Shaping the cellular landscape with Set2/SETD2 methylation
SL McDaniel, BD Strahl - Cellular and Molecular Life Sciences, 2017 - Springer
Chromatin structure is a major barrier to gene transcription that must be disrupted and re-set
during each round of transcription. Central to this process is the Set2/SETD2 …
during each round of transcription. Central to this process is the Set2/SETD2 …
SETD2: from chromatin modifier to multipronged regulator of the genome and beyond
TM Molenaar, F van Leeuwen - Cellular and Molecular Life Sciences, 2022 - Springer
Histone modifying enzymes play critical roles in many key cellular processes and are
appealing proteins for targeting by small molecules in disease. However, while the functions …
appealing proteins for targeting by small molecules in disease. However, while the functions …
Vitamin B12 is a limiting factor for induced cellular plasticity and tissue repair
M Kovatcheva, E Melendez, D Chondronasiou… - Nature …, 2023 - nature.com
Transient reprogramming by the expression of OCT4, SOX2, KLF4 and MYC (OSKM) is a
therapeutic strategy for tissue regeneration and rejuvenation, but little is known about its …
therapeutic strategy for tissue regeneration and rejuvenation, but little is known about its …
Histone lysine methylases and demethylases in the landscape of human developmental disorders
Histone lysine methyltransferases (KMTs) and demethylases (KDMs) underpin gene
regulation. Here we demonstrate that variants causing haploinsufficiency of KMTs and …
regulation. Here we demonstrate that variants causing haploinsufficiency of KMTs and …
A potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases
Protein arginine methyltransferases (PRMTs) play a crucial role in a variety of biological
processes. Overexpression of PRMTs has been implicated in various human diseases …
processes. Overexpression of PRMTs has been implicated in various human diseases …
Covalent inhibition of NSD1 histone methyltransferase
The nuclear receptor-binding SET domain (NSD) family of histone methyltransferases is
associated with various malignancies, including aggressive acute leukemia with NUP98 …
associated with various malignancies, including aggressive acute leukemia with NUP98 …
Discovery of a potent, selective, and cell-active dual inhibitor of protein arginine methyltransferase 4 and protein arginine methyltransferase 6
Well-characterized selective inhibitors of protein arginine methyltransferases (PRMTs) are
invaluable chemical tools for testing biological and therapeutic hypotheses. Based on 4, a …
invaluable chemical tools for testing biological and therapeutic hypotheses. Based on 4, a …
Metabolic fuel for epigenetic: nuclear production meets local consumption
R Boon - Frontiers in Genetics, 2021 - frontiersin.org
Epigenetic modifications are responsible for finetuning gene expression profiles to the
needs of cells, tissues, and organisms. To rapidly respond to environmental changes, the …
needs of cells, tissues, and organisms. To rapidly respond to environmental changes, the …
Discovery and characterization of a highly potent and selective aminopyrazoline-based in vivo probe (BAY-598) for the protein lysine methyltransferase SMYD2
E Eggert, RC Hillig, S Koehr, D Stöckigt… - Journal of medicinal …, 2016 - ACS Publications
Protein lysine methyltransferases have recently emerged as a new target class for the
development of inhibitors that modulate gene transcription or signaling pathways. SET and …
development of inhibitors that modulate gene transcription or signaling pathways. SET and …
Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity
ASH1L histone methyltransferase plays a crucial role in the pathogenesis of different
diseases, including acute leukemia. While ASH1L represents an attractive drug target …
diseases, including acute leukemia. While ASH1L represents an attractive drug target …