NSC-665353(NSC-665353) - 药物靶点：HIV envelope protein gp120_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

HIV envelope protein gp120

作用机制

HIV包膜蛋白gp120抑制剂

治疗领域

免疫系统疾病感染泌尿生殖系统疾病

在研适应症-

非在研适应症

HIV感染

原研机构

Ionis Pharmaceuticals, Inc.

在研机构-

非在研机构

Ionis Pharmaceuticals, Inc.

ImQuest BioSciences, Inc.

最高研发阶段终止临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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关联

100 项与 NSC-665353 相关的临床结果

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100 项与 NSC-665353 相关的转化医学

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100 项与 NSC-665353 相关的专利（医药）

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2

项与 NSC-665353 相关的文献（医药）

1999-02-01·Drugs in R & D4区 · 医学

NSC 665353

4区 · 医学

ArticleOA

作者: &NA;

1994-11-01·AIDS Research and Human Retroviruses4区 · 医学

Potent and Specific Inhibition of HIV Envelope-Mediated Cell Fusion and Virus Binding by G Quartet-Forming Oligonucleotide (ISIS 5320)

4区 · 医学

Article

作者: Vickers, Timothy A. ; Lackman-Smith, Carol ; Ecker, David J. ; Roberson, Joseph L. ; Wyatt, Jacqueline R. ; Buckheit, Robert W. Jr.

We have previously reported identification of a phosphorothioate oligonucleotide TTGGGGTT (ISIS 5320) as a potent inhibitor of HIV infection in vitro. The oligonucleotide forms a parallel-stranded, tetrameric guanosine quartet (G-quartet) structure that specifically binds to the HIV envelope glycoprotein (gp120) and inhibits both cell-to-cell and virus-to-cell infection at submicromolar concentrations. In the current study we demonstrate that the tetramer inhibits the infection of laboratory-derived isolates of HIV-1 and HIV-2 in a variety of phenotypically distinct, established human cell lines and a panel of biologically diverse clinical isolates in fresh human peripheral blood lymphocytes and macrophages. The compound was also active against all drug-resistant virus isolates tested. In combination with AZT, ISIS 5320 exhibits additive to slightly synergistic anti-HIV activity. Cell-based mechanism of action studies demonstrate that the compound inhibits the binding of infectious virus and virus-infected cells to uninfected target cells by binding to the cationic V3 loop of the envelope glycoprotein. The G-quartet structure is a potential candidate for use in anti-HIV chemotherapy.

100 项与 NSC-665353 相关的药物交易

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