The RAF Kinase Inhibitor Protein (RKIP): Good as Tumour Suppressor, Bad for the Heart
The RAF kinase inhibitor protein, RKIP, is a dual inhibitor of the RAF1 kinase and the G protein-coupled receptor kinase 2, GRK2. By inhibition of the RAF1-MAPK (mitogen-activated protein kinase) pathway, RKIP acts as a beneficial tumour suppressor.
Joshua Abd Alla, Ursula Quitterer
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GPER agonist G-1 decreases adrenocortical carcinoma (ACC) cell growth in vitro and in vivo [PDF]
We have previously demonstrated that estrogen receptor (ER) alpha (ESR1) increases proliferation of adrenocortical carcinoma (ACC) through both an estrogen-dependent and -independent (induced by IGF-II/IGF1R pathways) manner.
Amendola, Donatella +16 more
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Desensitization of vascular endothelin receptors by G protein-coupled receptor kinase 2 [PDF]
At the heart of receptor-mediated signal transduction are two intertwined processes: translation of signals carried by stimulating agents to cells through intracellular messenger molecules and termination/restriction of signalling by cells. The latter is a critical mechanism that protects cells from overreacting to an extended or appropriate stimulus ...
openaire +2 more sources
Caterina Iorio et al. use a high-throughput RNAi screen to identify the GPR3-SIK2-CDKN1B axis as key players involved in regulating pancreatic beta cell proliferation.
Caterina Iorio +7 more
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Paroxetine Attenuates Cardiac Hypertrophy Via Blocking GRK2 and ADRB1 Interaction in Hypertension
Background ADRB1 (adrenergic receptor beta 1) responds to neuroendocrine stimulations, which have great implications in hypertension. GRK2 (G protein‐coupled receptor kinase 2) is an essential regulator for many G protein‐coupled receptors and subsequent
Xuejing Sun +9 more
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Agonist-induced internalization and desensitization of the apelin receptor [PDF]
Apelin acts via the G protein-coupled apelin receptor (APJ) to mediate effects on cardiovascular and fluid homeostasis. G protein-coupled receptor (GPCR) trafficking has an important role in the regulation of receptor signalling pathways and cellular ...
Lolait, Stephen J. +4 more
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G protein-coupled receptor kinase 2 (GRK2) is localized to centrosomes and mediates epidermal growth factor-promoted centrosomal separation. [PDF]
G protein-coupled receptor kinases (GRKs) play a central role in regulating receptor signaling, but recent studies suggest a broader role in modulating normal cellular functions.
Benovic, Jeffrey L +4 more
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Smoothened Signal Transduction Is Promoted by G Protein-Coupled Receptor Kinase 2 [PDF]
Deregulation of the Sonic hedgehog pathway has been implicated in an increasing number of human cancers. In this pathway, the seven-transmembrane (7TM) signaling protein Smoothened regulates cellular proliferation and differentiation through activation of the transcription factor Gli.
Meloni, AR +7 more
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Lipid-mediated Regulation of G Protein-coupled Receptor Kinases 2 and 3 [PDF]
G protein-coupled receptor-mediated signaling is attenuated by a process referred to as desensitization, wherein agonist-dependent phosphorylation of receptors by G protein-coupled receptor kinases (GRKs) is proposed to be a key initial event. However, mechanisms that activate GRKs are not fully understood.
S K, DebBurman +5 more
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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 +7 more
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