Roles and regulation of histone methylation in animal development

A Jambhekar, A Dhall, Y Shi - Nature reviews Molecular cell biology, 2019 - nature.com
Histone methylation can occur at various sites in histone proteins, primarily on lysine and
arginine residues, and it can be governed by multiple positive and negative regulators, even …

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 …

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 …

A DNA hypomethylation signature predicts antitumor activity of LSD1 inhibitors in SCLC

HP Mohammad, KN Smitheman, CD Kamat, D Soong… - Cancer cell, 2015 - cell.com
Epigenetic dysregulation has emerged as an important mechanism in cancer. Alterations in
epigenetic machinery have become a major focus for targeted therapies. The current report …

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 …

LSD1: more than demethylation of histone lysine residues

B Perillo, A Tramontano, A Pezone… - Experimental & molecular …, 2020 - nature.com
Lysine-specific histone demethylase 1 (LSD1) represents the first example of an identified
nuclear protein with histone demethylase activity. In particular, it plays a special role in the …

LSD1 activates a lethal prostate cancer gene network independently of its demethylase function

A Sehrawat, L Gao, Y Wang… - Proceedings of the …, 2018 - National Acad Sciences
Medical castration that interferes with androgen receptor (AR) function is the principal
treatment for advanced prostate cancer. However, clinical progression is universal, and …

Targeting epigenetics in cancer

RL Bennett, JD Licht - Annual review of pharmacology and …, 2018 - annualreviews.org
Alterations of genes regulating epigenetic processes are frequently found as cancer drivers
and may cause widespread alterations of DNA methylation, histone modification patterns, or …

Inhibition of LSD1 with bomedemstat sensitizes small cell lung cancer to immune checkpoint blockade and T-cell killing

JB Hiatt, H Sandborg, SM Garrison, HU Arnold… - Clinical Cancer …, 2022 - AACR
Purpose: The addition of immune checkpoint blockade (ICB) to platinum/etoposide
chemotherapy changed the standard of care for small cell lung cancer (SCLC) treatment …

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 …