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Selective in vivo metabolic cell-labeling-mediated cancer targeting
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Selective in vivo metabolic cell-labeling-mediated cancer targeting
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Journal Article
Selective in vivo metabolic cell-labeling-mediated cancer targeting
2017
Overview
Metabolic labeling of the cell surface with a caged azide sugar enabled cleavage-mediated activation by enzymes overexpressed in cancer cells, allowing enhanced targeted delivery of a doxorubicin conjugate through copper-free click chemistry.
Distinguishing cancer cells from normal cells through surface receptors is vital for cancer diagnosis and targeted therapy. Metabolic glycoengineering of unnatural sugars provides a powerful tool to manually introduce chemical receptors onto the cell surface; however, cancer-selective labeling still remains a great challenge. Herein we report the design of sugars that can selectively label cancer cells both
in vitro
and
in vivo
. Specifically, we inhibit the cell-labeling activity of tetraacetyl-
N
-azidoacetylmannosamine (Ac
4
ManAz) by converting its anomeric acetyl group to a caged ether bond that can be selectively cleaved by cancer-overexpressed enzymes and thus enables the overexpression of azido groups on the surface of cancer cells. Histone deacetylase and cathepsin L-responsive acetylated azidomannosamine, one such enzymatically activatable Ac
4
ManAz analog developed, mediated cancer-selective labeling
in vivo
, which enhanced tumor accumulation of a dibenzocyclooctyne–doxorubicin conjugate via click chemistry and enabled targeted therapy against LS174T colon cancer, MDA-MB-231 triple-negative breast cancer and 4T1 metastatic breast cancer in mice.
Publisher
Nature Publishing Group US,Nature Publishing Group
Subject
/ Animals
/ Biology
/ Breast Neoplasms - diagnosis
/ Breast Neoplasms - drug therapy
/ Breast Neoplasms - metabolism
/ Carbohydrates - chemical synthesis
/ Cells
/ Colonic Neoplasms - diagnosis
/ Colonic Neoplasms - drug therapy
/ Colonic Neoplasms - metabolism
/ Dose-Response Relationship, Drug
/ Drug Screening Assays, Antitumor
/ Female
/ Humans
/ Mice
/ Molecular Probes - chemical synthesis
/ Molecular Probes - chemistry
/ Molecular Probes - metabolism
/ Molecular Targeted Therapy - methods
/ Neoplasms, Experimental - diagnosis
/ Neoplasms, Experimental - drug therapy
/ Neoplasms, Experimental - metabolism
/ Proteins
/ Structure-Activity Relationship
/ Sugar
