期刊
TRENDS IN BIOCHEMICAL SCIENCES
卷 34, 期 11, 页码 540-552出版社
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tibs.2009.07.005
关键词
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资金
- Deutsche Forschungsgemeinschaft [Sfb449, Sfb740]
G protein-coupled receptors (GPCRs) are ubiquitous signal transducers in cell membranes, as well as important drug targets. Interaction with extracellular agonists turns the seven transmembrane helix (7TM) scaffold of a GPCR into a catalyst for GDP and GTP exchange in heterotrimeric G alpha beta gamma proteins. Activation of the model GPCR, rhodopsin, is triggered by photoisomerization of its retinal ligand. From the augmentation of biochemical and biophysical studies by recent high-resolution 3D structures, its activation intermediates can now be interpreted as the stepwise engagement of protein domains. Rearrangement of TM5-TM6 opens a crevice at the cytoplasmic side of the receptor into which the C terminus of the G subunit can bind. The Got C-terminal helix is used as a transmission rod to the nucleotide binding site. The mechanism relies on dynamic interactions between conserved residues and could therefore be common to other GPCRs.
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