A cell-based fluorescent assay for FAP inhibitor discovery. Issue 14 (15th July 2020)

• Record Type: Journal Article
• Authors: Zhang, Bingye; Liu, Futao; Yang, Min-Fu; Xu, Jianfeng; Wang, Zheng; Zhang, Jianhua; Wang, Rongfu; Yang, Xing
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 30:Issue 14(2020)
• Publication Date: 2020-07-15
• Subjects: Suc-Gly-Pro-AMC -- FAP inhibitor -- Fibroblast activation protein -- Fluorescent assay; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2020.127253
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: To facilitate the discovery of FAP inhibitors, a convenient cell-based fluorescent assay was developed by using a commonly available U87MG cell line and a FAP-specific substrate Suc-Gly-Pro-AMC. The assay enabled the fast determination of multiple IC50 s by simply incubating a solution of phosphate-buffered saline in a 96-well plate within 30 min. The substrate specificity, cross-reaction and other related conditions were systematically optimized. This method was successfully applied to determine the IC50 s of seven known inhibitors. The results are in consistence with the trend reported, which indicating that this practical assay is a valuable method to accelerate the discovery of FAP inhibitor.