Structure activity relationships of anthranilic acid-based compounds on cellular and in vivo mitogen activated protein kinase-5 signaling pathways.

Suravi Chakrabarty,Darlene A Monlish,Mohit Gupta,Thomas D Wright,Van T Hoang, Mitchel Fedak,Ishveen Chopra,Patrick T Flaherty,Jeffry Madura, Shankar Mannepelli,Matthew E Burow,Jane E Cavanaugh

Bioorganic & Medicinal Chemistry Letters（2018）

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摘要

•Selective inhibition of MEK isoforms is possible with type III inhibitors.•Omission of the requisite halogen bond to Val127 (MEK1) is tolerated at MEK5.•Anionic anthranillate type III MEK inhibitors do not require an internal H-bond.

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acid-based

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