| Structural highlights
3zya 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: |
| | Related: | 2baj, 1wfc, 3zsi, 1w7h, 1wbo, 1kv2, 1yqj, 1bmk, 1bl7, 1zyj, 1a9u, 1wbt, 2i0h, 3zs5, 2yiw, 2baq, 1wbv, 1zz2, 1di9, 1w83, 1bl6, 1m7q, 3zsh, 1ian, 1oz1, 1wbn, 2bak, 3zsg, 2bal, 1wbs, 1ouy, 1ouk, 2y8o, 1r39, 2yis, 1kv1, 1wbw, 1w82, 2yix, 1r3c, 1ove, 1w84, 1zzl |
| Activity: | Mitogen-activated protein kinase, with EC number 2.7.11.24 |
| Resources: | FirstGlance, OCA, RCSB, PDBsum |
Publication Abstract from PubMed
Until now, a lack of inhibitors with high potency and selectivity in vivo has hampered investigation of the p38 mitogen-activated protein kinase (MAPK) signaling pathway. We describe the design of skepinone-L, which is, to our knowledge, the first ATP-competitive p38 MAPK inhibitor with excellent in vivo efficacy and selectivity. Therefore, skepinone-L is a valuable probe for chemical biology research, and it may foster the development of a unique class of kinase inhibitors.
Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor.,Koeberle SC, Romir J, Fischer S, Koeberle A, Schattel V, Albrecht W, Grutter C, Werz O, Rauh D, Stehle T, Laufer SA Nat Chem Biol. 2011 Dec 25. doi: 10.1038/nchembio.761. PMID:22198732[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Koeberle SC, Romir J, Fischer S, Koeberle A, Schattel V, Albrecht W, Grutter C, Werz O, Rauh D, Stehle T, Laufer SA. Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor. Nat Chem Biol. 2011 Dec 25. doi: 10.1038/nchembio.761. PMID:22198732 doi:10.1038/nchembio.761
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