Issue 7, 2016

Cationic pillar[6]arene/ATP host–guest recognition: selectivity, inhibition of ATP hydrolysis, and application in multidrug resistance treatment

Abstract

Due to the differences in the cavity size of the hosts and the charge and length of the guests, a cationic water-soluble pillar[6]arene (WP6) selectively complexes with ATP to form a stable 1 : 1 inclusion complex WP6⊃ATP. This host–guest complexation was utilized to efficiently inhibit the hydrolysis of ATP, arising from the existence of the hydrophobic cavity of WP6. A folic acid functionalized diblock copolymer (FA-PEG-b-PAA) was employed to PEGylate WP6 to endow the polyion complex (PIC) micelles with specific targeting ability, preferentially delivering WP6 to folate receptor over-expressing KB cell. This host–guest complexation was further used to block the efflux pump to transport anticancer drugs out of cells by cutting off the energy source, which enhanced the efficacy of the cancer chemotherapy of DOX·HCl towards drug resistant MCF-7/ADR cell. This supramolecular method provides an extremely distinct strategy to potentially overcome multidrug resistance (MDR).

Graphical abstract: Cationic pillar[6]arene/ATP host–guest recognition: selectivity, inhibition of ATP hydrolysis, and application in multidrug resistance treatment

Supplementary files

Article information

Article type
Edge Article
Submitted
03 2 2016
Accepted
02 3 2016
First published
02 3 2016
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., 2016,7, 4073-4078

Cationic pillar[6]arene/ATP host–guest recognition: selectivity, inhibition of ATP hydrolysis, and application in multidrug resistance treatment

G. Yu, J. Zhou, J. Shen, G. Tang and F. Huang, Chem. Sci., 2016, 7, 4073 DOI: 10.1039/C6SC00531D

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.

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