Institute for Molecules and Materials, Radboud University, Heyendaalseweg 135, 6525 AJ Nijmegen, The Netherlands.
Mercachem B.V., Kerkenbos 1013, 6546 BB Nijmegen, The Netherlands.
Chem Commun (Camb). 2020 Mar 10;56(20):3039-3042. doi: 10.1039/c9cc09098c.
We report synthesis and enzymatic assays on human histone lysine methyltransferase catalysed methylation of histones that possess lysine and its geometrically constrained analogues containing rigid (E)-alkene (KE), (Z)-alkene (KZ) and alkyne (Kyne) moieties. Methyltransferases G9a and GLP do have a capacity to catalyse methylation in the order K ≫ KE > KZ ∼ Kyne, whereas monomethyltransferase SETD8 catalyses only methylation of K and KE.
我们报告了人类组蛋白赖氨酸甲基转移酶催化具有赖氨酸的组蛋白和其刚性（E）-烯烃（KE）、（Z）-烯烃（KZ）和炔烃（Kyne）部分的几何约束类似物的甲基化的合成和酶促测定。甲基转移酶 G9a 和 GLP 确实具有按 K ≫ KE > KZ ∼ Kyne 的顺序催化甲基化的能力，而单甲基转移酶 SETD8 仅催化 K 和 KE 的甲基化。
