2377151-10-3

ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter[1][2][3].

BRD4 (BD1)

[1] Niu Q, et al. Structure-guided drug design identifies a BRD4-selective small molecule that suppresses HIV. J Clin Invest. 2019 Jul 22;129(8):3361-3373. DOI:10.1172/JCI120633
[2] Vansant G, et al. Block-And-Lock Strategies to Cure HIV Infection. Viruses. 2020 Jan 10;12(1). pii: E84. DOI:10.3390/v12010084
[3] Brasier AR, et al. Validation of the epigenetic reader bromodomain-containing protein 4 (BRD4) as a therapeutic target for treatment of airway remodeling. Drug Discov Today. 2020 Jan;25(1):126-132. DOI:10.1016/j.drudis.2019.11.002