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14
糖基修飾的核苷酸（糖基修飾 DNA/RNA）
核苷類藥物由于具有良好的抗病毒和抗腫瘤作用而在臨床上被廣泛應(yīng)用,近年來(lái)隨著合成方法和藥學(xué)研究手段的進(jìn)步,大量新型核苷化合物被制備并用于抗病毒和抗腫瘤的研究,如替比夫定（bivudine,L-dt）在2006年被FDA批準(zhǔn)用于乙型肝炎的治療。但對(duì)一些致病率高的病毒感染如乙型肝炎,和惡性腫瘤現(xiàn)有藥物尚不能*解決問(wèn)題,而且臨床治療中耐藥性問(wèn)題日益突出,嚴(yán)重地阻礙了此類藥物的發(fā)展。因此尋找高效低毒的抗病毒和抗腫瘤核苷藥物一直是人們研究的熱點(diǎn)。 核苷類化合物的抗病毒和抗腫瘤作用機(jī)制大都是由于具有與天然核苷類似的結(jié)構(gòu),摻入病毒或腫瘤細(xì)胞的DNA鏈中,干擾其DNA和蛋白質(zhì)的生物合成而起到抗病毒和抗腫瘤作用的。 核苷類化合物的修飾改造部位包括糖基和堿基部分,其中大部分為糖基修飾改造的產(chǎn)物。糖基改造修飾的類型包括無(wú)環(huán)核苷,脫氧核苷,雜原子引入,構(gòu)型變化,糖環(huán)大小的變化等。
TriLink公司的糖基修飾的核苷列表：
| N-1015-1 | 2'-O-Methyladenosine-5'-TP | 1umole | 467.5 |
| N-1015-10 | 2'-O-Methyladenosine-5'-TP | 10umoles | 3485 |
| N-1015-5 | 2'-O-Methyladenosine-5'-TP | 5umoles | 1955 |
| N-1016-1 | 2'-O-Methylcytidine-5'-TP | 1umole | 467.5 |
| N-1016-10 | 2'-O-Methylcytidine-5'-TP | 10umoles | 3485 |
| N-1016-5 | 2'-O-Methylcytidine-5'-TP | 5umoles | 1955 |
| N-1017-1 | 2'-O-Methylguanosine-5'-TP | 1umole | 467.5 |
| N-1017-10 | 2'-O-Methylguanosine-5'-TP | 10umoles | 3485 |
| N-1017-5 | 2'-O-Methylguanosine-5'-TP | 5umoles | 1955 |
| N-1018-1 | 2'-O-Methyluridine-5'-TP | 1umole | 467.5 |
| N-1018-10 | 2'-O-Methyluridine-5'-TP | 10umoles | 3485 |
| N-1018-5 | 2'-O-Methyluridine-5'-TP | 5umoles | 1955 |
| N-1021-1 | 2'-O-Methylinosine-5'-Triphosphate | 1umole | 1317.5 |
| N-1021-10 | 2'-O-Methylinosine-5'-Triphosphate | 10umoles | 10625 |
| N-1021-5 | 2'-O-Methylinosine-5'-Triphosphate | 5umoles | 6205 |
| N-1026-1 | 2'-Amino-2'-deoxycytidine-5'-TP | 1umole | 1317.5 |
| N-1026-10 | 2'-Amino-2'-deoxycytidine-5'-TP | 10umoles | 10625 |
| N-1026-5 | 2'-Amino-2'-deoxycytidine-5'-TP | 5umoles | 6205 |
| N-1027-1 | 2'-Amino-2'-deoxyuridine-5'-TP | 1umole | 1317.5 |
| N-1027-10 | 2'-Amino-2'-deoxyuridine-5'-TP | 10umoles | 10625 |
| N-1027-5 | 2'-Amino-2'-deoxyuridine-5'-TP | 5umoles | 6205 |
| N-1028-1 | 2'-Azido-2'-deoxycytidine-5'-TP | 1umole | 1317.5 |
| N-1028-10 | 2'-Azido-2'-deoxycytidine-5'-TP | 10umoles | 10625 |
| N-1028-5 | 2'-Azido-2'-deoxycytidine-5'-TP | 5umoles | 6205 |
| N-1029-1 | 2'-Azido-2'-deoxyuridine-5'-TP | 1umole | 1317.5 |
| N-1029-10 | 2'-Azido-2'-deoxyuridine-5'-TP | 10umoles | 10625 |
| N-1029-5 | 2'-Azido-2'-deoxyuridine-5'-TP | 5umoles | 6205 |
| N-1033-1 | Aracytidine-5'-Triphosphate | 1umole | 892.5 |
| N-1033-10 | Aracytidine-5'-Triphosphate | 10umoles | 7055 |
| N-1033-5 | Aracytidine-5'-Triphosphate | 5umoles | 4335 |
| N-1034-1 | Arauridine-5'-Triphosphate | 1umole | 1657.5 |
| N-1034-10 | Arauridine-5'-Triphosphate | 10umoles | 14450 |
| N-1034-5 | Arauridine-5'-Triphosphate | 5umoles | 7905 |
| N-1040-1 | 2'-O-Methyl-2-aminoadenosine-5'-TP | 1umole | 1317.5 |
| N-1040-10 | 2'-O-Methyl-2-aminoadenosine-5'-TP | 10umoles | 10625 |
| N-1040-5 | 2'-O-Methyl-2-aminoadenosine-5'-TP | 5umoles | 6205 |
| N-1041-1 | 2'-O-Methylpseudouridine-5'-TP | 1umole | 892.5 |
| N-1041-10 | 2'-O-Methylpseudouridine-5'-TP | 10umoles | 7055 |
| N-1041-5 | 2'-O-Methylpseudouridine-5'-TP | 5umoles | 4335 |
| N-1043-1 | 2'-O-Methyl-5-methyluridine-5'-TP | 1umole | 892.5 |
| N-1043-10 | 2'-O-Methyl-5-methyluridine-5'-TP | 10umoles | 7055 |
| N-1043-5 | 2'-O-Methyl-5-methyluridine-5'-TP | 5umoles | 4335 |
| N-1045-1 | 2'-Azido-2'-deoxyadenosine-5'-TP | 1umole | 1317.5 |
| N-1045-10 | 2'-Azido-2'-deoxyadenosine-5'-TP | 10umoles | 10625 |
| N-1045-5 | 2'-Azido-2'-deoxyadenosine-5'-TP | 5umoles | 6205 |
| N-1046-1 | 2'-Amino-2'-deoxyadenosine-5'-TP | 1umole | 892.5 |
| N-1046-10 | 2'-Amino-2'-deoxyadenosine-5'-TP | 10umoles | 7055 |
| N-1046-5 | 2'-Amino-2'-deoxyadenosine-5'-TP | 5umoles | 4335 |
| N-1048-1 | Araadenosine-5'-TP | 1umole | 1317.5 |
| N-1048-10 | Araadenosine-5'-TP | 10umoles | 10625 |
| N-1048-5 | Araadenosine-5'-TP | 5umoles | 6205 |
| N-1056-1 | 3'-O-Methyladenosine-5'-TP | 1umole | 1317.5 |
| N-1056-10 | 3'-O-Methyladenosine-5'-TP | 10umoles | 10625 |
| N-1056-5 | 3'-O-Methyladenosine-5'-TP | 5umoles | 6205 |
| N-1057-1 | 3'-O-Methylcytidine-5'-TP | 1umole | 1317.5 |
| N-1057-10 | 3'-O-Methylcytidine-5'-TP | 10umoles | 10625 |
| N-1057-5 | 3'-O-Methylcytidine-5'-TP | 5umoles | 6205 |
| N-1058-1 | 3'-O-Methylguanosine-5'-TP | 1umole | 1317.5 |
| N-1058-10 | 3'-O-Methylguanosine-5'-TP | 10umoles | 10625 |
| N-1058-5 | 3'-O-Methylguanosine-5'-TP | 5umoles | 6205 |
| N-1059-1 | 3'-O-Methyluridine-5'-TP | 1umole | 1317.5 |
| N-1059-10 | 3'-O-Methyluridine-5'-TP | 10umoles | 10625 |
| N-1059-5 | 3'-O-Methyluridine-5'-TP | 5umoles | 6205 |
| N-1063-1 | 2'-Azido-2'-deoxyguanosine-5'-TP | 1umole | 1317.5 |
| N-1063-10 | 2'-Azido-2'-deoxyguanosine-5'-TP | 10umoles | 10625 |
| N-1063-5 | 2'-Azido-2'-deoxyguanosine-5'-TP | 5umoles | 6205 |
| N-2053-1 | 2'-Deoxy-L-adenosine-5'-TP | 1umoles | |
| N-2053-10 | 2'-Deoxy-L-adenosine-5'-TP | 10umoles | 14450 |
| N-2053-5 | 2'-Deoxy-L-adenosine-5'-TP | 5umoles | 7905 |
| N-2054-1 | 2'-Deoxy-L-cytidine-5'-TP | 1umole | 1657.5 |
| N-2054-10 | 2'-Deoxy-L-cytidine-5'-TP | 10umoles | 14450 |
| N-2054-5 | 2'-Deoxy-L-cytidine-5'-TP | 5umoles | 7905 |
| N-2055-1 | 2'-Deoxy-L-guanosine-5'-TP | 1umole | 2975 |
| N-2055-10 | 2'-Deoxy-L-guanosine-5'-TP | 10umoles | 24650 |
| N-2055-5 | 2'-Deoxy-L-guanosine-5'-TP | 5umoles | 13175 |
| N-2056-1 | 2'-Deoxy-L-thymidine-5'-TP | 1umole | 1657.5 |
| N-2056-10 | 2'-Deoxy-L-thymidine-5'-TP | 10umoles | 14450 |
| N-2056-5 | 2'-Deoxy-L-thymidine-5'-TP | 5umoles | 7905 |
| N-3001-1 | 3'-Deoxyadenosine-5'-Triphosphate | 1umole | 1317.5 |
| N-3001-10 | 3'-Deoxyadenosine-5'-Triphosphate | 10umoles | 10625 |
| N-3001-5 | 3'-Deoxyadenosine-5'-Triphosphate | 5umoles | 6205 |
| N-3002-1 | 3'-Deoxyguanosine-5'-Triphosphate | 1umole | 1317.5 |
| N-3002-10 | 3'-Deoxyguanosine-5'-Triphosphate | 10umoles | 10625 |
| N-3002-5 | 3'-Deoxyguanosine-5'-Triphosphate | 5umoles | 6205 |
| N-3003-1 | 3'-Deoxycytidine-5'-Triphosphate | 1umole | 1317.5 |
| N-3003-10 | 3'-Deoxycytidine-5'-Triphosphate | 10umoles | 10625 |
| N-3003-5 | 3'-Deoxycytidine-5'-Triphosphate | 5umoles | 6205 |
| N-3004-1 | 3'-Deoxy-5-Methyluridine-5'-TP | 1umole | 1317.5 |
| N-3004-10 | 3'-Deoxy-5-Methyluridine-5'-TP | 10umoles | 10625 |
| N-3004-5 | 3'-Deoxy-5-Methyluridine-5'-TP | 5umoles | 6205 |
| N-3005-1 | 3'-Deoxyuridine-5'-Triphosphate | 1umole | 1317.5 |
| N-3005-10 | 3'-Deoxyuridine-5'-Triphosphate | 10umoles | 10625 |
| N-3005-5 | 3'-Deoxyuridine-5'-Triphosphate | 5umoles | 6205 |
| N-4001-1 | 2',3'-Dideoxyadenosine-5'-TP | 1umole | 467.5 |
| N-4001-10 | 2',3'-Dideoxyadenosine-5'-TP | 10umoles | 3485 |
| N-4001-5 | 2',3'-Dideoxyadenosine-5'-TP | 5umoles | 1955 |
| N-4002-1 | 2',3'-Dideoxyguanosine-5'-TP | 1umole | 467.5 |
| N-4002-10 | 2',3'-Dideoxyguanosine-5'-TP | 10umoles | 3485 |
| N-4002-5 | 2',3'-Dideoxyguanosine-5'-TP | 5umoles | 1955 |
| N-4003-1 | 2',3'-Dideoxyuridine-5'-Triphosphate | 1umole | 467.5 |
| N-4003-10 | 2',3'-Dideoxyuridine-5'-Triphosphate | 10umoles | 3485 |
| N-4003-5 | 2',3'-Dideoxyuridine-5'-Triphosphate | 5umoles | 1955 |
| N-4004-1 | 2',3'-Dideoxythymidine-5'-Triphosphate | 1umole | 467.5 |
| N-4004-10 | 2',3'-Dideoxythymidine-5'-Triphosphate | 10umoles | 3485 |
| N-4004-5 | 2',3'-Dideoxythymidine-5'-Triphosphate | 5umoles | 1955 |
| N-4005-1 | 2',3'-Dideoxycytidine-5'-Triphosphate | 1umole | 467.5 |
| N-4005-10 | 2',3'-Dideoxycytidine-5'-Triphosphate | 10umoles | 3485 |
| N-4005-5 | 2',3'-Dideoxycytidine-5'-Triphosphate | 5umoles | 1955 |
| N-4007-1 | 3'-Azido-2',3'-dideoxyadenosine-5'-TP | 1umole | 1657.5 |
| N-4007-10 | 3'-Azido-2',3'-dideoxyadenosine-5'-TP | 10umoles | 14450 |
| N-4007-5 | 3'-Azido-2',3'-dideoxyadenosine-5'-TP | 5umoles | 7905 |
| N-4008-1 | 3'-Azido-2',3'-dideoxyguanosine-5'-TP | 1umole | 1657.5 |
| N-4008-10 | 3'-Azido-2',3'-dideoxyguanosine-5'-TP | 10umoles | 14450 |
| N-4008-5 | 3'-Azido-2',3'-dideoxyguanosine-5'-TP | 5umoles | 7905 |
| N-4009-1 | 3'-Azido-2',3'-dideoxythymidine-5'-TP | 1umole | 1657.5 |
| N-4009-10 | 3'-Azido-2',3'-dideoxythymidine-5'-TP | 10umoles | 14450 |
| N-4009-5 | 3'-Azido-2',3'-dideoxythymidine-5'-TP | 5umoles | 7905 |
| N-4010-1 | 3'-Amino-2',3'-dideoxyadenosine-5'-TP | 1umole | 2975 |
| N-4010-10 | 3'-Amino-2',3'-dideoxyadenosine-5'-TP | 10umoles | 24650 |
| N-4010-5 | 3'-Amino-2',3'-dideoxyadenosine-5'-TP | 5umoles | 13175 |
| N-4011-1 | 3'-Amino-2',3'-dideoxycytidine-5'-TP | 1umole | 2975 |
| N-4011-10 | 3'-Amino-2',3'-dideoxycytidine-5'-TP | 10umoles | 24650 |
| N-4011-5 | 3'-Amino-2',3'-dideoxycytidine-5'-TP | 5umoles | 13175 |
| N-4012-1 | 3'-Amino-2',3'-dideoxyguanosine-5'-TP | 1umole | 2975 |
| N-4012-10 | 3'-Amino-2',3'-dideoxyguanosine-5'-TP | 10umoles | 24650 |
| N-4012-5 | 3'-Amino-2',3'-dideoxyguanosine-5'-TP | 5umoles | 13175 |
| N-4013-1 | 3'-Amino-2',3'-dideoxythymidine-5'-TP | 1umole | 1657.5 |
| N-4013-10 | 3'-Amino-2',3'-dideoxythymidine-5'-TP | 10umoles | 14450 |
| N-4013-5 | 3'-Amino-2',3'-dideoxythymidine-5'-TP | 5umoles | 7905 |
| N-4014-1 | 3'-Azido-2',3'-dideoxycytidine-5'-TP | 1umole | 1657.5 |
| N-4014-10 | 3'-Azido-2',3'-dideoxycytidine-5'-TP | 10umoles | 14450 |
| N-4014-5 | 3'-Azido-2',3'-dideoxycytidine-5'-TP | 5umoles | 7905 |
| N-4015-1 | 3'-Azido-2',3'-dideoxyuridine-5'-TP | 1umole | 1657.5 |
| N-4015-10 | 3'-Azido-2',3'-dideoxyuridine-5'-TP | 10umoles | 14450 |
| N-4015-5 | 3'-Azido-2',3'-dideoxyuridine-5'-TP | 5umoles | 7905 |
| N-4016-1 | 5-Bromo-2',3'-dideoxyuridine-5'-TP | 1umole | 1657.5 |
| N-4016-10 | 5-Bromo-2',3'-dideoxyuridine-5'-TP | 10umoles | 14450 |
| N-4016-5 | 5-Bromo-2',3'-dideoxyuridine-5'-TP | 5umoles | 7905 |
| N-4017-10 | 2',3'-Dideoxyinosine-5'-TP | 10umoles | 20995 |
| N-4017-5 | 2',3'-Dideoxyinosine-5'-TP | 5umoles | 11815 |
| N-9001-1 | Ganciclovir-5'-Triphosphate | 1umole | 1317.5 |
| N-9001-10 | Ganciclovir-5'-Triphosphate | 10umoles | 10625 |
