| Structural highlights
2gdo is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| | Ligands: | ,
| | Gene: | CHK1 (Homo sapiens) |
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 |
| Resources: | FirstGlance, OCA, RCSB, PDBsum |
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
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.
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[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ 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. 4-(Aminoalkylamino)-3-benzimidazole-quinolinones as potent CHK-1 inhibitors. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3121-4. Epub 2006 Apr 5. PMID:16603354 doi:10.1016/j.bmcl.2006.03.059
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