| Structural highlights
1ywr is a 1 chain structure with sequence from Mus musculus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| | Ligands: |
| | Related: | 1yw2 |
| Gene: | Mapk14, Crk1, Csbp1, Csbp2 (Mus musculus) |
| 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
4-Aryl-5-pyrimidyl based cytokine synthesis inhibitors that contain a novel monocyclic, pyrazolone heterocyclic core are described. Many of these inhibitors showed low nanomolar activity against LPS-induced TNF-alpha production. One of the compounds (6e) was found to be efficacious in the rat iodoacetate (RIA) in vivo model of osteoarthritis. The X-ray crystal structure of a pyrazolone inhibitor cocrystallized with mutated p38 (mp38) is presented.
The development of monocyclic pyrazolone based cytokine synthesis inhibitors.,Golebiowski A, Townes JA, Laufersweiler MJ, Brugel TA, Clark MP, Clark CM, Djung JF, Laughlin SK, Sabat MP, Bookland RG, VanRens JC, De B, Hsieh LC, Janusz MJ, Walter RL, Webster ME, Mekel MJ Bioorg Med Chem Lett. 2005 May 2;15(9):2285-9. PMID:15837310[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Golebiowski A, Townes JA, Laufersweiler MJ, Brugel TA, Clark MP, Clark CM, Djung JF, Laughlin SK, Sabat MP, Bookland RG, VanRens JC, De B, Hsieh LC, Janusz MJ, Walter RL, Webster ME, Mekel MJ. The development of monocyclic pyrazolone based cytokine synthesis inhibitors. Bioorg Med Chem Lett. 2005 May 2;15(9):2285-9. PMID:15837310 doi:10.1016/j.bmcl.2005.03.007
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