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新型基于triazolopyridine的BRD4抑制剂作为强大的HIV-1潜伏逆转剂

Yan-Kai Wang¹, Xu-Sheng Huang^2,3, Hao Sun¹

¹School of Pharmaceutical Sciences & Institute of Materia Medica, Shandong First Medical University & Shandong Academy of Medical Sciences, National Key Laboratory of Advanced Drug Delivery System, Key Laboratory for Biotechnology Drugs of National Health Commission (Shandong Academy of Medical Sciences), Key Lab for Rare & Uncommon Diseases of Shandong Province, Jinan 250117, Shandong, China.

ACS medicinal chemistry letters

|January 17, 2024

概括

新的三烯衍生物在抗HIV-1潜伏疗法中表现出具有前途的基胺含蛋白4 (BRD4) 抑制剂. 化合物13d有效地重新激活HIV-1,具有良好的安全性,并与其他药物协同作用.

科学领域:

药用化学医学化学
病毒学病毒学
分子生物学分子生物学

背景情况:

含基蛋白4 (BRD4) 抑制剂是潜伏HIV-1感染的有前途的治疗策略.
重新激活潜伏的HIV-1对于病毒根除至关重要.

研究的目的:

设计,合成和评估新型的三胺衍生物作为抗HIV-1延迟的BRD4抑制剂.
评估这些化合物的疗效,安全性和作用机制.

主要方法:

合成三烯酸衍生物.
对HIV-1潜伏逆转的生物评估.
与 prostratin 的协同效应研究.
行动研究的机制,包括BRD4向和Tat-依赖的延伸.
对抗病毒药物药物相互作用的评估.

主要成果:

化合物13d显示出强大的HIV-1重激活和有利的安全性,而不会诱导异常免疫激活.
化合物13d与前列腺素表现出强烈的协同作用.
13d的延迟逆转机制涉及BRD4抑制和刺激Tat依赖的HIV-1延长,类似于JQ1.1.
与各种抗病毒药物同时使用13d化合物的疗效没有受到影响,也没有影响它们的抗病毒活性.

结论:

三胺衍生物,特别是13d化合物,代表了用于HIV-1潜伏逆转的BRD4抑制剂的可行类别.
化合物13d显示出作为安全有效的延迟逆转剂的潜力,具有有利的协同作用和药物相互作用概况.

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