5 years ago

GalNAc Conjugated Atorvastatin with Enhanced Water Solubility and Cellular Internalization

GalNAc Conjugated Atorvastatin with Enhanced Water Solubility and Cellular Internalization
Xiaofang Chen, Yizhou Dong, Bin Li, Chunxi Zeng, Weiyu Zhao, Xiao Luo, Wenqing Li, Xinfu Zhang, Justin Jiang
Targeting ligands facilitate cell specific drug delivery and improve pharmaceutical properties. Herein, we designed two ligand drug conjugates by conjugating GalNAc (N-Acetylgalactosamine, a hepatocyte-targeting ligand) 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.

Publisher URL: http://dx.doi.org/10.1021/acs.bioconjchem.7b00295

DOI: 10.1021/acs.bioconjchem.7b00295

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