Publication: Development of a Cell-Based Assay for Identifying K<inf>Ca</inf>3.1 Inhibitors Using Intestinal Epithelial Cell Lines
Issued Date
2020-01-01
Resource Type
ISSN
24725560
24725552
24725552
Other identifier(s)
2-s2.0-85089779296
Rights
Mahidol University
Rights Holder(s)
SCOPUS
Bibliographic Citation
SLAS Discovery. (2020)
Suggested Citation
Chanon Jakakul, Phongthon Kanjanasirirat, Chatchai Muanprasat Development of a Cell-Based Assay for Identifying K<inf>Ca</inf>3.1 Inhibitors Using Intestinal Epithelial Cell Lines. SLAS Discovery. (2020). doi:10.1177/2472555220950661 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/58989
Research Projects
Organizational Units
Authors
Journal Issue
Thesis
Title
Development of a Cell-Based Assay for Identifying K<inf>Ca</inf>3.1 Inhibitors Using Intestinal Epithelial Cell Lines
Other Contributor(s)
Abstract
© Society for Laboratory Automation and Screening 2020. Inhibition of the KCa3.1 potassium channel has therapeutic potential in a variety of human diseases, including inflammation-associated disorders and cancers. However, KCa3.1 inhibitors with high therapeutic promise are currently not available. This study aimed to establish a screening assay for identifying inhibitors of KCa3.1 in native cells and from library compounds derived from natural products in Thailand. The screening platform was successfully developed based on a thallium flux assay in intestinal epithelial (T84) cells with a Z′ factor of 0.52. The screening of 1352 compounds and functional validation using electrophysiological analyses identified 8 compounds as novel KCa3.1 inhibitors with IC50 values ranging from 0.14 to 6.57 µM. These results indicate that the assay developed is of excellent quality for high-throughput screening and capable of identifying KCa3.1 inhibitors. This assay may be useful in identifying novel KCa3.1 inhibitors that may have therapeutic potential for inflammation-associated disorders and cancers.