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三种1型人类免疫缺陷病毒长末端重复序列定向基因表达和病毒复制的抑制剂。

Three inhibitors of type 1 human immunodeficiency virus long terminal repeat-directed gene expression and virus replication.

作者信息

Li C J, Zhang L J, Dezube B J, Crumpacker C S, Pardee A B

机构信息

Dana-Farber Cancer Institute, Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115.

出版信息

Proc Natl Acad Sci U S A. 1993 Mar 1;90(5):1839-42. doi: 10.1073/pnas.90.5.1839.

Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a8b3/45975/a7a847b9fdd3/pnas01464-0215-a.jpg

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