Issue 17, 2018

A halogen bond-mediated highly active artificial chloride channel with high anticancer activity

Abstract

Chloride-selective transmembrane carriers or channels might have possible uses in treating channelopathies or cancers. While chloride carriers have been extensively investigated, the corresponding chloride channels have remained limitedly studied. Moreover, all hitherto reported channel systems lack clearly definable and readily modifiable positions in their structures for the reliable construction and combinatorial optimization of their ion transport properties. As a result, the existing channels are limited by their large molecular weight, weak activity or low anion selectivity. In this report, we describe a readily accessible and robust monopeptide-based scaffold for the reliable construction of halogen bond-mediated artificial anion channels via directional assembly of electron-deficient iodine atoms, which create a transmembrane pathway for facilitating anion transport. The high intrinsic modularity of the backbone of the scaffold, which enables the rapid and combinatorial optimization of the transport activity and selectivity of channels, effectively delivers a highly active chloride channel A10. Such high activity in chloride transport subsequently leads to an excellent IC50 value of 20 μM toward inhibiting the growth of human breast cancer cells (BT-474), an anticancer activity that is even higher than that of the well-known anticancer agent cisplatin.

Graphical abstract: A halogen bond-mediated highly active artificial chloride channel with high anticancer activity

Supplementary files

Article information

Article type
Edge Article
Submitted
06 2 2018
Accepted
15 3 2018
First published
15 3 2018
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY license

Chem. Sci., 2018,9, 4044-4051

A halogen bond-mediated highly active artificial chloride channel with high anticancer activity

C. Ren, X. Ding, A. Roy, J. Shen, S. Zhou, F. Chen, S. F. Yau Li, H. Ren, Y. Y. Yang and H. Zeng, Chem. Sci., 2018, 9, 4044 DOI: 10.1039/C8SC00602D

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements