Aptamer-Drug Conjugates of Active Metabolites of Nucleoside Analogs and Cytotoxic Agents Inhibit Pancreatic Tumor Cell Growth
File(s)Yoon S et al Aptamer-conjugates Mole Ther 2017.pdf (2 MB)
Published version
Author(s)
Type
Journal Article
Abstract
Aptamer-drug conjugates (ApDCs) have the potential to improve the therapeutic index of traditional chemotherapeutic agents due to their ability to deliver cytotoxic drugs specifically to cancer cells while sparing normal cells. This study reports on the conjugation of cytotoxic drugs to an aptamer previously described by our group, the pancreatic cancer RNA aptamer P19. To this end, P19 was incorporated with gemcitabine and 5-fluorouracil (5-FU), or conjugated to monomethyl auristatin E (MMAE) and derivative of maytansine 1 (DM1). The ApDCs P19-dFdCMP and P19-5FdUMP were shown to induce the phosphorylation of histone H2AX on Ser139 (γ-H2AX) and significantly inhibited cell proliferation by 51%–53% in PANC-1 and by 54%–34% in the gemcitabine-resistant pancreatic cancer cell line AsPC-1 (p ≤ 0.0001). P19-MMAE and P19-DM1 caused mitotic G2/M phase arrest and inhibited cell proliferation by up to 56% in a dose-dependent manner when compared to the control group (p ≤ 0.001). In addition, the cytotoxicity of P19-MMAE and P19-DM1 in normal cells and the control human breast cancer cell line MCF7 was minimal. These results suggest that this approach may be useful in decreasing cytotoxic side effects in non-tumoral tissue.
Date Issued
2016-12-14
Date Acceptance
2016-11-02
Citation
MOLECULAR THERAPY-NUCLEIC ACIDS, 2016, 6, pp.80-88
ISSN
2162-2531
Publisher
CELL PRESS
Start Page
80
End Page
88
Journal / Book Title
MOLECULAR THERAPY-NUCLEIC ACIDS
Volume
6
Copyright Statement
© 2016 The Authors. This is an open access article under the CC BY-NC-ND license (
http://creativecommons.org/licenses/by-nc-nd/4.0/).
http://creativecommons.org/licenses/by-nc-nd/4.0/).
Sponsor
Mina Therapeutics Ltd
Identifier
http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000397092100007&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=1ba7043ffcc86c417c072aa74d649202
Grant Number
P58698
Subjects
Science & Technology
Life Sciences & Biomedicine
Medicine, Research & Experimental
Research & Experimental Medicine
NUCLEIC-ACID LIGANDS
TARGETED DELIVERY
CANCER
GEMCITABINE
MOLECULES
SELEX
CHEMOTHERAPY
SURVIVAL
ApDCs
aptamer-drug conjugates
cytotoxic agents
nucleoside analog
pancreatic cancer
Publication Status
Published