Pharmacological targeting of the cancer epigenome

NW Mabe, JA Perry, CF Malone, K Stegmaier - Nature Cancer, 2024 - nature.com
Epigenetic dysregulation is increasingly appreciated as a hallmark of cancer, including
disease initiation, maintenance and therapy resistance. As a result, there have been …

How I treat refractory and relapsed acute myeloid leukemia

F Thol, H Döhner, A Ganser - Blood, 2024 - ashpublications.org
Most patients with acute myeloid leukemia (AML) develop refractory/relapsed (R/R) disease
even in the presence of novel and targeted therapies. Given the biological complexity of the …

MEN1 mutations mediate clinical resistance to menin inhibition

F Perner, EM Stein, DV Wenge, S Singh, J Kim… - Nature, 2023 - nature.com
Chromatin-binding proteins are critical regulators of cell state in haematopoiesis,. Acute
leukaemias driven by rearrangement of the mixed lineage leukaemia 1 gene (KMT2A r) or …

A new genomic framework to categorize pediatric acute myeloid leukemia

M Umeda, J Ma, T Westover, Y Ni, G Song… - Nature Genetics, 2024 - nature.com
Recent studies on pediatric acute myeloid leukemia (pAML) have revealed pediatric-specific
driver alterations, many of which are underrepresented in the current classification schemas …

Menin Inhibition With Revumenib for KMT2A-Rearranged Relapsed or Refractory Acute Leukemia (AUGMENT-101)

GC Issa, I Aldoss, MJ Thirman, J DiPersio… - Journal of clinical …, 2025 - ascopubs.org
PURPOSE Revumenib, an oral, small molecule inhibitor of the menin-lysine
methyltransferase 2A (KMT2A) interaction, showed promising efficacy and safety in a phase …

Rearrangements involving 11q23.3/KMT2A in adult AML: mutational landscape and prognostic implications – a HARMONY study

A Hernández-Sánchez, T González, M Sobas, E Sträng… - Leukemia, 2024 - nature.com
Balanced rearrangements involving the KMT2A gene (KMT2A r) are recurrent genetic
abnormalities in acute myeloid leukemia (AML), but there is lack of consensus regarding the …

Ziftomenib in relapsed or refractory acute myeloid leukaemia (KOMET-001): A multicentre, open-label, multi-cohort, phase 1 trial

ES Wang, GC Issa, HP Erba, JK Altman… - The Lancet …, 2024 - thelancet.com
Summary Background Ziftomenib (KO-539) is an oral selective menin inhibitor with known
preclinical activity in menin-dependent acute myeloid leukaemia models. The primary …

Epigenetic therapies targeting histone lysine methylation: complex mechanisms and clinical challenges

S Gold, A Shilatifard - The Journal of Clinical Investigation, 2024 - jci.org
As epigenetic therapies continue to gain ground as potential treatment strategies for cancer
and other diseases, compounds that target histone lysine methylation and the enzyme …

CRISPR–ChIP reveals selective regulation of H3K79me2 by Menin in MLL leukemia

O Gilan, L Talarmain, CC Bell, D Neville… - Nature Structural & …, 2023 - nature.com
Chromatin regulation involves the selective recruitment of chromatin factors to facilitate DNA
repair, replication and transcription. Here we demonstrate the utility of coupling unbiased …

Current status and research directions in acute myeloid leukemia

H Kantarjian, G Borthakur, N Daver, CD DiNardo… - Blood cancer …, 2024 - nature.com
The understanding of the molecular pathobiology of acute myeloid leukemia (AML) has
spurred the identification of therapeutic targets and the development of corresponding novel …