Targeting transcription factors in cancer—from undruggable to reality

JH Bushweller - Nature Reviews Cancer, 2019 - nature.com
Mutated or dysregulated transcription factors represent a unique class of drug targets that
mediate aberrant gene expression, including blockade of differentiation and cell death gene …

[HTML][HTML] RUNX1 and cancer

TC Lin - Biochimica et biophysica acta (BBA)-reviews on cancer, 2022 - Elsevier
Runt-related transcription factor 1 (RUNX1) is frequently involved in the progression of acute
leukemia. However, emerging and discoverable RUNX1 somatic mutations, RUNX1 …

Precision medicine treatment in acute myeloid leukemia using prospective genomic profiling: feasibility and preliminary efficacy of the Beat AML Master Trial

A Burd, RL Levine, AS Ruppert, AS Mims, U Borate… - Nature medicine, 2020 - nature.com
Acute myeloid leukemia (AML) is the most common diagnosed leukemia. In older adults,
AML confers an adverse outcome,. AML originates from a dominant mutation, then acquires …

Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies

Y He, S Khan, Z Huo, D Lv, X Zhang, X Liu… - Journal of Hematology & …, 2020 - Springer
Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that
utilize the ubiquitin proteasome system (UPS) to degrade proteins of interest (POI) …

Secondary leukemia in patients with germline transcription factor mutations (RUNX1, GATA2, CEBPA)

AL Brown, CN Hahn, HS Scott - Blood, The Journal of the …, 2020 - ashpublications.org
Recognition that germline mutations can predispose individuals to blood cancers, often
presenting as secondary leukemias, has largely been driven in the last 20 years by studies …

Effective therapy for AML with RUNX1 mutation by cotreatment with inhibitors of protein translation and BCL2

CP Mill, W Fiskus, CD DiNardo… - Blood, The Journal …, 2022 - ashpublications.org
The majority of RUNX1 mutations in acute myeloid leukemia (AML) are missense or deletion-
truncation and behave as loss-of-function mutations. Following standard therapy, AML …

Translating recent advances in the pathogenesis of acute myeloid leukemia to the clinic

JP Bewersdorf, O Abdel-Wahab - Genes & Development, 2022 - genesdev.cshlp.org
Despite FDA approval of nine new drugs for patients with acute myeloid leukemia (AML) in
the United States over the last 4 years, AML remains a major area of unmet medical need …

Hereditary platelet disorders associated with germ line variants in RUNX1, ETV6, and ANKRD26

CC Homan, HS Scott, AL Brown - Blood, 2023 - ashpublications.org
Hereditary platelet disorders (HPDs) are a group of blood disorders with variable severity
and clinical impact. Although phenotypically there is much overlap, known genetic causes …

Targeting of epigenetic co-dependencies enhances anti-AML efficacy of Menin inhibitor in AML with MLL1-r or mutant NPM1

W Fiskus, CP Mill, C Birdwell, JA Davis, K Das… - Blood cancer …, 2023 - nature.com
Monotherapy with Menin inhibitor (MI), eg, SNDX-5613, induces clinical remissions in
patients with relapsed/refractory AML harboring MLL1-r or mtNPM1, but most patients either …

Recent Advances in Transcription Factors Biomarkers and Targeted Therapies Focusing on Epithelial–Mesenchymal Transition

KT Chuang, SS Chiou, SH Hsu - Cancers, 2023 - mdpi.com
Simple Summary The study discusses the potential of targeting transcription factors (TFs) for
cancer therapy and provide a systematic classification of various types of TFs involved in the …