Hypoxia-inducible factor (HIF) inhibitors: a patent survey (2011-2015)

HIF-1α suppressing small molecule, LW6, inhibits cancer cell growth by binding to calcineurin b homologous protein 1

(2015) Beom Seok Kim et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Design, synthesis, and structure–activity relationships of 1-ethylpyrazole-3-carboxamide compounds as novel hypoxia-inducible factor (HIF)-1 inhibitors

(2015) Yorinobu Yasuda et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Novel chalcone derivatives as hypoxia-inducible factor (HIF)-1 inhibitor: Synthesis, anti-invasive and anti-angiogenic properties

(2015) Lihui Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

New Inhibitors of Angiogenesis with Antitumor Activity in Vivo

(2015) Nagore I. Marín-Ramos et al.   JOURNAL OF MEDICINAL CHEMISTRY

Randomized placebo-controlled dose-ranging and pharmacodynamics study of roxadustat (FG-4592) to treat anemia in nondialysis-dependent chronic kidney disease (NDD-CKD) patients

(2015) Anatole Besarab et al.   NEPHROLOGY DIALYSIS TRANSPLANTATION

The role of hypoxia-inducible factor-2 in digestive system cancers

(2015) J Zhao et al.   Cell Death & Disease

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

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

Development of a Novel Class of Mitochondrial Ubiquinol–Cytochrome c Reductase Binding Protein (UQCRB) Modulators as Promising Antiangiogenic Leads

(2014) Hye Jin Jung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Diacylglycerol Kinase (DGK) Inhibitor II (R59949) Could Suppress Retinal Neovascularization and Protect Retinal Astrocytes in an Oxygen-Induced Retinopathy Model

(2014) Lu Yang et al.   JOURNAL OF MOLECULAR NEUROSCIENCE

EZH2: Not EZHY (Easy) to Deal

(2014) Gauri Deb et al.   MOLECULAR CANCER RESEARCH

Fructose-1,6-bisphosphatase opposes renal carcinoma progression

(2014) Bo Li et al.   NATURE

A Synthetic Manassantin A Derivative Inhibits Hypoxia-Inducible Factor 1 and Tumor Growth

(2014) Liwei Lang et al.   PLoS One

In vivo modulation of hypoxia-inducible signaling by topographical helix mimetics

(2014) B. B. Lao et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of Malate Dehydrogenase 2 as a Target Protein of the HIF-1 Inhibitor LW6 using Chemical Probes

(2013) Kyeong Lee et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

The novel toluidine sulphonamide EL102 shows pre-clinical in vitro and in vivo activity against prostate cancer and circumvents MDR1 resistance

(2013) A P Toner et al.   BRITISH JOURNAL OF CANCER

HIF-1 mediates metabolic responses to intratumoral hypoxia and oncogenic mutations

(2013) Gregg L. Semenza   JOURNAL OF CLINICAL INVESTIGATION

Hypoxia-Inducible Factor and Vascular Endothelial Growth Factor Pathway for the Study of Hypoxia in a New Model of Otitis Media with Effusion

(2012) Qiuhong Huang et al.   AUDIOLOGY AND NEURO-OTOLOGY

The HIF-pathway inhibitor NSC-134754 induces metabolic changes and anti-tumour activity while maintaining vascular function

(2012) L C J Baker et al.   BRITISH JOURNAL OF CANCER

Arylsulfonamide KCN1 Inhibits In Vivo Glioma Growth and Interferes with HIF Signaling by Disrupting HIF-1  Interaction with Cofactors p300/CBP

(2012) S. Yin et al.   CLINICAL CANCER RESEARCH

Targeting the von Hippel–Lindau E3 Ubiquitin Ligase Using Small Molecules To Disrupt the VHL/HIF-1α Interaction

(2012) Dennis L. Buckley et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

KCN1, a Novel Synthetic Sulfonamide Anticancer Agent: In Vitro and In Vivo Anti-Pancreatic Cancer Activities and Preclinical Pharmacology

(2012) Wei Wang et al.   PLoS One

Passing the baton: the HIF switch

(2012) Mei Yee Koh et al.   TRENDS IN BIOCHEMICAL SCIENCES

Manassantin A Isolated from Saururus chinensis Inhibits 5-Lipoxygenase-Dependent Leukotriene C4 Generation by Blocking Mitogen-Activated Protein Kinase Activation in Mast Cells

(2011) Su Jeong Kim et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

Targeting HIF1α Eliminates Cancer Stem Cells in Hematological Malignancies

(2011) Yin Wang et al.   Cell Stem Cell

HIF–VEGF Pathways Are Critical for Chronic Otitis Media in Junbo and Jeff Mouse Mutants

(2011) Michael T. Cheeseman et al.   PLoS Genetics

SR16388: a steroidal antiangiogenic agent with potent inhibitory effect on tumor growth in vivo

(2010) Wan-Ru Chao et al.   ANGIOGENESIS

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

Identification of a novel small molecule targeting UQCRB of mitochondrial complex III and its anti-angiogenic activity

(2010) Hye Jin Jung et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Analysis of HIF-1 inhibition by manassantin A and analogues with modified tetrahydrofuran configurations

(2009) Amanda C. Kasper et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Inhibition of Phenotypic and Functional Maturation of Dendritic Cells by Manassantin A

(2009) Jee Youn Kim et al.   JOURNAL OF PHARMACOLOGICAL SCIENCES

Pleiotropic Effects of YC-1 Selectively Inhibit Pathological Retinal Neovascularization and Promote Physiological Revascularization in a Mouse Model of Oxygen-Induced Retinopathy

(2009) M. DeNiro et al.   MOLECULAR PHARMACOLOGY

Bortezomib inhibits tumor adaptation to hypoxia by stimulating the FIH-mediated repression of hypoxia-inducible factor-1

(2008) D. H. Shin et al.   BLOOD

ENMD-1198, a novel tubulin-binding agent reduces HIF-1alpha and STAT3 activity in human hepatocellular carcinoma(HCC) cells, and inhibits growth and vascularization in vivo

(2008) Christian Moser et al.   BMC CANCER

Cancer Cell Metabolism: Warburg and Beyond

(2008) Peggy P. Hsu et al.   CELL

A novel mode of action of YC-1 in HIF inhibition: stimulation of FIH-dependent p300 dissociation from HIF-1 

(2008) S. H. Li et al.   MOLECULAR CANCER THERAPEUTICS

Significant antitumor activity in vivo following treatment with the microtubule agent ENMD-1198

(2008) Theresa M. LaVallee et al.   MOLECULAR CANCER THERAPEUTICS