Targeting epigenetic modifications in cancer therapy: erasing the roadmap to cancer

HP Mohammad, O Barbash, CL Creasy - Nature medicine, 2019 - nature.com
Epigenetic dysregulation is a common feature of most cancers, often occurring directly
through alteration of epigenetic machinery. Over the last several years, a new generation of …

Epigenetic tools (The Writers, The Readers and The Erasers) and their implications in cancer therapy

S Biswas, CM Rao - European journal of pharmacology, 2018 - Elsevier
Addition of chemical tags on the DNA and modification of histone proteins impart a distinct
feature on chromatin architecture. With the advancement in scientific research, the key …

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' …

A molecular glue degrader of the WIZ transcription factor for fetal hemoglobin induction

PY Ting, S Borikar, JR Kerrigan, NM Thomsen… - Science, 2024 - science.org
Sickle cell disease (SCD) is a prevalent, life-threatening condition attributable to a heritable
mutation in β-hemoglobin. Therapeutic induction of fetal hemoglobin (HbF) can ameliorate …

Epigenetics in cancer stem cells

TB Toh, JJ Lim, EKH Chow - Molecular cancer, 2017 - Springer
Compelling evidence have demonstrated that bulk tumors can arise from a unique subset of
cells commonly termed “cancer stem cells” that has been proposed to be a strong driving …

Cancer epigenetics: tumor heterogeneity, plasticity of stem-like states, and drug resistance

H Easwaran, HC Tsai, SB Baylin - Molecular cell, 2014 - cell.com
The existence of subpopulations of cells in cancers with increased tumor-initiating capacities
and self-renewal potential, often termed" cancer stem cells," is a much discussed and key …

Epigenetic protein families: a new frontier for drug discovery

CH Arrowsmith, C Bountra, PV Fish, K Lee… - Nature reviews Drug …, 2012 - nature.com
Epigenetic regulation of gene expression is a dynamic and reversible process that
establishes normal cellular phenotypes but also contributes to human diseases. At the …

Regional glutamine deficiency in tumours promotes dedifferentiation through inhibition of histone demethylation

M Pan, MA Reid, XH Lowman, RP Kulkarni… - Nature cell …, 2016 - nature.com
Poorly organized tumour vasculature often results in areas of limited nutrient supply and
hypoxia. Despite our understanding of solid tumour responses to hypoxia, how nutrient …

A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells

SK Knutson, TJ Wigle, NM Warholic… - Nature chemical …, 2012 - nature.com
EZH2 catalyzes trimethylation of histone H3 lysine 27 (H3K27). Point mutations of EZH2 at
Tyr641 and Ala677 occur in subpopulations of non-Hodgkin's lymphoma, where they drive …

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 …