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2g01

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[[Image:2g01.gif|left|200px]]
[[Image:2g01.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2g01 |SIZE=350|CAPTION= <scene name='initialview01'>2g01</scene>, resolution 3.50&Aring;
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The line below this paragraph, containing "STRUCTURE_2g01", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=73Q:6-CHLORO-9-HYDROXY-1,3-DIMETHYL-1,9-DIHYDRO-4H-PYRAZOLO[3,4-B]QUINOLIN-4-ONE'>73Q</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[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] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= MAPK8, JNK1, PRKM8 ([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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|DOMAIN=
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{{STRUCTURE_2g01| PDB=2g01 | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2g01 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2g01 OCA], [http://www.ebi.ac.uk/pdbsum/2g01 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2g01 RCSB]</span>
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}}
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'''Pyrazoloquinolones as Novel, Selective JNK1 inhibitors'''
'''Pyrazoloquinolones as Novel, Selective JNK1 inhibitors'''
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[[Category: Protein complex]]
[[Category: Protein complex]]
[[Category: Abad-Zapatero, C.]]
[[Category: Abad-Zapatero, C.]]
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[[Category: c-jun n-terminal kinase]]
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[[Category: C-jun n-terminal kinase]]
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[[Category: jnk1]]
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[[Category: Jnk1]]
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[[Category: protein kinase jnk1 inhibitor]]
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[[Category: Protein kinase jnk1 inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 04:31:42 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:10:02 2008''
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Revision as of 01:31, 4 May 2008

Image:2g01.gif

Template:STRUCTURE 2g01

Pyrazoloquinolones as Novel, Selective JNK1 inhibitors


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.

About this Structure

2G01 is a Protein complex structure of sequences from Homo sapiens. 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 Sun May 4 04:31:42 2008

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