2gtn
From Proteopedia
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| , resolution 1.80Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | and | ||||||
| Gene: | Mapk14 (Mus musculus) | ||||||
| Activity: | Mitogen-activated protein kinase, with EC number 2.7.11.24 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Mutated MAP kinase P38 (Mus Musculus) in complex with Inhbitor PG-951717
Overview
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 Structure
2GTN is a Single protein structure of sequence from Mus musculus. Full crystallographic information is available from OCA.
Reference
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
Page seeded by OCA on Thu Mar 20 17:08:55 2008
