Fluorescence imaging of drug target proteins using chemical probes

Hao Zhu; Itaru Hamachi

doi:10.1016/j.jpha.2020.05.013

Fluorescence imaging of drug target proteins using chemical probes

J Pharm Anal. 2020 Oct;10(5):426-433. doi: 10.1016/j.jpha.2020.05.013. Epub 2020 Jun 6.

Authors

Hao Zhu¹, Itaru Hamachi^{1

2}

Affiliations

¹ Department of Synthetic Chemistry and Biological Chemistry, Graduate School of Engineering, Kyoto University, Katsura, Nishikyo-ku, Kyoto, 615-8510, Japan.
² ERATO Innovative Molecular Technology for Neuroscience Project, Japan Science and Technology Agency (JST), Kyoto, 615-8530, Japan.

Abstract

Fluorescence imaging can provide valuable information on the expression, distribution, and activity of drug target proteins. Chemical probes are useful small-molecule tools for fluorescence imaging with high structural flexibility and biocompatibility. In this review, we briefly introduce two classes of fluorescent probes for the visualization of drug target proteins. Enzymatically activatable probes make use of the specific enzymatic transformations that generally produce a fluorogenic response upon reacting with target enzymes. Alternatively, specific imaging can be conferred with a ligand that drives the probes to target proteins, where the labeling relies on noncovalent binding, covalent inhibition, or traceless labeling by ligand-directed chemistry.

Keywords: Chemical probe; Drug target; Fluorescence imaging; Ligand-directed chemistry.

Publication types

Review