Metabolic-Pathway-Oriented Screening Targeting S-Adenosyl-l-methionine Reveals the Epigenetic Remodeling Activities of Naturally Occurring Catechols
- Resource Type
- Article
- Authors
- Ogihara, Shusuke; Komatsu, Toru; Itoh, Yukihiro; Miyake, Yuka; Suzuki, Takayoshi; Yanagi, Kouichi; Kimura, Yusuke; Ueno, Tasuku; Hanaoka, Kenjiro; Kojima, Hirotatsu; Okabe, Takayoshi; Nagano, Tetsuo; Urano, Yasuteru
- Source
- Journal of the American Chemical Society; January 2020, Vol. 142 Issue: 1 p21-26, 6p
- Subject
- Language
- ISSN
- 00027863; 15205126
Methyl transfer reactions play important roles in many biological phenomena, wherein the methylation cofactor S-adenosyl-l-methionine (SAM) serves as the important currency to orchestrate those reactions. We have developed a fluorescent-probe-based high-throughput screening (HTS) system to search for the compounds that control cellular SAM levels. HTS with a drug repositioning library revealed the importance of catechol-O-methyltransferase (COMT) and its substrates in controlling the SAM concentrations and histone methylation levels in colorectal tumor cells.