Division of Molecular Oncology, Department of Molecular Microbiology, Washington University School of Medicine, Box 8069, 660 S. Euclid Ave., St. Louis, MO 63110, USA.
Antimicrob Agents Chemother. 2011 May;55(5):2011-7. doi: 10.1128/AAC.01413-10. Epub 2011 Feb 22.
Drugs targeting the viral enzyme integrase have been in use for several years as part of the treatment regimen for patients with human immunodeficiency virus type 1 (HIV-1), and similar classes of compounds have been shown to inhibit human T-cell leukemia virus type 1 (HTLV-1) integration in vitro. The current study shows that the clinically approved HIV-1 integrase inhibitor, raltegravir, as well as the more recent diketo acid derivative, MK-2048, are active inhibitors of HTLV-1 infection in vitro. These agents were effective in inhibiting cell-free and cell-to-cell transmission of HTLV-1 in lymphoid and nonlymphoid cells. The drugs also inhibited HTLV-1 immortalization of human peripheral blood mononuclear cells. A novel adaptation of the Alu assay for viral integration was used to show that the drugs inhibit viral integration without affecting reverse transcription. These data support the administration of raltegravir and other integrase inhibitors as treatments for patients with HTLV-1-associated diseases.
靶向病毒酶整合酶的药物已被用于治疗人类免疫缺陷病毒 1 型(HIV-1)患者的治疗方案中数年,并且已证明类似的化合物类可抑制人 T 细胞白血病病毒 1 型(HTLV-1)的体外整合。本研究表明,临床上已批准的 HIV-1 整合酶抑制剂拉替拉韦以及最近的二酮酸衍生物 MK-2048,都是体外 HTLV-1 感染的有效抑制剂。这些药物可有效抑制淋巴样和非淋巴样细胞中游离细胞和细胞间的 HTLV-1 传播。这些药物还抑制了 HTLV-1 对人外周血单个核细胞的永生化作用。一种新的 Alu 测定法用于病毒整合的适应性分析表明,这些药物抑制病毒整合而不影响逆转录。这些数据支持使用拉替拉韦和其他整合酶抑制剂作为治疗 HTLV-1 相关疾病患者的治疗方法。