volume 15 issue 1 pages 238-246

A Novel Doxorubicin Prodrug with GRP78 Recognition and Nucleus-Targeting Ability for Safe and Effective Cancer Therapy

Publication typeJournal Article
Publication date2017-12-15
scimago Q1
wos Q1
SJR0.968
CiteScore7.8
Impact factor4.5
ISSN15438384, 15438392
Drug Discovery
Pharmaceutical Science
Molecular Medicine
Abstract
Glucose-regulated protein of 78 kDa (GRP78) has become an attractive and novel target for tumor therapy. Design and construction of powerful delivery systems that could efficiently transport doxorubicin (DOX) to a tumor-cell nucleus remains a formidable challenge for improving the tumor therapeutic index and mitigating side effects to normal tissues. Herein, a novel doxorubicin prodrug (NDP) with GRP78 recognition and nucleus-targeting ability was synthesized by a facile chemical route. NDP exhibited an enhanced antiproliferative activity against colorectal cancer cells and could efficiently enter the cell nucleus. Furthermore, it is inspiring to note that NDP displayed a much stronger inhibitory efficacy against the growth of colorectal cancer xenografts in nude mice than free DOX and showed superior in vivo safety. Together, the work provides a novel GRP78 and nucleus-targeting strategy, and the NDP holds great promise to be used as a potent and safe chemotherapeutic agent.
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GOST |
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GOST Copy
Ding G. et al. A Novel Doxorubicin Prodrug with GRP78 Recognition and Nucleus-Targeting Ability for Safe and Effective Cancer Therapy // Molecular Pharmaceutics. 2017. Vol. 15. No. 1. pp. 238-246.
GOST all authors (up to 50) Copy
Ding G., Sun J., Yang P., Li B., Gao Y., Li Z. A Novel Doxorubicin Prodrug with GRP78 Recognition and Nucleus-Targeting Ability for Safe and Effective Cancer Therapy // Molecular Pharmaceutics. 2017. Vol. 15. No. 1. pp. 238-246.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.1021/acs.molpharmaceut.7b00830
UR - https://doi.org/10.1021/acs.molpharmaceut.7b00830
TI - A Novel Doxorubicin Prodrug with GRP78 Recognition and Nucleus-Targeting Ability for Safe and Effective Cancer Therapy
T2 - Molecular Pharmaceutics
AU - Ding, Guo-Bin
AU - Sun, Junqing
AU - Yang, Peng
AU - Li, Bin-Chun
AU - Gao, Ying
AU - Li, Zhuoyu
PY - 2017
DA - 2017/12/15
PB - American Chemical Society (ACS)
SP - 238-246
IS - 1
VL - 15
PMID - 29207873
SN - 1543-8384
SN - 1543-8392
ER -
BibTex |
Cite this
BibTex (up to 50 authors) Copy
@article{2017_Ding,
author = {Guo-Bin Ding and Junqing Sun and Peng Yang and Bin-Chun Li and Ying Gao and Zhuoyu Li},
title = {A Novel Doxorubicin Prodrug with GRP78 Recognition and Nucleus-Targeting Ability for Safe and Effective Cancer Therapy},
journal = {Molecular Pharmaceutics},
year = {2017},
volume = {15},
publisher = {American Chemical Society (ACS)},
month = {dec},
url = {https://doi.org/10.1021/acs.molpharmaceut.7b00830},
number = {1},
pages = {238--246},
doi = {10.1021/acs.molpharmaceut.7b00830}
}
MLA
Cite this
MLA Copy
Ding, Guo-Bin, et al. “A Novel Doxorubicin Prodrug with GRP78 Recognition and Nucleus-Targeting Ability for Safe and Effective Cancer Therapy.” Molecular Pharmaceutics, vol. 15, no. 1, Dec. 2017, pp. 238-246. https://doi.org/10.1021/acs.molpharmaceut.7b00830.