Title
An Efficient Mini-Transporter for Cytosolic Protein Delivery
Author
Ning Zhang, Ziqiang Yan, Xue Zhao, Qing Chen, Mingming Ma
Year
2016
Journal
Applied Materials and Interfaces
Abstract
An efficient method to deliver active proteins into cytosol is highly desirable to advance protein-based therapeutics. Arginine-rich cell-penetrating peptides (RPPs) have been intensively studied for intracellular protein delivery, and their applications require further improvement on delivery efficiency, serum stability and cytotoxicity. Designing synthetic analogs of RPPs provides an alternative way to achieve efficient cytosolic protein delivery. Herein we report the design and synthesis of a dendritic small molecule TG6, which is composed of one rigid planar core and four flexible arms with one guanidinium on each arm. Protein structure and function are well preserved in the TG6-protein conjugates, which are readily internalized into cytosol. Our study demonstrates that TG6 is a serum-stable and low-toxic molecular transporter delivering both small cargoes and large active proteins efficiently into cytosol.
Full Article
Instrument
J-810
Keywords
Circular dichroism, Secondary structure, Biochemistry, Materials