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. 2021 May 27;12:688747. doi: 10.3389/fimmu.2021.688747

Table 3.

Summary of Latency-Reversal Agents.

Latency-Reversal Agents Class Stage References
Romidepsin (FK228), Vorinostat (SAHA), Panobinostat(LBH589) Histone deacetylase inhibitors Clinical trial NTC02092116 (65), NCT02092116 (65, 66), NCT01933594 (67, 68), NCT01319383 (6871), NTC02092116 (65), NCT01365065 (72, 73), NCT03803605 (74), NCT02336074 (75), NCT01680094 (69, 76), NCT02471430 (76)
Belinostat (PXD101), Givinostat (ITF2357), Nanatinostat(CHR-3996) Histone deacetylase inhibitors In vitro (77, 78)
Nicotinamide Histone deacetylase inhibitors Ex vivo (79)
JQ1, I-BET151, I-BET, MS417, UMB-136, OTX015, CPI-203, RVX-208, PFI-1, BI-2536, BI-6727, Apabetalone Small-molecule bromodomain inhibitors In vitro (8088)
GSK-343, EPZ-6438 (Tazemetostat) Small-molecule histone methyltransferase inhibitors targeted to EZH2 In vitro (89)
UNC-0638 Small-molecule histone methyltransferase inhibitors targeted to EHMT2 In vitro (89)
EED226, A-395 Small-molecule histone methyltransferase inhibitors targeted to EED In vitro (90)
DZNep Lysine-specific histone methyltransferase inhibitor targeted to EZH2 In vitro (91, 92)
BIX-01294 Lysine-specific histone methyltransferase inhibitor of the HKMT G9a In vitro (79, 92)
Chaetocin Lysine-specific histone methyltransferase inhibitor of the HKMT SUV39H1 In vitro (79, 92)
5-AzaC, 5-AzadC DNA methylation inhibitors In vitro (93)
Ingenol, Bryostatin-1 Protein kinase C activators Clinical trial NCT04503928 (94, 95), NCT02531295 (9697), NCT02269605 (98)
Prostratin Protein kinase C activators In vitro (99)
Tat-R5M4 Toll-like receptor agonist In vitro (100)
Pam3CSK4 Toll-like receptor 1/2 agonist In vitro (101)
GS-9620 Toll-like receptor 7 agonist Clinical trial NCT02858401 (102)
GS-986 Toll-like receptor 7 agonist In vivo (103)
R-848 Toll-like receptor 7/8 agonist In vitro (104)
3M-002 Toll-like receptor 8 agonist In vitro (104)
MGN 1703 Toll-like receptor 9 agonist Clinical trial NCT02443935 (105, 106)
CPG 7909 Toll-like receptor 9 agonist Clinical trial NCT00562939 (107)
nivolumab Monoclonal antibodies targeting PD-1 Case report (108)
pembrolizumab Monoclonal antibodies targeting PD-1 In vitro (108)
Ipilimumab Monoclonal antibodies targeting CTLA-4 (CD152) Case report (109)
BMS-936559 Monoclonal antibodies targeting PD-L1 Clinical trial NCT02028403 (110)
galectin-9 Human carbohydrate-binding immunomodulatory protein In vitro (111)
Procyanidin trimer C1 MAPK agonist In vitro (80)
Maraviroc CCR5 antagonist Clinical trial NCT01365065 (112), NCT00795444 (113)
N-803 Interleukin-15 Superagonist In vivo (114)
AZD5582, Ciapavir (SBI-0953294) Activator of the non-canonical NF- κB pathway In vivo (115, 116)
Disulfiram (C10H20N2S4) Activators of Akt signaling pathway Clinical trial NCT01944371 (117)

NF- κB, Nuclear Factor- κB; HKMT, histone-lysine methyltransferase; EHMT2, euchromatic histone-lysine N-methyltransferase 2; PD-1, programmed cell death protein; CTLA-4, cytotoxic T lymphocyte antigen 4; PD-L1, programmed cell death protein ligand 1.