@article{APS3892,
author = {Jie Fu and Zhong-ming Tang and Xin Gao and Fan Zhao and Hui Zhong and Mao-rong Wen and Xiao Sun and Hai-feng Song and Xiao-hong Qian},
title = {Optimal design and validation of antiviral siRNA for targeting hepatitis B virus},
journal = {Acta Pharmacologica Sinica},
volume = {29},
number = {12},
year = {2016},
keywords = {},
abstract = {Aim: Optimal design of antiviral short-interfering RNA (siRNA) targeting highly divergent hepatitis B virus (HBV) was validated by quantitative structure-activity relationship (QSAR) analysis.
Methods: The potency of 23 synthetic siRNAs targeting 23 sites throughout HBV pregenomic RNA were evaluated at 10 nmol/L by determining the inhibition on the expression of S/P/pregenomic mRNA and hepatitis B surface antigen (HBsAg) quantitatively in HepG2.2.15 cells. Genotype homology within HBV genomes was identified through plentiful computational analysis and the multiple linear regression analysis was made to validate the relationship between the functional siRNAs and primary characteristics. Based on the preliminary results, relationships between different determined endpoints [S/P mRNA, HBsAg, C/P mRNA, hepatitis B e antigen (HBeAg) and viral DNA load] and siRNA efficacy evaluation were investigated.
Results: Genotype homology, open reading frame (ORF) S/P, X and C had tight correlation with the ability of siRNAs on inhibiting the expression of S/P/Pregenomic mRNA and HBsAg (P},
issn = {1745-7254}, url = {http://www.chinaphar.com/article/view/3892}
}