2f57: Difference between revisions
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[[Image:2f57.gif|left|200px]] | [[Image:2f57.gif|left|200px]] | ||
'''Crystal Structure Of The Human P21-Activated Kinase 5''' | {{Structure | ||
|PDB= 2f57 |SIZE=350|CAPTION= <scene name='initialview01'>2f57</scene>, resolution 1.80Å | |||
|SITE= | |||
|LIGAND= <scene name='pdbligand=TRS:2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL'>TRS</scene> and <scene name='pdbligand=23D:N2-[(1R,2S)-2-AMINOCYCLOHEXYL]-N6-(3-CHLOROPHENYL)-9-ETHYL-9H-PURINE-2,6-DIAMINE'>23D</scene> | |||
|ACTIVITY= [http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] | |||
|GENE= | |||
}} | |||
'''Crystal Structure Of The Human P21-Activated Kinase 5''' | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
2F57 is a [ | 2F57 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2F57 OCA]. | ||
==Reference== | ==Reference== | ||
Crystal Structures of the p21-activated kinases PAK4, PAK5, and PAK6 reveal catalytic domain plasticity of active group II PAKs., Eswaran J, Lee WH, Debreczeni JE, Filippakopoulos P, Turnbull A, Fedorov O, Deacon SW, Peterson JR, Knapp S, Structure. 2007 Feb;15(2):201-13. PMID:[http:// | Crystal Structures of the p21-activated kinases PAK4, PAK5, and PAK6 reveal catalytic domain plasticity of active group II PAKs., Eswaran J, Lee WH, Debreczeni JE, Filippakopoulos P, Turnbull A, Fedorov O, Deacon SW, Peterson JR, Knapp S, Structure. 2007 Feb;15(2):201-13. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17292838 17292838] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Non-specific serine/threonine protein kinase]] | [[Category: Non-specific serine/threonine protein kinase]] | ||
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[[Category: 23D]] | [[Category: 23D]] | ||
[[Category: TRS]] | [[Category: TRS]] | ||
[[Category: groupii | [[Category: groupii pak]] | ||
[[Category: kinase | [[Category: kinase domain]] | ||
[[Category: pak5]] | [[Category: pak5]] | ||
[[Category: sgc]] | [[Category: sgc]] | ||
[[Category: structural | [[Category: structural genomic]] | ||
[[Category: structural genomics consortium]] | [[Category: structural genomics consortium]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 16:48:15 2008'' | ||
Revision as of 17:48, 20 March 2008
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| , resolution 1.80Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | and | ||||||
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Crystal Structure Of The Human P21-Activated Kinase 5
OverviewOverview
p21-activated kinases have been classified into two groups based on their domain architecture. Group II PAKs (PAK4-6) regulate a wide variety of cellular functions, and PAK deregulation has been linked to tumor development. Structural comparison of five high-resolution structures comprising all active, monophosphorylated group II catalytic domains revealed a surprising degree of domain plasticity, including a number of catalytically productive and nonproductive conformers. Rearrangements of helix alphaC, a key regulatory element of kinase function, resulted in an additional helical turn at the alphaC N terminus and a distortion of its C terminus, a movement hitherto unseen in protein kinases. The observed structural changes led to the formation of interactions between conserved residues that structurally link the glycine-rich loop, alphaC, and the activation segment and firmly anchor alphaC in an active conformation. Inhibitor screening identified six potent PAK inhibitors from which a tri-substituted purine inhibitor was cocrystallized with PAK4 and PAK5.
About this StructureAbout this Structure
2F57 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
ReferenceReference
Crystal Structures of the p21-activated kinases PAK4, PAK5, and PAK6 reveal catalytic domain plasticity of active group II PAKs., Eswaran J, Lee WH, Debreczeni JE, Filippakopoulos P, Turnbull A, Fedorov O, Deacon SW, Peterson JR, Knapp S, Structure. 2007 Feb;15(2):201-13. PMID:17292838
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Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCA- Pages with broken file links
- Homo sapiens
- Non-specific serine/threonine protein kinase
- Single protein
- Arrowsmith, C.
- Bray, J.
- Burgess, N.
- Das, S.
- Delft, F Von.
- Edwards, A.
- Eswaran, J.
- Fedorov, O.
- Filippakopoulos, P.
- Knapp, S.
- Papagrigoriou, E.
- SGC, Structural Genomics Consortium.
- Savitsky, P.
- Smee, C.
- Sundstrom, M.
- Turnbull, A.
- Ugochukwu, E.
- Weigelt, J.
- 23D
- TRS
- Groupii pak
- Kinase domain
- Pak5
- Sgc
- Structural genomic
- Structural genomics consortium