3c4x: Difference between revisions
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'''Crystal Structure of G protein coupled receptor kinase 1 bound to ATP and magnesium chloride at 2.9A''' | '''Crystal Structure of G protein coupled receptor kinase 1 bound to ATP and magnesium chloride at 2.9A''' | ||
==Overview== | |||
G protein-coupled receptor (GPCR) kinases (GRKs) phosphorylate activated heptahelical receptors, leading to their uncoupling from G proteins. Here we report six crystal structures of rhodopsin kinase (GRK1), revealing not only three distinct nucleotide-binding states of a GRK but also two key structural elements believed to be involved in the recognition of activated GPCRs. The first is the C-terminal extension of the kinase domain, which was observed in all nucleotide-bound GRK1 structures. The second is residues 5-30 of the N terminus, observed in one of the GRK1.(Mg(2+))(2).ATP structures. The N terminus was also clearly phosphorylated, leading to the identification of two novel phosphorylation sites by mass spectral analysis. Co-localization of the N terminus and the C-terminal extension near the hinge of the kinase domain suggests that activated GPCRs stimulate kinase activity by binding to this region to facilitate full closure of the kinase domain. | |||
==About this Structure== | ==About this Structure== | ||
3C4X is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3C4X OCA]. | 3C4X is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3C4X OCA]. | ||
==Reference== | |||
Structures of Rhodopsin Kinase in Different Ligand States Reveal Key Elements Involved in G Protein-coupled Receptor Kinase Activation., Singh P, Wang B, Maeda T, Palczewski K, Tesmer JJ, J Biol Chem. 2008 May 16;283(20):14053-62. Epub 2008 Mar 13. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/18339619 18339619] | |||
[[Category: Bos taurus]] | [[Category: Bos taurus]] | ||
[[Category: Rhodopsin kinase]] | [[Category: Rhodopsin kinase]] | ||
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[[Category: Serine/threonine-protein kinase]] | [[Category: Serine/threonine-protein kinase]] | ||
[[Category: Transferase]] | [[Category: Transferase]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu May 22 22:36:23 2008'' | ||