2p33

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[[Image:2p33.jpg|left|200px]]<br /><applet load="2p33" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2p33.jpg|left|200px]]
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caption="2p33, resolution 2.40&Aring;" />
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'''Synthesis and SAR of Aminopyrimidines as Novel c-Jun N-Terminal Kinase (JNK) Inhibitors'''<br />
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{{Structure
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|PDB= 2p33 |SIZE=350|CAPTION= <scene name='initialview01'>2p33</scene>, resolution 2.40&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=J07:4-{[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino}-N-ethylpiperidine-1-carboxamide'>J07</scene>
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|ACTIVITY= [http://en.wikipedia.org/wiki/Mitogen-activated_protein_kinase Mitogen-activated protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.24 2.7.11.24]
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|GENE= MAPK10, JNK3, JNK3A, PRKM10 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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}}
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'''Synthesis and SAR of Aminopyrimidines as Novel c-Jun N-Terminal Kinase (JNK) Inhibitors'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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2P33 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=J07:'>J07</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Mitogen-activated_protein_kinase Mitogen-activated protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.24 2.7.11.24] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2P33 OCA].
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2P33 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=2P33 OCA].
==Reference==
==Reference==
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Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors., Alam M, Beevers RE, Ceska T, Davenport RJ, Dickson KM, Fortunato M, Gowers L, Haughan AF, James LA, Jones MW, Kinsella N, Lowe C, Meissner JW, Nicolas AL, Perry BG, Phillips DJ, Pitt WR, Platt A, Ratcliffe AJ, Sharpe A, Tait LJ, Bioorg Med Chem Lett. 2007 Jun 15;17(12):3463-7. Epub 2007 Mar 30. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17459703 17459703]
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Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors., Alam M, Beevers RE, Ceska T, Davenport RJ, Dickson KM, Fortunato M, Gowers L, Haughan AF, James LA, Jones MW, Kinsella N, Lowe C, Meissner JW, Nicolas AL, Perry BG, Phillips DJ, Pitt WR, Platt A, Ratcliffe AJ, Sharpe A, Tait LJ, Bioorg Med Chem Lett. 2007 Jun 15;17(12):3463-7. Epub 2007 Mar 30. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17459703 17459703]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Mitogen-activated protein kinase]]
[[Category: Mitogen-activated protein kinase]]
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[[Category: jnk3 kinase]]
[[Category: jnk3 kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:25:27 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 18:07:57 2008''

Revision as of 16:07, 20 March 2008


PDB ID 2p33

Drag the structure with the mouse to rotate
, resolution 2.40Å
Ligands:
Gene: MAPK10, JNK3, JNK3A, PRKM10 (Homo sapiens)
Activity: Mitogen-activated protein kinase, with EC number 2.7.11.24
Coordinates: save as pdb, mmCIF, xml



Synthesis and SAR of Aminopyrimidines as Novel c-Jun N-Terminal Kinase (JNK) Inhibitors


Contents

Overview

The development of a series of novel aminopyrimidines as inhibitors of c-Jun N-terminal kinases is described. The synthesis, in vitro inhibitory values for JNK1, JNK2 and CDK2, and the in vitro inhibitory value for a c-Jun cellular assay are discussed.

Disease

Known diseases associated with this structure: Epileptic encephalopathy, Lennox-Gastaut type OMIM:[602897]

About this Structure

2P33 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors., Alam M, Beevers RE, Ceska T, Davenport RJ, Dickson KM, Fortunato M, Gowers L, Haughan AF, James LA, Jones MW, Kinsella N, Lowe C, Meissner JW, Nicolas AL, Perry BG, Phillips DJ, Pitt WR, Platt A, Ratcliffe AJ, Sharpe A, Tait LJ, Bioorg Med Chem Lett. 2007 Jun 15;17(12):3463-7. Epub 2007 Mar 30. PMID:17459703

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