Pharmacological targeting of the cancer epigenome
Epigenetic dysregulation is increasingly appreciated as a hallmark of cancer, including
disease initiation, maintenance and therapy resistance. As a result, there have been …
disease initiation, maintenance and therapy resistance. As a result, there have been …
How I treat refractory and relapsed acute myeloid leukemia
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 …
even in the presence of novel and targeted therapies. Given the biological complexity of the …
MEN1 mutations mediate clinical resistance to menin inhibition
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 …
leukaemias driven by rearrangement of the mixed lineage leukaemia 1 gene (KMT2A r) or …
A new genomic framework to categorize pediatric acute myeloid leukemia
Recent studies on pediatric acute myeloid leukemia (pAML) have revealed pediatric-specific
driver alterations, many of which are underrepresented in the current classification schemas …
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 …
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 …
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 …
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 …
and other diseases, compounds that target histone lysine methylation and the enzyme …
CRISPR–ChIP reveals selective regulation of H3K79me2 by Menin in MLL leukemia
Chromatin regulation involves the selective recruitment of chromatin factors to facilitate DNA
repair, replication and transcription. Here we demonstrate the utility of coupling unbiased …
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 …
spurred the identification of therapeutic targets and the development of corresponding novel …