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CONJUGATION OF C-MYC ANTISENSE OLIGONUCLEOTIDES WITH CHOLESTEROL TO SIGNIFICANTLY ENHANCE THEIR INHIBITORY EFFECT ON NEOINTIMAL HYPERPLASIA
CONJUGATION OF C-MYC ANTISENSE OLIGONUCLEOTIDES WITH CHOLESTEROL TO SIGNIFICANTLY ENHANCE THEIR INHIBITORY EFFECT ON NEOINTIMAL HYPERPLASIA
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机译:C-MYC反义寡核苷酸与胆固醇的结合可显着增强其对新内膜增生的抑制作用
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摘要
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.
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