Crystallographic analysis of the MAP kinase P38

Crystallization and preliminary crystallographic analysis of recombinant human P38 MAP kinase.

The recombinant human p38 MAP kinase has been expressed and purified from both Escherichia coli and SF9 cells, and has been crystallized in two forms by the hanging drop vapor diffusion method using PEG as precipitant. Both crystal forms belong to space group P2(1)2(1)2(1). The cell parameters for crystal form 1 are a = 65.2 A, b = 74.6 A and c = 78.1 A. Those for crystal form 2 are a = 58.3 A,...

Synthesis and Evaluation of Pyridinyltriazoles as Inhibitors of p38 MAP Kinase

Objective(s) Inhibitors of p38 MAP kinase are considered as suitable target in the treatment of inflammatory diseases such as rheumatoid arthritis and bowel inflammatory diseases. The development of 5-alkylthio-1-aryl-2-(4-pyridinyl) triazoles as inhibitors of p38 MAP kinase is described. These are analogues of 4- pyridinyl imidazole p38 MAP kinase inhibitor reported by Merck Research Laborator...

Application of 3D-QSAR on a Series of Potent P38-MAP Kinase Inhibitors

One of the most applied methods in drug industry for development of new drugs is 3D-QSAR methodology. As p38-mitogen-activated protein kinase (p38-MAPK) plays a crucial role in regulating the production of such proinflammatory cytokines as tumor necrosis factor-α (TNF-α) and interleukin-1, emerging as an attractive target for new anti-inflammatory agents, we used a 3D-QSAR based method of Compa...

application of 3d-qsar on a series of potent p38-map kinase inhibitors

The role of p38 MAP kinase in cancer cell apoptosis

Many extracellular stimuli are converted into specific cellular responses through the activation of mitogen-activated protein kinase (MAPK) signalling pathways. MAPKs are serine/threonine protein kinases that can phoshorylate both cytoplasmic and nuclear targets.1,2 Four distinct subgroups within the MAP kinase superfamily have been described: extracellular signal-regulated kinases (ERKs), c-ju...