Peptide conjugated, inosine-substituted antisense oligomer compound and method
US8877725B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Sep 23, 2011 |
| Grant date | Nov 4, 2014 |
| Priority date | — |
| Expiry date | Feb 1, 2032 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC12N2320/32
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A therapeutic oligomer-peptide conjugate, and methods of using the conjugate are disclosed. The 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) conjugated to the compound, an arginine-rich peptide 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 said 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 activity than the conjugate in the absence of inosine-for guanine substitutions.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.