| 摘要 |
<P>PROBLEM TO BE SOLVED: To provide a therapeutic oligomer-peptide conjugate, and methods of using the conjugate. <P>SOLUTION: The therapeutic oligomer-peptide conjugate includes (a) a substantially uncharged oligonucleotide analog compound having a base sequence that includes a string of bases that are complementary to four or more contiguous cytosine bases in a target nucleic acid region to which the compound is intended to bind, and (b) an arginine-rich peptide, conjugated to the compound, effective to enhance the uptake of the compound into target cells. The string of bases in the compound includes at least one inosine base positioned in the string so as to limit the number of contiguous guanine bases in the string to three or fewer. The conjugate has greater cellular uptake than the compound alone, by virtue of the arginine-rich peptide, and substantially greater antisense activity greater than that of the conjugate in the absence of inosine-for guanine substitutions. <P>COPYRIGHT: (C)2011,JPO&INPIT |
