2g01: Difference between revisions
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New page: left|200px<br /> <applet load="2g01" size="450" color="white" frame="true" align="right" spinBox="true" caption="2g01, resolution 3.50Å" /> '''Pyrazoloquinolones ... |
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[[Image:2g01.gif|left|200px]]<br /> | [[Image:2g01.gif|left|200px]]<br /><applet load="2g01" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="2g01" size=" | |||
caption="2g01, resolution 3.50Å" /> | caption="2g01, resolution 3.50Å" /> | ||
'''Pyrazoloquinolones as Novel, Selective JNK1 inhibitors'''<br /> | '''Pyrazoloquinolones as Novel, Selective JNK1 inhibitors'''<br /> | ||
==Overview== | ==Overview== | ||
A novel class of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as | A novel class of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as c-Jun-N-terminal kinase (JNK) inhibitors is described. These compounds were synthesized via the condensation of 2-nitrobenzaldehydes and hydroxypyrazoles. The structure-activity relationships (SAR) and kinase selectivity profile of the inhibitors are also discussed. Compound 16 was identified as a potent JNK inhibitor with good cellular potency. | ||
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
2G01 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SO4 and 73Q as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http:// | 2G01 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=SO4:'>SO4</scene> and <scene name='pdbligand=73Q:'>73Q</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2G01 OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: protein kinase jnk1 inhibitors]] | [[Category: protein kinase jnk1 inhibitors]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:26:53 2008'' | ||