Uncovering the action of a selective holophosphatase inhibitor

MRC Laboratory of Molecular Biology| Mon Jul 31 11:03:47 EDT 2017
Uncovering the action of a selective holophosphatase inhibitor
Guanabenz (G) and Sephin1 (S) selectively bind to R15A’s N-terminal, induce a conformational change, impairing recruitment of the substrate, eIF2a, and its dephosphorylation.

Proteins can be reversibly phosphorylated – phosphate groups are added to proteins by the action of kinase enzymes and can be removed by phosphatases. This controls a huge variety of cellular processes and targeting phosphorylation thus offers a board range of therapeutic opportunities. Indeed, kinases have received much....

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