MicroRNA compounds and methods for modulating miR-21 activity

摘要

Described herein are compositions and methods for the inhibition of miR-21 activity. The compositions have certain nucleoside modification patterns that yield potent inhibitors of miR-21 activity. The compositions may be used to inhibit miR-21, and also to treat diseases associated with abnormal expression of miR-21, such as fibrosis and cancer.

主权项

1. A compound comprising a modified oligonucleotide consisting of 12, 13, 14, or 15 linked nucleosides, wherein the nucleobase sequence of the modified oligonucleotide is complementary to miR-21 (SEQ ID NO: 1) and wherein the modified oligonucleotide comprises at least 12 contiguous nucleosides of the following nucleoside pattern VI in the 5′ to 3′ orientation:
NQ—NB—NB—NQ—(NB—NB—NQ—NQ)2—NB—NQ—NB wherein each NQ is a non-bicyclic nucleoside; and each NB is a bicyclic nucleoside.