Discovery of a potent and selective fragment-like inhibitor of methyllysine reader protein spindlin 1 (SPIN1)

By screening an epigenetic compound library, we identified that UNC0638, a highly potent inhibitor of the histone methyltransferases G9a and GLP, was a weak inhibitor of SPIN1 (spindlin 1), a methyllysine reader protein. Our optimization of this weak hit resulted in the discovery of a potent, select...

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Bibliografski detalji
Glavni autori: Xiong, Y, Greschik, H, Johansson, C, Seifert, L, Bacher, J, Park, K, Babault, N, Martini, M, Fagan, V, Li, F, Chau, I, Christott, T, Dilworth, D, Barsyte-Lovejoy, D, Vedadi, M, Arrowsmith, C, Brennan, P, Fedorov, O, Jung, M, Farnie, G, Liu, J, Oppermann, U, Schüle, R, Jin, J
Format: Journal article
Jezik:English
Izdano: American Chemical Society 2019