Appendix D.
Histone demethylases in cancer
| Name | Synonyms | Targets | Links to cancer |
|---|---|---|---|
| KDM1A | LSD1, AOF2 | H3K4me2/me1, H3K9me2/me1 | Overexpressed in prostate carcinoma, bladder cancer (Kauffman et al. 2011), ER-negative breast cancer (Lim et al. 2010), neuroblastoma (Schulte et al. 2009); inhibition in animal models of engrafted AML (Schenk et al. 2012) |
| KDM1B | LSD2, AOF1 | H3K4me2/me1 | |
| KDM2A | FBXL11A, JHDM1A | H3K36me2/me1 | Overexpressed in NSCLC; KDM2A knockdown inhibits NSCLC tumor growth in mouse xenografts (Wagner et al. 2013) |
| KDM2B | FBXL10B, JHDM1B | H3K36me2/me1, H3K4me3 | Required for initiation and maintenance of AML (He et al. 2011) |
| KDM3A | JMJD1A, JHDM2A | H3K9me2/me1 | High expression correlated with bad prognosis in colorectal cancer (Uemura et al. 2010), overexpressed in renal cell carcinoma (Guo et al. 2011) |
| KDM3B | JMJD1B, JHDM2B | H3K9me2/me1 | |
| KDM4A | JMJD2A, JHDM3A | H3K9me3/me2, H3K36me3/me2 | Required for proliferation of breast cancer cells (Lohse et al. 2011), attenuated expression in bladder cancer (Kauffman et al. 2011), required for latency and replication of viruses that cause cancer (Chang et al. 2011) |
| KDM4B | JMJD2B | H3K9me3/me2, H3K36me3/me2 | Overexpressed in gastric cancer (Li et al. 2011), required for proliferation and formation of metastasis in breast cancer cells (Kawazu et al. 2011) |
| KDM4C | JMJD2C, GASC1 | H3K9me3/me2, H3K36me3/me2 | Overexpressed in breast cancer (Liu et al. 2009), esophageal cancer (Yang et al. 2000), MALT lymphoma (Vinatzer et al. 2008), AML (Hélias et al. 2008), and lung sarcomatoid carcinoma (Italiano et al. 2006) |
| KDM4D | JMJD2D | H3K9me3/me2/me1, H3K36me3/me2 | Required for cell proliferation and survival in colon carcinoma cells (Kim et al. 2012a; Kim et al. 2012b) |
| KDM4E | JMJD2E | H3K9me3/me2 | |
| KDM5A | Jarid1A, RBP2 | H3K4me3/me2 | Involved in drug resistance (Sharma et al. 2010) |
| KDM5B | Jarid1B, PLU1 | H3K4me3/me2 | Tumor-suppressive function in metastatic melanoma cells (Roesch et al. 2006, 2008), proproliferative in breast cancer (Mitra et al. 2011), and overexpressed in prostate cancer |
| KDM5C | Jarid1C, SMCX | H3K4me3/me2 | Inactivating mutations found in clear cell renal carcinoma (Dalgliesh et al. 2010) |
| KDM5D | Jarid1D, SMCY | H3K4me3/me2 | |
| KDM6A | UTX, MGC141941 | H3K27me3/me2 | Tumor-suppressive function (Tsai et al. 2010) |
| KDM6B | JMJD3, KIAA0346, PHF8, KIAA1111, ZNF422 | H3K27me3/me2, H3K9me2/me1, H4K20me1 | Overexpressed in Hodgkin’s lymphoma (Anderton et al. 2011) |
| KDM7 | KIAA1718, JHDM1D (KDM7A) | H3K9me2/me1, H3K27me2/me1 | Increased expression of KDM7A suppresses tumor growth in HeLa and B16 xenograft models (Osawa et al. 2011) |
| KDM8 | JMJD5, FLJ13798 | H3K36me2 | Overexpressed in breast tumors; may play a critical role in regulation of cell cycle by activating the cyclin A1 locus via demethylation of H3K36me2 (Hsia et al. 2010) |
Adapted, with permission, from Hoffmann et al. 2012, © Elsevier.
From ER, estrogen receptor; AML, acute myloid leukemia; NSCLC, non-small-cell lung carcinoma; KDM2A, lysine demethylase 2A; MALT, mucosa-associated lymphoid tissue.