Recent Advances in Developing Inhibitors for Hypoxia-Inducible Factor Prolyl Hydroxylases and Their Therapeutic Implications

A Lactate-Induced Response to Hypoxia

(2015) Dong Chul Lee et al.   CELL

Discovery of novel 2-[2-(3-hydroxy-pyridin-2-yl)-thiazol-4-yl]-acetamide derivatives as HIF prolyl 4-hydroxylase inhibitors; SAR, synthesis and modeling evaluation

(2014) Yong Rae Hong et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

PHD3-mediated prolyl hydroxylation of nonmuscle actin impairs polymerization and cell motility

(2014) Weibo Luo et al.   MOLECULAR BIOLOGY OF THE CELL

Regulation of Wound Healing and Fibrosis by Hypoxia and Hypoxia-Inducible Factor-1

(2014) Robin J Ruthenborg et al.   MOLECULES AND CELLS

Targeting hypoxia signalling for the treatment of ischaemic and inflammatory diseases

(2014) Holger K. Eltzschig et al.   NATURE REVIEWS DRUG DISCOVERY

Effect of Proline Analogues on Activity of Human Prolyl Hydroxylase and the Regulation of HIF Signal Transduction Pathway

(2014) Xiaoyan Ma et al.   PLoS One

PHD3 regulates EGFR internalization and signalling in tumours

(2014) Boyan K. Garvalov et al.   Nature Communications

Prolyl 4-hydroxylases, master regulators of the hypoxia response

(2013) J. Myllyharju   Acta Physiologica

Myocardial ischemia-reperfusion injury: a neglected therapeutic target

(2013) Derek J. Hausenloy et al.   JOURNAL OF CLINICAL INVESTIGATION

Inhibition of Hypoxia-Inducible Factor Prolyl Hydroxylase Domain Oxygen Sensors: Tricking the Body into Mounting Orchestrated Survival and Repair Responses

(2013) Michael H. Rabinowitz   JOURNAL OF MEDICINAL CHEMISTRY

Loss of Epithelial Hypoxia-Inducible Factor Prolyl Hydroxylase 2 Accelerates Skin Wound Healing in Mice

(2013) Joanna Kalucka et al.   MOLECULAR AND CELLULAR BIOLOGY

A Novel Prolyl Hydroxylase Inhibitor Protects Against Cell Death After Hypoxia

(2013) Satoru Kontani et al.   NEUROCHEMICAL RESEARCH

Wound Healing Improvement with PHD-2 Silenced Fibroblasts in Diabetic Mice

(2013) Xiongliang Zhang et al.   PLoS One

Hypoxia-inducible factor 1 is required for remote ischemic preconditioning of the heart

(2013) Z. Cai et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Regulation of IL-1 -induced NF- B by hydroxylases links key hypoxic and inflammatory signaling pathways

(2013) C. C. Scholz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Hypoxia and inflammation are two sides of the same coin

(2013) K. Bartels et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

HIF1A Reduces Acute Lung Injury by Optimizing Carbohydrate Metabolism in the Alveolar Epithelium

(2013) Tobias Eckle et al.   PLOS BIOLOGY

Dynamic Combinatorial Chemistry Employing Boronic Acids/Boronate Esters Leads to Potent Oxygenase Inhibitors

(2012) Marina Demetriades et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibition: Robust New Target or Another Big Bust for Stroke Therapeutics?

(2012) Saravanan S Karuppagounder et al.   JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM

PHD3-dependent hydroxylation of HCLK2 promotes the DNA damage response

(2012) Liang Xie et al.   JOURNAL OF CLINICAL INVESTIGATION

Screening chelating inhibitors of HIF-prolyl hydroxylase domain 2 (PHD2) and factor inhibiting HIF (FIH)

(2012) Shannon C. Flagg et al.   JOURNAL OF INORGANIC BIOCHEMISTRY

1,3,8-Triazaspiro[4.5]decane-2,4-diones as Efficacious Pan-Inhibitors of Hypoxia-Inducible Factor Prolyl Hydroxylase 1–3 (HIF PHD1–3) for the Treatment of Anemia

(2012) Petr Vachal et al.   JOURNAL OF MEDICINAL CHEMISTRY

Reporter Ligand NMR Screening Method for 2-Oxoglutarate Oxygenase Inhibitors

(2012) Ivanhoe K. H. Leung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Adora2b-elicited Per2 stabilization promotes a HIF-dependent metabolic switch crucial for myocardial adaptation to ischemia

(2012) Tobias Eckle et al.   NATURE MEDICINE

Inhibition of a prolyl hydroxylase domain (PHD) by substrate analog peptides

(2011) Hyuk Sung Kwon et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of a new molecular probe ML228: An activator of the hypoxia inducible factor (HIF) pathway

(2011) Jimmy R. Theriault et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Pyruvate Kinase M2 Is a PHD3-Stimulated Coactivator for Hypoxia-Inducible Factor 1

(2011) Weibo Luo et al.   CELL

HIF-1α dysfunction in diabetes

(2011) Hariharan Thangarajah et al.   CELL CYCLE

HIF prolyl hydroxylase inhibitors for anemia

(2011) Eugene Muchnik et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Pharmacological Characterization of 1-(5-Chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic Acid (JNJ-42041935), a Potent and Selective Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor

(2011) T. D. Barrett et al.   MOLECULAR PHARMACOLOGY

Hypoxia and Inflammation

(2011) Holger K. Eltzschig et al.   NEW ENGLAND JOURNAL OF MEDICINE

Endogenous 2-oxoglutarate levels impact potencies of competitive HIF prolyl hydroxylase inhibitors

(2011) Kenneth Thirstrup et al.   PHARMACOLOGICAL RESEARCH

von Hippel–Lindau β-domain–luciferase fusion protein as a bioluminescent hydroxyproline sensor for a hypoxia-inducible factor prolyl hydroxylase assay

(2010) Sungchae Hong et al.   ANALYTICAL BIOCHEMISTRY

Utilization of an In Vivo Reporter for High Throughput Identification of Branched Small Molecule Regulators of Hypoxic Adaptation

(2010) Natalya A. Smirnova et al.   CHEMISTRY & BIOLOGY

Prolyl hydroxylase domain-containing protein inhibitors as stabilizers of hypoxia-inducible factor: small molecule-based therapeutics for anemia

(2010) Lin Yan et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Prolyl Hydroxylase Domain (PHD) 2 Affects Cell Migration and F-actin Formation via RhoA/Rho-associated Kinase-dependent Cofilin Phosphorylation

(2010) Sabine Vogel et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Neuroprotection by Dimethyloxalylglycine following Permanent and Transient Focal Cerebral Ischemia in Rats

(2010) Simon Nagel et al.   JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM

Reactivation of Hepatic EPO Synthesis in Mice After PHD Loss

(2010) Y. A. Minamishima et al.   SCIENCE

HIF pathway mutations and erythrocytosis

(2010) Mary Frances McMullin   Expert Review of Hematology

Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues

(2010) Mark D. Rosen et al.   ACS Medicinal Chemistry Letters

Inhibition of Prolyl Hydroxylase Domain-Containing Protein Suppressed Lipopolysaccharide-Induced TNF-α Expression

(2009) Kotaro Takeda et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

HIF-1α peptide derivatives with modifications at the hydroxyproline residue as activators of HIF-1α

(2009) Dae-Ro Ahn et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Control of Cyclin D1 and Breast Tumorigenesis by the EglN2 Prolyl Hydroxylase

(2009) Qing Zhang et al.   CANCER CELL

Heterozygous Deficiency of PHD2 Restores Tumor Oxygenation and Inhibits Metastasis via Endothelial Normalization

(2009) Massimiliano Mazzone et al.   CELL

Application of a Proteolysis/Mass Spectrometry Method for Investigating the Effects of Inhibitors on Hydroxylase Structure

(2009) Christopher J. Stubbs et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of oxygen sensors as a therapeutic strategy for ischaemic and inflammatory disease

(2009) Peter Fraisl et al.   NATURE REVIEWS DRUG DISCOVERY

Defining the role of hypoxia-inducible factor 1 in cancer biology and therapeutics

(2009) G L Semenza   ONCOGENE

Proteomics-based identification of two novel direct targets of hypoxia-inducible factor-1 and their potential roles in migration/invasion of cancer cells

(2009) Shi-Hua Liao et al.   PROTEOMICS

Structural Basis for Binding of Hypoxia-Inducible Factor to the Oxygen-Sensing Prolyl Hydroxylases

(2009) Rasheduzzaman Chowdhury et al.   STRUCTURE

Hypoxia. Regulation of NFκB signalling during inflammation: the role of hydroxylases

(2009) Kathryn M Oliver et al.   ARTHRITIS RESEARCH & THERAPY

In vivofunctions of the prolyl-4-hydroxylase domain oxygen sensors: direct route to the treatment of anaemia and the protection of ischaemic tissues

(2008) D. M. Katschinski   Acta Physiologica

Kinetic characterization and identification of a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 using a time-resolved fluorescence resonance energy transfer-based assay technology

(2008) Jennifer H. Dao et al.   ANALYTICAL BIOCHEMISTRY

Structure-guided design of substituted aza-benzimidazoles as potent hypoxia inducible factor-1α prolyl hydroxylase-2 inhibitors

(2008) Mike Frohn et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Hypoxia-Inducible Factor-1 Is Central to Cardioprotection

(2008) Tobias Eckle et al.   CIRCULATION

Baicalein Induces Functional Hypoxia-Inducible Factor-1  and Angiogenesis

(2008) H. Cho et al.   MOLECULAR PHARMACOLOGY

Stabilization of HIF-1  is critical to improve wound healing in diabetic mice

(2008) I. R. Botusan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Hydroxylase Inhibitor Dimethyloxalylglycine Is Protective in a Murine Model of Colitis

(2007) Eoin P. Cummins et al.   GASTROENTEROLOGY

Mucosal Protection by Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibition

(2007) Andreas Robinson et al.   GASTROENTEROLOGY