ATPase activity profiling of three human DExD/H-box RNA helicases
Human DExD/H-box RNA helicases are ubiquitous molecular motors that unwind and rearrange RNA secondary structures in an ATP-dependent manner. These enzymes play essential roles in nearly all aspects of RNA metabolism. While their biological functions are well-characterized, the kinetic mechanisms remain relatively understudied in vitro. In this study, we describe the development and optimization of a bioluminescence-based assay to characterize the ATPase activity of three human RNA helicases: MDA5, LGP2, and DDX1. The assays were conducted using annealed 24-mer ds-RNA (blunt-ended double-stranded RNA) or double-stranded RNA with a 25-nt 3' overhang (partial ds-RNA). These findings establish a robust and high-throughput in vitro assay suitable for a 384-well format, enabling the discovery and characterization of inhibitors targeting MDA5, LGP2, and DDX1. This work provides a valuable resource for advancing our understanding of these helicases and their therapeutic potential in Alzheimer's disease.
Authors
- Levon Halabelian (ORCID: https://orcid.org/0000-0003-4361-3619)
- Irene Chau (ORCID: https://orcid.org/0000-0002-2313-973X)
- Fengling Li (ORCID: https://orcid.org/0000-0002-7962-9033)
- Julia Garcia Perez (ORCID: https://orcid.org/0000-0003-3630-4404)
- Hong Zeng
- Yanjun Li (ORCID: https://orcid.org/0000-0002-9512-5265)
- Alma Seitova
- U Hang Chan
Institutions
- University of Toronto (CA)
- Structural Genomics Consortium (CA)
Publication Details
- Journal
- SLAS DISCOVERY
- Published
- 2025-04-01
- DOI
- https://doi.org/10.1016/j.slasd.2025.100229
- Citations
- 3
- Primary Topic
- RNA Research and Splicing
- Type
- article
- Field-Weighted Citation Impact
- 2.42