The transcriptional factors HIF-1 and HIF-2 and their novel inhibitors in cancer therapy

Phase I Dose-Escalation Trial of PT2385, a First-in-Class Hypoxia-Inducible Factor-2α Antagonist in Patients With Previously Treated Advanced Clear Cell Renal Cell Carcinoma

(2018) Kevin D. Courtney et al.   JOURNAL OF CLINICAL ONCOLOGY

Reciprocal loop of hypoxia-inducible factor-1α (HIF-1α) and metastasis-associated protein 2 (MTA2) contributes to the progression of pancreatic carcinoma by suppressing E-cadherin transcription

(2018) Shuai Zhu et al.   JOURNAL OF PATHOLOGY

LBH589 Inhibits Glioblastoma Growth and Angiogenesis Through Suppression of HIF-1α Expression

(2017) Zhi-Gang Yao et al.   JOURNAL OF NEUROPATHOLOGY AND EXPERIMENTAL NEUROLOGY

Inhibition of the H3K9 methyltransferase G9A attenuates oncogenicity and activates the hypoxia signaling pathway

(2017) Jolene Caifeng Ho et al.   PLoS One

The novel hypoxia-inducible factor-1α inhibitor IDF-11774 regulates cancer metabolism, thereby suppressing tumor growth

(2017) Hyun Seung Ban et al.   Cell Death & Disease

Panobinostat: A histone deacetylase inhibitor for the treatment of relapsed or refractory multiple myeloma

(2016) K. Wahaib et al.   AMERICAN JOURNAL OF HEALTH-SYSTEM PHARMACY

Identification of Targets of the HIF-1 Inhibitor IDF-11774 Using Alkyne-Conjugated Photoaffinity Probes

(2016) Hyun Seung Ban et al.   BIOCONJUGATE CHEMISTRY

Phase 2 study of panobinostat with or without rituximab in relapsed diffuse large B-cell lymphoma

(2016) S. E. Assouline et al.   BLOOD

Preclinical Efficacy of Bevacizumab with CRLX101, an Investigational Nanoparticle-Drug Conjugate, in Treatment of Metastatic Triple-Negative Breast Cancer

(2016) E. Pham et al.   CANCER RESEARCH

A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma

(2016) Eli M. Wallace et al.   CANCER RESEARCH

HIF-2α phosphorylation by CK1δ promotes erythropoietin secretion in liver cancer cells under hypoxia

(2016) Evanthia Pangou et al.   JOURNAL OF CELL SCIENCE

Cardenolides from Calotropis gigantea as potent inhibitors of hypoxia-inducible factor-1 transcriptional activity

(2016) Supawadee Parhira et al.   JOURNAL OF ETHNOPHARMACOLOGY

Targeting renal cell carcinoma with a HIF-2 antagonist

(2016) Wenfang Chen et al.   NATURE

On-target efficacy of a HIF-2α antagonist in preclinical kidney cancer models

(2016) Hyejin Cho et al.   NATURE

A Phase II Trial of a Histone Deacetylase Inhibitor Panobinostat in Patients With Low-Grade Neuroendocrine Tumors

(2016) Ning Jin et al.   ONCOLOGIST

CRLX101 nanoparticles localize in human tumors and not in adjacent, nonneoplastic tissue after intravenous dosing

(2016) Andrew J. Clark et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Protein kinase A–dependent phosphorylation stimulates the transcriptional activity of hypoxia-inducible factor 1

(2016) John W. Bullen et al.   Science Signaling

Protein kinase A–dependent phosphorylation stimulates the transcriptional activity of hypoxia-inducible factor 1

(2016) John W. Bullen et al.   Science Signaling

PI3K–mTORC2 but not PI3K–mTORC1 Regulates Transcription of HIF2A/EPAS1 and Vascularization in Neuroblastoma

(2015) Sofie Mohlin et al.   CANCER RESEARCH

CK1δ restrains lipin-1 induction, lipid droplet formation and cell proliferation under hypoxia by reducing HIF-1α/ARNT complex formation

(2015) Maria Kourti et al.   CELLULAR SIGNALLING

Synergistic Leukemia Eradication by Combined Treatment with Retinoic Acid and HIF Inhibition by EZN-2208 (PEG-SN38) in Preclinical Models of PML-RAR  and PLZF-RAR -Driven Leukemia

(2015) N. Coltella et al.   CLINICAL CANCER RESEARCH

HIF3α: the little we know

(2015) Linda Ravenna et al.   FEBS Journal

The Histone Methyltransferase Inhibitor BIX01294 Inhibits HIF-1α Stability and Angiogenesis

(2015) Su Young Oh et al.   MOLECULES AND CELLS

Phase II study of panobinostat in combination with bevacizumab for recurrent glioblastoma and anaplastic glioma

(2015) E. Q. Lee et al.   NEURO-ONCOLOGY

HIF-1α pathway: role, regulation and intervention for cancer therapy

(2015) Georgina N. Masoud et al.   Acta Pharmaceutica Sinica B

Indole-3-ethylsulfamoylphenylacrylamides: Potent histone deacetylase inhibitors with anti-inflammatory activity

(2014) Samir Mehndiratta et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A Group of Novel HIF-1α Inhibitors, Glyceollins, Blocks HIF-1α Synthesis and Decreases Its Stability via Inhibition of the PI3K/AKT/mTOR Pathway and Hsp90 Binding

(2014) Sun-Hee Lee et al.   JOURNAL OF CELLULAR PHYSIOLOGY

NNC 55-0396, a T-type Ca2+ channel inhibitor, inhibits angiogenesis via suppression of hypoxia-inducible factor-1α signal transduction

(2014) Ki Hyun Kim et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

The Histone Deacetylase Inhibitor, Vorinostat, Represses Hypoxia Inducible Factor 1 Alpha Expression through Translational Inhibition

(2014) Darren M. Hutt et al.   PLoS One

Hypoxia-inducible factors are required for chemotherapy resistance of breast cancer stem cells

(2014) Debangshu Samanta et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

CDK1 stabilizes HIF-1α via direct phosphorylation of Ser668 to promote tumor growth

(2013) Noel A Warfel et al.   CELL CYCLE

First-in-human phase 1/2a trial of CRLX101, a cyclodextrin-containing polymer-camptothecin nanopharmaceutical in patients with advanced solid tumor malignancies

(2013) Glen J. Weiss et al.   INVESTIGATIONAL NEW DRUGS

Integrated molecular analysis of clear-cell renal cell carcinoma

(2013) Yusuke Sato et al.   NATURE GENETICS

STAT3 and HIF1α cooperatively activate HIF1 target genes in MDA-MB-231 and RCC4 cells

(2013) M R Pawlus et al.   ONCOGENE

Molecular, functional, and gene expression analysis of zebrafish hypoxia-inducible factor-3α

(2012) Peng Zhang et al.   AMERICAN JOURNAL OF PHYSIOLOGY-REGULATORY INTEGRATIVE AND COMPARATIVE PHYSIOLOGY

From stem cells to cancer stem cells: HIF takes the stage

(2012) Kyoung Eun Lee et al.   CURRENT OPINION IN CELL BIOLOGY

Recent advances in hypoxia-inducible factor (HIF)-1 inhibitors

(2012) Yan Xia et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The Acetylase/Deacetylase Couple CREB-binding Protein/Sirtuin 1 Controls Hypoxia-inducible Factor 2 Signaling

(2012) Rui Chen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

HIF1α Protein Stability Is Increased by Acetylation at Lysine 709

(2012) Hao Geng et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Combination therapy for hepatocellular carcinoma: Additive preclinical efficacy of the HDAC inhibitor panobinostat with sorafenib

(2012) Anja Lachenmayer et al.   JOURNAL OF HEPATOLOGY

Synthesis and Structure–Activity Relationship of (E)-Phenoxyacrylic Amide Derivatives as Hypoxia-Inducible Factor (HIF) 1α Inhibitors

(2012) Ravi Naik et al.   JOURNAL OF MEDICINAL CHEMISTRY

Upstream Stimulatory Factor 2 and Hypoxia-Inducible Factor 2  (HIF2 ) Cooperatively Activate HIF2 Target Genes during Hypoxia

(2012) M. R. Pawlus et al.   MOLECULAR AND CELLULAR BIOLOGY

Glyceollins, a novel class of soy phytoalexins, inhibit angiogenesis by blocking the VEGF and bFGF signaling pathways

(2012) Sun H. Lee et al.   MOLECULAR NUTRITION & FOOD RESEARCH

Adaptive and Maladaptive Cardiorespiratory Responses to Continuous and Intermittent Hypoxia Mediated by Hypoxia-Inducible Factors 1 and 2

(2012) Nanduri R. Prabhakar et al.   PHYSIOLOGICAL REVIEWS

Potent and sustained inhibition of HIF-1α and downstream genes by a polyethyleneglycol-SN38 conjugate, EZN-2208, results in anti-angiogenic effects

(2011) Puja Sapra et al.   ANGIOGENESIS

Biochemical characterization of human HIF hydroxylases using HIF protein substrates that contain all three hydroxylation sites

(2011) Melissa B. Pappalardi et al.   BIOCHEMICAL JOURNAL

Inhibitory effect of glyceollin isolated from soybean against melanogenesis in B16 melanoma cells

(2011) Young-Sang Lee et al.   BMB Reports

The Hypoxia-Associated Factor Switches Cells from HIF-1 - to HIF-2 -Dependent Signaling Promoting Stem Cell Characteristics, Aggressive Tumor Growth and Invasion

(2011) M. Y. Koh et al.   CANCER RESEARCH

H3K9 methyltransferase G9a and the related molecule GLP

(2011) Y. Shinkai et al.   GENES & DEVELOPMENT

HDAC4 Protein Regulates HIF1α Protein Lysine Acetylation and Cancer Cell Response to Hypoxia

(2011) Hao Geng et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Chromosome 14q loss defines a molecular subtype of clear-cell renal cell carcinoma associated with poor prognosis

(2011) Federico A Monzon et al.   MODERN PATHOLOGY

Preclinical study of the cyclodextrin-polymer conjugate of camptothecin CRLX101 for the treatment of gastric cancer

(2011) Shikha Gaur et al.   Nanomedicine-Nanotechnology Biology and Medicine

LW6, a novel HIF-1 inhibitor, promotes proteasomal degradation of HIF-1α via upregulation of VHL in a colon cancer cell line

(2010) Kyeong Lee et al.   BIOCHEMICAL PHARMACOLOGY

Hypoxia-inducible factor (HIF)-3α is subject to extensive alternative splicing in human tissues and cancer cells and is regulated by HIF-1 but not HIF-2

(2010) Annika Pasanen et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Glyceollins, One of the Phytoalexins Derived from Soybeans under Fungal Stress, Enhance Insulin Sensitivity and Exert Insulinotropic Actions

(2010) Sunmin Park et al.   JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

Plk3 Functions as an Essential Component of the Hypoxia Regulatory Pathway by Direct Phosphorylation of HIF-1α

(2010) Dazhong Xu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Casein kinase 1 regulates human hypoxia-inducible factor HIF-1

(2010) A. Kalousi et al.   JOURNAL OF CELL SCIENCE

mTORC1 Signaling under Hypoxic Conditions Is Controlled by ATM-Dependent Phosphorylation of HIF-1α

(2010) Hakan Cam et al.   MOLECULAR CELL

Sirtuin 1 Modulates Cellular Responses to Hypoxia by Deacetylating Hypoxia-Inducible Factor 1α

(2010) Ji-Hong Lim et al.   MOLECULAR CELL

Effects of glyceollin I on vascular contraction in rat aorta

(2010) Min-Ji Song et al.   NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

Hypoxia-Inducible Factor-3α Functions as an Accelerator of 3T3-L1 Adipose Differentiation

(2009) Misaki Hatanaka et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

Hsp70 and CHIP Selectively Mediate Ubiquitination and Degradation of Hypoxia-inducible Factor (HIF)-1α but Not HIF-2α

(2009) Weibo Luo et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Hypoxia/Reoxygenation-Induced Mutations in Mammalian Cells Detected by the Flow Cytometry Mutation Assay and Characterized by Mutant Spectrum

(2009) Stephen B. Keysar et al.   RADIATION RESEARCH

Regulation of Hypoxia-Inducible Factor 2  Signaling by the Stress-Responsive Deacetylase Sirtuin 1

(2009) E. M. Dioum et al.   SCIENCE

Novel Prodrugs of SN38 Using Multiarm Poly(ethylene glycol) Linkers

(2008) Hong Zhao et al.   BIOCONJUGATE CHEMISTRY

Novel Delivery of SN38 Markedly Inhibits Tumor Growth in Xenografts, Including a Camptothecin-11-Refractory Model

(2008) P. Sapra et al.   CLINICAL CANCER RESEARCH

Differential Dependence of Hypoxia-inducible Factors 1α and 2α on mTORC1 and mTORC2

(2008) Alfredo Toschi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Hypoxia-Associated Factor, a Novel E3-Ubiquitin Ligase, Binds and Ubiquitinates Hypoxia-Inducible Factor 1 , Leading to Its Oxygen-Independent Degradation

(2008) M. Y. Koh et al.   MOLECULAR AND CELLULAR BIOLOGY