@article{258155dd572243b5a1891c449277c0af,
title = "Integrated Mass Spectrometry Reveals Celastrol As a Novel Catechol-O-methyltransferase Inhibitor",
abstract = "Natural product celastrol is known to have various biological activities, yet its molecular targets that correspond to many activities remain unclear. Here, we used multiple mass-spectrometry-based approaches to identify catechol-O-methyltransferase (COMT) as a major binding target of celastrol and characterized their interaction comprehensively. Celastrol was found to inhibit the enzymatic activity of COMT and increased the dopamine level in neuroendocrine chromaffin cells significantly. Our study not only revealed a novel binding target of celastrol but also provided a new scaffold and cysteine hot spot for developing new generation COMT inhibitors in combating neurological disorders.",
author = "Haijun Guo and Yang Yang and Qi Zhang and Jie-Ren Deng and Ying Yang and Shuqi Li and Pui-Kin So and Lam, {Thomas C.} and Man-kin Wong and Qian Zhao",
note = "Funding Information: We acknowledge the funding support from Research Grants Council-ECS 25301518, GRF 15304819, CRF C5033-19E, and RGC-RIF R5050-18, NSFC 21705136. We thank the support from Centre for Eye and Vision Research (CEVR) and Laboratory for Synthetic Chemistry and Chemical Biology Limited (LSCCB) under the Health@InnoHK Programme launched by ITC, HKSAR. We thank Research Institute for Future Food (RiFood), the PolyU Research Facilities UCEA and ULS, C. Tsang, for technical support. Publisher Copyright: {\textcopyright} 2022 American Chemical Society.",
year = "2022",
month = mar,
day = "18",
doi = "10.1021/acschembio.2c00011",
language = "English",
volume = "17",
pages = "2003--2009",
journal = "ACS Chemical Biology",
issn = "1554-8929",
publisher = "American Chemical Society",
number = "8",
}