GlcNAc Conjugated Atorvastatin with Enhanced Water Solubility and Cellular Internalization

Xinfu Zhang; Xiaofang Chen; Weiyu Zhao; Chunxi Zeng; Xiao Luo; Wenqing Li; Bin Li; Justin Jiang; Yizhou Dong

doi:10.1021/acs.bioconjchem.7b00295

GlcNAc Conjugated Atorvastatin with Enhanced Water Solubility and Cellular Internalization

Xinfu Zhang, Xiaofang Chen, Weiyu Zhao, Chunxi Zeng, Xiao Luo, Wenqing Li, Bin Li, Justin Jiang, Yizhou Dong

Research output: Contribution to journal › Article › peer-review

3 Scopus citations

Abstract

Targeting ligands facilitate cell specific drug delivery and improve pharmaceutical properties. Herein, we designed two ligand drug conjugates by conjugating GlcNAc (N-acetylglucosamine) with atorvastatin. These two conjugates, termed G-AT and G-K-AT, exhibited enhanced water solubility and cellular uptake. Moreover, both G-AT and G-K-AT were able to release atorvastatin and consequently achieve significant inhibition against 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase.

Original language	English
Pages (from-to)	2109-2113
Number of pages	5
Journal	Bioconjugate Chemistry
Volume	28
Issue number	8
DOIs	https://doi.org/10.1021/acs.bioconjchem.7b00295
State	Published - 16 Aug 2017
Externally published	Yes

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title = "GlcNAc Conjugated Atorvastatin with Enhanced Water Solubility and Cellular Internalization",

abstract = "Targeting ligands facilitate cell specific drug delivery and improve pharmaceutical properties. Herein, we designed two ligand drug conjugates by conjugating GlcNAc (N-acetylglucosamine) with atorvastatin. These two conjugates, termed G-AT and G-K-AT, exhibited enhanced water solubility and cellular uptake. Moreover, both G-AT and G-K-AT were able to release atorvastatin and consequently achieve significant inhibition against 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase.",

author = "Xinfu Zhang and Xiaofang Chen and Weiyu Zhao and Chunxi Zeng and Xiao Luo and Wenqing Li and Bin Li and Justin Jiang and Yizhou Dong",

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doi = "10.1021/acs.bioconjchem.7b00295",

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T1 - GlcNAc Conjugated Atorvastatin with Enhanced Water Solubility and Cellular Internalization

AU - Zhang, Xinfu

AU - Chen, Xiaofang

AU - Zhao, Weiyu

AU - Zeng, Chunxi

AU - Luo, Xiao

AU - Li, Wenqing

AU - Li, Bin

AU - Jiang, Justin

AU - Dong, Yizhou

PY - 2017/8/16

Y1 - 2017/8/16

N2 - Targeting ligands facilitate cell specific drug delivery and improve pharmaceutical properties. Herein, we designed two ligand drug conjugates by conjugating GlcNAc (N-acetylglucosamine) with atorvastatin. These two conjugates, termed G-AT and G-K-AT, exhibited enhanced water solubility and cellular uptake. Moreover, both G-AT and G-K-AT were able to release atorvastatin and consequently achieve significant inhibition against 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase.

AB - Targeting ligands facilitate cell specific drug delivery and improve pharmaceutical properties. Herein, we designed two ligand drug conjugates by conjugating GlcNAc (N-acetylglucosamine) with atorvastatin. These two conjugates, termed G-AT and G-K-AT, exhibited enhanced water solubility and cellular uptake. Moreover, both G-AT and G-K-AT were able to release atorvastatin and consequently achieve significant inhibition against 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase.

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EP - 2113

JO - Bioconjugate Chemistry

JF - Bioconjugate Chemistry

IS - 8

ER -

GlcNAc Conjugated Atorvastatin with Enhanced Water Solubility and Cellular Internalization

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