2p33
From Proteopedia
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|PDB= 2p33 |SIZE=350|CAPTION= <scene name='initialview01'>2p33</scene>, resolution 2.40Å | |PDB= 2p33 |SIZE=350|CAPTION= <scene name='initialview01'>2p33</scene>, resolution 2.40Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= <scene name='pdbligand=J07:4-{[5- | + | |LIGAND= <scene name='pdbligand=J07:4-{[5-CHLORO-4-(1H-INDOL-3-YL)PYRIMIDIN-2-YL]AMINO}-N-ETHYLPIPERIDINE-1-CARBOXAMIDE'>J07</scene> |
| - | |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] | + | |ACTIVITY= <span class='plainlinks'>[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] </span> |
|GENE= MAPK10, JNK3, JNK3A, PRKM10 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |GENE= MAPK10, JNK3, JNK3A, PRKM10 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY= | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2p33 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2p33 OCA], [http://www.ebi.ac.uk/pdbsum/2p33 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2p33 RCSB]</span> | ||
}} | }} | ||
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==Overview== | ==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. | 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:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=602897 602897]] | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Platt, A.]] | [[Category: Platt, A.]] | ||
[[Category: Sharpe, A.]] | [[Category: Sharpe, A.]] | ||
| - | [[Category: J07]] | ||
[[Category: inhibitor]] | [[Category: inhibitor]] | ||
[[Category: jnk3 kinase]] | [[Category: jnk3 kinase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:28:10 2008'' |
Revision as of 01:28, 31 March 2008
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| , resolution 2.40Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Gene: | MAPK10, JNK3, JNK3A, PRKM10 (Homo sapiens) | ||||||
| Activity: | Mitogen-activated protein kinase, with EC number 2.7.11.24 | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Synthesis and SAR of Aminopyrimidines as Novel c-Jun N-Terminal Kinase (JNK) Inhibitors
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.
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
Page seeded by OCA on Mon Mar 31 04:28:10 2008
