Temperature vaulting: A method for screening selective, slow- and tight-binding inhibitors targeting kinases in their non-native state
Sora Suzuki, Koji Umezawa, Gaku Furuie, Masaki Kikuchi, Daichi Nakamura, Nanae Fukahori, Ninako Kimura, Masato Yamakawa, Takashi Niwa, Takashi Umehara, Takamitsu Hosoya, Isao Kii
This paper introduces a method called 'temperature vaulting' to screen inhibitors targeting kinases in their non-native state, demonstrating its effectiveness with the inhibitor FINDY (1) against DYRK1A.
European Journal of Medicinal Chemistry · May 20, 2025Peer-reviewedBiophysics