2. Academic Validation
  3. A cell-based fluorescent assay for FAP inhibitor discovery

A cell-based fluorescent assay for FAP inhibitor discovery

  • Bioorg Med Chem Lett. 2020 Jul 15;30(14):127253. doi: 10.1016/j.bmcl.2020.127253.
Bingye Zhang 1,  Futao Liu 1,  Min-Fu Yang 2,  Jianfeng Xu 3,  Zheng Wang 3,  Jianhua Zhang 1,  Rongfu Wang 4,  Xing Yang 5
Affiliations

Affiliations

  • 1 Department of Nuclear Medicine, Peking University First Hospital, Beijing 100034, China.
  • 2 Department of Nuclear Medicine, Beijing Chaoyang Hospital, Capital Medical University, Beijing 100020, China.
  • 3 JYAMS PET Research & Development Limited., Nanjing 211100, China.
  • 4 Department of Nuclear Medicine, Peking University First Hospital, Beijing 100034, China. Electronic address: [email protected].
  • 5 Department of Nuclear Medicine, Peking University First Hospital, Beijing 100034, China; Institute of Medical Technology, Peking University, Beijing 100191, China. Electronic address: [email protected].
PMID: 32527554 DOI: 10.1016/j.bmcl.2020.127253
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 IC50s 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 IC50s 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.

Keywords

FAP inhibitor; Fibroblast activation protein; Fluorescent assay; Suc-Gly-Pro-AMC.

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