“ATR-258, a synthetic small molecule, has favourable pharmacokinetics and in Phase 1 clinical trials has been administered just once a day as a capsule, making it a straightforward, patient-friendly ...

Nitric oxide (NO) and S-nitrosothiol (SNO) have cardiovascular-protective properties and we have shown that one mechanism is through SNO-modification of G protein-coupled receptor (GPCR) kinase 2 ...

Background: The G-protein coupled receptor kinase 5 (GRK5) plays a crucial role in regulating G protein-coupled receptors (GPCRs), which are a diverse group of cell surface receptors. GRK5 ...

In October, the pharma giant entered into a collaboration and licensing deal with Nimbus Therapeutics to drug the AMPK-activated protein kinase, a central target in metabolic diseases. In total, Lilly ...

The canonical view of GPCRs is that they sit on the cell membrane where they activate a variety of reactions, including an enzyme called extracellular-signal-regulated kinase (ERK), which triggers a ...

Writing in Nature, Chen et al. 1 report the first structure of a GPCR–GRK complex: the light-responsive receptor rhodopsin bound to its specific kinase, GRK1 (also known as rhodopsin kinase).

GPCR phosphorylation patterns are also influenced by second messenger kinases like protein kinase A (PKA) or protein kinase C (PKC) (Figure 2D). Those kinases are activated via the primary G s or G q ...

G protein-coupled receptor kinase 2 (GRK2) is an adapter protein that modulates G protein-coupled receptor (GPCR) signaling. It also regulates the functions and activity of other intracellular ...

Cahill T et al. Distinct conformations of GPCR–β-arrestin complexes mediate desensitization, signaling, and endocytosis. Proc Natl Acad Sci USA. 2017 Mar 7;114 (10):2562-2567.

We aimed to understand how spatial compartmentalization in the plasma membrane might contribute to the functions of the ubiquitous class IA phosphoinositide 3-kinase (PI3K) isoforms, p110α and p110β.

Therefore, it is important to assess other cellular effectors activated by GPCRs such as the extracellular signal-regulated kinase (ERK), which can be activated by both G protein and β-arrestin.