Tag Archives: G protein
Ca2+ dynamics and allosterism in synergistic action between Beta2-adrenergic agonists and muscarinic antagonists
G proteins (Gs, Gi)/large conductance Ca2+-activated K+ (KCa) channels/L-type voltage-dependent Ca2+ (VDC) channels linkage (Ca2+ dynamics) may play key roles in β2-adrenergic relaxation and muscarinic contraction in the airways. β2-Adrenergic receptor agonists and muscarinic receptor antagonists are
Substrate phosphoswitching: a novel way to regulate enzymatic activity by phosphorylation of its substrate
Cells sense a vast variety of signals by receptors that are distributed on their surface. This perception transduces internal physiological responses using signal pathways, a cascade of protein interacting to bring a change in the cell behavior.
A selective AC1 inhibitor relieves pain
Adenylyl cyclases (AC) are proteins expressed throughout the human body. ACs have a central role in cellular and neuronal function. A number of different proteins and ions can interact with ACs and modulate their activity. ACs have
Watching caveolae under stress
The plasma membrane of many cells contain many protein-dense invaginations called caveolae or ‘little caves’. Caveolae are composed of ~140 molecules of caveolin proteins along with other components. Caveolae are thought to act like springs and flatten
Direct regulation of G protein signal strength as a new drug target?
Heterotrimeric GTP-binding proteins (G proteins) remain an important but elusive target in drug discovery. G proteins adapt cell behavior in response to signals generated by cell surface receptors, G protein coupled receptors (GPCRs). Clinical interest in G
G protein signaling: a major culprit of essential hypertension
Blood pressure (BP) is the driving force that distributes the blood to the organs of the body according to their instantanous needs. It may be increased by pressor agents acting on the heart, vessels, and blood volume,
Active-state of AT1 receptor attenuates inverse agonism of ARBs through changes in specific ligand-receptor interactions
G protein – coupled receptors (GPCRs) constitute one of the largest gene superfamilies in the human genome. The angiotensin II ( Ang II ) type 1 receptor ( AT1R ) belongs to G – protein coupled receptor
Phospholipases have a second job, regulating their G proteins
Can we make a weak heart healthy? Can we prevent decline in memory and cognitive ability? The answer may depend on a class of enzymes, phospholipase C (PLC), and their under-investigated ability to directly regulate their specific
