Hypoxia-Activated Prodrug TH-302 Targets Hypoxic Bone Marrow Niches in Preclinical Leukemia Models

No abstract is available for this paper.

• Publication year

  2015

• Venue

  Clinical Cancer Research

• Publication date

  2015-11-24

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.1158/1078-0432.CCR-14-3378PMID 26603259PMCID PMC4818660
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Phase I/II study of the hypoxia-activated prodrug PR104 in refractory/relapsed acute myeloid leukemia and acute lymphoblastic leukemia

  2015cited by this paper
• Reciprocal leukemia-stroma VCAM-1/VLA-4-dependent activation of NF-κB mediates chemoresistance.

  2014cited by this paper
• Phase II study of the safety and antitumor activity of the hypoxia-activated prodrug TH-302 in combination with doxorubicin in patients with advanced soft tissue sarcoma.

  2014cited by this paper
• Dual Targeting of Hypoxia and Homologous Recombination Repair Dysfunction in Triple-Negative Breast Cancer

  2014cited by this paper
• Metabolic implication of tumor:stroma crosstalk in breast cancer

  2014cited by this paper
• Comparing cancer vs normal gene expression profiles identifies new disease entities and common transcriptional programs in AML patients.

  2014cited by this paper
• Identification of the angiogenic gene signature induced by EGF and hypoxia in colorectal cancer

  2013cited by this paper
• Hypoxia-inducing factors as master regulators of stemness properties and altered metabolism of cancer- and metastasis-initiating cells

  2013cited by this paper
• HIF-2α protects human hematopoietic stem/progenitors and acute myeloid leukemic cells from apoptosis induced by endoplasmic reticulum stress.

  2013cited by this paper
• Hypoxia-inducible factor (HIF)-1α suppression in myeloma cells blocks tumoral growth in vivo inhibiting angiogenesis and bone destruction

  2013cited by this paper
• Activity of the Hypoxia-Activated Prodrug, TH-302, in Preclinical Human Acute Myeloid Leukemia Models

  2013cited by this paper
• A 26-Gene Hypoxia Signature Predicts Benefit from Hypoxia-Modifying Therapy in Laryngeal Cancer but Not Bladder Cancer

  2013cited by this paper
• HIF-1 mediates metabolic responses to intratumoral hypoxia and oncogenic mutations.

  2013cited by this paper
• Metabolic Imaging of Patients with Prostate Cancer Using Hyperpolarized [1-13C]Pyruvate

  2013cited by this paper
• Acute myeloid leukemia: 2013 update on risk‐stratification and management

  2013cited by this paper
• Targeting hypoxia in the leukemia microenvironment.

  2013cited by this paper
• TH-302, a hypoxia-activated prodrug with broad in vivo preclinical combination therapy efficacy: optimization of dosing regimens and schedules

  2012cited by this paper
• Diflavin Oxidoreductases Activate the Bioreductive Prodrug PR-104A under Hypoxia

  2012cited by this paper
• Phase I study of TH-302, a hypoxia-activated cytotoxic prodrug, in subjects with advanced leukemias.

  2012cited by this paper
• Glycolytic Inhibition Alters Anaplastic Thyroid Carcinoma Tumor Metabolism and Improves Response to Conventional Chemotherapy and Radiation

  2012cited by this paper
• Recent advances in hypoxia-inducible factor (HIF)-1 inhibitors.

  2012cited by this paper
• Elevated HIF-1α expression of acute myelogenous leukemia stem cells in the endosteal hypoxic zone may be a cause of minimal residual disease in bone marrow after chemotherapy.

  2012cited by this paper
• Lung Cancer Signature Biomarkers: tissue specific semantic similarity based clustering of Digital Differential Display (DDD) data

  2012cited by this paper
• Roles of the hypoxia response system in hematopoietic and leukemic stem cells

  2012cited by this paper
• Regulation of HIF-1α signaling and chemoresistance in acute lymphocytic leukemia under hypoxic conditions of the bone marrow microenvironment

  2012cited by this paper
• Reciprocal metabolic reprogramming through lactate shuttle coordinately influences tumor-stroma interplay.

  2012cited by this paper
• Hyperpolarized [1-13C]-Ascorbic and Dehydroascorbic Acid: Vitamin C as a Probe for Imaging Redox Status in Vivo

  2011cited by this paper
• Pronounced Hypoxia in Models of Murine and Human Leukemia: High Efficacy of Hypoxia-Activated Prodrug PR-104

  2011cited by this paper
• The 2-Nitroimidazole EF5 Is a Biomarker for Oxidoreductases That Activate the Bioreductive Prodrug CEN-209 under Hypoxia

  2011cited by this paper
• Molecular and Cellular Pharmacology of the Hypoxia-Activated Prodrug TH-302

  2011cited by this paper
• Targeting HIF1α eliminates cancer stem cells in hematological malignancies.

  2011cited by this paper
• Tumor imaging using hyperpolarized 13C magnetic resonance spectroscopy

  2011cited by this paper
• Hypoxia promotes dissemination of multiple myeloma through acquisition of epithelial to mesenchymal transition-like features.

  2011cited by this paper
• Leukemia stem cells and microenvironment: biology and therapeutic targeting.

  2011cited by this paper
• Targeting multiple signal pathways simultaneously might provide effective therapeutic strategies in acute myeloid leukemia.

  2011cited by this paper
• Primary myelofibrosis: 2012 update on diagnosis, risk stratification, and management

  2011cited by this paper
• Targeting tumour angiogenesis with small molecule inhibitors of hypoxia inducible factor.

  2011cited by this paper
• Targeting the multiple myeloma hypoxic niche with TH-302, a hypoxia-activated prodrug.

  2010cited by this paper
• Understanding the "lethal" drivers of tumor-stroma co-evolution

  2010cited by this paper
• Development of HIF-1 inhibitors for cancer therapy

  2009cited by this paper
• Mouse models of human AML accurately predict chemotherapy response.

  2009cited by this paper
• Hypoxia-inducible factors in stem cells and cancer

  2009cited by this paper
• HIF-1alpha modulates energy metabolism in cancer cells by inducing over-expression of specific glycolytic isoforms.

  2009cited by this paper
• The warburg effect in leukemia-stroma cocultures is mediated by mitochondrial uncoupling associated with uncoupling protein 2 activation.

  2008cited by this paper
• Time-course-dependent microvascular alterations in a model of myeloid leukemia in vivo

  2008cited by this paper
• Overexpression of HIF1 Alpha Predicts Worse Overall and Event-Free Survival in Patients with Philadelphia Chromosome-Negative Precursor B-Lymphoblastic Leukemia

  2008cited by this paper
• Identification of human reductases that activate the dinitrobenzamide mustard prodrug PR-104A: a role for NADPH:cytochrome P450 oxidoreductase under hypoxia.

  2007cited by this paper
• Metabolic profiling, metabolomic and metabonomic procedures for NMR spectroscopy of urine, plasma, serum and tissue extracts

  2007cited by this paper
• Hypoxia signalling in cancer and approaches to enforce tumour regression

  2006cited by this paper
• Real-time metabolic imaging.

  2006cited by this paper
• HIF-1-mediated expression of pyruvate dehydrogenase kinase: a metabolic switch required for cellular adaptation to hypoxia.

  2006cited by this paper
• Metabolic imaging by hyperpolarized 13C magnetic resonance imaging for in vivo tumor diagnosis.

  2006cited by this paper
• Increase in signal-to-noise ratio of > 10,000 times in liquid-state NMR

  2003cited by this paper
• Regulation of the Chemokine Receptor CXCR4 by Hypoxia

  2003influential reference
• Targeting HIF-1 for cancer therapy

  2003cited by this paper
• Metabonomics: NMR spectroscopy and pattern recognition analysis of body fluids and tissues for characterisation of xenobiotic toxicity and disease diagnosis.

  2003cited by this paper
• The role of catalytic superoxide formation in the O2 inhibition of nitroreductase.

  1975cited by this paper

• Preclinical targeting of leukemia-initiating cells in the development future biologics for acute myeloid leukemia

  2025cites this paper
• Targeting hypoxia-inducible factor 1α in chronic graft-versus-host disease to enhance graft-versus-leukemia responses: implications for nanotherapeutics

  2025cites this paper
• Biomarker-Driven Approaches to Bone Metastases: From Molecular Mechanisms to Clinical Applications

  2025cites this paper
• The hypoxia signaling pathway in the development of acute myeloid leukemia.

  2025cites this paper
• PISTOL MRI allows noninvasive assessment of changes in tumor oxygenation post hypoxia targeted therapy

  2025cites this paper
• Hypoxia-activated selectivity-improved anti-PKM2 antibody combined with prodrug TH-302 for potentiated targeting therapy in hepatocellular carcinoma

  2024cites this paper
• Glutaminase inhibition in combination with azacytidine in myelodysplastic syndromes: a phase 1b/2 clinical trial and correlative analyses

  2024cites this paper
• Glutaminase inhibition in combination with azacytidine in myelodysplastic syndromes: Clinical efficacy and correlative analyses

  2023cites this paper
• Influence of the Hypoxia-Activated Prodrug Evofosfamide (TH-302) on Glycolytic Metabolism of Canine Glioma: A Potential Improvement in Cancer Metabolism

  2023cites this paper
• Crosstalk between DNA methylation and hypoxia in acute myeloid leukaemia

  2023cites this paper
• In Vitro Insights Into the Influence of Marrow Mesodermal/Mesenchymal Progenitor Cells on Acute Myelogenous Leukemia and Myelodysplastic Syndromes.

  2023cites this paper
• Enhancing Cancer Diagnosis with Real-Time Feedback: Tumor Metabolism through Hyperpolarized 1-13C Pyruvate MRSI

  2023cites this paper
• Stromal bone marrow fibroblasts and mesenchymal stem cells support acute myeloid leukaemia cells and promote therapy resistance

  2023cites this paper
• Therapeutic inhibition of PPARα-HIF1α-PGK1 signaling targets leukemia stem and progenitor cells in acute myeloid leukemia.

  2022cites this paper
• Bone Marrow Microenvironment as a Source of New Drug Targets for the Treatment of Acute Myeloid Leukaemia

  2022cites this paper
• The genesis and evolution of acute myeloid leukemia stem cells in the microenvironment: From biology to therapeutic targeting

  2022cites this paper
• Leukemic Stem Cell: A Mini-Review on Clinical Perspectives

  2022cites this paper
• Engineering Next-Generation CAR-T Cells: Overcoming Tumor Hypoxia and Metabolism.

  2022cites this paper
• Put in a “Ca2+ll” to Acute Myeloid Leukemia

  2022cites this paper
• The Hypoxia-Activated Prodrug TH-302: Exploiting Hypoxia in Cancer Therapy

  2021cites this paper
• Establishment of Prognosis Model in Acute Myeloid Leukemia Based on Hypoxia Microenvironment, and Exploration of Hypoxia-Related Mechanisms

  2021cites this paper
• Leukemic Stem Cells: From Leukemic Niche Biology to Treatment Opportunities

  2021cites this paper
• Targeting Hypoxia: Hypoxia-Activated Prodrugs in Cancer Therapy

  2021cites this paper
• Leukemia stem cell-bone marrow microenvironment interplay in acute myeloid leukemia development

  2021cites this paper
• The Role of Hypoxic Bone Marrow Microenvironment in Acute Myeloid Leukemia and Future Therapeutic Opportunities

  2021cites this paper
• Therapeutic Targeting of the Leukaemia Microenvironment

  2021cites this paper
• The Dynamic Interface Between the Bone Marrow Vascular Niche and Hematopoietic Stem Cells in Myeloid Malignancy

  2021cites this paper
• Acute Myeloid Leukemia Mutations and Future Mechanistic Target to Overcome Resistance

  2021cites this paper
• Escape From Treatment; the Different Faces of Leukemic Stem Cells and Therapy Resistance in Acute Myeloid Leukemia

  2021cites this paper
• Lactonization of the Oncometabolite D-2-Hydroxyglutarate Produces a Novel Endogenous Metabolite

  2021cites this paper
• Inhibition of Oxidative Phosphorylation Reverses Bone Marrow Hypoxia Visualized in Imageable Syngeneic B-ALL Mouse Model

  2020cites this paper
• Dynamic responses of the haematopoietic stem cell niche to diverse stresses

  2020cites this paper
• The bone marrow stromal niche: a therapeutic target of hematological myeloid malignancies

  2020cites this paper
• Biomimetic, Hypoxia‐Responsive Nanoparticles Overcome Residual Chemoresistant Leukemic Cells with Co‐Targeting of Therapy‐Induced Bone Marrow Niches

  2020cites this paper
• Role of hyperoxic treatment in cancer

  2020cites this paper
• Bone Marrow Stromal Niche: A New Master Regulator of Hematological Myeloid Malignancies

  2020cites this paper
• Location First: Targeting Acute Myeloid Leukemia Within Its Niche

  2020cites this paper
• Bioreducible Phosphonoamidate Pro-drug Inhibitor of Enolase: Proof of Concept Study.

  2020cites this paper
• Hypoxia Impairs NK Cell Cytotoxicity through SHP-1-Mediated Attenuation of STAT3 and ERK Signaling Pathways

  2020cites this paper
• An Enolase Inhibitor for the Targeted Treatment of ENO1-Deleted Cancers

  2020cites this paper
• An enolase inhibitor for the targeted treatment of ENO1-deleted cancers

  2020cites this paper
• Assessing Metabolic Intervention with a Glutaminase Inhibitor in Real-Time by Hyperpolarized Magnetic Resonance in Acute Myeloid Leukemia

  2019cites this paper
• Updates on the hematologic tumor microenvironment and its therapeutic targeting

  2019cites this paper
• Androgen Receptor Signaling in Castration-Resistant Prostate Cancer Alters Hyperpolarized Pyruvate to Lactate Conversion and Lactate Levels In Vivo

  2019cites this paper
• Nitrogen Mustards As Anticancer Chemotherapies: Historic Perspective, Current Developments, And Future Trends.

  2019cites this paper
• Targeting Leukemia Stem Cell-Niche Dynamics: A New Challenge in AML Treatment

  2019cites this paper
• New attempts for central nervous infiltration of pediatric acute lymphoblastic leukemia

  2019cites this paper
• The Induction of a Permissive Environment to Promote T Cell Immune Evasion in Acute Myeloid Leukemia: The Metabolic Perspective

  2019cites this paper
• Mechanisms of extramedullary relapse in acute lymphoblastic leukemia: Reconciling biological concepts and clinical issues.

  2019cites this paper
• Assessing Therapeutic Efficacy in Real-time by Hyperpolarized Magnetic Resonance Metabolic Imaging

  2019cites this paper
• Photoacoustic-based oxygen saturation assessment of murine femoral bone marrow in a preclinical model of leukemia

  2019cites this paper
• Tumor hypoxia impairs NK cell cytotoxicity through SHP-1-mediated attenuation of STAT3 and ERK signaling pathways

  2019cites this paper
• Evofosfamide for the treatment of human papillomavirus-negative head and neck squamous cell carcinoma.

  2018cites this paper
• The Bone Marrow Microenvironment in Health and Myeloid Malignancy.

  2018cites this paper
• Administration of Hypoxia-Activated Prodrug Evofosfamide after Conventional Adjuvant Therapy Enhances Therapeutic Outcome and Targets Cancer-Initiating Cells in Preclinical Models of Colorectal Cancer

  2018cites this paper
• Eradication of ENO1-deleted Glioblastoma through Collateral Lethality

  2018cites this paper
• Recruitment, phenotype and function of tumour-infiltrating regulatory T cells in the lung microenvironment

  2018cites this paper
• Self-Assembling Peptide Hydrogel for Local Anticancer Prodrug Delivery in the Treatment of Glioblastoma Multiforme

  2018influential citation
• Osteogenic niche in the regulation of normal hematopoiesis and leukemogenesis

  2018cites this paper
• The bone marrow microenvironment in health and disease at a glance

  2018cites this paper
• Targeting the bone marrow microenvironment in acute leukemia

  2018cites this paper
• Molecular Pathways: Hypoxia-Activated Prodrugs in Cancer Therapy

  2017cites this paper
• Novel CD123-aptamer-originated targeted drug trains for selectively delivering cytotoxic agent to tumor cells in acute myeloid leukemia theranostics

  2017cites this paper
• IDENTIFYING THE IMMUNE RELATED METABOLIC PROPERTIES OF PANCREATIC CANCER USING NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY AND DYNAMIC MAGNETIC RESONANCE SPECTROSCOPIC IMAGING WITH HYPERPOLARIZED PYRUVATE

  2017cites this paper
• Alterations of HSC Niche in Myeloid Malignancies

  2017cites this paper
• MRI Guided Analysis of Changes in Tumor Oxygenation in Response to Hypoxia Activated/Targeted Therapeutics

  2017cites this paper
• Metabolic interrogation as a tool to optimize chemotherapeutic regimens

  2017cites this paper
• The hypoxia signalling pathway in haematological malignancies

  2017cites this paper
• Hypoxia-activated prodrugs in the treatment of advanced pancreatic adenocarcinoma.

  2017cites this paper
• Phase I study of evofosfamide, an investigational hypoxia‐activated prodrug, in patients with advanced leukemia

  2016cites this paper
• Hypoxia-activated prodrugs: paths forward in the era of personalised medicine

  2016cites this paper
• Microenvironmental oxygen partial pressure in acute myeloid leukemia: Is there really a role for hypoxia?

  2016cites this paper