Metabolic reprogramming and epigenetic modifications on the path to cancer

L Sun, H Zhang, P Gao - Protein & cell, 2022 - academic.oup.com
Metabolic rewiring and epigenetic remodeling, which are closely linked and reciprocally
regulate each other, are among the well-known cancer hallmarks. Recent evidence …

Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease

KP Bhat, H Ümit Kaniskan, J **… - Nature Reviews Drug …, 2021 - nature.com
Protein lysine methylation is a crucial post-translational modification that regulates the
functions of both histone and non-histone proteins. Deregulation of the enzymes or 'writers' …

The DOT1L inhibitor pinometostat reduces H3K79 methylation and has modest clinical activity in adult acute leukemia

EM Stein, G Garcia-Manero, DA Rizzieri… - Blood, The Journal …, 2018 - ashpublications.org
Abstract Pinometostat (EPZ-5676) is a first-in-class small-molecule inhibitor of the histone
methyltransferase disrupter of telomeric silencing 1-like (DOT1L). In this phase 1 study …

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 …

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

SR Daigle, EJ Olhava, CA Therkelsen… - Blood, The Journal …, 2013 - ashpublications.org
Rearrangements of the MLL gene define a genetically distinct subset of acute leukemias
with poor prognosis. Current treatment options are of limited effectiveness; thus, there is a …

Targeting histone methyltransferases and demethylases in clinical trials for cancer therapy

L Morera, M Lübbert, M Jung - Clinical epigenetics, 2016 - Springer
The term epigenetics is defined as heritable changes in gene expression that are not due to
alterations of the DNA sequence. In the last years, it has become more and more evident …

Marked for death: targeting epigenetic changes in cancer

SX Pfister, A Ashworth - Nature reviews Drug discovery, 2017 - nature.com
In the past few years, it has become clear that mutations in epigenetic regulatory genes are
common in human cancers. Therapeutic strategies are now being developed to target …

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 …

The Ten-Eleven Translocation-2 (TET2) gene in hematopoiesis and hematopoietic diseases

E Solary, OA Bernard, A Tefferi, F Fuks, W Vainchenker - Leukemia, 2014 - nature.com
Abstract Ten-Eleven Translocation-2 (TET2) inactivation through loss-of-function mutation,
deletion and IDH1/2 (Isocitrate Dehydrogenase 1 and 2) gene mutation is a common event …

Emerging therapeutic drugs for AML

EM Stein, MS Tallman - Blood, The Journal of the American …, 2016 - ashpublications.org
Multiple new drugs are being developed to treat acute myeloid leukemia (AML), including
novel formulations of traditional chemotherapy-antibody drug conjugates and agents that …