Tibotec BVBA, Beerse, Belgium.
J Acquir Immune Defic Syndr. 2011 Sep 1;58(1):18-22. doi: 10.1097/QAI.0b013e3182237f74.
The contribution of E138 mutations to etravirine resistance was investigated. Amino acids at position E138 after failure with etravirine in DUET were A (n = 1), G (n = 5), K (n = 3), P (n = 1), Q (n = 5), and V (n = 2). At baseline, only E138A and Q were found at 3.0% and 2.5%, respectively. Virologic response (less than 50 copies/mL) was observed in six of 12 and eight of 10 patients with E138A and E138Q, respectively. Site-directed mutants harboring E138A/G/K/Q/R or S showed etravirine fold change values of 2.9, 2.4, 2.6, 3.0, 3.6, and 2.8, respectively. E138G, K, and Q were added to the existing etravirine-weighted genotypic score including 17 etravirine resistance-associated mutations.
研究了 E138 突变对依曲韦林耐药的贡献。在 DUET 中依曲韦林治疗失败后，E138 位的氨基酸为 A（n = 1）、G（n = 5）、K（n = 3）、P（n = 1）、Q（n = 5）和 V（n = 2）。基线时，仅发现 E138A 和 Q 分别为 3.0%和 2.5%。E138A 和 E138Q 分别有 6/12 和 8/10 名患者出现病毒学应答（<50 拷贝/mL）。携带 E138A/G/K/Q/R 或 S 的定点突变体的依曲韦林 fold change 值分别为 2.9、2.4、2.6、3.0、3.6 和 2.8。E138G、K 和 Q 被添加到包括 17 种依曲韦林耐药相关突变的现有依曲韦林加权基因型评分中。
