abstract |
The present invention relates to an LNA oligonucleotide consisting of a sequence selected from the group consisting of beta-D-hydroxy-LNA nucleotide analogue indicated in capital letters, 2-deoxynucleotide is indicated in lowercase letters, beta-D-hydroxy-LNA nucleotide analogue is underlined, or 2-deoxynucleotide, subscript āsā denotes a phosphorothioate bond between adjacent nucleotides / LNA nucleotide analogs and subscript āxā denotes either a phosphorothioate bond or a phosphodiester linkage between a neighbor of nucleotides / LNA nucleotide analogues, and where the sequence optionally increased by adding up to five 2-deoxynucleotide units. LNA oligonucleotides are useful for modulating the expression of hypoxia-induced factor - 1a (HIF-1a), for example, in the treatment of cancer, inhibiting angiogenesis, inducing apoptosis, preventing cell proliferation or treating angiogenic disease, for example, diabetic retinopathy, macular degeneration (ARMD), psoriasis, rheumatoid arthritis and other inflammatory diseases. |