High-performance mass spectrometry as a drug discovery tool: a high-throughput screening assay to identify RNA-binding ligands

Kristin A. Sannes-Lowery; Jared J. Drader; Richard H. Griffey; Steven A. Hofstadler

doi:10.1117/12.424586

16 April 2001 High-performance mass spectrometry as a drug discovery tool: a high-throughput screening assay to identify RNA-binding ligands

Kristin A. Sannes-Lowery, Jared J. Drader, Richard H. Griffey, Steven A. Hofstadler

Author Affiliations +

Proceedings Volume 4264, Genomics and Proteomics Technologies; (2001) https://doi.org/10.1117/12.424586
Event: BiOS 2001 The International Symposium on Biomedical Optics, 2001, San Jose, CA, United States

Abstract

Fourier transform mass spectrometry (FTMS) is increasingly being used as a drug discovery tool. We describe the development of a parallel high-throughput screening (HTS) strategy to identify small molecules that bind RNA targets using FTMS as an alternative to classical high-throughput biological screening methods for combinatorial libraries. The Multitarget Affinity/Specificity Screening (MASS) assay takes advantage of the "intrinsic mass" label of each compound and target RNA by employing high resolution, high precision mass measurements. The ability to analyze complex mixtures allows large compound libraries to be screened in the presence of multiple RNA targets simultaneously. The identity of the small molecule(s) which bind, the RNA target to which it binds, the compound-specific binding affinity and the location of the binding site on the RNA can be determined in one set of rapid experiments. The MASS technology detects complexes with dissociation constants of < 5 mM, with high sensitivity.

Citation Download Citation

Kristin A. Sannes-Lowery, Jared J. Drader, Richard H. Griffey, and Steven A. Hofstadler "High-performance mass spectrometry as a drug discovery tool: a high-throughput screening assay to identify RNA-binding ligands", Proc. SPIE 4264, Genomics and Proteomics Technologies, (16 April 2001); https://doi.org/10.1117/12.424586

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