Binding compentent oligomers containing unsaturated 3',5' and 2',5' linkages
AssigneeGilead Sciences, Inc.
InventorsMark D. Matteucci, Xiaodong Cao
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Abstract
Oligonucleotide analogs having one or more substitute linkages of the formula 2'/3'--S--CH.sub.2 --CH.dbd.5' or 2'/3'--O--CH.sub.2 --CH.dbd.5' between adjacent nucleomonomers are disclosed. The substitute linkage replace the usual phosphodiester linkage found in unmodified nucleic acids. The oligonucleotide analogs are easy to synthesize, stable in vivo, resistant to endogenous nucleases and are able to hybridize to target nucleic acid sequences in a sequence specific manner.
Claims9
An oligomer comprising at least one substitute linkage between the 3' and 5' or 2' and 5' position of adjacent nucleomonomers, said substitute linkage having the formula 2'--O--CH.sub.2 --CH.dbd.5' or 3'--O--CH.sub.2 --CH.dbd.5' or 3'--S--CH.sub.2 --CH.dbd.5'.
An oligomer of the formula I or Ia:
- ##STR10## wherein;
- X is S, O, CH.sub.2, CHF or CF.sub.2 ;
- X.sup.1 is O or S;
- R.sup.1 independently is H, OH, an oligomer or a blocking group;
- R.sup.2 independently is --O--alkyl,--S--alkyl, H, OH, OCH.sub.3, SCH.sub.3, OCH.sub.2 CHCH.sub.2, OC.sub.3 H.sub.7, SCH.sub.2 CHCH.sub.2, or a halogen;
- B is independently a base;
- and n is 0-100.
Dependencies are inferred from the claim text.