Development of novel apoferritin formulations for antitumour benzothiazoles.

ABSTRACT:

Background

The benzothiazole structure is important in medicinal chemistry, and 5-fluoro-2-(3,4-dimethoxyphenyl) benzothiazole (GW 610) is of particular interest as it shows outstanding anticancer activity in sensitive breast and colorectal carcinoma cell lines via generation of lethal DNA adducts in sensitive cancer cells. Despite promising activity, poor water solubility limits its applications. The apoferritin (AFt) protein cage has been proposed as a robust and biocompatible drug delivery vehicle.

Aims

Here, we aim to enhance solubility of GW 610 by developing amino acid prodrug conjugates and utilizing the AFt capsule as drug delivery vessel.

Methods and results

The potent experimental antitumour agent, GW 610, has been successfully encapsulated within AFt with m

SUBMITTER: Breen AF 

PROVIDER: S-EPMC7941424 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature