A cell-based fluorescent assay for FAP inhibitor discovery.
Bioorg Med Chem Lett
; 30(14): 127253, 2020 07 15.
Article
em En
| MEDLINE
| ID: mdl-32527554
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.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Gelatinases
/
Descoberta de Drogas
/
Imagem Óptica
/
Corantes Fluorescentes
/
Proteínas de Membrana
Limite:
Humans
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article