1jpa
From Proteopedia
(New page: 200px<br /><applet load="1jpa" size="450" color="white" frame="true" align="right" spinBox="true" caption="1jpa, resolution 1.91Å" /> '''Crystal Structure of...) |
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| - | [[Image:1jpa.jpg|left|200px]]<br /><applet load="1jpa" size=" | + | [[Image:1jpa.jpg|left|200px]]<br /><applet load="1jpa" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1jpa, resolution 1.91Å" /> | caption="1jpa, resolution 1.91Å" /> | ||
'''Crystal Structure of unphosphorylated EphB2 receptor tyrosine kinase and juxtamembrane region'''<br /> | '''Crystal Structure of unphosphorylated EphB2 receptor tyrosine kinase and juxtamembrane region'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The Eph receptor tyrosine kinase family is regulated by | + | The Eph receptor tyrosine kinase family is regulated by autophosphorylation within the juxtamembrane region and the kinase activation segment. We have solved the X-ray crystal structure to 1.9 A resolution of an autoinhibited, unphosphorylated form of EphB2 comprised of the juxtamembrane region and the kinase domain. The structure, supported by mutagenesis data, reveals that the juxtamembrane segment adopts a helical conformation that distorts the small lobe of the kinase domain, and blocks the activation segment from attaining an activated conformation. Phosphorylation of conserved juxtamembrane tyrosines would relieve this autoinhibition by disturbing the association of the juxtamembrane segment with the kinase domain, while liberating phosphotyrosine sites for binding SH2 domains of target proteins. We propose that the autoinhibitory mechanism employed by EphB2 is a more general device through which receptor tyrosine kinases are controlled. |
==About this Structure== | ==About this Structure== | ||
| - | 1JPA is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus] with ANP as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 1JPA is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus] with <scene name='pdbligand=ANP:'>ANP</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1JPA OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Pawson, T.]] | [[Category: Pawson, T.]] | ||
[[Category: Sicheri, F.]] | [[Category: Sicheri, F.]] | ||
| - | [[Category: Wybenga-Groot, L | + | [[Category: Wybenga-Groot, L E.]] |
[[Category: ANP]] | [[Category: ANP]] | ||
[[Category: autoinhibited]] | [[Category: autoinhibited]] | ||
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[[Category: unphosphorylated]] | [[Category: unphosphorylated]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 13:25:13 2008'' |
Revision as of 11:25, 21 February 2008
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Crystal Structure of unphosphorylated EphB2 receptor tyrosine kinase and juxtamembrane region
Overview
The Eph receptor tyrosine kinase family is regulated by autophosphorylation within the juxtamembrane region and the kinase activation segment. We have solved the X-ray crystal structure to 1.9 A resolution of an autoinhibited, unphosphorylated form of EphB2 comprised of the juxtamembrane region and the kinase domain. The structure, supported by mutagenesis data, reveals that the juxtamembrane segment adopts a helical conformation that distorts the small lobe of the kinase domain, and blocks the activation segment from attaining an activated conformation. Phosphorylation of conserved juxtamembrane tyrosines would relieve this autoinhibition by disturbing the association of the juxtamembrane segment with the kinase domain, while liberating phosphotyrosine sites for binding SH2 domains of target proteins. We propose that the autoinhibitory mechanism employed by EphB2 is a more general device through which receptor tyrosine kinases are controlled.
About this Structure
1JPA is a Single protein structure of sequence from Mus musculus with as ligand. Full crystallographic information is available from OCA.
Reference
Structural basis for autoinhibition of the Ephb2 receptor tyrosine kinase by the unphosphorylated juxtamembrane region., Wybenga-Groot LE, Baskin B, Ong SH, Tong J, Pawson T, Sicheri F, Cell. 2001 Sep 21;106(6):745-57. PMID:11572780
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