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Catalog Peptides> | … The C-terminal kinase domain of murine RSK2 (residues 400–740) including a N-terminal polyhistidine tag (His 8 ), a linker (DYDIPTT) and a Tobacco Etch Virus (TEV) protease site (Glu-Asn-Leu-Tyr-Phe-Gln-Gly) in PET-22b was purchased from Genscript (RSK2-pET-22b) … | Get A Quote |
Dimethyl fumarate (DMF) has been applied for decades in the treatment of psoriasis and now also multiple sclerosis. However, the mechanism of action has remained obscure and involves high dose over long time of this small, reactive compound implicating many potential targets. Based on a 1.9 Å resolution crystal structure of the C-terminal kinase domain of the mouse p90 Ribosomal S6 Kinase 2 (RSK2) inhibited by DMF we describe a central binding site in RSKs and the closely related Mitogen and Stress-activated Kinases (MSKs). DMF reacts covalently as a Michael acceptor to a conserved cysteine residue in the αF-helix of RSK/MSKs. Binding of DMF prevents the activation loop of the kinase from engaging sub... More