic kidney (HEK) 293 cells. Receptor activation with the agonist l-2-amino-4-phosphonobutanoate (l-AP4) stimulated at least two distinct signaling pathways: inhibition of ...
IACOVELLI, LUISA, L. Capobianco, M. Iula, V. Di Giorgi Gerevini, A. Picascia, J. Blahos, MELCHIORRI, Daniela, NICOLETTI, Ferdinando, DE BLASI, ANTONIO   +8 more
openaire   +2 more sources

Design of substrates and inhibitors of G protein-coupled receptor kinase 2 (GRK2) based on its phosphorylation reaction

Amino Acids, 2020
The G protein-coupled receptor kinase (GRK) family consists of seven cytosolic serine/threonine (Ser/Thr) protein kinases, and among them, GRK2 is involved in the regulation of an enormous range of both G protein-coupled receptors (GPCRs) and non-GPCR substrates that participate in or regulate many critical cellular processes.
Jeong-Hun Kang, Riki Toita, Takahito Kawano, Masaharu Murata, Daisuke Asai   +4 more
openaire   +2 more sources

Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor

Bioorganic & Medicinal Chemistry Letters, 2020
G-protein coupled receptor kinase 2 (GRK2), which is upregulated in the failing heart, appears to play a critical role in heart failure (HF) progression in part because enhanced GRK2 activity promotes dysfunction of β-adrenergic signaling and myocyte death.
Guozhang Xu, Michael D. Gaul, Zhijie Liu, Renee L. DesJarlais, Jenson Qi, Weixue Wang, Daniel Krosky, Ioanna Petrounia, Cynthia M. Milligan, An Hermans, Hua-Rong Lu, Devine Zheng Huang, June Zhi Xu, John C. Spurlino   +13 more
openaire   +2 more sources

Investigation of G protein‐coupled receptor kinase 2 (GRK2) regulation of D ₂ dopamine receptor signaling: effects of GRK2 functional domains and pharmacologic and genetic inhibition of GRK2 activity

The FASEB Journal, 2020
The D2 dopamine (DA) receptor (D2R) signals through two major pathways, namely activation of G proteins and recruitment of β‐arrestin. Agonist binding stabilizes a receptor state that activates G proteins and facilitates receptor phosphorylation by one or more members of the G protein ...
Kayla Anne Schardien, Marta Sanchez Soto, Laura Inbody, Yamina Berchiche, John H. Kehrl, Clinton Bradfield, R. Benjamin Free, David R. Sibley   +7 more
openaire   +1 more source

G protein-coupled receptor kinase 2 (GRK2) as an integrative signalling node in the regulation of cardiovascular function and metabolic homeostasis

Cellular Signalling, 2018
G protein-coupled receptor kinase 2 (GRK2) is emerging as a pivotal signalling hub able to integrate different transduction cascades. This ability appears to underlie its central role in different physiological and pathological conditions. Key mediators of cardiovascular function (such as catecholamines or angiotensin II) and components of the systemic
Federico, Mayor, Marta, Cruces-Sande, Alba C, Arcones, Rocío, Vila-Bedmar, Ana M, Briones, Mercedes, Salaices, Cristina, Murga   +6 more
openaire   +2 more sources

Tyrosine phosphorylation of G-protein-coupled-receptor kinase 2 (GRK2) by c-Src modulates its interaction with Gαq

Cellular Signalling, 2006
G-protein-coupled-receptor kinase 2 (GRK2) plays a key role in the modulation of G-protein-coupled-receptor (GPCR) signaling by both phosphorylating agonist-occupied GPCRs and by directly binding to activated Galphaq subunits, inhibiting downstream effectors activation.
MARIGGIO S, GARCIA HOZ C, SARNAGO S, DE BLASI, ANTONIO, MAYOR F. JR, RIBAS C.   +5 more
openaire   +3 more sources