Synthesis of an Alkynyl Methylglyoxal Probe to Investigate Nonenzymatic Histone Glycation

炔基甲基乙二醛探针的合成及其用于研究非酶组蛋白糖基化

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作者:Qingfei Zheng, Igor Maksimovic, Akhil Upad, David Guber, Yael David

Abstract

Methylglyoxal (MGO) is a reactive dicarbonyl metabolite that modifies histones in vivo and induces changes in chromatin structure and function. Here we report the synthesis and application of a chemical probe for investigating MGO-glycation. A two-step synthesis of a Cu-click compatible alkynyl oxoaldehyde probe (AlkMGO) via sequential Dess-Martin and Riley oxidations is presented. This synthesis elevates the accessibility and utility of an important tool for tracking, enriching, and studying MGO-glycation to aid in understanding its underlying biochemical functions.

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