| Structural highlights
3s4q 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: | CSBP, CSBP1, CSBP2, CSPB1, MAPK14, MXI2 (Homo sapiens) |
| Activity: | Mitogen-activated protein kinase, with EC number 2.7.11.24 |
| Resources: | FirstGlance, OCA, RCSB, PDBsum |
Publication Abstract from PubMed
Pyrrolo[2,1-f][1,2,4]triazine based inhibitors of p38alpha have been prepared exploring functional group modifications at the C6 position. Incorporation of aryl and heteroaryl ketones at this position led to potent inhibitors with efficacy in in vivo models of acute and chronic inflammation.
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38alpha MAP kinase inhibitors.,Dyckman AJ, Li T, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly KM, Shuster DJ, Doweyko AM, Sack JS, Kish K, Kiefer SE, Newitt JA, Zhang H, Marathe PH, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K Bioorg Med Chem Lett. 2011 Aug 1;21(15):4633-7. Epub 2011 May 30. PMID:21705217[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Dyckman AJ, Li T, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly KM, Shuster DJ, Doweyko AM, Sack JS, Kish K, Kiefer SE, Newitt JA, Zhang H, Marathe PH, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K. Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38alpha MAP kinase inhibitors. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4633-7. Epub 2011 May 30. PMID:21705217 doi:10.1016/j.bmcl.2011.05.091
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