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GalNAc Conjugated Atorvastatin with Enhanced Water Solubility and Cellular Internalization
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2017-08-07 00:00:00 , DOI: 10.1021/acs.bioconjchem.7b00295 Xinfu Zhang 1 , Xiaofang Chen 1 , Weiyu Zhao 1 , Chunxi Zeng 1 , Xiao Luo 1 , Wenqing Li 1 , Bin Li 1 , Justin Jiang 1 , Yizhou Dong 1
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2017-08-07 00:00:00 , DOI: 10.1021/acs.bioconjchem.7b00295 Xinfu Zhang 1 , Xiaofang Chen 1 , Weiyu Zhao 1 , Chunxi Zeng 1 , Xiao Luo 1 , Wenqing Li 1 , Bin Li 1 , Justin Jiang 1 , Yizhou Dong 1
Affiliation
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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.
中文翻译：
GalNAc共轭阿托伐他汀具有增强的水溶性和细胞内在化作用
靶向配体促进细胞特异性药物递送并改善药物性质。本文中，我们通过将GalNAc（N-乙酰半乳糖胺，一种肝细胞靶向配体）与阿托伐他汀偶联来设计了两种配体药物结合物。这两种缀合物，称为G-AT和GK-AT，表现出增强的水溶性和细胞摄取。此外，G-AT和GK-AT均能够释放阿托伐他汀，因此对3-羟基-3-甲基-戊二酰辅酶A（HMG-CoA）还原酶具有明显的抑制作用。
更新日期：2017-08-07
中文翻译：
GalNAc共轭阿托伐他汀具有增强的水溶性和细胞内在化作用
靶向配体促进细胞特异性药物递送并改善药物性质。本文中，我们通过将GalNAc（N-乙酰半乳糖胺，一种肝细胞靶向配体）与阿托伐他汀偶联来设计了两种配体药物结合物。这两种缀合物，称为G-AT和GK-AT，表现出增强的水溶性和细胞摄取。此外，G-AT和GK-AT均能够释放阿托伐他汀，因此对3-羟基-3-甲基-戊二酰辅酶A（HMG-CoA）还原酶具有明显的抑制作用。
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