Please use this identifier to cite or link to this item:
http://hdl.handle.net/10397/92563
Title: | Integrated mass spectrometry reveals celastrol as a novel Catechol-O-methyltransferase inhibitor | Authors: | Guo, H Yang, Y Zhang, Q Deng, JR Yang, Y Li, S So, PK Lam, TC Wong, M Zhao, Q |
Issue Date: | 19-Aug-2022 | Source: | ACS chemical biology, 19 Aug. 2022, v. 17, no. 8, p. 2003–2009 | 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. | Publisher: | American Chemical Society | Journal: | ACS chemical biology | ISSN: | 1554-8929 | EISSN: | 1554-8937 | DOI: | 10.1021/acschembio.2c00011 | Rights: | © 2022 American Chemical Society This document is the Accepted Manuscript version of a Published Work that appeared in final form in ACS Chemical Biology, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see https://dx.doi.org/10.1021/acschembio.2c00011. |
Appears in Collections: | Journal/Magazine Article |
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File | Description | Size | Format | |
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Guo_Mass_Spectrometry_Catechol-O-methyltransferase.pdf | Pre-Published version | 2.25 MB | Adobe PDF | View/Open |
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