2gdo
From Proteopedia
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| - | [[Image:2gdo.jpg|left|200px]] | + | [[Image:2gdo.jpg|left|200px]] |
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| - | '''4-(Aminoalkylamino)-3-Benzimidazole-Quinolinones As Potent CHK1 Inhibitors''' | + | {{Structure |
| + | |PDB= 2gdo |SIZE=350|CAPTION= <scene name='initialview01'>2gdo</scene>, resolution 3.00Å | ||
| + | |SITE= | ||
| + | |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> | ||
| + | |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] | ||
| + | |GENE= CHK1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | }} | ||
| + | |||
| + | '''4-(Aminoalkylamino)-3-Benzimidazole-Quinolinones As Potent CHK1 Inhibitors''' | ||
| + | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2GDO is a [ | + | 2GDO is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2GDO OCA]. |
==Reference== | ==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:[http:// | + | 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:[http://www.ncbi.nlm.nih.gov/pubmed/16603354 16603354] |
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Non-specific serine/threonine protein kinase]] | [[Category: Non-specific serine/threonine protein kinase]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 17:03:29 2008'' |
Revision as of 15:03, 20 March 2008
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| , resolution 3.00Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | and | ||||||
| Gene: | CHK1 (Homo sapiens) | ||||||
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 | ||||||
| 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
Page seeded by OCA on Thu Mar 20 17:03:29 2008
