FIELD: organic chemistry, biochemistry, nucleic acids.
SUBSTANCE: invention elates to LNA-modified oligonucleotide comprising at least one nucleoside analogue (LNA) of the general formula (I)
wherein X means -O-; B means a nitrogen (nucleotide) base; P is a point for joining inter-nucleoside "bridge" or 5'-terminal group that is taken among hydroxyl, monophosphate, diphosphate and triphosphate; R3 or R3* is inter-nucleoside "bridge" by 3'-terminal group; R2* and R4* means biradical taken among -(CR*R*)r-O-(CR*R*)s-, -(CR*R*)r-S-(CR*R*)s-, -(CR*R*)r-N(R*)-(CR*R*)s-. Each among R1*, R2, R3*, R3, R5* and R5 not taking part in formation of biradical or inter-nucleoside "bridge" means hydrogen, halogen atom, hydroxy-, mercapto-, amino-, azido-group; or R2 and R3 mean biradical -(CR*R*)r-O-(CR*R*)s- wherein R2* is taken among hydrogen atom, hydroxy-group and optionally substituted (C1-C6)-alkoxy-group; R1*, R4*, R5 and R5* mean hydrogen atom wherein each among r and s = 0-4 under condition that sum r + s = 1-4 and each R* represents hydrogen atom or (C1-C6)-alkyl; or its basic salt or acid-additive salt. Also, invention proposes the corresponding nucleoside analogue (LNA) and the solid backing material with immobilized LNA. LNA-modified oligonucleotides elicit the enhanced affinity and specificity level with respect to complementary DNA and RNA-oligomers.
EFFECT: valuable properties of analogues.
62 cl, 44 dwg, 14 tbl, 161 ex
