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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.

SUBMITTER: Zhang X 

PROVIDER: S-EPMC5896756 | biostudies-literature | 2017 Aug

REPOSITORIES: biostudies-literature

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GlcNAc Conjugated Atorvastatin with Enhanced Water Solubility and Cellular Internalization.

Zhang Xinfu X   Chen Xiaofang X   Zhao Weiyu W   Zeng Chunxi C   Luo Xiao X   Li Wenqing W   Li Bin B   Jiang Justin J   Dong Yizhou Y  

Bioconjugate chemistry 20170807 8


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. ...[more]

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