Search

Search

这页已由机器翻译。其他页面可能仍然显示为英文。 View in English

首页
...
研究领域生物医学和临床科学药理学和制药科学药物基因组学
设计,合成和生物评估双部位HIV-1抑制剂,同时针对NNRTI结合口袋和具有有利耐药性概况的相邻部位

设计,合成和生物评估双部位HIV-1抑制剂,同时针对NNRTI结合口袋和具有有利耐药性概况的相邻部位

Xiangkai Ji ¹, Xiangyi Jiang ¹, Xing Huang ¹, Heng Gao ¹, Zhen Gao ¹, Ping Gao ², Erik De Clercq ³, Christophe Pannecouque ³, Dongwei Kang ⁴, Peng Zhan ⁴, Xinyong Liu ⁴

Xiangkai Ji ¹, Xiangyi Jiang ¹, Xing Huang ¹

¹Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, China.
²Department of Pharmacy, Shandong Provincial Hospital Affiliated to Shandong First Medical University, Jinan, Shandong 250021, China.
³Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, K.U.Leuven, Herestraat 49 Postbus 1043 (09.A097), B-3000 Leuven, Belgium.
⁴Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, China; China-Belgium Collaborative Research Center for Innovative Antiviral Drugs of Shandong Province, 250012 Jinan, China.

⁰Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, China.

Bioorganic Chemistry +

|

2025年八月31日

相关实验视频

These videos have been matched automatically. Contact us if they are not relevant.

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

Published on: May 9, 2025

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors

Published on: April 9, 2014

An Affordable HIV-1 Drug Resistance Monitoring Method for Resource Limited Settings

An Affordable HIV-1 Drug Resistance Monitoring Method for Resource Limited Settings

Published on: March 30, 2014

See all related videos

在PubMed上查看摘要

概括

此摘要是机器生成的。

科学家开发了针对HIV-1逆转录酶 (RT) 的两个位点的新型双位点抑制剂,以对抗抗药性. 化合物11×对野生型和突变型HIV-1菌株具有强烈活性,为治疗提供了有前途的新疗法.

科学领域

病毒学
医学化学
药物发现

背景情况

人类免疫缺陷病毒1型 (HIV-1) 的高突变率导致对非核酸逆转录酶抑制剂 (NNRTIs) 的耐药性.
针对HIV-1逆转录酶 (RT) 的新结合点是克服耐药性的关键策略.

研究的目的

设计和合成针对经典非核酸抑制剂结合口袋 (NNIBP) 和NNRTIs相邻位点 (NNIAS) 的新型双位点HIV-1抑制剂.
评估这些新型化合物的抗病毒活性对抗野生型 (WT) 和抗药性HIV-1菌株.

主要方法

合成26种新型双部位HIV-1抑制剂.
使用EC50值对WT HIV-1进行抗病毒评估.
对七种临床相关的HIV-1突变菌株的活性评估.
与酶相关的免疫吸收试验 (ELISA) 来证实HIV-1RT的抑制.
分子对接研究以阐明结合模式.

主要成果

所有合成的化合物对WT HIV-1具有强烈的活性,EC50值在4. 1至86nM之间.
化合物11×对WT和7种突变的HIV-1菌株表现出强烈的活性.
ELISA证实了11×对HIV-1RT的显著抑制作用.
分子对接显示了11×的双结合模式,解释了它对抗耐药菌株的有效性.

结论

化合物11×是一种具有广谱活性的有前途的双部位HIV-1抑制剂.
这种双重向策略在克服HIV-1药物耐药性方面是有效的.
作为一种潜在的HIV-1感染治疗药物,该药物需要进一步开发.

关键词:

双部位抑制剂艾滋病毒-1非转基因药物分子对接合理的药物设计电阻配置文件

相关实验视频

这些视频已自动匹配 Contact us 如果它们不相关

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

Published on: May 9, 2025

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors

Published on: April 9, 2014

An Affordable HIV-1 Drug Resistance Monitoring Method for Resource Limited Settings

An Affordable HIV-1 Drug Resistance Monitoring Method for Resource Limited Settings

Published on: March 30, 2014

See all related videos

相关概念视频

Retrovirus Life Cycles

Retrovirus Life Cycles

Retroviruses have a single-stranded RNA genome that undergoes a special form of replication. Once the retrovirus has entered the host cell, an enzyme called reverse transcriptase synthesizes double-stranded DNA from the retroviral RNA genome. This DNA copy of the genome is then integrated into the host’s genome inside the nucleus via an enzyme called integrase. Consequently, the retroviral genome is transcribed into RNA whenever the host’s genome is transcribed, allowing the...

Share

X
Facebook
LinkedIn
YouTube

ABOUT JoVE

Overview
Leadership
Blog
JoVE Help Center

AUTHORS

Publishing Process
Editorial Board
Scope & Policies
Peer Review
FAQ
Submit

LIBRARIANS

Testimonials
Subscriptions
Access
Resources
Library Advisory Board
FAQ

RESEARCH

JoVE Journal
Methods Collections
JoVE Encyclopedia of Experiments
Archive

EDUCATION

JoVE Core
JoVE Business
JoVE Science Education
JoVE Lab Manual
Faculty Resource Center
Faculty Site

Terms & Conditions of Use
Privacy Policy
Policies