English Journal

Effects of the new ultra-long-acting β2 -AR agonist indacaterol in chronic treatment alone or in combination with the β1 -AR blocker metoprolol on cardiac remodelling.

Rinaldi B1, Donniacuo M, Sodano L, Gritti G, Martuscelli E, Orlandi A, Rafaniello C, Rossi F, Calzetta L, Capuano A, Matera MG.
British journal of pharmacology.Br J Pharmacol.2015 Mar 30. doi: 10.1111/bph.13148. [Epub ahead of print]
BACKGROUND AND PURPOSE: The role and the mechanism of a chronic treatment with indacaterol, a new ultra-long-acting a β2 -AR agonist on the reverse cardiac remodelling and its effects in combination with metoprolol, a selective β1 -AR antagonist, have been investigated in a myocardial infarction (
PMID 25825265

IL-13 desensitizes β2-adrenergic receptors in human airway epithelial cells through a 15-lipoxygenase/G protein receptor kinase 2 mechanism.

Albano GD1, Zhao J2, Etling EB3, Park SY4, Hu H3, Trudeau JB3, Profita M5, Wenzel SE3.
The Journal of allergy and clinical immunology.J Allergy Clin Immunol.2015 Mar 24. pii: S0091-6749(15)00226-2. doi: 10.1016/j.jaci.2015.02.006. [Epub ahead of print]
BACKGROUND: β2-Adrenergic receptor (β2AR) agonists are critical treatments for asthma. However, receptor desensitization can lead to loss of therapeutic effects. Although desensitization to repeated use of β2-agonists is well studied, type 2 inflammation could also affect β2AR function.OBJECTIVE
PMID 25819984

G protein-coupled receptor kinases of the GRK4 subfamily phosphorylate inactive GPCRs.

Li L1, Homan KT2, Vishnivetskiy SA1, Manglik A3, Tesmer JJ2, Gurevich VV1, Gurevich EV4.
The Journal of biological chemistry.J Biol Chem.2015 Mar 13. pii: jbc.M115.644773. [Epub ahead of print]
G protein-coupled receptor (GPCR) kinases (GRKs) play key role in homologous desensitization of GPCRs. It is widely assumed that most GRKs selectively phosphorylate only active GPCRs. Here we show that although this seems to be the case for GRK2/3 subfamily, GRK5/6 effectively phosphorylate inactive
PMID 25770216

Japanese Journal

Y1-3 2型糖尿病時におけるAkt/NOS経路を介した血管弛緩反応減弱とGRK2/β-Arrestin2の関係(優秀演題賞候補口演1,第53回日本平滑筋学会総会)

田口久美子,小林恒雄,松本貴之,鎌田勝雄
日本平滑筋学会雑誌 15(1), "J-16", 2011-07-06
NAID 110008686524

S3-6 2型糖尿病時におけるGRK2を介したAkt/eNOS経路の抑制と血管弛緩反応の減弱(平滑筋におけるシグナル伝達研究のカッティングエッジ,シンポジウム3,第52回日本平滑筋学会総会)

田口久美子,小林恒雄,松本貴之,鎌田勝雄
日本平滑筋学会雑誌 14(1), "J-16", 2010-06-11
NAID 110007643186

Related Pictures

The Gα q -GRK2-Gβγ heterotrimer (Tesmer GRK2+GD]GRK2+ Yellow Gold implications of the GRK2 interactome GRK2 inhibition for heart failure therapy Figure 1. 切れ角も十分すぎるほど切れて GRK2 カラー：パープル No.GRK2-PP Excitation Contraction Coupling Skeletal