1ywr
From Proteopedia
| |||||||
| , resolution 1.95Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Gene: | Mapk14, Crk1, Csbp1, Csbp2 (Mus musculus) | ||||||
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 | ||||||
| Related: | 1YW2
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Crystal Structure Analysis of inactive P38 kinase domain in complex with a Monocyclic Pyrazolone Inhibitor
Overview
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.
About this Structure
1YWR is a Single protein structure of sequence from Mus musculus. Full crystallographic information is available from OCA.
Reference
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
Page seeded by OCA on Mon Mar 31 01:25:24 2008
Categories: Mus musculus | Non-specific serine/threonine protein kinase | Single protein | Bookland, R G. | Brugel, T A. | Clark, C M. | Clark, M P. | De, B. | Djung, J F. | Golebiowski, A. | Hsieh, L C. | Janusz, M J. | Laufersweiler, M J. | Laughlin, S K. | Mekel, M J. | Sabat, M P. | Townes, J A. | Vanrens, J C. | Walter, R L. | Webster, M E. | Moncyclic pyrazolone | P38 kinase
