Immunoproteasome function maintains oncogenic gene expression in KMT2A-complex driven leukemia
N Tubío-Santamaría, AK Jayavelu, TM Schnoeder… - Molecular Cancer, 2023 - Springer
Pharmacologic targeting of chromatin-associated protein complexes has shown significant
responses in KMT2A-rearranged (KMT2A-r) acute myeloid leukemia (AML) but resistance …
responses in KMT2A-rearranged (KMT2A-r) acute myeloid leukemia (AML) but resistance …
Therapeutic targeting of the menin–KMT2A interaction
PR Freire, JA Cutler… - Annual Review of Cancer …, 2024 - annualreviews.org
The direct targeting of chromatin-associated proteins is increasingly recognized as a
potential therapeutic strategy for the treatment of cancer. In this review, we discuss a …
potential therapeutic strategy for the treatment of cancer. In this review, we discuss a …
Distinct Responses to Menin Inhibition and Synergy with DOT1L Inhibition in KMT2A-Rearranged Acute Lymphoblastic and Myeloid Leukemia
FRS Adriaanse, P Schneider… - International Journal of …, 2024 - mdpi.com
Pediatric acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) exhibit
favorable survival rates. However, for AML and ALL patients carrying KMT2A gene …
favorable survival rates. However, for AML and ALL patients carrying KMT2A gene …
Update on a phase 1/2 first-in-human study of the menin-KMT2A (MLL) inhibitor ziftomenib (KO-539) in patients with relapsed or refractory acute myeloid leukemia
HP Erba, AT Fathi, GC Issa, JK Altman, P Montesinos… - Blood, 2022 - ashpublications.org
Abstract Histone-lysine-N-methyltransferase 2A (KMT2A) is a central regulator of target
genes that drive leukemogenic transformation. KMT2A rearrangements (KMT2Ar) and …
genes that drive leukemogenic transformation. KMT2A rearrangements (KMT2Ar) and …
Pharmacological characterization of JNJ-75276617, a menin-KMT2A inhibitor, as targeted treatment for KMT2A-altered and NPM1-mutant acute leukemia
MC Kwon, O Querolle, X Dai, JW Thuring, T Verhulst… - Blood, 2022 - ashpublications.org
Background: AML is characterized by a differentiation block leading to the accumulation of
immature cells. Therefore therapies capable of inducing differentiation of these immature …
immature cells. Therefore therapies capable of inducing differentiation of these immature …
Targeting menin: a promising therapeutic strategy for susceptible acute leukemia subtypes
P Di Fazio - Signal Transduction and Targeted Therapy, 2023 - nature.com
Two recent studies published in Nature focused on the clinical efficacy of the menin inhibitor
revumenib (SNDX-5613) in KMT2A (histone-lysine N-methyltransferase 2A)-rearranged or …
revumenib (SNDX-5613) in KMT2A (histone-lysine N-methyltransferase 2A)-rearranged or …
The menin inhibitor SNDX-5613 (revumenib) leads to durable responses in patients (Pts) with KMT2A-rearranged or NPM1 mutant AML: updated results of a phase …
GC Issa, I Aldoss, JF DiPersio, B Cuglievan, RM Stone… - Blood, 2022 - ashpublications.org
Introduction: The interaction of menin with the epigenetic regulator KMT2A in acute leukemia
with KMT2A rearrangement (KMT2Ar) or mutant NPM1 (mNPM1, NPM1c) leads to …
with KMT2A rearrangement (KMT2Ar) or mutant NPM1 (mNPM1, NPM1c) leads to …
[HTML][HTML] Clinical-Stage Menin Inhibitor KO-539 Is Synergistically Active with Multiple Classes of Targeted Agents in KMT2A-r and NPM1-Mutant AML Models
JA Davis, WC Fiskus, N Daver, CP Mill, C Birdwell… - Blood, 2021 - Elsevier
The N-terminus of the histone-lysine-N-methyltransferase MLL1 (KMT2A) contains the
menin binding domain (MBD). Menin is a scaffold protein that binds to MBD and tethers …
menin binding domain (MBD). Menin is a scaffold protein that binds to MBD and tethers …
[HTML][HTML] Preliminary data on a phase 1/2A first in human study of the menin-KMT2A (MLL) inhibitor KO-539 in patients with relapsed or refractory acute myeloid …
ES Wang, JK Altman, K Pettit, S De Botton, RP Walter… - Blood, 2020 - Elsevier
The histone-lysine-N-methyltransferase 2A (KMT2A) gene (formerly known as mixed-
lineage leukemia (MLL)) plays an essential role in regulating gene expression including …
lineage leukemia (MLL)) plays an essential role in regulating gene expression including …
CBFβ-SMMHC inhibition triggers apoptosis by disrupting MYC chromatin dynamics in acute myeloid leukemia
The fusion oncoprotein CBFβ-SMMHC, expressed in leukemia cases with chromosome 16
inversion, drives leukemia development and maintenance by altering the activity of the …
inversion, drives leukemia development and maintenance by altering the activity of the …