1yw2

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1yw2, resolution 2.01Å

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Mutated Mus Musculus P38 Kinase (mP38)

Overview

4-Aryl-3-pyridyl and 4-aryl-3-pyrimidinyl based tumor necrosis, factor-alpha (TNF-alpha) inhibitors, which contain a novel isoxazolone, five-membered heterocyclic core are described. Many showed sub-micromolar, activity against lipopolysaccharide-induced TNF-alpha production.

About this Structure

1YW2 is a Single protein structure of sequence from Mus musculus with PGJ as ligand. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Full crystallographic information is available from OCA.

Reference

The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-alpha) production., Laughlin SK, Clark MP, Djung JF, Golebiowski A, Brugel TA, Sabat M, Bookland RG, Laufersweiler MJ, VanRens JC, Townes JA, De B, Hsieh LC, Xu SC, Walter RL, Mekel MJ, Janusz MJ, Bioorg Med Chem Lett. 2005 May 2;15(9):2399-403. PMID:15837333

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