Advances in acute myeloid leukemia differentiation therapy: A critical review

AK Abdel-Aziz - Biochemical Pharmacology, 2023 - Elsevier
Acute myeloid leukemia (AML) is characterized by impaired differentiation and indefinite
proliferation of abnormal myeloid progenitors. Although differentiating agents were deemed …

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 …

Activity of menin inhibitor ziftomenib (KO-539) as monotherapy or in combinations against AML cells with MLL1 rearrangement or mutant NPM1

W Fiskus, N Daver, S Boettcher, CP Mill, K Sasaki… - Leukemia, 2022 - nature.com
In MLL1-rearranged AML (MLL1-r), the MLL1 fusion protein (MLLFP) causes dysregulated
expression of HOXA9, MEIS1, PBX3, MEF2C and CDK6 [1, 2]. HOXA9 and its co-factor …

Identification and classification of papain-like cysteine proteinases

F Ozhelvaci, K Steczkiewicz - Journal of Biological Chemistry, 2023 - ASBMB
Papain-like cysteine peptidases form a big and highly diverse superfamily of proteins
involved in many important biological functions, such as protein turnover, deubiquitination …

[HTML][HTML] TALE transcription factors: Cofactors no more

N Bobola, CG Sagerström - Seminars in Cell & Developmental Biology, 2024 - Elsevier
Abstract Exd/PBX, Hth/MEIS and PREP proteins belong to the TALE (three-amino-acid loop
extension) superclass of transcription factors (TFs) with an atypical homedomain (HD) …

A molecular switch between mammalian MLL complexes dictates response to Menin–MLL inhibition

YM Soto-Feliciano, FJ Sánchez-Rivera, F Perner… - Cancer discovery, 2023 - AACR
Menin interacts with oncogenic MLL1-fusion proteins, and small molecules that disrupt these
associations are in clinical trials for leukemia treatment. By integrating chromatin-focused …

Targeting cytohesin-1 suppresses acute myeloid leukemia progression and overcomes resistance to ABT-199

W Ren, H Guo, S Lin, S Chen, Y Long, L Xu… - Acta Pharmacologica …, 2024 - nature.com
Adhesion molecules play essential roles in the homeostatic regulation and malignant
transformation of hematopoietic cells. The dysregulated expression of adhesion molecules …

[HTML][HTML] Menin inhibitor ziftomenib (KO-539) synergizes with drugs targeting chromatin regulation or apoptosis and sensitizes acute myeloid leukemia with MLL …

J Rausch, MM Dzama, N Dolgikh, HL Stiller… - …, 2023 - ncbi.nlm.nih.gov
Acute myeloid leukemia (AML) represents a genetically heterogeneous group of myeloid
neoplasms derived from early hematopoietic progenitors. Mutations in the NPM1 gene and …

[HTML][HTML] Advances in molecular characterization of pediatric acute megakaryoblastic leukemia not associated with Down syndrome; impact on therapy development

J Li, ML Kalev‐Zylinska - Frontiers in Cell and Developmental Biology, 2023 - frontiersin.org
Acute megakaryoblastic leukemia (AMKL) is a rare subtype of acute myeloid leukemia
(AML) in which leukemic blasts have megakaryocytic features. AMKL makes up 4-15% of …

Mezigdomide is effective alone and in combination with menin inhibition in preclinical models of KMT2A-r and NPM1c AML

W Bourgeois, JA Cutler, BJ Aubrey, DV Wenge… - Blood, 2024 - ashpublications.org
Small molecules that target the menin-KMT2A protein-protein interaction (menin inhibitors)
have recently entered clinical trials in lysine methyltransferase 2A (KMT2A or MLL1) …