Structural Connection between Activation Microswitch and Allosteric Sodium Site in GPCR Signaling
نویسندگان
چکیده
منابع مشابه
Allosteric communication between protomers of dopamine Class A GPCR dimers modulates activation
A major obstacle to understanding the functional importance of dimerization between class A G protein-coupled receptors (GPCRs) has been the methodological limitation in achieving control of the identity of the components comprising the signaling unit. We have developed a functional complementation assay that enables such control, and we demonstrate it here for the human dopamine D2 receptor. T...
متن کاملMolecular Mechanisms of GPCR Signaling: A Structural Perspective
G protein-coupled receptors (GPCRs) are cell surface receptors that respond to a wide variety of stimuli, from light, odorants, hormones, and neurotransmitters to proteins and extracellular calcium. GPCRs represent the largest family of signaling proteins targeted by many clinically used drugs. Recent studies shed light on the conformational changes that accompany GPCR activation and the struct...
متن کاملNovel allosteric activation site in Escherichia coli fructose-1,6-bisphosphatase.
Fructose-1,6-bisphosphatase (FBPase) governs a key step in gluconeogenesis, the conversion of fructose 1,6-bisphosphate into fructose 6-phosphate. In mammals, the enzyme is subject to metabolic regulation, but regulatory mechanisms of bacterial FBPases are not well understood. Presented here is the crystal structure (resolution, 1.45A) of recombinant FBPase from Escherichia coli, the first stru...
متن کاملAllosteric Nanobodies Reveal the Dynamic Range and Diverse Mechanisms of GPCR Activation
G-protein-coupled receptors (GPCRs) modulate many physiological processes by transducing a variety of extracellular cues into intracellular responses. Ligand binding to an extracellular orthosteric pocket propagates conformational change to the receptor cytosolic region to promote binding and activation of downstream signalling effectors such as G proteins and β-arrestins. It is well known that...
متن کاملUncovering the intimate relationship between lipids, cholesterol and GPCR activation.
The membrane bilayer has a significant influence over the proteins embedded within it. G protein-coupled receptors (GPCRs) form a large group of membrane proteins with a vast array of critical functions, and direct and indirect interactions with the bilayer are thought to control various essential aspects of receptor function. The presence of cholesterol, in particular, has been the focus of a ...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Structure
سال: 2018
ISSN: 0969-2126
DOI: 10.1016/j.str.2017.12.013