This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.
Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.
2g01
From Proteopedia
(New page: 200px<br /> <applet load="2g01" size="450" color="white" frame="true" align="right" spinBox="true" caption="2g01, resolution 3.50Å" /> '''Pyrazoloquinolones ...) |
|||
| Line 1: | Line 1: | ||
| - | [[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== | ||
| Line 11: | Line 10: | ||
==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== | ||
| Line 25: | Line 24: | ||
[[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'' |
Revision as of 15:26, 21 February 2008
|
Pyrazoloquinolones as Novel, Selective JNK1 inhibitors
Contents |
Overview
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
Known diseases associated with this structure: Diabetes mellitus, noninsulin-dependent OMIM:[604641]
About this Structure
2G01 is a Protein complex structure of sequences from Homo sapiens with and as ligands. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Full crystallographic information is available from OCA.
Reference
Synthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors., Liu M, Xin Z, Clampit JE, Wang S, Gum RJ, Haasch DL, Trevillyan JM, Abad-Zapatero C, Fry EH, Sham HL, Liu G, Bioorg Med Chem Lett. 2006 May 15;16(10):2590-4. Epub 2006 Mar 9. PMID:16527482
Page seeded by OCA on Thu Feb 21 17:26:53 2008
