IVERSEN, PATRICK L.,WELLER, DWIGHT D.,HASSINGER, JED N.
申请号：
CA2565103
公开号：
CA2565103C
申请日:
2005.05.24
申请国别(地区):
CA
年份:
2014
代理人:
摘要：
A therapeutic oligomer-peptide conjugate, and methods of using the conjugateare disclosed. The conjugate includes (a) a substantially unchargedoligonucleotide analog compound having a base sequence that includes a stringof bases that are complementary to four or more contiguous cytosine bases in atarget nucleic acid region to which the compound is intended to bind, and (b)conjugated to the compound, an arginine-rich peptide effective to enhance theuptake of the compound into target cells. The string of bases in the compoundincludes at least one inosine base positioned in the string so as to limit thenumber of contiguous guanine bases in said string to three or fewer. Theconjugate has greater cellular uptake than the compound alone, by virtue ofthe arginine-rich peptide, and substantially greater antisense activitygreater activity than the conjugate in the absence of inosine-for guaninesubstitutions.
