Targeting transcription factors for cancer treatment

M Lambert, S Jambon, S Depauw… - Molecules, 2018 - mdpi.com
Transcription factors are involved in a large number of human diseases such as cancers for
which they account for about 20% of all oncogenes identified so far. For long time, with the …

Inhibitors of protein methyltransferases and demethylases

HU Kaniskan, ML Martini, J ** - Chemical reviews, 2018 - ACS Publications
Post-translational modifications of histones by protein methyltransferases (PMTs) and
histone demethylases (KDMs) play an important role in the regulation of gene expression …

Discovery of cancer drug targets by CRISPR-Cas9 screening of protein domains

J Shi, E Wang, JP Milazzo, Z Wang, JB Kinney… - Nature …, 2015 - nature.com
CRISPR-Cas9 genome editing technology holds great promise for discovering therapeutic
targets in cancer and other diseases. Current screening strategies target CRISPR-Cas9 …

Critical roles of non-histone protein lysine methylation in human tumorigenesis

R Hamamoto, V Saloura, Y Nakamura - Nature Reviews Cancer, 2015 - nature.com
Several protein lysine methyltransferases and demethylases have been identified to have
critical roles in histone modification. A large body of evidence has indicated that their …

Escape from treatment; the different faces of leukemic stem cells and therapy resistance in acute myeloid leukemia

N Van Gils, F Denkers, L Smit - Frontiers in oncology, 2021 - frontiersin.org
Standard induction chemotherapy, consisting of an anthracycline and cytarabine, has been
the first-line therapy for many years to treat acute myeloid leukemia (AML). Although this …

Epigenetic control of adult stem cell function

A Avgustinova, SA Benitah - Nature reviews Molecular cell biology, 2016 - nature.com
Mammalian embryonic development is a tightly regulated process that, from a single zygote,
produces a large number of cell types with hugely divergent functions. Distinct cellular …

Functional role of G9a histone methyltransferase in cancer

F Casciello, K Windloch, F Gannon, JS Lee - Frontiers in immunology, 2015 - frontiersin.org
Post-translational modifications of DNA and histones are epigenetic mechanisms, which
affect the chromatin structure, ultimately leading to gene expression changes. A number of …

Mutant IDH1 downregulates ATM and alters DNA repair and sensitivity to DNA damage independent of TET2

S Inoue, WY Li, A Tseng, I Beerman, AJ Elia… - Cancer cell, 2016 - cell.com
Mutations in the isocitrate dehydrogenase-1 gene (IDH1) are common drivers of acute
myeloid leukemia (AML) but their mechanism is not fully understood. It is thought that IDH1 …

Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment

X Peng, Z Sun, P Kuang, J Chen - European Journal of Medicinal Chemistry, 2020 - Elsevier
Histone deacetylases (HDACs) are a class of enzymes that remove acetyl from the ε-N-
acetyl lysine of histones, allowing histones to wrap DNA more tightly. HDACs play an …

EHMT1/EHMT2 in EMT, cancer stemness and drug resistance: emerging evidence and mechanisms

A Nachiyappan, N Gupta, R Taneja - The FEBS Journal, 2022 - Wiley Online Library
Metastasis, therapy failure and tumour recurrence are major clinical challenges in cancer.
The interplay between tumour‐initiating cells (TICs) and epithelial–mesenchymal transition …