Targeting mitochondrial respiration for the treatment of acute myeloid leukemia

Dual metabolic reprogramming by ONC201/TIC10 and 2-Deoxyglucose induces energy depletion and synergistic anti-cancer activity in glioblastoma

(2020) Maximilian Pruss et al.   BRITISH JOURNAL OF CANCER

Imipridone Anticancer Compounds Ectopically Activate the ClpP Protease and Represent a New Scaffold for Antibiotic Development

(2020) Samuel Jacques et al.   GENETICS

Fatty Acid Metabolism, Bone Marrow Adipocytes, and AML

(2020) Yoko Tabe et al.   Frontiers in Oncology

IACS-010759, a potent inhibitor of glycolysis-deficient hypoxic tumor cells, inhibits mitochondrial respiratory complex I through a unique mechanism

(2020) Atsuhito Tsuji et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Utilizing Synergistic Potential of Mitochondria-Targeting Drugs for Leukemia Therapy

(2020) Svetlana B. Panina et al.   Frontiers in Oncology

Voltage-Dependent Anion Channels Influence Cytotoxicity of ME-344, a Therapeutic Isoflavone

(2020) Leilei Zhang et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Venetoclax causes metabolic reprogramming independent of BCL-2 inhibition

(2020) Alba Roca-Portoles et al.   Cell Death & Disease

Patterns of care and clinical outcomes with cytarabine-anthracycline induction chemotherapy for AML patients in the United States

(2020) Amer M. Zeidan et al.   Blood Advances

Cotargeting of Mitochondrial Complex I and Bcl-2 Shows Antileukemic Activity against Acute Myeloid Leukemia Cells Reliant on Oxidative Phosphorylation

(2020) Fangbing Liu et al.   Cancers

Inhibition of Amino Acid Metabolism Selectively Targets Human Leukemia Stem Cells

(2019) Courtney L. Jones et al.   CANCER CELL

Mitochondrial Protease ClpP is a Target for the Anticancer Compounds ONC201 and Related Analogues

(2019) Paul R. Graves et al.   ACS Chemical Biology

Mitochondrial ClpP-Mediated Proteolysis Induces Selective Cancer Cell Lethality

(2019) Jo Ishizawa et al.   CANCER CELL

The Direct Molecular Target for Imipridone ONC201 Is Finally Established

(2019) Shaomeng Wang et al.   CANCER CELL

Imipridone ONC212 activates orphan G protein-coupled receptor GPR132 and integrated stress response in acute myeloid leukemia

(2019) Takenobu Nii et al.   LEUKEMIA

Metabolic reprogramming toward oxidative phosphorylation identifies a therapeutic target for mantle cell lymphoma

(2019) Liang Zhang et al.   Science Translational Medicine

Energy metabolism and drug response in myeloid leukaemic stem cells

(2019) Alfonso E. Bencomo-Alvarez et al.   BRITISH JOURNAL OF HAEMATOLOGY

Isoflavone ME-344 disrupts redox homeostasis and mitochondrial function by targeting Heme Oxygenase 1.

(2019) Leilei Zhang et al.   CANCER RESEARCH

Immunotherapy-Based Targeting and Elimination of Leukemic Stem Cells in AML and CML

(2019) Peter Valent et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Randomized Phase 0/I Trial of the Mitochondrial Inhibitor ME-344 or Placebo Added to Bevacizumab in Early HER2-Negative Breast Cancer

(2019) Miguel Quintela-Fandino et al.   CLINICAL CANCER RESEARCH

Can we selectively target AML stem cells?

(2019) Craig T. Jordan   BEST PRACTICE & RESEARCH CLINICAL HAEMATOLOGY

ONC201 shows promise in AML treatment

(2018) Holly Edwards et al.   CELL CYCLE

The role of IDH mutations in acute myeloid leukemia

(2018) Guillermo Montalban-Bravo et al.   Future Oncology

An inhibitor of oxidative phosphorylation exploits cancer vulnerability

(2018) Jennifer R. Molina et al.   NATURE MEDICINE

ONC201 kills breast cancer cells in vitro by targeting mitochondria

(2018) Yoshimi Endo Greer et al.   Oncotarget

Biological and metabolic effects of IACS-010759, an OxPhos inhibitor, on chronic lymphocytic leukemia cells

(2018) Hima V. Vangapandu et al.   Oncotarget

Role of Dopamine Receptors in the Anticancer Activity of ONC201

(2018) Christina Leah B. Kline et al.   NEOPLASIA

Venetoclax combined with decitabine or azacitidine in treatment-naive, elderly patients with acute myeloid leukemia

(2018) Courtney D. DiNardo et al.   BLOOD

Inhibition of Amino Acid Metabolism Selectively Targets Human Leukemia Stem Cells

(2018) Courtney L. Jones et al.   CANCER CELL

Venetoclax with azacitidine disrupts energy metabolism and targets leukemia stem cells in patients with acute myeloid leukemia

(2018) Daniel A. Pollyea et al.   NATURE MEDICINE

Phase Ib study of the mitochondrial inhibitor ME-344 plus topotecan in patients with previously treated, locally advanced or metastatic small cell lung, ovarian and cervical cancers

(2017) Jennifer R. Diamond et al.   INVESTIGATIONAL NEW DRUGS

Tracing the origins of relapse in acute myeloid leukaemia to stem cells

(2017) Liran I. Shlush et al.   NATURE

CD99 is a therapeutic target on disease stem cells in myeloid malignancies

(2017) Stephen S. Chung et al.   Science Translational Medicine

ONC201 activates ER stress to inhibit the growth of triple-negative breast cancer cells

(2017) Xun Yuan et al.   Oncotarget

A phase 2 study of the first imipridone ONC201, a selective DRD2 antagonist for oncology, administered every three weeks in recurrent glioblastoma

(2017) Isabel Arrillaga-Romany et al.   Oncotarget

Evolution of acute myelogenous leukemia stem cell properties after treatment and progression

(2016) T.-C. Ho et al.   BLOOD

ONC201 kills solid tumor cells by triggering an integrated stress response dependent on ATF4 activation by specific eIF2α kinases

(2016) C. Leah B. Kline et al.   Science Signaling

ATF4 induction through an atypical integrated stress response to ONC201 triggers p53-independent apoptosis in hematological malignancies

(2016) Jo Ishizawa et al.   Science Signaling

A novel isoflavone, ME-344, targets the cytoskeleton in acute myeloid leukemia

(2016) Danny V. Jeyaraju et al.   Oncotarget

Discovery and clinical introduction of first-in-class imipridone ONC201

(2016) Joshua E. Allen et al.   Oncotarget

ONC201 kills solid tumor cells by triggering an integrated stress response dependent on ATF4 activation by specific eIF2α kinases

(2016) C. Leah B. Kline et al.   Science Signaling

ATF4 induction through an atypical integrated stress response to ONC201 triggers p53-independent apoptosis in hematological malignancies

(2016) Jo Ishizawa et al.   Science Signaling

Characteristics, clinical outcome, and prognostic significance of IDH mutations in AML

(2015) Courtney D. DiNardo et al.   AMERICAN JOURNAL OF HEMATOLOGY

AML cells have low spare reserve capacity in their respiratory chain that renders them susceptible to oxidative metabolic stress

(2015) S. Sriskanthadevan et al.   BLOOD

Inhibition of the Mitochondrial Protease ClpP as a Therapeutic Strategy for Human Acute Myeloid Leukemia

(2015) Alicia Cole et al.   CANCER CELL

Mitochondrial dependency in progression of acute myeloid leukemia

(2015) Nandini Pal Basak et al.   MITOCHONDRION

Sp1 and c-Myc modulate drug resistance of leukemia stem cells by regulating survivin expression through the ERK-MSK MAPK signaling pathway

(2015) Yi Zhang et al.   Molecular Cancer

Isocitrate dehydrogenase 1 and 2 mutations induce BCL-2 dependence in acute myeloid leukemia

(2015) Steven M Chan et al.   NATURE MEDICINE

Acute Myeloid Leukemia

(2015) Hartmut Döhner et al.   NEW ENGLAND JOURNAL OF MEDICINE

Oxidative phosphorylation-dependent regulation of cancer cell apoptosis in response to anticancer agents

(2015) N Yadav et al.   Cell Death & Disease

Phase 1, open-label, dose escalation, safety, and pharmacokinetics study of ME-344 as a single agent in patients with refractory solid tumors

(2014) Johanna C. Bendell et al.   CANCER

IDH1 Mutations Alter Citric Acid Cycle Metabolism and Increase Dependence on Oxidative Mitochondrial Metabolism

(2014) A. R. Grassian et al.   CANCER RESEARCH

BCL-2 Inhibition Targets Oxidative Phosphorylation and Selectively Eradicates Quiescent Human Leukemia Stem Cells

(2013) Eleni D. Lagadinou et al.   Cell Stem Cell

Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation

(2013) F. Wang et al.   SCIENCE

Dual Inactivation of Akt and ERK by TIC10 Signals Foxo3a Nuclear Translocation, TRAIL Gene Induction, and Potent Antitumor Effects

(2013) J. E. Allen et al.   Science Translational Medicine

Overexpression of IL-1 receptor accessory protein in stem and progenitor cells and outcome correlation in AML and MDS

(2012) L. Barreyro et al.   BLOOD

Inhibition of Mitochondrial Translation as a Therapeutic Strategy for Human Acute Myeloid Leukemia

(2011) Marko Škrtić et al.   CANCER CELL

Coexistence of LMPP-like and GMP-like Leukemia Stem Cells in Acute Myeloid Leukemia

(2011) Nicolas Goardon et al.   CANCER CELL

Targeting the Mitochondria Activates Two Independent Cell Death Pathways in Ovarian Cancer Stem Cells

(2011) A. B. Alvero et al.   MOLECULAR CANCER THERAPEUTICS

The Common Feature of Leukemia-Associated IDH1 and IDH2 Mutations Is a Neomorphic Enzyme Activity Converting α-Ketoglutarate to 2-Hydroxyglutarate

(2010) Patrick S. Ward et al.   CANCER CELL

TIM-3 Is a Promising Target to Selectively Kill Acute Myeloid Leukemia Stem Cells

(2010) Yoshikane Kikushige et al.   Cell Stem Cell

The Distinct Metabolic Profile of Hematopoietic Stem Cells Reflects Their Location in a Hypoxic Niche

(2010) Tugba Simsek et al.   Cell Stem Cell

IDH1andIDH2Gene Mutations Identify Novel Molecular Subsets Within De Novo Cytogenetically Normal Acute Myeloid Leukemia: A Cancer and Leukemia Group B Study

(2010) Guido Marcucci et al.   JOURNAL OF CLINICAL ONCOLOGY

Identification of Therapeutic Targets for Quiescent, Chemotherapy-Resistant Human Leukemia Stem Cells

(2010) Y. Saito et al.   Science Translational Medicine

NV-128, a novel isoflavone derivative, induces caspase-independent cell death through the Akt/mammalian target of rapamycin pathway

(2009) Ayesha B. Alvero et al.   CANCER

CD47 Is an Adverse Prognostic Factor and Therapeutic Antibody Target on Human Acute Myeloid Leukemia Stem Cells

(2009) Ravindra Majeti et al.   CELL

Monoclonal Antibody-Mediated Targeting of CD123, IL-3 Receptor α Chain, Eliminates Human Acute Myeloid Leukemic Stem Cells

(2009) Liqing Jin et al.   Cell Stem Cell