A Suite of Biochemical Assays for Screening RNA Methyltransferase BCDIN3D. (January 2017)

• Record Type: Journal Article
• Authors: Blazer, Levi L.; Li, Fengling; Kennedy, Steven; Zheng, Yujun George; Arrowsmith, Cheryl H.; Vedadi, Masoud
• Is Part Of: Journal of biomolecular screening. Volume 22:Number 1(2017)
• Page Start: 32
• Page End: 39
• Publication Date: 2017-01
• Subjects: O-methyltransferase -- BCDIN3D -- microRNA -- RNA methyltransferase; Drugs -- Analysis -- Periodicals; Drugs -- Testing -- Periodicals; Biomolecules -- Analysis -- Periodicals; 572.36
• DOI: 10.1177/1087057116666276
• Languages: English
• ISSNs: 1087-0571

Abstract

BCDIN3D is an RNA-methyltransferase that O-methylates the 5′ phosphate of RNA and regulates microRNA maturation. To discover small-molecule inhibitors of BCDIN3D, a suite of biochemical assays was developed. A radiometric methyltransferase assay and fluorescence polarization–based S-adenosylmethionine and RNA displacement assays are described. In addition, differential scanning fluorimetry and surface plasmon resonance were used to characterize binding. These assays provide a comprehensive package for the development of small-molecule modulators of BCDIN3D activity.