Drug Repurposing for Targeting Acute Leukemia With KMT2A (MLL)—Gene Rearrangements

Functional reconstruction of human AML reveals stem cell origin and vulnerability of treatment-resistant MLL-rearranged leukemia

(2021) Bernd B. Zeisig et al.   Science Translational Medicine

Convergent organization of aberrant MYB complex controls oncogenic gene expression in acute myeloid leukemia

(2021) Sumiko Takao et al.   eLife

High-throughput drug screening reveals Pyrvinium pamoate as effective candidate against pediatric MLL-rearranged acute myeloid leukemia

(2021) Priscilla Wander et al.   Translational Oncology

Proton pump inhibitors selectively suppress MLL rearranged leukemia cells via disrupting MLL1-WDR5 protein-protein interaction

(2020) Wei-Lin Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Current pharmacological treatments for COVID‐19: What's next?

(2020) Cristina Scavone et al.   BRITISH JOURNAL OF PHARMACOLOGY

Drug repurposing approach to fight COVID-19

(2020) Thakur Uttam Singh et al.   Pharmacological Reports

Thioridazine requires calcium influx to induce MLL-AF6–rearranged AML cell death

(2020) Claudia Tregnago et al.   Blood Advances

Human MLL/KMT2A gene exhibits a second breakpoint cluster region for recurrent MLL–USP2 fusions

(2019) Claus Meyer et al.   LEUKEMIA

The AAA+ATPase RUVBL2 is essential for the oncogenic function of c-MYB in acute myeloid leukemia

(2019) Elena Armenteros-Monterroso et al.   LEUKEMIA

Outcome of Infants Younger Than 1 Year With Acute Lymphoblastic Leukemia Treated With the Interfant-06 Protocol: Results From an International Phase III Randomized Study

(2019) Rob Pieters et al.   JOURNAL OF CLINICAL ONCOLOGY

SETD1A protects from senescence through regulation of the mitotic gene expression program

(2019) Ken Tajima et al.   Nature Communications

Rewiring the Epigenetic Networks in MLL-Rearranged Leukemias: Epigenetic Dysregulation and Pharmacological Interventions

(2019) Anthony K. N. Chan et al.   Frontiers in Cell and Developmental Biology

Co-inhibition of HDAC and MLL-menin interaction targets MLL-rearranged acute myeloid leukemia cells via disruption of DNA damage checkpoint and DNA repair

(2019) Jing Ye et al.   Clinical Epigenetics

A Non-catalytic Function of SETD1A Regulates Cyclin K and the DNA Damage Response

(2018) Takayuki Hoshii et al.   CELL

Anlotinib: First Global Approval

(2018) Yahiya Y. Syed   DRUGS

Inactivation of DNA-PK by knockdown DNA-PKcs or NU7441 impairs non-homologous end-joining of radiation-induced double strand break repair

(2018) Jun Dong et al.   ONCOLOGY REPORTS

Anthelmintic pyrvinium pamoate blocks Wnt/β-catenin and induces apoptosis in multiple myeloma cells

(2018) Fang Xu et al.   Oncology Letters

Peptidomimetic blockade of MYB in acute myeloid leukemia

(2018) Kavitha Ramaswamy et al.   Nature Communications

CDK6 Antagonizes p53-Induced Responses during Tumorigenesis

(2018) Florian Bellutti et al.   Cancer Discovery

Stabilization of NF-κB-Inducing Kinase Suppresses MLL-AF9-Induced Acute Myeloid Leukemia

(2018) Yan Xiu et al.   Cell Reports

Anlotinib induces hepatocellular carcinoma apoptosis and inhibits proliferation via Erk and Akt pathway

(2018) Chao He et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Anlotinib: a novel multi-targeting tyrosine kinase inhibitor in clinical development

(2018) Guoshuang Shen et al.   Journal of Hematology & Oncology

Effect of Anlotinib as a Third-Line or Further Treatment on Overall Survival of Patients With Advanced Non–Small Cell Lung Cancer

(2018) Baohui Han et al.   JAMA Oncology

Drug repurposing: progress, challenges and recommendations

(2018) Sudeep Pushpakom et al.   NATURE REVIEWS DRUG DISCOVERY

ATR inhibition disrupts rewired homologous recombination and fork protection pathways in PARP inhibitor-resistant BRCA-deficient cancer cells

(2017) Stephanie A. Yazinski et al.   GENES & DEVELOPMENT

The MLL recombinome of acute leukemias in 2017

(2017) C Meyer et al.   LEUKEMIA

Targeting acute myeloid leukemia by drug-induced c-MYB degradation

(2017) V Walf-Vorderwülbecke et al.   LEUKEMIA

Antileukemic activity and cellular effects of the antimalarial agent artesunate in acute myeloid leukemia

(2017) Bijender Kumar et al.   LEUKEMIA RESEARCH

Opportunities and challenges in phenotypic drug discovery: an industry perspective

(2017) John G. Moffat et al.   NATURE REVIEWS DRUG DISCOVERY

Data Portal for the Library of Integrated Network-based Cellular Signatures (LINCS) program: integrated access to diverse large-scale cellular perturbation response data

(2017) Amar Koleti et al.   NUCLEIC ACIDS RESEARCH

CC-115, a dual inhibitor of mTOR Kinase and DNA-PK, blocks DNA damage repair pathways and selectively inhibits ATM-deficient cell growth in vitro

(2017) Toshiya Tsuji et al.   Oncotarget

GEAR: A database of Genomic Elements Associated with drug Resistance

(2017) Yin-Ying Wang et al.   Scientific Reports

MLL-Rearranged Leukemias—An Update on Science and Clinical Approaches

(2017) Amanda C. Winters et al.   Frontiers in Pediatrics

First-in-human trial of a poly(ADP-ribose) polymerase (PARP) inhibitor MK-4827 in advanced cancer patients (pts) with antitumor activity in BRCA-deficient and sporadic ovarian cancers.

(2017) S. K. Sandhu et al.   JOURNAL OF CLINICAL ONCOLOGY

Pyrvinium selectively induces apoptosis of lymphoma cells through impairing mitochondrial functions and JAK2/STAT5

(2016) Meifang Xiao et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Dual TORK/DNA-PK inhibition blocks critical signaling pathways in chronic lymphocytic leukemia

(2016) R. Thijssen et al.   BLOOD

Non-Photoinduced Biological Properties of Verteporfin

(2016) Floriane Gibault et al.   CURRENT MEDICINAL CHEMISTRY

PARP-inhibitor-induced synthetic lethality for acute myeloid leukemia treatment

(2016) Lu Zhao et al.   EXPERIMENTAL HEMATOLOGY

Safety, pharmacokinetics, and antitumor properties of anlotinib, an oral multi-target tyrosine kinase inhibitor, in patients with advanced refractory solid tumors

(2016) Yongkun Sun et al.   Journal of Hematology & Oncology

Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein–Protein Interaction between Menin and Mixed Lineage Leukemia (MLL)

(2016) Dmitry Borkin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Repurposing of approved cardiovascular drugs

(2016) Junichi Ishida et al.   Journal of Translational Medicine

Can you teach old drugs new tricks?

(2016) Nicola Nosengo   NATURE

Identification of novel small-molecule inhibitors targeting menin–MLL interaction, repurposing the antidiarrheal loperamide

(2016) Liyan Yue et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

The photosensitizer verteporfin has light-independent anti-leukemic activity for Ph-positive acute lymphoblastic leukemia and synergistically works with dasatinib

(2016) Takanobu Morishita et al.   Oncotarget

Progress towards small molecule menin-mixed lineage leukemia (MLL) interaction inhibitors with in vivo utility

(2015) Timothy Senter et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeting acute myeloid leukemia with a small molecule inhibitor of the Myb/p300 interaction

(2015) Sagar Uttarkar et al.   BLOOD

CDK6 Levels Regulate Quiescence Exit in Human Hematopoietic Stem Cells

(2015) Elisa Laurenti et al.   Cell Stem Cell

Menin-MLL inhibitors block oncogenic transformation by MLL-fusion proteins in a fusion partner-independent manner

(2015) S He et al.   LEUKEMIA

Trends in survival outcomes of B-lineage acute lymphoblastic leukemia in elderly patients: analysis of Surveillance, Epidemiology, and End Results database

(2015) Guru Subramanian Guru Murthy et al.   LEUKEMIA & LYMPHOMA

Synthetic lethal targeting of oncogenic transcription factors in acute leukemia by PARP inhibitors

(2015) Maria Teresa Esposito et al.   NATURE MEDICINE

Glycogen synthase kinase-3 (GSK3): Regulation, actions, and diseases

(2015) Eleonore Beurel et al.   PHARMACOLOGY & THERAPEUTICS

ATM and ATR as therapeutic targets in cancer

(2015) Anika Maria Weber et al.   PHARMACOLOGY & THERAPEUTICS

Pyrvinium selectively targets blast phase-chronic myeloid leukemia through inhibition of mitochondrial respiration

(2015) Wei Xiang et al.   Oncotarget

Requirement for CDK6 in MLL-rearranged acute myeloid leukemia

(2014) T. Placke et al.   BLOOD

MLL fusion-driven activation ofCDK6potentiates proliferation inMLL-rearranged infant ALL

(2014) Marieke Van der Linden et al.   CELL CYCLE

Mll2 is required for H3K4 trimethylation on bivalent promoters in embryonic stem cells, whereas Mll1 is redundant

(2014) S. Denissov et al.   DEVELOPMENT

The H3K4 methyltransferase Setd1a is first required at the epiblast stage, whereas Setd1b becomes essential after gastrulation

(2014) A. S. Bledau et al.   DEVELOPMENT

Targeting MLL1 H3K4 Methyltransferase Activity in Mixed-Lineage Leukemia

(2014) Fang Cao et al.   MOLECULAR CELL

DNA-damage-induced differentiation of leukaemic cells as an anti-cancer barrier

(2014) Margarida A. Santos et al.   NATURE

Distinct pathways regulated by menin and by MLL1 in hematopoietic stem cells and developing B cells

(2013) B. E. Li et al.   BLOOD

DNA-PK inhibition by NU7441 sensitizes breast cancer cells to ionizing radiation and doxorubicin

(2013) Wojciech M. Ciszewski et al.   BREAST CANCER RESEARCH AND TREATMENT

A Kinase-Independent Function of CDK6 Links the Cell Cycle to Tumor Angiogenesis

(2013) Karoline Kollmann et al.   CANCER CELL

BMN 673, a Novel and Highly Potent PARP1/2 Inhibitor for the Treatment of Human Cancers with DNA Repair Deficiency

(2013) Y. Shen et al.   CLINICAL CANCER RESEARCH

Mixed lineage leukemia protein in normal and leukemic stem cells

(2013) Bon Ham Yip et al.   EXPERIMENTAL BIOLOGY AND MEDICINE

Palbociclib (PD 0332991): targeting the cell cycle machinery in breast cancer

(2013) Andrea Rocca et al.   EXPERT OPINION ON PHARMACOTHERAPY

RUNX1 meets MLL: epigenetic regulation of hematopoiesis by two leukemia genes

(2013) C P Koh et al.   LEUKEMIA

PARP-1 and gene regulation: Progress and puzzles

(2013) W. Lee Kraus et al.   MOLECULAR ASPECTS OF MEDICINE

Mutational landscape and significance across 12 major cancer types

(2013) Cyriac Kandoth et al.   NATURE

The NHGRI GWAS Catalog, a curated resource of SNP-trait associations

(2013) Danielle Welter et al.   NUCLEIC ACIDS RESEARCH

Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay

(2013) D. M. Molina et al.   SCIENCE

Therapeutic Targeting of a Robust Non-Oncogene Addiction to PRKDC in ATM-Defective Tumors

(2013) A. Riabinska et al.   Science Translational Medicine

Lithium chloride attenuates cell death in oculopharyngeal muscular dystrophy by perturbing Wnt/β-catenin pathway

(2013) A Abu-Baker et al.   Cell Death & Disease

Structural insights into inhibition of the bivalent menin-MLL interaction by small molecules in leukemia

(2012) A. Shi et al.   BLOOD

DNA Damage Response and Inflammatory Signaling Limit the MLL-ENL-Induced Leukemogenesis In Vivo

(2012) Sylvia Takacova et al.   CANCER CELL

Molecular dynamics simulations and statistical coupling analysis reveal functional coevolution network of oncogenic mutations in the CDKN2A-CDK6 complex

(2012) Jingwen Wang et al.   FEBS LETTERS

High-Affinity, Small-Molecule Peptidomimetic Inhibitors of MLL1/WDR5 Protein–Protein Interaction

(2012) Hacer Karatas et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Role and potential for therapeutic targeting of MYB in leukemia

(2012) D R Pattabiraman et al.   LEUKEMIA

Reprogramming cellular events by poly(ADP-ribose)-binding proteins

(2012) Jana Krietsch et al.   MOLECULAR ASPECTS OF MEDICINE

Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia

(2012) Jolanta Grembecka et al.   Nature Chemical Biology

Diagnosing the decline in pharmaceutical R&D efficiency

(2012) Jack W. Scannell et al.   NATURE REVIEWS DRUG DISCOVERY

Safety and efficacy of fidaxomicin in the treatment of Clostridium difficile-associated diarrhea

(2012) Yoav Golan et al.   Therapeutic Advances in Gastroenterology

Functional Crosstalk between Bmi1 and MLL/Hoxa9 Axis in Establishment of Normal Hematopoietic and Leukemic Stem Cells

(2011) Lan-Lan Smith et al.   Cell Stem Cell

An integrated approach to dissecting oncogene addiction implicates a Myb-coordinated self-renewal program as essential for leukemia maintenance

(2011) J. Zuber et al.   GENES & DEVELOPMENT

Oncogenic stress sensitizes murine cancers to hypomorphic suppression of ATR

(2011) David W. Schoppy et al.   JOURNAL OF CLINICAL INVESTIGATION

Mitoxantrone in combination with an inhibitor of DNA-dependent protein kinase: a potential therapy for high risk B-cell chronic lymphocytic leukaemia

(2010) Sarah L. Elliott et al.   BRITISH JOURNAL OF HAEMATOLOGY

MLL-AF9-Induced Leukemogenesis Requires Coexpression of the Wild-Type Mll Allele

(2010) Austin T. Thiel et al.   CANCER CELL

GSK-3 Promotes Conditional Association of CREB and Its Coactivators with MEIS1 to Facilitate HOX-Mediated Transcription and Oncogenesis

(2010) Zhong Wang et al.   CANCER CELL

β-Catenin Mediates the Establishment and Drug Resistance of MLL Leukemic Stem Cells

(2010) Jenny Yeung et al.   CANCER CELL

Reversing HOXA9 Oncogene Activation by PI3K Inhibition: Epigenetic Mechanism and Prognostic Significance in Human Glioblastoma

(2010) B. M. Costa et al.   CANCER RESEARCH

Cytogenetics of Childhood Acute Myeloid Leukemia: United Kingdom Medical Research Council Treatment Trials AML 10 and 12

(2010) Christine J. Harrison et al.   JOURNAL OF CLINICAL ONCOLOGY

Hierarchical Maintenance of MLL Myeloid Leukemia Stem Cells Employs a Transcriptional Program Shared with Embryonic Rather Than Adult Stem Cells

(2009) Tim C.P. Somervaille et al.   Cell Stem Cell

PARP is activated at stalled forks to mediate Mre11-dependent replication restart and recombination

(2009) Helen E Bryant et al.   EMBO JOURNAL

3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione (SB216763), a Glycogen Synthase Kinase-3 Inhibitor, Displays Therapeutic Properties in a Mouse Model of Pulmonary Inflammation and Fibrosis

(2009) C. Gurrieri et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Lessons from 60 years of pharmaceutical innovation

(2009) Bernard Munos   NATURE REVIEWS DRUG DISCOVERY

Thalidomide for treatment of multiple myeloma: 10 years later

(2008) A. Palumbo et al.   BLOOD

Selective Inhibition of BRCA2-Deficient Mammary Tumor Cell Growth by AZD2281 and Cisplatin

(2008) B. Evers et al.   CLINICAL CANCER RESEARCH

Interaction between S100A8/A9 and Annexin A6 Is Involved in the Calcium-induced Cell Surface Exposition of S100A8/A9

(2008) Günther Bode et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Glycogen synthase kinase 3 in MLL leukaemia maintenance and targeted therapy

(2008) Zhong Wang et al.   NATURE