Novel Triazolopyridine-Based BRD4 Inhibitors as Potent HIV-1 Latency Reversing Agents

	Novel Triazolopyridine-Based BRD4 Inhibitors as Potent HIV-1 Latency Reversing Agents
	Wang, YK; Huang, XS; Sun, H; Ma, MD; Yu, HP; Hu, W; Li, ZY; Li, Z; Luo, RH; Tian, RR; Xiao, TF; Yang, LM; Zheng, YT; Li, X
	2023
发表期刊	ACS MEDICINAL CHEMISTRY LETTERS
ISSN	1948-5875
卷号	15 期号:1 页码:60-68
摘要	Bromodomain-containing protein 4 (BRD4) inhibitors have been proven to be a promising option for anti-HIV-1 latency therapeutics. We herein describe the design, synthesis, and anti-HIV-1 latency bioevaluation of triazolopyridine derivatives as BRD4 inhibitors. Among them, compound 13d displayed favorable HIV-1 reactivation and prominent safety profile without triggering abnormal immune activation. It exerted strong synergism when combined with the PKC activator prostratin and has the same BRD4-targeting latency mechanism as observed with JQ1, by stimulating Tat-dependent HIV-1 elongation. Besides, it neither affected the antiviral efficacies of antiviral drugs nor caused secondary infections to uninfected cells and the latency reversing potency of 13d, in turn, was not affected by different classes of antiviral drugs.
收录类别	SCI
语种	英语
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/152453/13963
专题	科研部门_分子免疫药理学（郑永唐）
推荐引用方式 GB/T 7714	Wang, YK,Huang, XS,Sun, H,et al. Novel Triazolopyridine-Based BRD4 Inhibitors as Potent HIV-1 Latency Reversing Agents[J]. ACS MEDICINAL CHEMISTRY LETTERS,2023,15(1):60-68.
APA	Wang, YK.,Huang, XS.,Sun, H.,Ma, MD.,Yu, HP.,...&Li, X.(2023).Novel Triazolopyridine-Based BRD4 Inhibitors as Potent HIV-1 Latency Reversing Agents.ACS MEDICINAL CHEMISTRY LETTERS,15(1),60-68.
MLA	Wang, YK,et al."Novel Triazolopyridine-Based BRD4 Inhibitors as Potent HIV-1 Latency Reversing Agents".ACS MEDICINAL CHEMISTRY LETTERS 15.1(2023):60-68.

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