Department of Virology, Bristol-Myers Squibb Research and Development, Wallingford, Connecticut, USA.
Antimicrob Agents Chemother. 2012 Mar;56(3):1588-90. doi: 10.1128/AAC.06169-11. Epub 2011 Dec 27.
The antiviral profile of BMS-790052, a potent hepatitis C virus (HCV) replication complex inhibitor targeting nonstructural protein NS5A, is well characterized for HCV genotype-1. Here, we report that BMS-790052 inhibits hybrid replicons containing HCV genotype-4 NS5A genes with 50% effective concentrations (EC(50)s) ranging from 7 to 13 pM. NS5A residue 30 was an important site for BMS-790052-selected resistance in the hybrid replicons. Our results support the potential of BMS-790052 as a valuable component of combination therapy for HCV genotype-4 chronic infection.
BMS-790052 是一种针对非结构蛋白 NS5A 的强效丙型肝炎病毒 (HCV) 复制复合物抑制剂，其对 HCV 基因型-1 的抗病毒特性已得到充分描述。在这里，我们报告 BMS-790052 可抑制含有 HCV 基因型-4 NS5A 基因的杂交复制子，其 50%有效浓度 (EC(50)s) 范围为 7 至 13 pM。NS5A 残基 30 是 BMS-790052 在杂交复制子中选择耐药性的重要位点。我们的结果支持 BMS-790052 作为 HCV 基因型-4 慢性感染联合治疗有价值的组成部分的潜力。
