Therapeutic implications of menin inhibition in acute leukemias

GC Issa, F Ravandi, CD DiNardo, E Jabbour… - Leukemia, 2021 - nature.com
Menin inhibitors are novel targeted agents currently in clinical development for the treatment
of genetically defined subsets of acute leukemia. Menin has a tumor suppressor function in …

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 …

[HTML][HTML] The future: genetics advances in MEN1 therapeutic approaches and management strategies

SK Agarwal - Endocrine-related cancer, 2017 - ncbi.nlm.nih.gov
The identification of the multiple endocrine neoplasia type 1 (MEN1) gene in 1997 has
shown that germline heterozygous mutations in the MEN1 gene located on chromosome …

[HTML][HTML] Systematic multi-omics cell line profiling uncovers principles of Ewing sarcoma fusion oncogene-mediated gene regulation

MF Orth, D Surdez, T Faehling, AC Ehlers, A Marchetto… - Cell reports, 2022 - cell.com
Ewing sarcoma (EwS) is characterized by EWSR1-ETS fusion transcription factors
converting polymorphic GGAA microsatellites (mSats) into potent neo-enhancers. Although …

[HTML][HTML] The importance of fusion protein activity in Ewing sarcoma and the cell intrinsic and extrinsic factors that regulate it: A review

AA Apfelbaum, ED Wrenn, ER Lawlor - Frontiers in oncology, 2022 - frontiersin.org
Accumulating evidence shows that despite clonal origins tumors eventually become
complex communities comprised of phenotypically distinct cell subpopulations. This …

[HTML][HTML] Menin‑MLL inhibitors induce ferroptosis and enhance the anti‑proliferative activity of auranofin in several types of cancer cells

I Kato, T Kasukabe, S Kumakura - … Journal of Oncology, 2020 - spandidos-publications.com
Menin‑mixed‑lineage leukemia (MLL) inhibitors have potential for use as therapeutic agents
for MLL‑rearranged leukemia. They are also effective against solid cancers, such as breast …

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 …

Complexity of blocking bivalent protein–protein interactions: development of a highly potent inhibitor of the menin–mixed-lineage leukemia interaction

D Borkin, S Klossowski, J Pollock, H Miao… - Journal of medicinal …, 2018 - ACS Publications
The protein–protein interaction between menin and mixed-lineage leukemia 1 (MLL1) plays
an important role in development of acute leukemia with translocations of the MLL1 gene …

Vascular modulation through exercise improves chemotherapy efficacy in Ewing sarcoma

MBG Morrell, C Alvarez‐Florez, A Zhang… - Pediatric blood & …, 2019 - Wiley Online Library
Recent studies in mouse models of cancer have shown that exercise improves tumor
vascular function, thereby improving chemotherapy delivery and efficacy. However, the …

[HTML][HTML] One oncogene, several vulnerabilities: EWS/FLI targeted therapies for Ewing sarcoma

G Flores, PJ Grohar - Journal of bone oncology, 2021 - Elsevier
EWS/FLI is the defining mutation of Ewing sarcoma. This oncogene drives malignant
transformation and progression and occurs in a genetic background characterized by few …