A Suite of Biochemical Assays for Screening RNA Methyltransferase BCDIN3D-Reference-Cited by-同舟云学术

A Suite of Biochemical Assays for Screening RNA Methyltransferase BCDIN3D

Published:2016-09-27 Issue:1 Volume:22 Page:32-39
ISSN:2472-5552
Container-title:SLAS DISCOVERY: Advancing the Science of Drug Discovery
language:en
Short-container-title:SLAS DISCOVERY: Advancing the Science of Drug Discovery

Author:

Blazer Levi L.¹,Li Fengling¹,Kennedy Steven¹,Zheng Yujun George²,Arrowsmith Cheryl H.¹³,Vedadi Masoud¹⁴

Affiliation:

1. Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada

2. Department of Pharmaceutical and Biomedical Sciences, University of Georgia, Athens, GA, USA

3. Princess Margaret Cancer Centre and Department of Medical Biophysics, University of Toronto, Toronto, ON, Canada

4. Department of Pharmacology and Toxicology, University of Toronto, Toronto, ON, Canada

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.

Publisher

Elsevier BV

Subject

Molecular Medicine,Biochemistry,Analytical Chemistry,Biotechnology

Link

http://journals.sagepub.com/doi/pdf/10.1177/1087057116666276

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