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Stepwise solid-phase synthesis of peptide-oligonucleotide conjugates and supports therefor
Stepwise solid-phase synthesis of peptide-oligonucleotide conjugates and supports therefor
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机译:肽-寡核苷酸缀合物及其支持物的逐步固相合成
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摘要
A support for peptide-oligonucleotide conjugate synthesis includes an article of manufacture according to the formula: chemistry chemdraw filechemistry mol file;wherein: (a) substitutent A includes a polymeric base material and/or a silica base material; (b) one of substituents B and C includes an NHFmoc-containing group and/or a peptide-containing group; (c) one of substituents B and C includes an NHBoc-containing group, an O-DMTr-containing group, and/or an oligonucleotide-containing group; and (d) each X independently represents ═O, S, and/or NH. Suitable supports include those according to the formula: chemistry chemdraw filechemistry mol file;wherein substituents A, B, and C have the meanings described above. When used to synthesize a peptide-oligonucleotide conjugate, the resulting conjugate may have the formula: chemistry chemdraw filechemistry mol file;wherein substituent B includes a peptide and substituent C includes an oligonucleotide.
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机译:肽-寡核苷酸缀合物合成的支持物包括根据下式的制品: <图像文件=“ US20040054161A1-20040318-C00001.GIF” he =“ 65.772” id =“ EMI-C00001” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 132.98985“ /> 化学化学绘图文件 ExternalFileRef> 化学mol文件 ExternalFileRef> Chemistry>;其中:(a)取代基A包括聚合物基材料和/或二氧化硅基材料; (b)取代基B和C之一包括含NHFmoc的基团和/或含肽的基团; (c)取代基B和C之一包括含NHBoc的基团,含O-DMTr的基团和/或含寡核苷酸的基团; (d)每个X独立地代表&boxH; O,S和/或NH。合适的支撑物包括根据以下公式的支撑物: <图像文件=“ US20040054161A1-20040318-C00002.GIF” he =“ 65.9988” id =“ EMI-C00002” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 188.1873“ /> 化学化学绘图文件 ExternalFileRef> 化学mol文件 ExternalFileRef> Chemistry>;其中取代基A,B和C具有上述含义。当用于合成肽-寡核苷酸缀合物时,所得的缀合物可以具有下式: <图像文件=“ US20040054161A1-20040318-C00003.GIF” he =“ 100.10385” id =“ EMI-C00003” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 188.66925“ /> 化学化学绘图文件 ExternalFileRef> 化学mol文件 ExternalFileRef> Chemistry>;其中取代基B包括肽,而取代基C包括寡核苷酸。
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