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Figure 3 | Journal of Neuroinflammation

Figure 3

From: A novel p38α MAPK inhibitor suppresses brain proinflammatory cytokine up-regulation and attenuates synaptic dysfunction and behavioral deficits in an Alzheimer's disease mouse model

Figure 3

Inhibition of p38α MAPK enzyme activity and validation of design for selective interactions. A) MW01-2-069A-SRM inhibits p38α MAPK enzyme activity in a concentration-dependent manner. B) In contrast, the 069A analogs are > 100-fold less active. These include the starting scaffold (MW01-3-183WH), an analog (MW01-4-119SRM) with a different orientation of the pyridine ring nitrogen such that potential H-bond interactions are minimized, and an analog (MW01-6-189WH) with the pyridine ring at a different position on the scaffold. The in vitro phosphorylation of the standard protein substrate, myelin basic protein, by purified p38α MAPK was measured as described in Methods, in the absence or presence of increasing concentrations of compound. Data are expressed as percent of the maximal enzyme activity, where enzyme activity in the presence of solvent only (absence of inhibitor) is taken as 100%. Data are a representative example of five experiments.

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Journal of Neuroinflammation

ISSN: 1742-2094