Next Article in Journal
Low Basal CB2R in Dopamine Neurons and Microglia Influences Cannabinoid Tetrad Effects
Next Article in Special Issue
The Potential of Aptamer-Mediated Liquid Biopsy for Early Detection of Cancer
Previous Article in Journal
Identification and Analysis of MicroRNAs Associated with Wing Polyphenism in the Brown Planthopper, Nilaparvata lugens
Previous Article in Special Issue
Advances in Oligonucleotide Aptamers for NSCLC Targeting
 
 
Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
Journals
IJMS
Volume 21
Issue 24
10.3390/ijms21249764
ijms-logo
Submit to this Journal Review for this Journal Propose a Special Issue
► Article Menu

Article Menu

share Share announcement Help format_quote Cite question_answer Discuss in SciProfiles
first_page
settings
Order Article Reprints
Font Type:
Arial Georgia Verdana
Font Size:
Aa Aa Aa
Line Spacing:
Column Width:
Background:
Article

Development of HER2-Specific Aptamer-Drug Conjugate for Breast Cancer Therapy

by
Hwa Yeon Jeong
1,
Hyeri Kim
1,
Myunghwa Lee
1,
Jinju Hong
1,
Joo Han Lee
1,
Jeonghyeon Kim
1,
Moon Jung Choi
2,
Yong Serk Park
2,* and
Sung-Chun Kim
1,*
1
Biois Co., Ltd., Seoul 08390, Korea
2
Department of Biomedical Laboratory Science, Yonsei University, Wonju 26493, Korea
*
Authors to whom correspondence should be addressed.
Int. J. Mol. Sci. 2020, 21(24), 9764; https://doi.org/10.3390/ijms21249764
Submission received: 12 November 2020 / Revised: 18 December 2020 / Accepted: 18 December 2020 / Published: 21 December 2020
(This article belongs to the Special Issue Aptamer-Mediated Cancer Theranostics)
Browse Figures
Review Reports Versions Notes

Abstract

In this study, HER2 RNA aptamers were conjugated to mertansine (DM1) and the anti-cancer effectiveness of the conjugate was evaluated in HER2-overexpressing breast cancer models. The conjugate of HER2 aptamer and anticancer drug DM1 (aptamer-drug conjugate, ApDC) was prepared and analyzed using HPLC and mass spectrometry. The cell-binding affinity and cytotoxicity of the conjugate were determined using confocal microscopy and WST-1 assay. The in vivo anti-tumoral efficacy of ApDC was also evaluated in mice carrying BT-474 breast tumors overexpressing HER2. The synthesized HER2-specific RNA aptamers were able to specifically and efficiently bind to HER-positive BT-474 breast cancer cells, but not to HER2-negative MDA-MB-231 breast cancer cells. Also, the HER2-specific ApDC showed strong toxicity to the target cells, BT-474, but not to MDA-MB-231 cells. According to the in vivo analyses drawn from the mouse xenografts of BT-747 tumor, the ApDC was able to more effectively inhibit the tumor growth. Compared to the control group, the mice treated with the ApDC showed a significant reduction of tumor growth. Besides, any significant body weight losses or hepatic toxicities were monitored in the ApDC-treated mice. This research suggests the HER2 aptamer-DM1 conjugate as a target-specific anti-cancer modality and provides experimental evidence supporting its enhanced effectiveness for HER2-overexpressing target tumors. This type of aptamer-conjugated anticancer drug would be utilized as a platform structure for the development of versatile targeted high-performance anticancer drugs by adopting the easy deformability and high affinity of aptamers.
Keywords: HER2-positive cancer; RNA aptamer; mertansine; aptamer delivery HER2-positive cancer; RNA aptamer; mertansine; aptamer delivery

Share and Cite

MDPI and ACS Style

Jeong, H.Y.; Kim, H.; Lee, M.; Hong, J.; Lee, J.H.; Kim, J.; Choi, M.J.; Park, Y.S.; Kim, S.-C. Development of HER2-Specific Aptamer-Drug Conjugate for Breast Cancer Therapy. Int. J. Mol. Sci. 2020, 21, 9764. https://doi.org/10.3390/ijms21249764

AMA Style

Jeong HY, Kim H, Lee M, Hong J, Lee JH, Kim J, Choi MJ, Park YS, Kim S-C. Development of HER2-Specific Aptamer-Drug Conjugate for Breast Cancer Therapy. International Journal of Molecular Sciences. 2020; 21(24):9764. https://doi.org/10.3390/ijms21249764

Chicago/Turabian Style

Jeong, Hwa Yeon, Hyeri Kim, Myunghwa Lee, Jinju Hong, Joo Han Lee, Jeonghyeon Kim, Moon Jung Choi, Yong Serk Park, and Sung-Chun Kim. 2020. "Development of HER2-Specific Aptamer-Drug Conjugate for Breast Cancer Therapy" International Journal of Molecular Sciences 21, no. 24: 9764. https://doi.org/10.3390/ijms21249764

APA Style

Jeong, H. Y., Kim, H., Lee, M., Hong, J., Lee, J. H., Kim, J., Choi, M. J., Park, Y. S., & Kim, S.-C. (2020). Development of HER2-Specific Aptamer-Drug Conjugate for Breast Cancer Therapy. International Journal of Molecular Sciences, 21(24), 9764. https://doi.org/10.3390/ijms21249764

Note that from the first issue of 2016, this journal uses article numbers instead of page numbers. See further details here.

Article Metrics

Back to TopTop