Zhang Xinfu, Chen Xiaofang, Zhao Weiyu, Zeng Chunxi, Luo Xiao, Li Wenqing, Li Bin, Jiang Justin, Dong Yizhou
Division of Pharmaceutics & Pharmaceutical Chemistry, College of Pharmacy, ‡Department of Biomedical Engineering, §The Center for Clinical and Translational Science, ∥The Comprehensive Cancer Center, ⊥Dorothy M. Davis Heart & Lung Research Institute, and ¶Department of Radiation Oncology, The Ohio State University , Columbus, Ohio 43210, United States.
Bioconjug Chem. 2017 Aug 16;28(8):2109-2113. doi: 10.1021/acs.bioconjchem.7b00295. Epub 2017 Aug 7.
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.
靶向配体有助于细胞特异性药物递送并改善药物性质。在此，我们通过将N-乙酰葡糖胺（GlcNAc）与阿托伐他汀偶联设计了两种配体-药物偶联物。这两种偶联物，称为G-AT和G-K-AT，表现出增强的水溶性和细胞摄取。此外，G-AT和G-K-AT均能够释放阿托伐他汀，从而对3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶产生显著抑制作用。
