IVERSEN, PATRICK L.,MOULTON, HONG M.,NELSON, MICHELLE H.,KROEKER, ANDREW D.,STEIN, DAVID A.
申请号：
ES10174646
公开号：
ES2500921T3
申请日:
2004.04.29
申请国别(地区):
ES
年份:
2014
代理人:
摘要：
A peptide-nucleic acid analog comprising a peptide covalently linked to a nucleic acid analogue, nucleic acid analog comprising a main chain substantially uncharged and a base sequence of addressing, and peptide consisting of eight sixteen subunits and comprising at least six subunits X, at least two subunits Y and up to three optional subunits Z, where> 50% of the subunits are subunits X, wherein (a) each subunit X is independently arginine or an analogue arginine, arginine analogue being one α-amino acid comprising a cationic side chain structure R1N> = C (NH2) R2, where R1 is H or R R2 is R, NH2, NHR or NR2 where R is lower alkyl or lower alkenyl and optionally comprising oxygen or nitrogen, or R1 and R2 may together form a ring and wherein the side chain is attached to the amino acid through R1 or R2 (B) the at least two subunits and comprise two subunits of α-amino neutral hydrophobic comprising a substituted aralkyl side alkyl chain, alkenyl, alkynyl, aryl or or unsubstituted, wherein the side chain alkyl, alkenyl or alkynyl includes at most one heteroatom per six carbon atoms, and wherein the subunits and are contiguous or are flanking a connector component and (c) each Z independently represents a subunit subunit amino acid selected from alanine, asparagine, cysteine, glutamine, glycine, histidine, lysine, methionine, serine and threonine wherein the peptide is optionally bound to the nucleic acid analog through a linker selected from among: (i) a subunit of cysteine (Ii) a connector component not uncharged amino acid (Iii) an α-amino acid neutral hydrophobic comprising a substituted aralkyl side alkyl chain, alkenyl, alkynyl, aryl or or unsubstituted, wherein the side chain alkyl, alkenyl or alkynyl includes at most one heteroatom for every two atoms carbon and (iv) a neutral hydrophobic amino acid having the following structure: -C (O) - (CH2) n-1 (CHR) -NHen where n is from 2 to 7 and R is H or methyl.Un conjugado de péptido-análogo de ácido nucleico, que
