Molecular pathogenesis of Merkel cell carcinoma

JA DeCaprio - Annual Review of Pathology: Mechanisms of …, 2021 - annualreviews.org
Merkel cell carcinoma (MCC) is an aggressive neuroendocrine carcinoma of the skin with
two distinct etiologies. Clonal integration of Merkel cell polyomavirus DNA into the tumor …

Pharmacological inhibition of LSD1 for cancer treatment

GJ Yang, PM Lei, SY Wong, DL Ma, CH Leung - Molecules, 2018 - mdpi.com
Lysine-specific demethylase 1A (LSD1, also named KDM1A) is a demethylase that can
remove methyl groups from histones H3K4me1/2 and H3K9me1/2. It is aberrantly expressed …

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 …

A PML/RARα direct target atlas redefines transcriptional deregulation in acute promyelocytic leukemia

Y Tan, X Wang, H Song, Y Zhang… - Blood, The Journal …, 2021 - ashpublications.org
Transcriptional deregulation initiated by oncogenic fusion proteins plays a vital role in
leukemia. The prevailing view is that the oncogenic fusion protein promyelocytic …

Therapeutic potential of targeting LSD1/KDM1A in cancers

X Zhang, X Wang, T Wu, W Yin, J Yan, Y Sun… - Pharmacological …, 2022 - Elsevier
LSD1 was the first histone demethylase identified by Professor Shi Yang and his team
members in 2004. LSD1 employs FAD as its cofactor, which catalyzes the demethylation of …

Lysine-specific demethylase 1A as a promising target in acute myeloid leukemia

D Magliulo, R Bernardi, S Messina - Frontiers in Oncology, 2018 - frontiersin.org
Acute myeloid leukemia (AML) is a heterogeneous hematopoietic malignancy characterized
by the accumulation of incompletely differentiated progenitor cells (blasts) in the bone …

Lsd1 as a therapeutic target in Gfi1-activated medulloblastoma

C Lee, VA Rudneva, S Erkek, M Zapatka… - Nature …, 2019 - nature.com
Drugs that modify the epigenome are powerful tools for treating cancer, but these drugs
often have pleiotropic effects, and identifying patients who will benefit from them remains a …

Superior efficacy of co-targeting GFI1/KDM1A and BRD4 against AML and post-MPN secondary AML cells

W Fiskus, CP Mill, B Nabet, D Perera, C Birdwell… - Blood cancer …, 2021 - nature.com
There is an unmet need to overcome nongenetic therapy-resistance to improve outcomes in
AML, especially post-myeloproliferative neoplasm (MPN) secondary (s) AML. Studies …

Targeting histone methyltransferase and demethylase in acute myeloid leukemia therapy

G Castelli, E Pelosi, U Testa - OncoTargets and therapy, 2017 - Taylor & Francis
Acute myeloid leukemia (AML) is a clonal disorder of myeloid progenitors characterized by
the acquisition of chromosomal abnormalities, somatic mutations, and epigenetic changes …

Novel dual LSD1/HDAC6 inhibitor for the treatment of cancer

C Gajendran, SJ Tantry, Z Mohammed, P Dewang… - Plos one, 2023 - journals.plos.org
Dually targeting the epigenetic proteins lysine specific demethylase 1 (LSD1) and histone
deacetylases (HDACs) that play a key role in cancer cells by modulating gene repressor …