The MAPK signaling cascade, comprised of several linear and intersecting pathways, propagates signaling into the nucleus resulting in cytokine and chemokine release. The Map Kinase Kinase isoforms 3 and 6 (MKK3 and MKK6) are responsible for the phosphorylation and activation of p38, and are hypothesized to play a key role in regulating this pathway without the redundancy seen in downstream effectors. Using Fragment Based Drug Discovery, we have discovered efficient and selective inhibitors of MKK3 and MKK6 that can be used to further understand the role of these kinases in MAPK signaling, and the potential impact of inhibiting kinases upstream of p38.

Fragment-based drug discovery of potent and selective MKK3/6 inhibitors

251st National Meeting (2016)

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