Li C J, Zhang L J, Dezube B J, Crumpacker C S, Pardee A B
Dana-Farber Cancer Institute, Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115.
Proc Natl Acad Sci U S A. 1993 Mar 1;90(5):1839-42. doi: 10.1073/pnas.90.5.1839.
Transcription of type 1 human immunodeficiency virus (HIV-1) provirus is governed by the viral long terminal repeat (LTR). Drugs can block HIV-1 replication by inhibiting activity of its LTR. We report that topotecan, beta-lapachone, and curcumin are potent and selective inhibitors of HIV-1 LTR-directed gene expression, at concentrations that have minor effects on cells. At these concentrations, each drug inhibited p24 antigen production in cells either acutely or chronically infected with HIV-1. Their target is transcriptional function of the LTR.
1型人类免疫缺陷病毒（HIV-1）前病毒的转录受病毒长末端重复序列（LTR）调控。药物可通过抑制其LTR的活性来阻断HIV-1复制。我们报告称，拓扑替康、β-拉帕醌和姜黄素是HIV-1 LTR指导的基因表达的强效和选择性抑制剂，其浓度对细胞影响较小。在这些浓度下，每种药物均可抑制急性或慢性感染HIV-1的细胞中p24抗原的产生。它们的靶点是LTR的转录功能。
