METHODS AND COMPOSITIONS FOR ENHANCING DELIVERY OF DOUBLE-STRANDED RNA OR A DOUBLE-STRANDED HYBRID NUCLEIC ACID TO REGULATE GENE EXPRESSION IN MAMMALIAN CELLS
AHMADIAN, MOHAMMAD,CUI, KUNYUAN,CHEN, LISHAN,QUAY, SHU-CHIH CHEN,HOUSTON, MICHAEL E., JR.
申请号：
CA2564616
公开号：
CA2564616C
申请日:
2005.04.15
申请国别(地区):
CA
年份:
2016
代理人:
摘要：
Cholesterol moieties are linked to specific ends of double-stranded RNA,preferably a small, interfering (si)RNA or to a dsHybrid. The dsHybrid has onestrand comprised of DNA and one strand comprised of RNA. Preferably the sensestrand is the DNA strand and the antisense strand is the RNA strand of thedsHybrid. The present invention is based upon the discovery that a cholesterolmoiety, if linked to a specific end or ends of the sense or antisense strandsof a siRNA, can enhance the delivery and silencing efficiency of the siRNAdirected against its target message, in comparison with a corresponding, non-conjugated siRNA. Conjugated siRNAs and dsHybrids of the invention areoptionally formulated with, or coordinately administered with, a secondarydelivery-enhancing agent, such as a delivery-enhancing peptide, to enhanceintracellular delivery and uptake of the conjugated siRNAs or dsHybrid.
