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Functional l-arginine derivative as an efficient vector for intracellular protein delivery for potential cancer therapy

Functional l-arginine derivative as an efficient vector for intracellular protein delivery for potential cancer therapy

He X, Qu Y, Xiong S, Jiang Z, Tang Y, Yan F, Deng Y, Sun Y (2023) Functional l-arginine derivative as an efficient vector for intracellular protein delivery for potential cancer therapy. J Funct Biomater 14(6):301. doi: 10.3390/jfb14060301 PMID: 37367265

Objective: To address the instability of the 9-fluorenylmethyloxycarbonyl (Fmoc) group in aqueous medium.

Summary: The Fmoc ligand neighboring arginine was substituted for dibenzocyclooctyne (DBCO) with a similar structure to Fmoc to obtain stable DBCO-functionalized L-arginine derivative (DR). DBCO-functionalized L-arginine derivative represents an excellent potential vector for protein-based cancer therapy.

Usage: The synthesized DR monomer was first dissolved in sterilized ultrapure water with a concentration of 1 mg/mL, then mixed with protein solution at a weight ratio of 5:1 for saporin (DR:SA) for 10 min at room temperature. Saporin was added at 110μg/mL to MDA-MB-231 cells (DR: SA-FITC: HA,w:w:w, 5:1:25)