Open AccessThe anti‐human cytomegalovirus drug tricin inhibits cyclin‐dependent kinase 9
Author(s) -
Sadanari Hidetaka,
Fujimoto Kazuhiro J.,
Sugihara Yuto,
Ishida Tomoki,
Takemoto Masaya,
Daikoku Tohru,
Murayama Tsugiya
Publication year - 2018
Publication title -
febs open bio
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.718
H-Index - 31
ISSN - 2211-5463
DOI - 10.1002/2211-5463.12398
Subject(s) - tricin , pharmacology , kinase , drug , chemistry , human cytomegalovirus , virology , medicine , biochemistry , virus , flavonoid , antioxidant
4′,5,7‐trihydroxy‐3′,5′‐dimethoxyflavone (tricin), derived from Sasa albo‐marginata , has been reported to suppress significantly human cytomegalovirus ( HCMV ) replication in human embryonic lung ( HEL ) fibroblast cells. However, the target protein of tricin remains unclear. This study focused on the anti‐ HCMV activity of tricin in terms of its binding affinity to cyclin‐dependent kinase 9 ( CDK 9). A molecular docking study predicted that tricin binds well to the ATP ‐binding site of CDK 9. Experimental measurements then revealed that tricin inhibits the kinase activity of CDK 9 and affects the phosphorylation of the carboxy‐terminal domain of RNA polymerase II . Based on these results, we conclude that CDK 9 is one of the target proteins of tricin. We also found that tricin possesses anti‐ HCMV activity with no cytotoxicity against HEL cells.