1f3m
From Proteopedia
(New page: 200px<br /> <applet load="1f3m" size="450" color="white" frame="true" align="right" spinBox="true" caption="1f3m, resolution 2.3Å" /> '''CRYSTAL STRUCTURE OF...) |
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| - | [[Image:1f3m.gif|left|200px]]<br /> | + | [[Image:1f3m.gif|left|200px]]<br /><applet load="1f3m" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1f3m" size=" | + | |
caption="1f3m, resolution 2.3Å" /> | caption="1f3m, resolution 2.3Å" /> | ||
'''CRYSTAL STRUCTURE OF HUMAN SERINE/THREONINE KINASE PAK1'''<br /> | '''CRYSTAL STRUCTURE OF HUMAN SERINE/THREONINE KINASE PAK1'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The p21-activated kinases (PAKs), stimulated by binding with GTP-liganded | + | The p21-activated kinases (PAKs), stimulated by binding with GTP-liganded forms of Cdc42 or Rac, modulate cytoskeletal actin assembly and activate MAP-kinase pathways. The 2.3 A resolution crystal structure of a complex between the N-terminal autoregulatory fragment and the C-terminal kinase domain of PAK1 shows that GTPase binding will trigger a series of conformational changes, beginning with disruption of a PAK1 dimer and ending with rearrangement of the kinase active site into a catalytically competent state. An inhibitory switch (IS) domain, which overlaps the GTPase binding region of PAK1, positions a polypeptide segment across the kinase cleft. GTPase binding will refold part of the IS domain and unfold the rest. A related switch has been seen in the Wiskott-Aldrich syndrome protein (WASP). |
==About this Structure== | ==About this Structure== | ||
| - | 1F3M is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with IOD as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 1F3M is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=IOD:'>IOD</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1F3M OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Eck, M | + | [[Category: Eck, M J.]] |
| - | [[Category: Harrison, S | + | [[Category: Harrison, S C.]] |
[[Category: Lei, M.]] | [[Category: Lei, M.]] | ||
[[Category: Lu, W.]] | [[Category: Lu, W.]] | ||
| - | [[Category: Mayer, B | + | [[Category: Mayer, B J.]] |
[[Category: Meng, W.]] | [[Category: Meng, W.]] | ||
[[Category: Parrini, M-C.]] | [[Category: Parrini, M-C.]] | ||
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[[Category: kinase domain]] | [[Category: kinase domain]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:34:31 2008'' |
Revision as of 10:34, 21 February 2008
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CRYSTAL STRUCTURE OF HUMAN SERINE/THREONINE KINASE PAK1
Overview
The p21-activated kinases (PAKs), stimulated by binding with GTP-liganded forms of Cdc42 or Rac, modulate cytoskeletal actin assembly and activate MAP-kinase pathways. The 2.3 A resolution crystal structure of a complex between the N-terminal autoregulatory fragment and the C-terminal kinase domain of PAK1 shows that GTPase binding will trigger a series of conformational changes, beginning with disruption of a PAK1 dimer and ending with rearrangement of the kinase active site into a catalytically competent state. An inhibitory switch (IS) domain, which overlaps the GTPase binding region of PAK1, positions a polypeptide segment across the kinase cleft. GTPase binding will refold part of the IS domain and unfold the rest. A related switch has been seen in the Wiskott-Aldrich syndrome protein (WASP).
About this Structure
1F3M is a Single protein structure of sequence from Homo sapiens with as ligand. Full crystallographic information is available from OCA.
Reference
Structure of PAK1 in an autoinhibited conformation reveals a multistage activation switch., Lei M, Lu W, Meng W, Parrini MC, Eck MJ, Mayer BJ, Harrison SC, Cell. 2000 Aug 4;102(3):387-97. PMID:10975528
Page seeded by OCA on Thu Feb 21 12:34:31 2008
Categories: Homo sapiens | Single protein | Eck, M J. | Harrison, S C. | Lei, M. | Lu, W. | Mayer, B J. | Meng, W. | Parrini, M-C. | IOD | Autoinhibitory fragment | Homodimer | Kinase domain
