Aspartate/asparagine-β-hydroxylase: a high-throughput mass spectrometric assay for discovery of small molecule inhibitors

[1]  C. Schofield,et al.  Kinetic parameters of human aspartate/asparagine–β-hydroxylase suggest that it has a possible function in oxygen sensing , 2020, The Journal of Biological Chemistry.

[2]  M. Hung,et al.  ASPH-notch Axis guided Exosomal delivery of Prometastatic Secretome renders breast Cancer multi-organ metastasis , 2019, Molecular Cancer.

[3]  P. Handford,et al.  Aspartate/asparagine-β-hydroxylase crystal structures reveal an unexpected epidermal growth factor-like domain substrate disulfide pattern , 2019, Nature Communications.

[4]  Catalina Carrasco-Pozo,et al.  The Anti-Cancer Effect of Quercetin: Molecular Implications in Cancer Metabolism , 2019, International journal of molecular sciences.

[5]  H. Ghanbari,et al.  Anti-tumor activity of antibody drug conjugate targeting aspartate-β-hydroxylase in pancreatic ductal adenocarcinoma. , 2019, Cancer letters.

[6]  Wai Hoong Chang,et al.  Dual prognostic role of 2-oxoglutarate-dependent oxygenases in ten cancer types: implications for cell cycle regulation and cell adhesion maintenance , 2019, Cancer communications.

[7]  M. Iwasaki,et al.  Roxadustat Treatment of Chronic Kidney Disease-Associated Anemia in Japanese Patients Not on Dialysis: A Phase 2, Randomized, Double-Blind, Placebo-Controlled Trial , 2019, Advances in Therapy.

[8]  M. Thangaraju,et al.  Deferiprone: Pan-selective Histone Lysine Demethylase Inhibition Activity and Structure Activity Relationship Study , 2019, Scientific Reports.

[9]  W. Figg,et al.  Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c8md00548f , 2019, MedChemComm.

[10]  W. Sippl,et al.  The Clinically Used Iron Chelator Deferasirox is an Inhibitor of Epigenetic JumonjiC Domain-Containing Histone Demethylases. , 2019, ACS chemical biology.

[11]  E. Souzeau,et al.  Loss of ciliary zonule protein hydroxylation and lens stability as a predicted consequence of biallelic ASPH variation , 2019, Ophthalmic genetics.

[12]  X. Bai,et al.  Recent advances in research on aspartate β-hydroxylase (ASPH) in pancreatic cancer: A brief update. , 2018, Bosnian journal of basic medical sciences.

[13]  R. Hennekam,et al.  A novel ASPH variant extends the phenotype of Shawaf‐Traboulsi syndrome , 2018, American journal of medical genetics. Part A.

[14]  T. Pawlik,et al.  Hydroxylase Activity of ASPH Promotes Hepatocellular Carcinoma Metastasis Through Epithelial-to-Mesenchymal Transition Pathway , 2018, EBioMedicine.

[15]  Mukul R Jain,et al.  Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases. , 2018, Journal of medicinal chemistry.

[16]  J. Keldenich,et al.  Discovery of Molidustat (BAY 85‐3934): A Small‐Molecule Oral HIF‐Prolyl Hydroxylase (HIF‐PH) Inhibitor for the Treatment of Renal Anemia , 2018, ChemMedChem.

[17]  F. Lee,et al.  Faculty of 1000 evaluation for Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials. , 2018 .

[18]  M. Pappalardi,et al.  Discovery and Preclinical Characterization of GSK1278863 (Daprodustat), a Small Molecule Hypoxia Inducible Factor–Prolyl Hydroxylase Inhibitor for Anemia , 2017, The Journal of Pharmacology and Experimental Therapeutics.

[19]  O. Fedorov,et al.  Discovery of a Highly Selective Cell‐Active Inhibitor of the Histone Lysine Demethylases KDM2/7 , 2017, Angewandte Chemie.

[20]  H. Ghanbari,et al.  Lambda phage-based vaccine induces antitumor immunity in hepatocellular carcinoma , 2017, Heliyon.

[21]  H. Patel,et al.  Phase I Clinical Study of ZYAN1, A Novel Prolyl-Hydroxylase (PHD) Inhibitor to Evaluate the Safety, Tolerability, and Pharmacokinetics Following Oral Administration in Healthy Volunteers , 2017, Clinical Pharmacokinetics.

[22]  X. Xue,et al.  Development of a novel anti-human aspartyl-(asparaginyl) β-hydroxylase monoclonal antibody with diagnostic and therapeutic potential. , 2017, Oncology letters.

[23]  L. Sturla,et al.  Aspartate-β-hydroxylase (ASPH): A potential therapeutic target in human malignant gliomas , 2016, Heliyon.

[24]  G. Koek,et al.  How we manage patients with hereditary haemochromatosis , 2016, British journal of haematology.

[25]  V. Haase,et al.  Vadadustat, a novel oral HIF stabilizer, provides effective anemia treatment in nondialysis-dependent chronic kidney disease. , 2016, Kidney international.

[26]  P. Trojer,et al.  An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. , 2016, Nature chemical biology.

[27]  Yu Zhang,et al.  Conversion of human fibroblasts into functional cardiomyocytes by small molecules , 2016, Science.

[28]  Miran Kim,et al.  Aspartate β‐hydroxylase modulates cellular senescence through glycogen synthase kinase 3β in hepatocellular carcinoma , 2016, Hepatology.

[29]  J. Wands,et al.  Anti-Tumor Effects of Second Generation β-Hydroxylase Inhibitors on Cholangiocarcinoma Development and Progression , 2016, PloS one.

[30]  Douglas W. Thomson,et al.  Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives. , 2016, Journal of medicinal chemistry.

[31]  M. Koury,et al.  Anaemia in kidney disease: harnessing hypoxia responses for therapy , 2015, Nature Reviews Nephrology.

[32]  Y. Li,et al.  Aspartate β-hydroxylase expression promotes a malignant pancreatic cellular phenotype , 2014, Oncotarget.

[33]  J. Wands,et al.  A cell‐surface β‐hydroxylase is a biomarker and therapeutic target for hepatocellular carcinoma , 2014, Hepatology.

[34]  Kristian Helin,et al.  Inhibition of demethylases by GSK-J1/J4 , 2014, Nature.

[35]  Elias I Traboulsi,et al.  Mutations in ASPH cause facial dysmorphism, lens dislocation, anterior-segment abnormalities, and spontaneous filtering blebs, or Traboulsi syndrome. , 2014, American journal of human genetics.

[36]  V. Isaac,et al.  Caffeic acid: a review of its potential use in medications and cosmetics , 2014 .

[37]  Yang Liu,et al.  Crystal Structures of the Human RNA Demethylase Alkbh5 Reveal Basis for Substrate Recognition* , 2014, The Journal of Biological Chemistry.

[38]  K. Sak.  Site-Specific Anticancer Effects of Dietary Flavonoid Quercetin , 2014, Nutrition and cancer.

[39]  Timothy L. Foley,et al.  Discovery of ML324, a JMJD2 demethylase inhibitor with demonstrated antiviral activity , 2013 .

[40]  M. H. Rabinowitz,et al.  Inhibition of hypoxia-inducible factor prolyl hydroxylase domain oxygen sensors: tricking the body into mounting orchestrated survival and repair responses. , 2013, Journal of medicinal chemistry.

[41]  P. Zhan,et al.  Identification of the KDM2/7 Histone Lysine Demethylase Subfamily Inhibitor and its Antiproliferative Activity , 2013, Journal of medicinal chemistry.

[42]  R. Klose,et al.  5-Carboxy-8-hydroxyquinoline is a Broad Spectrum 2-Oxoglutarate Oxygenase Inhibitor which Causes Iron Translocation. , 2013, Chemical science.

[43]  S. Peña-Llopis,et al.  A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth , 2013, Nature Communications.

[44]  Michael A McDonough,et al.  Structural basis for inhibition of the fat mass and obesity associated protein (FTO). , 2013, Journal of medicinal chemistry.

[45]  Alan J. Tackett,et al.  Identification of Small Molecule Inhibitors of Jumonji AT-rich Interactive Domain 1B (JARID1B) Histone Demethylase by a Sensitive High Throughput Screen* , 2013, The Journal of Biological Chemistry.

[46]  Christopher J. Schofield,et al.  A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response , 2012, Nature.

[47]  R. Klose,et al.  Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases. , 2012, Journal of medicinal chemistry.

[48]  K. Helin,et al.  Identification of catechols as histone–lysine demethylase inhibitors , 2012, FEBS Letters.

[49]  J. Wands,et al.  Immunization with aspartate‐β‐hydroxylase–loaded dendritic cells produces antitumor effects in a rat model of intrahepatic cholangiocarcinoma , 2012, Hepatology.

[50]  Melanie V. Leveridge,et al.  Enabling Lead Discovery for Histone Lysine Demethylases by High-Throughput RapidFire Mass Spectrometry , 2012, Journal of biomolecular screening.

[51]  Melanie Leveridge,et al.  Configuration of a High-Content Imaging Platform for Hit Identification and Pharmacological Assessment of JMJD3 Demethylase Enzyme Inhibitors , 2012, Journal of biomolecular screening.

[52]  田中 俊典.  National Center for Biotechnology Information (NCBI) , 2012 .

[53]  S. M. de la Monte,et al.  siRNA inhibition of aspartyl-asparaginyl β-hydroxylase expression impairs cell motility, Notch signaling, and fetal growth. , 2011, Pathology, research and practice.

[54]  C. Schofield,et al.  Inhibition of 2-oxoglutarate dependent oxygenases. , 2011, Chemical Society reviews.

[55]  E. Cooper,et al.  Quercetin and Cancer Chemoprevention , 2011, Evidence-based complementary and alternative medicine : eCAM.

[56]  A. Jadhav,et al.  Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors , 2010, PloS one.

[57]  K. Song,et al.  The distribution and expression profiles of human Aspartyl/Asparaginyl beta-hydroxylase in tumor cell lines and human tissues. , 2010, Oncology reports.

[58]  A. Conejo-García,et al.  Structural basis for binding of cyclic 2-oxoglutarate analogues to factor-inhibiting hypoxia-inducible factor. , 2010, Bioorganic & medicinal chemistry letters.

[59]  C. Schofield,et al.  2-Oxoglutarate oxygenases are inhibited by a range of transition metals. , 2010, Metallomics : integrated biometal science.

[60]  P. Emsley,et al.  Features and development of Coot , 2010, Acta crystallographica. Section D, Biological crystallography.

[61]  Graeme Winter,et al.  xia2: an expert system for macromolecular crystallography data reduction , 2010 .

[62]  Randy J. Read,et al.  Acta Crystallographica Section D Biological , 2003 .

[63]  A. Jadhav,et al.  A miniaturized screen for inhibitors of Jumonji histone demethylases. , 2010, Molecular bioSystems.

[64]  Yi Zhang,et al.  Nickel Ions Inhibit Histone Demethylase JMJD1A and DNA Repair Enzyme ABH2 by Replacing the Ferrous Iron in the Catalytic Centers* , 2009, The Journal of Biological Chemistry.

[65]  C. Schofield,et al.  Inhibition of the histone lysine demethylase JMJD2A by ejection of structural Zn(II). , 2009, Chemical communications.

[66]  K. Sun,et al.  Monoclonal antibodies against human aspartyl (asparaginyl) beta-hydroxylase developed by DNA immunization. , 2009, Hybridoma.

[67]  Michael Q. Zhang,et al.  An integrative genomics approach identifies Hypoxia Inducible Factor-1 (HIF-1)-target genes that form the core response to hypoxia , 2009, Nucleic acids research.

[68]  Jiyi Wang,et al.  Prognostic value of aspartyl (asparaginyl)-beta-hydroxylase/humbug expression in non-small cell lung carcinoma. , 2009, Human pathology.

[69]  P. Hergenrother,et al.  PAC-1 activates procaspase-3 in vitro through relief of zinc-mediated inhibition. , 2009, Journal of molecular biology.

[70]  Max Costa,et al.  Iron- and 2-oxoglutarate-dependent Dioxygenases: an emerging group of molecular targets for nickel toxicity and carcinogenicity , 2009, BioMetals.

[71]  H. Ghanbari,et al.  Isolation and characterization of human antibodies targeting human aspartyl (asparaginyl) beta-hydroxylase. , 2008, Human antibodies.

[72]  F. Niesen,et al.  The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability , 2007, Nature Protocols.

[73]  Randy J. Read,et al.  Phaser crystallographic software , 2007, Journal of applied crystallography.

[74]  Michael J. Rybak,et al.  Tigecycline: First of a New Class of Antimicrobial Agents , 2006, Pharmacotherapy.

[75]  Jiannis Ragoussis,et al.  Concordant Regulation of Gene Expression by Hypoxia and 2-Oxoglutarate-dependent Dioxygenase Inhibition , 2006, Journal of Biological Chemistry.

[76]  Marcus Wiedmann,et al.  Aspartyl-(asparaginyl)-beta-hydroxylase regulates hepatocellular carcinoma invasiveness. , 2006, Journal of hepatology.

[77]  C. Schofield,et al.  Structural studies on 2-oxoglutarate oxygenases and related double-stranded beta-helix fold proteins. , 2006, Journal of inorganic biochemistry.

[78]  Kim E. Garbison,et al.  The Minimum Significant Ratio: A Statistical Parameter to Characterize the Reproducibility of Potency Estimates from Concentration-Response Assays and Estimation by Replicate-Experiment Studies , 2006, Journal of biomolecular screening.

[79]  Aleksandrs Gutcaits,et al.  Mildronate: an antiischemic drug for neurological indications. , 2006, CNS drug reviews.

[80]  R. Hausinger,et al.  Kinetic and spectroscopic investigation of CoII, NiII, and N-oxalylglycine inhibition of the FeII/alpha-ketoglutarate dioxygenase, TauD. , 2005, Biochemical and biophysical research communications.

[81]  K. Kavanagh,et al.  Structure of Human Phytanoyl-CoA 2-Hydroxylase Identifies Molecular Mechanisms of Refsum Disease* , 2005, Journal of Biological Chemistry.

[82]  J. Hogenesch,et al.  Gene expression profiling of hypoxia signaling in human hepatocellular carcinoma cells. , 2005, Physiological genomics.

[83]  K. Kivirikko,et al.  Effect of desferrioxamine and metals on the hydroxylases in the oxygen sensing pathway , 2005, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

[84]  C. Schofield,et al.  Selective inhibition of factor inhibiting hypoxia-inducible factor. , 2005, Journal of the American Chemical Society.

[85]  R. Gambari,et al.  Myocyte Enhancer Factor 2 Activates Promoter Sequences of the Human AβH-J-J Locus, Encoding Aspartyl-β-Hydroxylase, Junctin, and Junctate , 2005, Molecular and Cellular Biology.

[86]  C. Austin,et al.  Minimum Significant Ratio – A Statistic to Assess Assay Variability -- Assay Guidance Manual , 2013 .

[87]  M. Pfeffer,et al.  Effects of candesartan on mortality and morbidity in patients with chronic heart failure: the CHARM-Overall programme , 2003, The Lancet.

[88]  R. Wenger,et al.  The antimycotic ciclopirox olamine induces HIF‐1α stability, VEGF expression, and angiogenesis , 2003, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

[89]  H. Kleinman,et al.  The antifungal drug ciclopirox inhibits deoxyhypusine and proline hydroxylation, endothelial cell growth and angiogenesis in vitro , 2002, International journal of cancer.

[90]  J. Wands,et al.  Human Aspartyl (Asparaginyl) &bgr;-Hydroxylase Monoclonal Antibodies: Potential Biomarkers for Pancreatic Carcinoma , 2002, Pancreas.

[91]  N. Neff,et al.  Absence of Post-translational Aspartyl β-Hydroxylation of Epidermal Growth Factor Domains in Mice Leads to Developmental Defects and an Increased Incidence of Intestinal Neoplasia* , 2002, The Journal of Biological Chemistry.

[92]  A. Stern,et al.  Partial Purification and Characterization of Bovine Liver Aspartyl , & Hydroxylase * , 2001 .

[93]  D. Tulshian,et al.  SCH-202676: An allosteric modulator of both agonist and antagonist binding to G protein-coupled receptors. , 2001, Molecular pharmacology.

[94]  P. Portoghese,et al.  5'-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist , 2000 .

[95]  J. Wands,et al.  Overexpression of human aspartyl (asparaginyl) beta-hydroxylase is associated with malignant transformation. , 2000, Cancer research.

[96]  P. A. Harris,et al.  The discovery of potent cRaf1 kinase inhibitors. , 2000, Bioorganic & medicinal chemistry letters.

[97]  Thomas D. Y. Chung,et al.  A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays , 1999, Journal of biomolecular screening.

[98]  J. Wands,et al.  Overexpression of human aspartyl(asparaginyl)beta-hydroxylase in hepatocellular carcinoma and cholangiocarcinoma. , 1996, The Journal of clinical investigation.

[99]  Andrew Simon Bell,et al.  Sildenafil (VIAGRATM), a potent and selective inhibitor of type 5 cGMP phosphodiesterase with utility for the treatment of male erectile dysfunction , 1996 .

[100]  V. Garsky,et al.  Site-directed mutagenesis of residues in a conserved region of bovine aspartyl (asparaginyl) beta-hydroxylase: evidence that histidine 675 has a role in binding Fe2+. , 1996, Biochemistry.

[101]  Artur,et al.  Specific inhibition of eIF-5A and collagen hydroxylation by a single agent. Antiproliferative and fibrosuppressive effects on smooth muscle cells from human coronary arteries. , 1995, The Journal of clinical investigation.

[102]  C. Gieffers,et al.  Cloning and characterization of the human gene encoding aspartyl beta-hydroxylase. , 1994, Gene.

[103]  G. Semenza,et al.  Desferrioxamine induces erythropoietin gene expression and hypoxia-inducible factor 1 DNA-binding activity: implications for models of hypoxia signal transduction. , 1993, Blood.

[104]  P. Bork,et al.  Epidermal growth factor-like modules , 1993 .

[105]  Peter C. H. Hollman,et al.  Content of potentially anticarcinogenic flavonoids of 28 vegetables and 9 fruits commonly consumed in the Netherlands , 1992 .

[106]  H P Rang,et al.  Capsazepine: a competitive antagonist of the sensory neurone excitant capsaicin , 1992, British journal of pharmacology.

[107]  V. Garsky,et al.  Bovine liver aspartyl beta-hydroxylase. Purification and characterization. , 1991, The Journal of biological chemistry.

[108]  V. Garsky,et al.  Partial purification and characterization of bovine liver aspartyl beta-hydroxylase. , 1990, The Journal of biological chemistry.

[109]  V. Garsky,et al.  Aspartyl beta-hydroxylase: in vitro hydroxylation of a synthetic peptide based on the structure of the first growth factor-like domain of human factor IX. , 1989, Proceedings of the National Academy of Sciences of the United States of America.

[110]  D. Denis,et al.  L-663,536 (MK-886) (3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-isopropylindol-2-yl]-2,2 - dimethylpropanoic acid), a novel, orally active leukotriene biosynthesis inhibitor. , 1989, Canadian journal of physiology and pharmacology.

[111]  K. Berkner,et al.  Inhibitors of 2-ketoglutarate-dependent dioxygenases block aspartyl beta-hydroxylation of recombinant human factor IX in several mammalian expression systems. , 1989, The Journal of biological chemistry.

[112]  L. H. Huang,et al.  Hydroxylation of aspartic acid in domains homologous to the epidermal growth factor precursor is catalyzed by a 2-oxoglutarate-dependent dioxygenase. , 1989, Proceedings of the National Academy of Sciences of the United States of America.

[113]  G. M. Sapers,et al.  Varietal differences in distribution of quercetin and kaempferol in onion (Allium cepa L.) tissue , 1984 .

[114]  P. Fernlund,et al.  Beta-hydroxyaspartic acid in vitamin K-dependent proteins. , 1983, The Journal of biological chemistry.

[115]  K. Fujikawa,et al.  Complete amino acid sequence of the light chain of human blood coagulation factor X: evidence for identification of residue 63 as beta-hydroxyaspartic acid. , 1983, Biochemistry.

[116]  B J Abbott,et al.  Microbial transformation of A23187, a divalent cation ionophore antibiotic , 1979, Antimicrobial Agents and Chemotherapy.

[117]  M. S. Edwards,et al.  Use of cobaltous chloride in anaemia of maintenance hemodialysis patients. , 1971, Lancet.

[118]  W. Burkard,et al.  Increase of Cerebral Catecholamines caused by 3,4-Dihydroxyphenylalanine after Inhibition of Peripheral Decarboxylase , 1967, Nature.

[119]  E. Abraham,et al.  The structure of cephalosporin C , 1961 .