You, J. S. & Jones, P. A. Cancer genetics and epigenetics: two sides of the same coin? Cancer Cell 22, 9–20 (2012).
Rideout, W. M. 3rd, Coetzee, G. A., Olumi, A. F. & Jones, P. A. 5-Methylcytosine as an endogenous mutagen in the human LDL receptor and p53 genes. Science 249, 1288–1290 (1990).
Riggs, A. D. & Jones, P. A. 5-Methylcytosine, gene regulation, and cancer. Adv. Cancer Res. 40, 1–30 (1983).This is one of the first reviews published linking DNA methylation to cancer.
Jones, P. A., Issa, J. P. & Baylin, S. Targeting the cancer epigenome for therapy. Nat. Rev. Genet. 17, 630–641 (2016).
Yoder, J. A., Walsh, C. P. & Bestor, T. H. Cytosine methylation and the ecology of intragenomic parasites. Trends Genet. 13, 335–340 (1997).
Issa, J. P. & Kantarjian, H. M. Targeting DNA methylation. Clin. Cancer Res. 15, 3938–3946 (2009).
Loo Yau, H., Ettayebi, I. & De Carvalho, D. D. The cancer epigenome: exploiting its vulnerabilities for immunotherapy. Trends Cell Biol. 29, 31–43 (2018).
Ishak, C. A., Classon, M. & De Carvalho, D. D. Deregulation of retroelements as an emerging therapeutic opportunity in cancer. Trends Cancer 4, 583–597 (2018).
Smith, C. C. et al. Endogenous retroviral signatures predict immunotherapy response in clear cell renal cell carcinoma. J. Clin. Invest. 128, 4804–4820 (2018).
Brocks, D. et al. DNMT and HDAC inhibitors induce cryptic transcription start sites encoded in long terminal repeats. Nat. Genet. 49, 1052–1060 (2017). This paper reveals that DNMTi and HDACi independently lead to cryptic transcription of the ERV9–LTR12 family members.
Roulois, D. et al. DNA-demethylating agents target colorectal cancer cells by inducing viral mimicry by endogenous transcripts. Cell 162, 961–973 (2015).
Chiappinelli, K. B. et al. Inhibiting DNA methylation causes an interferon response in cancer via dsRNA including endogenous retroviruses. Cell 162, 974–986 (2015). References 11 and 12 show that DNMTi treatment leads to formation of dsRNA and activation of an antiviral response (viral mimicry) by cancer cells.
Constantinides, P. G., Taylor, S. M. & Jones, P. A. Phenotypic conversion of cultured mouse embryo cells by aza pyrimidine nucleosides. Dev. Biol. 66, 57–71 (1978).
Sen, D. R. et al. The epigenetic landscape of T cell exhaustion. Science 354, 1165–1169 (2016). This paper reveals that exhausted T cells have a distinct epigenome as compared with effector and memory T cells.
Pauken, K. E. et al. Epigenetic stability of exhausted T cells limits durability of reinvigoration by PD-1 blockade. Science 354, 1160–1165 (2016). This paper shows that epigenetic regulation could limit the success of immunotherapy to reinvigorate exhausted T cells.
Ghoneim, H. E. et al. De novo epigenetic programs inhibit PD-1 blockade-mediated T cell rejuvenation. Cell 170, 142–157 (2017). This paper reveals that blocking an exhaustion-associated DNA methylation programme increases PD1 blockade-mediated T cell rejuvenation.
Philip, M. et al. Chromatin states define tumour-specific T cell dysfunction and reprogramming. Nature 545, 452–456 (2017). This paper reveals that T cell dysfunction occurs through two chromatin states: plastic and fixed.
Cuellar, T. L. et al. Silencing of retrotransposons by SETDB1 inhibits the interferon response in acute myeloid leukemia. J. Cell Biol. 216, 3535–3549 (2017).
Sheng, W. et al. LSD1 ablation stimulates anti-tumor immunity and enables checkpoint blockade. Cell 174, 549–563 (2018). This paper reveals that LSD1 inhibition can also lead to viral mimicry in cancer cells.
Zhang, H. et al. Targeting CDK9 reactivates epigenetically silenced genes in cancer. Cell 175, 1244–1258 (2018).
Unnikrishnan, A. et al. Integrative genomics identifies the molecular basis of resistance to azacitidine therapy in myelodysplastic syndromes. Cell Rep. 20, 572–585 (2017).
Von Hoff, D. D., Slavik, M. & Muggia, F. M. 5-Azacytidine. A new anticancer drug with effectiveness in acute myelogenous leukemia. Ann. Intern. Med. 85, 237–245 (1976). This is the first clinical trial with 5-azacytidine in adults.
Fenaux, P. et al. Efficacy of azacitidine compared with that of conventional care regimens in the treatment of higher-risk myelodysplastic syndromes: a randomised, open-label, phase III study. Lancet Oncol. 10, 223–232 (2009). This is a pivotal paper demonstrating the efficacy of 5-azacytidine in patients with MDS in a phase III study.
Jones, P. A. & Taylor, S. M. Cellular differentiation, cytidine analogs and DNA methylation. Cell 20, 85–93 (1980). This is the first paper to link DNA methylation to differentiation and gene expression.
Yoo, C. B. et al. Delivery of 5-aza-2΄-deoxycytidine to cells using oligodeoxynucleotides. Cancer Res. 67, 6400–6408 (2007).
Issa, J. J. et al. Safety and tolerability of guadecitabine (SGI-110) in patients with myelodysplastic syndrome and acute myeloid leukaemia: a multicentre, randomised, dose-escalation phase 1 study. Lancet Oncol. 16, 1099–1110 (2015).
Duvic, M. et al. Phase 2 trial of oral vorinostat (suberoylanilide hydroxamic acid, SAHA) for refractory cutaneous T cell lymphoma (CTCL). Blood 109, 31–39 (2007).
Kelly, W. K., Marks, P. & Richon, V. M. CCR 20th anniversary commentary: vorinostat-gateway to epigenetic therapy. Clin. Cancer Res. 21, 2198–2200 (2015).
Dawson, M. A. et al. Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature 478, 529–533 (2011).
Boffo, S., Damato, A., Alfano, L. & Giordano, A. CDK9 inhibitors in acute myeloid leukemia. J. Exp. Clin. Cancer Res. 37, 36 (2018).
Jahangeer, S., Elliott, R. M. & Henneberry, R. C. beta-Adrenergic receptor induction in HeLa cells: synergistic effect of 5-azacytidine and butyrate. Biochem. Biophys. Res. Commun. 108, 1434–1440 (1982).
Ginder, G. D., Whitters, M. J. & Pohlman, J. K. Activation of a chicken embryonic globin gene in adult erythroid cells by 5-azacytidine and sodium butyrate. Proc. Natl Acad. Sci. USA 81, 3954–3958 (1984). References 31 and 32 are two of the first papers to use combinations of DNMTi with HDACi.
Cameron, E. E., Bachman, K. E., Myohanen, S., Herman, J. G. & Baylin, S. B. Synergy of demethylation and histone deacetylase inhibition in the re-expression of genes silenced in cancer. Nat. Genet. 21, 103–107 (1999).
Saito, Y. et al. Specific activation of microRNA-127 with downregulation of the proto-oncogene BCL6 by chromatin-modifying drugs in human cancer cells. Cancer Cell 9, 435–443 (2006).
Lay, F. D. et al. The role of DNA methylation in directing the functional organization of the cancer epigenome. Genome Res. 25, 467–477 (2015).
Gal-Yam, E. N. et al. Frequent switching of Polycomb repressive marks and DNA hypermethylation in the PC3 prostate cancer cell line. Proc. Natl Acad. Sci. USA 105, 12979–12984 (2008).
Ohtani, H., Liu, M., Zhou, W., Liang, G. & Jones, P. A. Switching roles for DNA and histone methylation depend on evolutionary ages of human endogenous retroviruses. Genome Res. 28, 1147–1157 (2018).
Liu, M. et al. Vitamin C increases viral mimicry induced by 5-aza-2΄-deoxycytidine. Proc. Natl Acad. Sci. USA 113, 10238–10244 (2016).
Stone, M. L. et al. Epigenetic therapy activates type I interferon signaling in murine ovarian cancer to reduce immunosuppression and tumor burden. Proc. Natl Acad. Sci. USA 114, E10981–E10990 (2017).
Lander, E. S. et al. Initial sequencing and analysis of the human genome. Nature 409, 860–921 (2001).
Takai, D. & Jones, P. A. Origins of bidirectional promoters: computational analyses of intergenic distance in the human genome. Mol. Biol. Evol. 21, 463–467 (2004).
Niwa, O. & Sugahara, T. 5-Azacytidine induction of mouse endogenous type C virus and suppression of DNA methylation. Proc. Natl Acad. Sci. USA 78, 6290–6294 (1981).
Conklin, K. F., Coffin, J. M., Robinson, H. L., Groudine, M. & Eisenman, R. Role of methylation in the induced and spontaneous expression of the avian endogenous virus ev-1: DNA structure and gene products. Mol. Cell. Biol. 2, 638–652 (1982).
Tang, W. W. et al. A unique gene regulatory network resets the human germline epigenome for development. Cell 161, 1453–1467 (2015).
Coulondre, C., Miller, J. H., Farabaugh, P. J. & Gilbert, W. Molecular basis of base substitution hotspots in Escherichia coli. Nature 274, 775–780 (1978).
Yang, A. S. et al. The rate of CpG mutation in Alu repetitive elements within the p53 tumor suppressor gene in the primate germline. J. Mol. Biol. 258, 240–250 (1996).
Leung, D. C. & Lorincz, M. C. Silencing of endogenous retroviruses: when and why do histone marks predominate? Trends Biochem. Sci. 37, 127–133 (2012).
Jacobs, F. M. et al. An evolutionary arms race between KRAB zinc-finger genes ZNF91/93 and SVA/L1 retrotransposons. Nature 516, 242–245 (2014).
Maksakova, I. A. et al. Distinct roles of KAP1, HP1 and G9a/GLP in silencing of the two-cell-specific retrotransposon MERVL in mouse ES cells. Epigenetics Chromatin 6, 15 (2013).
Ishak, C. A. et al. An RB-EZH2 complex mediates silencing of repetitive DNA sequences. Mol. Cell 64, 1074–1087 (2016).
Goel, S. et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature 548, 471–475 (2017).
Keskinen, P., Ronni, T., Matikainen, S., Lehtonen, A. & Julkunen, I. Regulation of HLA class I and II expression by interferons and influenza A virus in human peripheral blood mononuclear cells. Immunology 91, 421–429 (1997).
Snell, L. M., McGaha, T. L. & Brooks, D. G. Type I interferon in chronic virus infection and cancer. Trends Immunol. 38, 542–557 (2017).
Sade-Feldman, M. et al. Resistance to checkpoint blockade therapy through inactivation of antigen presentation. Nat. Commun. 8, 1136 (2017).
Rooney, M. S., Shukla, S. A., Wu, C. J., Getz, G. & Hacohen, N. Molecular and genetic properties of tumors associated with local immune cytolytic activity. Cell 160, 48–61 (2015).
Martincorena, I. et al. Universal patterns of selection in cancer and somatic tissues. Cell 171, 1029–1041 (2017).
McGranahan, N. et al. Allele-specific HLA loss and immune escape in lung cancer evolution. Cell 171, 1259–1271 (2017).
Gao, J. et al. Loss of IFN-gamma pathway genes in tumor cells as a mechanism of resistance to anti-CTLA-4 therapy. Cell 167, 397–404 (2016).
Zaretsky, J. M. et al. Mutations associated with acquired resistance to PD-1 blockade in melanoma. N. Engl. J. Med. 375, 819–829 (2016).
Peng, D. et al. Epigenetic silencing of TH1-type chemokines shapes tumour immunity and immunotherapy. Nature 527, 249–253 (2015).
Nagarsheth, N. et al. PRC2 epigenetically silences Th1-type chemokines to suppress effector T-cell trafficking in colon cancer. Cancer Res. 76, 275–282 (2016).
Booth, L., Roberts, J. L., Poklepovic, A., Kirkwood, J. & Dent, P. HDAC inhibitors enhance the immunotherapy response of melanoma cells. Oncotarget 8, 83155–83170 (2017).
Chuong, E. B., Elde, N. C. & Feschotte, C. Regulatory evolution of innate immunity through co-option of endogenous retroviruses. Science 351, 1083–1087 (2016).
Cañadas, I. et al. Tumor innate immunity primed by specific interferon-stimulated endogenous retroviruses. Nat. Med. 24, 1143–1150 (2018).
Solovyov, A. et al. Global cancer transcriptome quantifies repeat element polarization between immunotherapy responsive and T cell suppressive classes. Cell Rep. 23, 512–521 (2018).
Panda, A. et al. Endogenous retrovirus expression is associated with response to immune checkpoint blockade in clear cell renal cell carcinoma. JCI Insight 3, 121522 (2018).
Whitehurst, A. W. Cause and consequence of cancer/testis antigen activation in cancer. Annu. Rev. Pharmacol. Toxicol. 54, 251–272 (2014).
De Carvalho, D. D. et al. BCR-ABL-mediated upregulation of PRAME is responsible for knocking down TRAIL in CML patients. Oncogene 30, 223–233 (2011).
Weber, J. et al. Expression of the MAGE-1 tumor antigen is up-regulated by the demethylating agent 5-aza-2΄-deoxycytidine. Cancer Res. 54, 1766–1771 (1994).
Qiu, X. et al. Equitoxic doses of 5-azacytidine and 5-aza-2’deoxycytidine induce diverse immediate and overlapping heritable changes in the transcriptome. PLOS ONE 5, e12994 (2010).
Odunsi, K. et al. Efficacy of vaccination with recombinant vaccinia and fowlpox vectors expressing NY-ESO-1 antigen in ovarian cancer and melanoma patients. Proc. Natl Acad. Sci. USA 109, 5797–5802 (2012).
Rapoport, A. P. et al. NY-ESO-1-specific TCR-engineered T cells mediate sustained antigen-specific antitumor effects in myeloma. Nat. Med. 21, 914–921 (2015).
Morgan, R. A. et al. Cancer regression and neurological toxicity following anti-MAGE-A3 TCR gene therapy. J. Immunother. 36, 133–151 (2013).
Linette, G. P. et al. Cardiovascular toxicity and titin cross-reactivity of affinity-enhanced T cells in myeloma and melanoma. Blood 122, 863–871 (2013).
McGranahan, N. et al. Clonal neoantigens elicit T cell immunoreactivity and sensitivity to immune checkpoint blockade. Science 351, 1463–1469 (2016).
Chen, D. S. & Mellman, I. Elements of cancer immunity and the cancer-immune set point. Nature 541, 321–330 (2017).
Ayers, M. et al. IFN-gamma-related mRNA profile predicts clinical response to PD-1 blockade. J. Clin. Invest. 127, 2930–2940 (2017).
Riaz, N. et al. Tumor and microenvironment evolution during immunotherapy with nivolumab. Cell 171, 934–949 (2017).
Topper, M. J. et al. Epigenetic therapy ties MYC depletion to reversing immune evasion and treating lung cancer. Cell 171, 1284–1300 (2017).
Spranger, S., Bao, R. & Gajewski, T. F. Melanoma-intrinsic beta-catenin signalling prevents anti-tumour immunity. Nature 523, 231–235 (2015).
Yang, X. et al. Gene body methylation can alter gene expression and is a therapeutic target in cancer. Cancer Cell 26, 577–590 (2014).
Meissner, T. B. et al. NLR family member NLRC5 is a transcriptional regulator of MHC class I genes. Proc. Natl Acad. Sci. USA 107, 13794–13799 (2010).
Yoshihama, S. et al. NLRC5/MHC class I transactivator is a target for immune evasion in cancer. Proc. Natl Acad. Sci. USA 113, 5999–6004 (2016).
Lal, G. et al. Epigenetic regulation of Foxp3 expression in regulatory T cells by DNA methylation. J. Immunol. 182, 259–273 (2009).
Albrengues, J. et al. Epigenetic switch drives the conversion of fibroblasts into proinvasive cancer-associated fibroblasts. Nat. Commun. 6, 10204 (2015).
Rodriguez-Ubreva, J. et al. Prostaglandin E2 leads to the acquisition of DNMT3A-dependent tolerogenic functions in human myeloid-derived suppressor cells. Cell Rep. 21, 154–167 (2017).
Daniel, B. et al. The nuclear receptor PPARgamma controls progressive macrophage polarization as a ligand-insensitive epigenomic ratchet of transcriptional memory. Immunity 49, 615–626 (2018).
Youngblood, B. et al. Effector CD8 T cells dedifferentiate into long-lived memory cells. Nature 552, 404–409 (2017).
Scharer, C. D., Barwick, B. G., Youngblood, B. A., Ahmed, R. & Boss, J. M. Global DNA methylation remodeling accompanies CD8 T cell effector function. J. Immunol. 191, 3419–3429 (2013).
Russ, B. E. et al. Distinct epigenetic signatures delineate transcriptional programs during virus-specific CD8(+) T cell differentiation. Immunity 41, 853–865 (2014).
Zajac, A. J. et al. Viral immune evasion due to persistence of activated T cells without effector function. J. Exp. Med. 188, 2205–2213 (1998).
Blackburn, S. D., Shin, H., Freeman, G. J. & Wherry, E. J. Selective expansion of a subset of exhausted CD8 T cells by alphaPD-L1 blockade. Proc. Natl Acad. Sci. USA 105, 15016–15021 (2008).
Im, S. J. et al. Defining CD8+ T cells that provide the proliferative burst after PD-1 therapy. Nature 537, 417–421 (2016).
He, S. et al. The histone methyltransferase Ezh2 is a crucial epigenetic regulator of allogeneic T cell responses mediating graft-versus-host disease. Blood 122, 4119–4128 (2013).
Ehx, G. et al. Azacytidine prevents experimental xenogeneic graft-versus-host disease without abrogating graft-versus-leukemia effects. Oncoimmunology 6, e1314425 (2017).
Orskov, A. D. et al. Hypomethylation and up-regulation of PD-1 in T cells by azacytidine in MDS/AML patients: A rationale for combined targeting of PD-1 and DNA methylation. Oncotarget 6, 9612–9626 (2015).
Hodi, F. S. et al. Improved survival with ipilimumab in patients with metastatic melanoma. N. Engl. J. Med. 363, 711–723 (2010).
Robert, C. et al. Pembrolizumab versus ipilimumab in advanced melanoma. N. Engl. J. Med. 372, 2521–2532 (2015).
Pardoll, D. M. The blockade of immune checkpoints in cancer immunotherapy. Nat. Rev. Cancer 12, 252–264 (2012).
Wei, S. C., Duffy, C. R. & Allison, J. P. Fundamental mechanisms of immune checkpoint blockade therapy. Cancer Discov. 8, 1069–1086 (2018).
Yu, J. et al. Myeloid-derived suppressor cells suppress antitumor immune responses through IDO expression and correlate with lymph node metastasis in patients with breast cancer. J. Immunol. 190, 3783–3797 (2013).
Chen, L. et al. CD38-mediated immunosuppression as a mechanism of tumor cell escape from PD-1/PD-L1 blockade. Cancer Discov. 8, 1156–1175 (2018).
Reck, M. et al. Pembrolizumab versus chemotherapy for PD-L1-positive non-small-cell lung cancer. N. Engl. J. Med. 375, 1823–1833 (2016).
Bellmunt, J. et al. Pembrolizumab as second-line therapy for advanced urothelial carcinoma. N. Engl. J. Med. 376, 1015–1026 (2017).
Nghiem, P. T. et al. PD-1 blockade with pembrolizumab in advanced Merkel-Cell carcinoma. N. Engl. J. Med. 374, 2542–2552 (2016).
Le, D. T. & Durham, J. N. Mismatch repair deficiency predicts response of solid tumors to PD-1 blockade. Science 357, 409–413 (2017).
Dempke, W. C. M., Fenchel, K., Uciechowski, P. & Dale, S. P. Second- and third-generation drugs for immuno-oncology treatment — the more the better? Eur. J. Cancer 74, 55–72 (2017).
Chen, D. S. & Mellman, I. Oncology meets immunology: the cancer-immunity cycle. Immunity 39, 1–10 (2013).
Rakoff-Nahoum, S. & Medzhitov, R. Toll-like receptors and cancer. Nat. Rev. Cancer 9, 57–63 (2009).
Vidal, D., Matias-Guiu, X. & Alomar, A. Fifty-five basal cell carcinomas treated with topical imiquimod: outcome at 5-year follow-up. Arch. Dermatol. 143, 266–268 (2007).
Kyi, C. et al. Therapeutic immune modulation against solid cancers with intratumoral Poly-ICLC: a pilot trial. Clin. Cancer Res. 24, 4937–4948 (2018).
Ott, P. A. et al. An immunogenic personal neoantigen vaccine for patients with melanoma. Nature 547, 217–221 (2017).
Ager, C. R. et al. Intratumoral STING activation with T cell checkpoint modulation generates systemic antitumor immunity. Cancer Immunol. Res. 5, 676–684 (2017).
Gadkaree, S. K. et al. Induction of tumor regression by intratumoral STING agonists combined with anti-programmed death-L1 blocking antibody in a preclinical squamous cell carcinoma model. Head Neck 39, 1086–1094 (2017).
Ribas, A. et al. Oncolytic virotherapy promotes intratumoral T cell infiltration and improves anti-PD-1 immunotherapy. Cell 174, 1031–1032 (2018).
Desjardins, A. et al. Recurrent glioblastoma treated with recombinant poliovirus. N. Engl. J. Med. 379, 150–161 (2018).
Brown, M. C. & Holl, E. K. Cancer immunotherapy with recombinant poliovirus induces IFN-dominant activation of dendritic cells and tumor antigen-specific CTLs. Sci. Transl Med. 9, eaan4220 (2017).
Connolly, R. M. et al. Combination epigenetic therapy in advanced breast cancer with 5-azacitidine and entinostat: a phase II National Cancer Institute/Stand Up to Cancer study. Clin. Cancer Res. 23, 2691–2701 (2017).
Azad, N. S. et al. Combination epigenetic therapy in metastatic colorectal cancer (mCRC) with subcutaneous 5-azacitidine and entinostat: a phase 2 consortium/stand up 2 cancer study. Oncotarget 8, 35326–35338 (2017).
Liu, M. et al. Dual inhibition of DNA and histone methyltransferases increases viral mimicry in ovarian cancer cells. Cancer Res. 78, 5754–5766 (2018).
Takeshima, H., Wakabayashi, M., Hattori, N., Yamashita, S. & Ushijima, T. Identification of coexistence of DNA methylation and H3K27me3 specifically in cancer cells as a promising target for epigenetic therapy. Carcinogenesis 36, 192–201 (2015).
Laliberte, J., Marquez, V. E. & Momparler, R. L. Potent inhibitors for the deamination of cytosine arabinoside and 5-aza-2΄-deoxycytidine by human cytidine deaminase. Cancer Chemother. Pharmacol. 30, 7–11 (1992).
Lemaire, M., Momparler, L. F., Bernstein, M. L., Marquez, V. E. & Momparler, R. L. Enhancement of antineoplastic action of 5-aza-2΄-deoxycytidine by zebularine on L1210 leukemia. Anticancer Drugs 16, 301–308 (2005).
Garcia-Manero, G. et al. Phase 2 dose-confirmation study of oral ASTX727, a combination of oral decitabine with a cytidine deaminase inhibitor (CDAi) cedazuridine (E7727), in subjects with myelodysplastic syndromes (MDS). Blood 130, 4274 (2017).
Muvarak, N. E. et al. Enhancing the cytotoxic effects of PARP inhibitors with DNA demethylating agents — a potential therapy for cancer. Cancer Cell 30, 637–650 (2016).
Pulliam, N. et al. An effective epigenetic-PARP inhibitor combination therapy for breast and ovarian cancers independent of BRCA mutations. Clin. Cancer Res. 24, 3163–3175 (2018).
Lee, V. et al. A phase I trial of a guadecitabine (SGI-110) and irinotecan in metastatic colorectal cancer patients previously exposed to irinotecan. Clin. Cancer Res. 24, 6160–6167 (2018).
Matei, D. et al. A phase I clinical trial of guadecitabine and carboplatin in platinum-resistant, recurrent ovarian cancer: clinical, pharmacokinetic, and pharmacodynamic analyses. Clin. Cancer Res. 24, 2285–2293 (2018).
Matei, D. et al. Epigenetic resensitization to platinum in ovarian cancer. Cancer Res. 72, 2197–2205 (2012).
Sun, W. et al. A phase 1 study of azacitidine combined with chemotherapy in childhood leukemia: a report from the TACL consortium. Blood 131, 1145–1148 (2018).
Li, H. et al. Immune regulation by low doses of the DNA methyltransferase inhibitor 5-azacitidine in common human epithelial cancers. Oncotarget 5, 587–598 (2014).
Wrangle, J. et al. Alterations of immune response of non-small cell lung cancer with azacytidine. Oncotarget 4, 2067–2079 (2013).
Sommer, S. et al. Decitabine in combination with donor lymphocyte infusions can induce remissions in relapsed myeloid malignancies with higher leukemic burden after allogeneic hematopoietic cell transplantation. Leuk. Res. 72, 20–26 (2018).
Bogenberger, J. M. et al. BCL-2 family proteins as 5-azacytidine-sensitizing targets and determinants of response in myeloid malignancies. Leukemia 28, 1657–1665 (2014).
DiNardo, C. D. et al. Venetoclax combined with decitabine or azacitidine in treatment-naive, elderly patients with acute myeloid leukemia. Blood 133, 7–17 (2019).