2gtm
Mutated Mouse P38 MAP Kinase Domain in complex with Inhibitor PG-892579
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| , resolution 1.90Å | |||||||
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| Ligands: | |||||||
| Gene: | Mapk14 (Mus musculus) | ||||||
| Activity: | Mitogen-activated protein kinase, with EC number 2.7.11.24 | ||||||
| Related: | 1YW2, 1YWR, 2GHM, 2GHL
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
OverviewOverview
A series of C-2, C-8, and N-9 trisubstituted purine based inhibitors of TNF-alpha production are described. The most potent analogs showed low nanomolar activity against LPS-induced TNF-alpha production in a THP-1 cell based assay. The SAR of the series was optimized with the aid of X-ray co-crystal structures of these inhibitors bound with mutated p38 (mp38).
About this StructureAbout this Structure
2GTM is a Single protein structure of sequence from Mus musculus. Full crystallographic information is available from OCA.
ReferenceReference
The development of novel C-2, C-8, and N-9 trisubstituted purines as inhibitors of TNF-alpha production., Sabat M, Vanrens JC, Clark MP, Brugel TA, Maier J, Bookland RG, Laufersweiler MJ, Laughlin SK, Golebiowski A, De B, Hsieh LC, Walter RL, Mekel MJ, Janusz MJ, Bioorg Med Chem Lett. 2006 Aug 15;16(16):4360-5. Epub 2006 Jun 5. PMID:16750367
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