2ojg: Difference between revisions

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|PDB= 2ojg |SIZE=350|CAPTION= <scene name='initialview01'>2ojg</scene>, resolution 2.000&Aring;
|PDB= 2ojg |SIZE=350|CAPTION= <scene name='initialview01'>2ojg</scene>, resolution 2.000&Aring;
|SITE=  
|SITE=  
|LIGAND= <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene> and <scene name='pdbligand=19A:N,N-DIMETHYL-4-(4-PHENYL-1H-PYRAZOL-3-YL)-1H-PYRROLE-2-CARBOXAMIDE'>19A</scene>
|LIGAND= <scene name='pdbligand=19A:N,N-DIMETHYL-4-(4-PHENYL-1H-PYRAZOL-3-YL)-1H-PYRROLE-2-CARBOXAMIDE'>19A</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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= MAPK1, ERK2, PRKM1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
|GENE= MAPK1, ERK2, PRKM1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
|DOMAIN=
|RELATEDENTRY=[[2oji|2OJI]], [[2ojj|2OJJ]], [[2ok1|2OK1]]
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2ojg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ojg OCA], [http://www.ebi.ac.uk/pdbsum/2ojg PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2ojg RCSB]</span>
}}
}}


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==Overview==
==Overview==
The Ras/Raf/MEK/ERK signal transduction is a key oncogenic pathway implicated in a variety of human cancers. We have identified a novel series of pyrazolylpyrroles as inhibitors of ERK. Aided by the discovery of two distinct binding modes for the pyrazolylpyrrole scaffold, structure-guided optimization culminated in the discovery of 6p, a potent and selective inhibitor of ERK.
The Ras/Raf/MEK/ERK signal transduction is a key oncogenic pathway implicated in a variety of human cancers. We have identified a novel series of pyrazolylpyrroles as inhibitors of ERK. Aided by the discovery of two distinct binding modes for the pyrazolylpyrrole scaffold, structure-guided optimization culminated in the discovery of 6p, a potent and selective inhibitor of ERK.
==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: Jacobs, M D.]]
[[Category: Jacobs, M D.]]
[[Category: Xie, X.]]
[[Category: Xie, X.]]
[[Category: 19A]]
[[Category: SO4]]
[[Category: kinase inhibitor]]
[[Category: kinase inhibitor]]


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