2gdo

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|PDB= 2gdo |SIZE=350|CAPTION= <scene name='initialview01'>2gdo</scene>, resolution 3.00&Aring;
|PDB= 2gdo |SIZE=350|CAPTION= <scene name='initialview01'>2gdo</scene>, resolution 3.00&Aring;
|SITE=
|SITE=
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|LIGAND= <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene> and <scene name='pdbligand=12C:4-[(3S)-1-AZABICYCLO[2.2.2]OCT-3-YLAMINO]-3-(1H-BENZIMIDAZOL-2-YL)-6-CHLOROQUINOLIN-2(1H)-ONE'>12C</scene>
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|LIGAND= <scene name='pdbligand=12C:4-[(3S)-1-AZABICYCLO[2.2.2]OCT-3-YLAMINO]-3-(1H-BENZIMIDAZOL-2-YL)-6-CHLOROQUINOLIN-2(1H)-ONE'>12C</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>
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|ACTIVITY= [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]
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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>
|GENE= CHK1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
|GENE= CHK1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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|DOMAIN=
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2gdo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2gdo OCA], [http://www.ebi.ac.uk/pdbsum/2gdo PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2gdo RCSB]</span>
}}
}}
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[[Category: Fang, E.]]
[[Category: Fang, E.]]
[[Category: Le, V.]]
[[Category: Le, V.]]
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[[Category: 12C]]
 
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[[Category: SO4]]
 
[[Category: atp-binding]]
[[Category: atp-binding]]
[[Category: cell cycle]]
[[Category: cell cycle]]
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[[Category: transferase]]
[[Category: transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 17:03:29 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:15:16 2008''

Revision as of 00:15, 31 March 2008


PDB ID 2gdo

Drag the structure with the mouse to rotate
, resolution 3.00Å
Ligands: ,
Gene: CHK1 (Homo sapiens)
Activity: Non-specific serine/threonine protein kinase, with EC number 2.7.11.1
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



4-(Aminoalkylamino)-3-Benzimidazole-Quinolinones As Potent CHK1 Inhibitors


Overview

CHK-1 is one of the key enzymes regulating checkpoints in cellular growth cycles. Novel 4-(amino-alkylamino)-3-benzimidazole-quinolinones were prepared and assayed for their ability to inhibit CHK-1. These compounds are potent cell permeable CHK-1 inhibitors and showed synergistic effect with a DNA-damaging agent, camptothecin.

About this Structure

2GDO is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

4-(Aminoalkylamino)-3-benzimidazole-quinolinones as potent CHK-1 inhibitors., Ni ZJ, Barsanti P, Brammeier N, Diebes A, Poon DJ, Ng S, Pecchi S, Pfister K, Renhowe PA, Ramurthy S, Wagman AS, Bussiere DE, Le V, Zhou Y, Jansen JM, Ma S, Gesner TG, Bioorg Med Chem Lett. 2006 Jun 15;16(12):3121-4. Epub 2006 Apr 5. PMID:16603354

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