Next Article in Journal
An Improved Time-Frequency Analysis Method in Interference Detection for GNSS Receivers
Next Article in Special Issue
Field Effect Sensors for Nucleic Acid Detection: Recent Advances and Future Perspectives
Previous Article in Journal
Study of Multi-Armed Bandits for Energy Conservation in Cognitive Radio Sensor Networks
Previous Article in Special Issue
Calculation of the Electronic Parameters of an Al/DNA/p-Si Schottky Barrier Diode Influenced by Alpha Radiation
Article Menu

Export Article

Open AccessArticle
Sensors 2015, 15(4), 9388-9403;

A mRNA-Responsive G-Quadruplex-Based Drug Release System

Advanced Research Division, Panasonic Corporation, 3-4 Hikaridai, Seika-cho, Soraku-gun, Kyoto 619-0237, Japan
Faculty of Frontiers of Innovative Research in Science and Technology (FIRST), Konan University, 7-1-20 Minatojima-Minamimachi, Chuo-ku, Kobe 650-0047, Japan
Frontier Institute for Biomolecular Engineering Research (FIBER), Konan University, 7-1-20 Minatojima-Minamimachi, Chuo-ku, Kobe 650-0047, Japan
Author to whom correspondence should be addressed.
Academic Editor: Matteo Castronovo
Received: 6 February 2015 / Revised: 8 April 2015 / Accepted: 8 April 2015 / Published: 21 April 2015
(This article belongs to the Special Issue Next-Generation Nucleic Acid Sensors)
Full-Text   |   PDF [1159 KB, uploaded 21 April 2015]   |  


G-quadruplex-based drug delivery carriers (GDDCs) were designed to capture and release a telomerase inhibitor in response to a target mRNA. Hybridization between a loop on the GDDC structure and the mRNA should cause the G-quadruplex structure of the GDDC to unfold and release the bound inhibitor, anionic copper(II) phthalocyanine (CuAPC). As a proof of concept, GDDCs were designed with a 10-30-mer loop, which can hybridize with a target sequence in epidermal growth factor receptor (EGFR) mRNA. Structural analysis using circular dichroism (CD) spectroscopy showed that the GDDCs form a (3 + 1) type G-quadruplex structure in 100 mM KCl and 10 mM MgCl2 in the absence of the target RNA. Visible absorbance titration experiments showed that the GDDCs bind to CuAPC with Ka values of 1.5 × 105 to 5.9 × 105 M−1 (Kd values of 6.7 to 1.7 μM) at 25 °C, depending on the loop length. Fluorescence titration further showed that the G-quadruplex structure unfolds upon binding to the target RNA with Ka values above 1.0 × 108 M−1 (Kd values below 0.01 μM) at 25 °C. These results suggest the carrier can sense and bind to the target RNA, which should result in release of the bound drug. Finally, visible absorbance titration experiments demonstrated that the GDDC release CuAPC in response to the target RNA. View Full-Text
Keywords: drug delivery carrier; G-quadruplex; anionic phthalocyanine; cancer; mRNA; telomerase drug delivery carrier; G-quadruplex; anionic phthalocyanine; cancer; mRNA; telomerase

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Supplementary materials


Share & Cite This Article

MDPI and ACS Style

Yaku, H.; Murashima, T.; Miyoshi, D.; Sugimoto, N. A mRNA-Responsive G-Quadruplex-Based Drug Release System. Sensors 2015, 15, 9388-9403.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Sensors EISSN 1424-8220 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top