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bioRxiv · 10.1101/2021.12.09.471985

Fast in-vitro screening of FLT3-ITD inhibitors using silkworm-baculovirus protein expression system

Yamamoto, N.·Kikuchi, J.·Furukawa, Y.·Shibayama, N.
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Abstract

We report expression and purification of a FLT3 protein with ITD mutation (FLT3-ITD) with a steady tyrosine kinase activity using a silkworm-baculovirus system, and its application as a fast screening system of tyrosine kinase inhibitors. The FLT3-ITD protein was expressed in Bombyx mori L. pupae infected by gene-modified nucleopolyhedrovirus, and was purified as an active state. We performed an inhibition assay using 17 potential kinase inhibitors, and succeeded in identifying two potent inhibitors for FLT3-ITD. The result has paved the way for screening FLT3-ITD inhibitors in a fast and easy manner, and also for structural studies.

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Yamamoto, N., Kikuchi, J., Furukawa, Y., Shibayama, N.. 2021-12-09. Fast in-vitro screening of FLT3-ITD inhibitors using silkworm-baculovirus protein expression system. https://doi.org/10.1101/2021.12.09.471985

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