Ontology highlight
ABSTRACT:
SUBMITTER: Li J
PROVIDER: S-EPMC5949721 | biostudies-literature | 2018 May
REPOSITORIES: biostudies-literature
Li Jing J Li Shanshan S Guo Jianshuang J Li Qiuying Q Long Jing J Ma Cheng C Ding Yahui Y Yan Chunli C Li Liangwei L Wu Zhigang Z Zhu He H Li Keqin Kathy KK Wen Liuqing L Zhang Quan Q Xue Qingqing Q Zhao Caili C Liu Ning N Ivanov Ivaylo I Luo Ming M Xi Rimo R Long Haibo H Wang Peng George PG Chen Yue Y
Journal of medicinal chemistry 20180429 9
Metabolic reprogramming of cancer cells is essential for tumorigenesis in which pyruvate kinase M2 (PKM2), the low activity isoform of pyruvate kinase, plays a critical role. Herein, we describe the identification of a nature-product-derived micheliolide (MCL) that selectively activates PKM2 through the covalent binding at residue cysteine424 (C424), which is not contained in PKM1. This interaction promotes more tetramer formation, inhibits the lysine433 (K433) acetylation, and influences the tr ...[more]