Literature DB >> 28745862

GlcNAc Conjugated Atorvastatin with Enhanced Water Solubility and Cellular Internalization.

Xinfu Zhang1, Xiaofang Chen1, Weiyu Zhao1, Chunxi Zeng1, Xiao Luo1, Wenqing Li1, Bin Li1, Justin Jiang1, Yizhou Dong1.   

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.

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Year:  2017        PMID： 28745862      PMCID： PMC5896756          DOI： 10.1021/acs.bioconjchem.7b00295

Source DB:  PubMed          Journal:  Bioconjug Chem        ISSN： 1043-1802            Impact factor:   4.774


  24 in total

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