Same substrate, many reactions: oxygen activation in flavoenzymes

E Romero, JR Gómez Castellanos, G Gadda… - Chemical …, 2018 - ACS Publications
Over time, organisms have evolved strategies to cope with the abundance of dioxygen on
Earth. Oxygen-utilizing enzymes tightly control the reactions involving O2 mostly by …

The enigmatic reaction of flavins with oxygen

P Chaiyen, MW Fraaije, A Mattevi - Trends in biochemical sciences, 2012 - cell.com
The reaction of flavoenzymes with oxygen remains a fascinating area of research because
of its relevance for reactive oxygen species (ROS) generation. Several exciting recent …

ORY-1001, a potent and selective covalent KDM1A inhibitor, for the treatment of acute leukemia

T Maes, C Mascaró, I Tirapu, A Estiarte, F Ciceri… - Cancer cell, 2018 - cell.com
The lysine-specific demethylase KDM1A is a key regulator of stem cell potential in acute
myeloid leukemia (AML). ORY-1001 is a highly potent and selective KDM1A inhibitor that …

Enhancer activation by pharmacologic displacement of LSD1 from GFI1 induces differentiation in acute myeloid leukemia

A Maiques-Diaz, GJ Spencer, JT Lynch, F Ciceri… - Cell reports, 2018 - cell.com
Pharmacologic inhibition of LSD1 promotes blast cell differentiation in acute myeloid
leukemia (AML) with MLL translocations. The assumption has been that differentiation is …

Sperm histone H3 lysine 4 trimethylation is altered in a genetic mouse model of transgenerational epigenetic inheritance

A Lismer, K Siklenka, C Lafleur, V Dumeaux… - Nucleic acids …, 2020 - academic.oup.com
Advancing the molecular knowledge surrounding fertility and inheritance has become
critical given the halving of sperm counts in the last 40 years, and the rise in complex …

Mechanism of crosstalk between the LSD1 demethylase and HDAC1 deacetylase in the CoREST complex

Y Song, L Dagil, L Fairall, N Robertson, M Wu… - Cell Reports, 2020 - cell.com
The transcriptional corepressor complex CoREST is one of seven histone deacetylase
complexes that regulate the genome through controlling chromatin acetylation. The CoREST …

Tranylcypromine based lysine-specific demethylase 1 inhibitor: summary and perspective

XJ Dai, Y Liu, XP Xiong, LP Xue… - Journal of Medicinal …, 2020 - ACS Publications
Histone lysine-specific demethylase 1 (LSD1/KDM1A) has become an important and
promising anticancer target since it was first identified in 2004 and specially demethylates …

LSD1-mediated epigenetic modification contributes to proliferation and metastasis of colon cancer

J Ding, ZM Zhang, Y Xia, GQ Liao, Y Pan, S Liu… - British journal of …, 2013 - nature.com
Background: Emerging evidence has demonstrated that lysine-specific demethylase 1
(LSD1) has an important role in many pathological processes of cancer cells, such as …

CRISPR-suppressor scanning reveals a nonenzymatic role of LSD1 in AML

ME Vinyard, C Su, AP Siegenfeld, AL Waterbury… - Nature chemical …, 2019 - nature.com
Understanding the mechanism of small molecules is a critical challenge in chemical biology
and drug discovery. Medicinal chemistry is essential for elucidating drug mechanism …

Epigenetic regulation of EMT: the Snail story

Y Lin, C Dong, BP Zhou - Current pharmaceutical design, 2014 - ingentaconnect.com
While the epithelial-mesenchymal transition (EMT) plays a fundamental role during
development, its deregulation can adversely promote tumor metastasis. The phenotypic and …