Skip to main content

Table 2 Therapeutic agents shown to stimulate ERV expression in preclinical models of cancer

From: Endogenous retroviruses in the origins and treatment of cancer

Compound Target Cancer model Possible ERV-related clinical effects References
5-azacytidine
5-aza-2-deoxycytidine (5-aza-CdR)
DNMT1 Epithelial ovarian cancer cell lines
B16-F10 mouse melanoma model
Colorectal cancer cell line
dsRNA mediated viral mimicry
Sensitizes cells to checkpoint inhibitor α-CTLA-4
[101, 102]
GSK-LSD1 LSD1 (KDM1A) Breast cancer cell line
B16 mouse melanoma model
dsRNA viral mimicry
Sensitizes cells to checkpoint inhibitor α-PD-1
[103]
Vorinostat
Pracinostat
+ 5-aza-CdR
pan-HDAC
HDAC class I/II/IV
HDAC + DNMT1
Lung cancer cell line Activates ERV cryptic transcription start sites
Stimulates interferon response
[42]
GSK126
GSK343
EZH2 Resistant chemorefractory small-cell lung cancer
Taxane-resistant triple negative breast cancer cell lines
Promotes dsRNA production
Alters innate immune signalling and promotes EMT
Induces viral mimicry
[104, 105]
UNC0638 + 5-aza-CdR G9a + DNMT1 Ovarian cancer cell lines Induces viral mimicry [106]
MC180295 CDK9 Colorectal cancer cell line
Ovarian cancer cell line injected into mice
Induces viral mimicry
Sensitizes cells to checkpoint inhibitor α-PD-1
[107]
Abemaciclib CDK4/6 Mouse breast cancer models Inhibits DNMT1 expression thereby inducing viral mimicry [108]
Vitamin C TET enzymes AML, colorectal, breast, and liver cancer cell lines Induces viral mimicry [109]
RRX-001 Hemoglobin Colon cancer cell lines Decreases DNMT expression to induce viral mimicry [110]