G Maga, M Amacker, U Hübscher, G Gosselin, J L Imbach, C Mathé, A Faraj, J P Sommadossi, S Spadari
{"title":"HIV-1逆转录酶对(β)- l -脱氧和二脱氧嘧啶核苷三磷酸立体选择性的结构决定因素:l -二脱氧核苷类似物与非核苷抑制剂联合抗HIV化疗的分子基础","authors":"G Maga, M Amacker, U Hübscher, G Gosselin, J L Imbach, C Mathé, A Faraj, J P Sommadossi, S Spadari","doi":"10.1080/15257779908041566","DOIUrl":null,"url":null,"abstract":"<p><p>We have compared the HIV-1 RT mutants containing the single substitutions L100I, K103N, V106A, V179D, Y181I and Y188L, known to confer NNI-resistance in treated patients, to HIV-1 RT wt for their sensitivity towards inhibition by D- and L-deoxy- and dideoxy-nucleoside tiphosphates. The results showed a differential effect of the substitutions on the affinity for both D- and L-enantiomers of deoxy- and dideoxy-nucleoside triphosphates and provide a rationale for the utilization of L-dideoxynucleoside analogs with NNI in combination chemotherapy.</p>","PeriodicalId":19222,"journal":{"name":"Nucleosides & nucleotides","volume":"18 4-5","pages":"795-805"},"PeriodicalIF":0.0000,"publicationDate":"1999-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1080/15257779908041566","citationCount":"3","resultStr":"{\"title\":\"Structural determinants of HIV-1 reverse transcriptase stereoselectivity towards (beta)-L-deoxy- and dideoxy-pyrimidine nucleoside triphosphates: molecular basis for the combination of L-dideoxynucleoside analogs with non-nucleoside inhibitors in anti HIV chemotherapy.\",\"authors\":\"G Maga, M Amacker, U Hübscher, G Gosselin, J L Imbach, C Mathé, A Faraj, J P Sommadossi, S Spadari\",\"doi\":\"10.1080/15257779908041566\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>We have compared the HIV-1 RT mutants containing the single substitutions L100I, K103N, V106A, V179D, Y181I and Y188L, known to confer NNI-resistance in treated patients, to HIV-1 RT wt for their sensitivity towards inhibition by D- and L-deoxy- and dideoxy-nucleoside tiphosphates. The results showed a differential effect of the substitutions on the affinity for both D- and L-enantiomers of deoxy- and dideoxy-nucleoside triphosphates and provide a rationale for the utilization of L-dideoxynucleoside analogs with NNI in combination chemotherapy.</p>\",\"PeriodicalId\":19222,\"journal\":{\"name\":\"Nucleosides & nucleotides\",\"volume\":\"18 4-5\",\"pages\":\"795-805\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1999-04-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1080/15257779908041566\",\"citationCount\":\"3\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Nucleosides & nucleotides\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1080/15257779908041566\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Nucleosides & nucleotides","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1080/15257779908041566","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Structural determinants of HIV-1 reverse transcriptase stereoselectivity towards (beta)-L-deoxy- and dideoxy-pyrimidine nucleoside triphosphates: molecular basis for the combination of L-dideoxynucleoside analogs with non-nucleoside inhibitors in anti HIV chemotherapy.
We have compared the HIV-1 RT mutants containing the single substitutions L100I, K103N, V106A, V179D, Y181I and Y188L, known to confer NNI-resistance in treated patients, to HIV-1 RT wt for their sensitivity towards inhibition by D- and L-deoxy- and dideoxy-nucleoside tiphosphates. The results showed a differential effect of the substitutions on the affinity for both D- and L-enantiomers of deoxy- and dideoxy-nucleoside triphosphates and provide a rationale for the utilization of L-dideoxynucleoside analogs with NNI in combination chemotherapy.
求助内容：
应助结果提醒方式：
京公网安备 11010802042870号
