1u5q
From Proteopedia
(New page: 200px<br /><applet load="1u5q" size="450" color="white" frame="true" align="right" spinBox="true" caption="1u5q, resolution 2.1Å" /> '''Crystal Structure of ...) |
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| - | [[Image:1u5q.gif|left|200px]]<br /><applet load="1u5q" size=" | + | [[Image:1u5q.gif|left|200px]]<br /><applet load="1u5q" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1u5q, resolution 2.1Å" /> | caption="1u5q, resolution 2.1Å" /> | ||
'''Crystal Structure of the TAO2 Kinase Domain: Activation and Specifity of a Ste20p MAP3K'''<br /> | '''Crystal Structure of the TAO2 Kinase Domain: Activation and Specifity of a Ste20p MAP3K'''<br /> | ||
==Overview== | ==Overview== | ||
| - | TAO2 is a mitogen-activated protein kinase kinase kinase (MAP3K) that | + | TAO2 is a mitogen-activated protein kinase kinase kinase (MAP3K) that doubly phosphorylates and activates the MAP kinase kinases (MAP2Ks) MEK3 and MEK6. The structure of the kinase domain of TAO2 (1-320) has been solved in its phosphorylated active conformation. The structure, together with structure-based mutagenic analysis, reveals that positively charged residues in the substrate binding groove mediate the first step in the dual phosphorylation of MEK6, on the threonine residue in the motif DS*VAKT*I (*denotes phosphorylation site) of MEK6. TAO2 is a Ste20p homolog, and the structure of active TAO2, in comparison with that of low-activity p21-activated protein kinase (PAK1), a Ste20p-related MAP4K, reveals how this group of kinases is activated by phosphorylation. Finally, active TAO2 displays unusual interactions with ATP, involving, in part, a subgroup-specific C-terminal extension of TAO2. The observed interactions may be useful in making specific inhibitors of TAO kinases. |
==About this Structure== | ==About this Structure== | ||
| - | 1U5Q is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with CA as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 1U5Q is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with <scene name='pdbligand=CA:'>CA</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1U5Q OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Chen, Z.]] | [[Category: Chen, Z.]] | ||
| - | [[Category: Cobb, M | + | [[Category: Cobb, M H.]] |
[[Category: Earnest, S.]] | [[Category: Earnest, S.]] | ||
[[Category: Gao, Y.]] | [[Category: Gao, Y.]] | ||
| - | [[Category: Goldsmith, E | + | [[Category: Goldsmith, E J.]] |
[[Category: Machius, M.]] | [[Category: Machius, M.]] | ||
[[Category: Raman, M.]] | [[Category: Raman, M.]] | ||
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[[Category: serine/threonine protein kinase]] | [[Category: serine/threonine protein kinase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:20:48 2008'' |
Revision as of 13:20, 21 February 2008
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Crystal Structure of the TAO2 Kinase Domain: Activation and Specifity of a Ste20p MAP3K
Overview
TAO2 is a mitogen-activated protein kinase kinase kinase (MAP3K) that doubly phosphorylates and activates the MAP kinase kinases (MAP2Ks) MEK3 and MEK6. The structure of the kinase domain of TAO2 (1-320) has been solved in its phosphorylated active conformation. The structure, together with structure-based mutagenic analysis, reveals that positively charged residues in the substrate binding groove mediate the first step in the dual phosphorylation of MEK6, on the threonine residue in the motif DS*VAKT*I (*denotes phosphorylation site) of MEK6. TAO2 is a Ste20p homolog, and the structure of active TAO2, in comparison with that of low-activity p21-activated protein kinase (PAK1), a Ste20p-related MAP4K, reveals how this group of kinases is activated by phosphorylation. Finally, active TAO2 displays unusual interactions with ATP, involving, in part, a subgroup-specific C-terminal extension of TAO2. The observed interactions may be useful in making specific inhibitors of TAO kinases.
About this Structure
1U5Q is a Single protein structure of sequence from Rattus norvegicus with as ligand. Full crystallographic information is available from OCA.
Reference
Crystal structure of the TAO2 kinase domain: activation and specificity of a Ste20p MAP3K., Zhou T, Raman M, Gao Y, Earnest S, Chen Z, Machius M, Cobb MH, Goldsmith EJ, Structure. 2004 Oct;12(10):1891-900. PMID:15458637
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