Primary sequence requirements forS-acylation of β2-adrenergic receptor peptides
نویسندگان
چکیده
منابع مشابه
Activation mechanism of the β2-adrenergic receptor.
A third of marketed drugs act by binding to a G-protein-coupled receptor (GPCR) and either triggering or preventing receptor activation. Although recent crystal structures have provided snapshots of both active and inactive functional states of GPCRs, these structures do not reveal the mechanism by which GPCRs transition between these states. Here we propose an activation mechanism for the β(2)...
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N-hydroxysuccinimide (NHS) esters are derivatizing agents that target primary amine groups. However, even a small molar excess of NHS may lead to acylation of hydroxyl-containing amino acids as a side reaction. We report a straightforward method for the selective removal of ester-linked acyl groups after NHS ester-mediated acylation of peptides and proteins. It is based on incubation in a boili...
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There is evidence that lipids can be allosteric regulators of membrane protein structure and activation. However, there are no data showing how exactly the regulation emerges from specific lipid-protein interactions. Here we show in atomistic detail how the human β2-adrenergic receptor (β2AR) - a prototypical G protein-coupled receptor - is modulated by cholesterol in an allosteric fashion. Ext...
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Typically phospholipids in cell membranes are not symmetrically distributed between the inner and outer leaflets. The resulting asymmetry is crucial in several cellular functions, such as apoptosis and secretary vesicle formation and fusion. The rate of spontaneous phospholipid diffusion across the membranes is slow with half-times varying from hours to weeks. Still, a number of membrane protei...
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G-protein-coupled receptors (GPCRs) can modulate diverse signaling pathways, often in a ligand-specific manner. The full range of functionally relevant GPCR conformations is poorly understood. Here, we use NMR spectroscopy to characterize the conformational dynamics of the transmembrane core of the β(2)-adrenergic receptor (β(2)AR), a prototypical GPCR. We labeled β(2)AR with (13)CH(3)ε-methion...
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ژورنال
عنوان ژورنال: FEBS Letters
سال: 2001
ISSN: 0014-5793
DOI: 10.1016/s0014-5793(01)02513-3