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What role could epigenetics have in cancer?
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Where could epigenetics lead us?
Epigenetics is the change of gene expression without alteration of the DNA sequence.1-3 A hallmark of cancer cells, epigenetic dysregulation may drive disease progression.3
One epigenetic regulator is enhancer of zeste homolog 2 (EZH2), which is a histone methyltransferase.3 This is of interest as elevated EZH2 has been shown to correlate with certain types of cancer growth.4
EZH2 and cancer progression
Targeting the EZH2 cascade is a potential novel direction in cancer.4 EZH2 is an epigenetic regulator of genes and is implicated in the initiation and proliferation of cancer cells.1,2 With a role in certain lymphomas and lung, breast, ovarian, and prostate cancer, EZH2 may be involved in a broad range of solid and hematological malignancies.1,5 By epigenetic silencing of tumor suppressor genes and activating the androgen receptor signaling pathway, EZH2 may drive cancer growth.4,6,7
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Uncovering new potential applications in cancer
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We at Pfizer are committed to helping cancer patients by investigating epigenetic modifiers like EZH2. One area where we see potential is in prostate cancer, where 1 in 8 men will be diagnosed with it in their lifetime.8 With research in this area we can gain a deeper understanding of this mechanism.
Through the power of science, discovery, and collaboration, Pfizer aims to reveal EZH2 as a potentially important therapeutic target.
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References: 1. Kung PP, et al. J Med Chem 2018;61(3):650-665. 2. Kim J, et al. Cell Rep 2018;25(10):2808-2820.e4. 3. Ragavi R, et al. Urol Oncol 2023;41(8):340-353. 4. Park SH, et al. Oncogene 2021;40(39):5788-5798. 5. Zhang L, et al. Nat Commun 2022;13(1):2543. 6. Han H, et al. Cell Rep 2022;39(1):110595. 7. Bai Y, et al. J Biol Chem 2019;294(25):9911-9923. 8. Siegel RL, et al. CA Cancer J Clin 2024;74(1):12-49.