Histone lysine demethylases as targets for anticancer therapy

JW Højfeldt, K Agger, K Helin - Nature reviews Drug discovery, 2013 - nature.com
It has recently been demonstrated that the genes controlling the epigenetic programmes that
are required for maintaining chromatin structure and cell identity include genes that drive …

LSD1: biologic roles and therapeutic targeting

A Maiques-Diaz, TCP Somervaille - Epigenomics, 2016 - Taylor & Francis
LSD1 (KDM1A; BHC110; AOF2) was the first protein reported to exhibit histone demethylase
activity and has since been shown to have multiple essential roles in mammalian biology …

Specific regulation of BACH1 by the hotspot mutant p53R175H reveals a distinct gain-of-function mechanism

Z Su, N Kon, J Yi, H Zhao, W Zhang, Q Tang, H Li… - Nature cancer, 2023 - nature.com
Although the gain of function (GOF) of p53 mutants is well recognized, it remains unclear
whether different p53 mutants share the same cofactors to induce GOFs. In a proteomic …

[HTML][HTML] Transcription factor protein interactomes reveal genetic determinants in heart disease

B Gonzalez-Teran, M Pittman, F Felix, R Thomas… - Cell, 2022 - cell.com
Congenital heart disease (CHD) is present in 1% of live births, yet identification of causal
mutations remains challenging. We hypothesized that genetic determinants for CHDs may …

Dynamic changes in histone modifications precede de novo DNA methylation in oocytes

KR Stewart, L Veselovska, J Kim, J Huang… - Genes & …, 2015 - genesdev.cshlp.org
Erasure and subsequent reinstatement of DNA methylation in the germline, especially at
imprinted CpG islands (CGIs), is crucial to embryogenesis in mammals. The mechanisms …

A systematic review of histone lysine‐specific demethylase 1 and its inhibitors

YC Zheng, J Ma, Z Wang, J Li, B Jiang… - Medicinal research …, 2015 - Wiley Online Library
Histone lysine‐specific demethylase 1 (LSD1) is the first discovered and reported histone
demethylase by Dr. Shi Yang's group in 2004. It is classified as a member of amine oxidase …

Interrogating epigenetic mechanisms with chemically customized chromatin

N Hananya, S Koren, TW Muir - Nature Reviews Genetics, 2024 - nature.com
Genetic and genomic techniques have proven incredibly powerful for identifying and
studying molecular players implicated in the epigenetic regulation of DNA-templated …

Crystal structure of the LSD1/CoREST histone demethylase bound to its nucleosome substrate

SA Kim, J Zhu, N Yennawar, P Eek, S Tan - Molecular cell, 2020 - cell.com
LSD1 (lysine specific demethylase; also known as KDM1A), the first histone demethylase
discovered, regulates cell-fate determination and is overexpressed in multiple cancers …

Structure and function of the nucleosome-binding PWWP domain

S Qin, J Min - Trends in biochemical sciences, 2014 - cell.com
PWWP domain-containing proteins are often involved in chromatin-associated biological
processes, such as transcriptional regulation and DNA repair, and recent studies have …

[HTML][HTML] Targeting histone lysine demethylases—progress, challenges, and the future

CC Thinnes, KS England, A Kawamura… - … et Biophysica Acta (BBA …, 2014 - Elsevier
N-Methylation of lysine and arginine residues has emerged as a major mechanism of
transcriptional regulation in eukaryotes. In humans, N ε-methyllysine residue demethylation …