发明名称 CONJUGATION OF C-MYC ANTISENSE OLIGONUCLEOTIDES WITH CHOLESTEROL TO SIGNIFICANTLY ENHANCE THEIR INHIBITORY EFFECT ON NEOINTIMAL HYPERPLASIA
摘要 <p>Antisense oligonucleotides have recently been proposed as a pharmacological approach to prevent neointimal hyperplasia following balloon angioplasty. This study reports the significant enhancement on in vivo restenosis prevention conferred by the conjugation of cholesterol to a c-myc antisense oligomer when compared to a non conjugated oligonucleotide. The inhibitory potential of the conjugate was increased 2.4-fold, reaching a reduction of intimal hyperplasia of 84.7 % vs. control arteries. Enhancement of hyperplasia prevention may be related to the 2.7-fold increase in oligomer vascular retention conferred by the cholesterol moieties, sufficient to cover a significant portion of the proliferation window that typically follows balloon angioplasty.</p>
申请公布号 WO1997014440(A1) 申请公布日期 1997.04.24
申请号 US1996016796 申请日期 1996.10.18
申请人 发明人
分类号 主分类号
代理机构 代理人
主权项
地址