Research Topics
Species | Mark von ItzsteinSummaryAffiliation: Griffith University Country: Australia Publications
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Detail Information
Publications
Avian influenza virus, a very sticky situationMark von Itzstein
Institute for Glycomics, Gold Coast Campus, Griffith University, Queensland 4222, Australia
Curr Opin Chem Biol 12:102-8. 2008..This has provided new opportunity for the development of Group 1-specific anti-influenza drugs. Furthermore, a number of next generation sialidase inhibitors as anti-influenza drugs have also been developed...- Disease-associated carbohydrate-recognising proteins and structure-based inhibitor designMark von Itzstein
Institute for Glycomics, Gold Coast Campus, Griffith University, Queensland 4222, Australia
Curr Opin Struct Biol 18:558-66. 2008..The role of siglecs and galectins in a range of disease processes such as inflammation, apoptosis and cancer progression has also inspired significant structure-based inhibitor design research... 
The war against influenza: discovery and development of sialidase inhibitorsMark von Itzstein
Institute for Glycomics, Gold Coast Campus, Griffith University, Queensland 4222, Australia
Nat Rev Drug Discov 6:967-74. 2007..This article provides a historical perspective on the discovery and development of these drugs--zanamivir and oseltamivir--and highlights the value of structure-based drug design in this process...- STD NMR spectroscopy and molecular modeling investigation of the binding of N-acetylneuraminic acid derivatives to rhesus rotavirus VP8* coreThomas Haselhorst
Institute for Glycomics, Griffith University, Gold Coast Campus, PMB 50 Gold Coast Mail Centre, Queensland 9726, Australia
Glycobiology 17:68-81. 2007..NMR spectroscopic, molecular modeling, and infectivity inhibition results are in excellent agreement and provide valuable information for the design of inhibitors of rotavirus infection... - Synthesis and evaluation of novel 3-C-alkylated-Neu5Ac2en derivatives as probes of influenza virus sialidase 150-loop flexibilitySantosh Rudrawar
Institute for Glycomics, Gold Coast Campus, Griffith University, Queensland 4222, Australia
Org Biomol Chem 10:8628-39. 2012..This new class of inhibitors, which can 'trap' the open 150-loop form of the sialidase, should prove useful as probes of 150-loop flexibility... - Effects on sialic acid recognition of amino acid mutations in the carbohydrate-binding cleft of the rotavirus spike proteinMark J Kraschnefski
Institute for Glycomics, Gold Coast Campus, Griffith University, Queensland 4222, Australia
Glycobiology 19:194-200. 2009.... 
Crystallization and preliminary X-ray diffraction analysis of the carbohydrate-recognizing domain (VP8*) of bovine rotavirus strain NCDVXing Yu
Institute for Glycomics, Gold Coast Campus, Griffith University, Queensland 4222, Australia
Acta Crystallogr Sect F Struct Biol Cryst Commun 64:509-11. 2008..X-ray diffraction data were collected to a resolution of 2.0 A and the crystallographic structure of NCDV VP8*(64-224) was determined by molecular replacement...- Exploring the interactions of unsaturated glucuronides with influenza virus sialidaseBeenu Bhatt
Institute for Glycomics, Gold Coast Campus, Griffith University, Queensland 4222, Australia
J Med Chem 55:8963-8. 2012..The parent compound inhibits influenza virus sialidase at a sub-μM level; the introduction of small alkyl substituents or an acetyl group at C3 is also tolerated... - Synthesis of simple heparanase substratesAndrew G Pearson
Institute for Glycomics, Griffith University, Gold Coast Campus, Queensland 4222, Australia
Org Biomol Chem 9:4614-25. 2011..These compounds represent the simplest substrates of heparanase reported to date... - Cloning, expression, purification, crystallization and preliminary X-ray diffraction analysis of the VP8* carbohydrate-binding protein of the human rotavirus strain WaMark J Kraschnefski
Institute for Glycomics, Griffith University, PMB 50 Gold Coast Mail Centre, Queensland 9726, Australia
Acta Crystallograph Sect F Struct Biol Cryst Commun 61:989-93. 2005..Two crystal forms (trigonal P3(2)21 and monoclinic P2(1)) have been obtained and X-ray diffraction data have been collected, enabling determination of the VP8*(64-223) structure by molecular replacement... - Modelling, synthesis and biological evaluation of novel glucuronide-based probes of Vibrio cholerae sialidaseMaretta C Mann
Institute for Glycomics, Griffith University (Gold Coast Campus, Australia
Bioorg Med Chem 14:1518-37. 2006..cholerae sialidase complexed with Neu5Ac2en (1). All Neu5Ac2en mimetics tested were found to inhibit V. cholerae sialidase as determined using a standard fluorometric assay... - Novel structural insights into rotavirus recognition of ganglioside glycan receptorsXing Yu
Institute for Glycomics, Gold Coast Campus, Griffith University, Queensland 4222, Australia
J Mol Biol 413:929-39. 2011..These novel results also indicate the potential binding interactions of rotavirus VP8* with other sialic acid-containing gangliosides... - A 1H STD NMR spectroscopic investigation of sialylnucleoside mimetics as probes of CMP-Kdn synthetaseThomas Haselhorst
Institute for Glycomics, Griffith University (Gold Coast Campus, PMB 50 Gold Coast Mail Centre, Queensland 9726, Australia
Glycoconj J 23:371-5. 2006.... - Sialic acid dependence in rotavirus host cell invasionThomas Haselhorst
Institute for Glycomics, Gold Coast Campus, Griffith University, Parklands Drive, Southport, Queensland 4222, Australia
Nat Chem Biol 5:91-3. 2009..This is in contrast to the widely accepted paradigm that sialic acids are irrelevant in host cell recognition by sialidase-insensitive rotaviruses... - Insight into host cell carbohydrate-recognition by human and porcine rotavirus from crystal structures of the virion spike associated carbohydrate-binding domain (VP8*)Helen Blanchard
Institute for Glycomics, Griffith University, Gold Coast Campus, PMB 50 Gold Coast Mail Centre, Queensland, 9726, Australia
J Mol Biol 367:1215-26. 2007.... - Targeting the expression of functional murine CMP-sialic acid transporter to the E. coli inner membraneAndrea Maggioni
Institute for Glycomics, Gold Coast Campus Griffith University, Queensland 4222, Australia
Biochem Biophys Res Commun 362:779-84. 2007..coli and mixed phosphatidylcholine-E. coli inner membrane proteoliposomes incorporating recombinant CMP-sialic acid transporter to accumulate CMP-sialic acid in vitro... - Structural basis of rotavirus strain preference toward N-acetyl- or N-glycolylneuraminic acid-containing receptorsXing Yu
Institute for Glycomics, Griffith University, Gold Coast, Queensland, Australia
J Virol 86:13456-66. 2012.... - Synthesis and biological evaluation of galactofuranosyl alkyl thioglycosides as inhibitors of mycobacteriaChris B Davis
Institute for Glycomics, Griffith University Gold Coast Campus, PMB 50 Gold Coast Mail Centre, Queensland 9726, Australia
Carbohydr Res 342:1773-80. 2007..Both Galf 9-heptadecyl thioglycoside and sulfone displayed in vitro inhibition (MIC) of the growth of Mycobacterium smegmatis below 5 microg/mL, while Galf 1-octyl thioglycoside gave no inhibition at or below 32 microg/mL... - Unsaturated N-acetyl- D-glucosaminuronic acid glycosides as inhibitors of influenza virus sialidaseMaretta C Mann
Institute for Glycomics, Griffith University, Gold Coast Campus, PMB 50 Gold Coast Mail Centre, Queensland 9726, Australia
Glycoconj J 23:127-33. 2006..We have employed a sialidase inhibition assay for biological evaluation of the target compounds and to our delight these mimetics have displayed significant inhibition of influenza virus sialidase... - The synthesis and biological evaluation of lactose-based sialylmimetics as inhibitors of rotaviral infectionAngela Liakatos
Institute for Glycomics, Griffith University (Gold Coast Campus, PMB 50 Gold Coast Mail Centre, QLD 9726, Australia
Bioorg Med Chem 14:739-57. 2006.... - The evolution of galactose alpha2,3-sialyltransferase: Ciona intestinalis ST3GAL I/II and Takifugu rubripes ST3GAL II sialylate Galbeta1,3GalNAc structures on glycoproteins but not glycolipidsFriederike Lehmann
Institute for Glycomics, Gold Coast Campus, Griffith University, QLD, 4222, Australia
Glycoconj J 25:323-34. 2008..This suggests that during the evolution of the ST3Gal II, probably following the separation of the teleosts, a significant shift in substrate specificity enabling the sialylation of gangliosides took place... - Anti-influenza drug discovery: are we ready for the next pandemic?Tasneem Islam
Institute for Glycomics, Griffith University Gold Coast Campus, PMB50, Gold Coast Mail Centre, Queensland 9726, Australia
Adv Carbohydr Chem Biochem 61:293-352. 2007 - Direct detection of ligand binding to Sepharose-immobilised protein using saturation transfer double difference (STDD) NMR spectroscopyThomas Haselhorst
Institute for Glycomics, Griffith University Gold Coast Campus, PMB 50 Gold Coast Mail Centre, QLD 9726, Australia
Biochem Biophys Res Commun 359:866-70. 2007.... - Endosialidase NF appears to bind polySia DP5 in a helical conformationThomas Haselhorst
Institute for Glycomics, Griffith University (Gold Coast Campus, PMB 50 Gold Coast Mail Centre, Queensland 9726, Australia
Chembiochem 7:1875-7. 2006 - Synthesis and evaluation of 4-O-alkylated 2-deoxy-2,3-didehydro-N-acetylneuraminic acid derivatives as inhibitors of human parainfluenza virus type-3 sialidase activityDavid J Tindal
Institute for Glycomics, Griffith University Gold Coast Campus, PMB 50 Gold Coast Mail Centre, Queensland 9726, Australia
Bioorg Med Chem Lett 17:1655-8. 2007..This is comparable or improved activity compared to the parent 4-hydroxy compound... - Cracking the code for H5N1-bird flu and beyondRobin J Thomson
Institute for Glycomics, Griffith University, Gold Coast Campus, Parklands Drive, Southport, Queensland 4222, Australia
Curr Drug Deliv 6:343-6. 2009..Important advances in the interrogation of influenza virus' surface glycoprotein haemagglutinin by NMR spectroscopy have been made in recent times. An overview of some of these advances is provided... - Saturation transfer difference (STD) 1H-NMR experiments and in silico docking experiments to probe the binding of N-acetylneuraminic acid and derivatives to Vibrio cholerae sialidaseThomas Haselhorst
Institute for Glycomics, Griffith University Gold Coast Campus, Queensland, Australia
Proteins 56:346-53. 2004.... - Differential carbohydrate binding and cell surface glycosylation of human cancer cell linesNadia X Arndt
Institute for Glycomics, Gold Coast Campus, Griffith University, Queensland 4222, Australia
J Cell Biochem 112:2230-40. 2011..The findings of this study provide the groundwork for further investigation into the numerous glycan-lectin interactions that are exhibited by immortalised cell lines... - An efficient approach to N-acetyl-D-glucosaminuronic acid-based sialylmimetics as potential sialidase inhibitorsMaretta C Mann
Institute for Glycomics, Griffith University (Gold Coast Campus, PMB 50 Gold Coast Mail Centre, Queensland 9726, Australia
Bioorg Med Chem Lett 14:5555-8. 2004..Elaboration of glucosaminuronides 15 and 18 provided novel sialylmimetics 21 and 22, which showed inhibition of Vibrio cholerae sialidase... - Synthesis and evaluation of galactofuranosyl N,N-dialkyl sulfenamides and sulfonamides as antimycobacterial agentsDavid J Owen
Institute for Glycomics, Griffith University Gold Coast Campus, PMB 50 Gold Coast Mail Centre, Queensland 9726, Australia
Bioorg Med Chem Lett 17:2274-7. 2007..The most potent compound, the Galf N,N-didecyl sulfenamide 8d, displayed anti-mycobacterial activity (MIC) of 1 microg/mL in a cell based assay against a representative strain of Mycobacterium smegmatis... - Differential carbohydrate recognition by Campylobacter jejuni strain 11168: influences of temperature and growth conditionsChristopher J Day
Institute for Glycomics, Griffith University Gold Coast Campus, Queensland, Australia
PLoS ONE 4:e4927. 2009..jejuni to a Caco-2 intestinal cell line. Our data suggests that the binding of mannose and/or N-acetylneuraminic acid may provide the initial interactions important for colonisation following environmental exposure... - Avian influenza H5-containing virus-like particles (VLPs): host-cell receptor specificity by STD NMR spectroscopyThomas Haselhorst
Institute for Glycomics, Griffith University, Gold Coast Campus, Queensland, 4222, Australia
Angew Chem Int Ed Engl 47:1910-2. 2008 - Crystallization and preliminary X-ray diffraction analysis of the sialic acid-binding domain (VP8*) of porcine rotavirus strain CRW-8Stacy A Scott
Institute for Glycomics, Griffith University, PMB 50, Gold Coast Mail Centre, Queensland 9726, Australia
Acta Crystallograph Sect F Struct Biol Cryst Commun 61:617-20. 2005..Diffraction data have been collected to 2.3 A resolution, enabling the determination of the VP8* structure by molecular replacement... - C-4 Modified Sialosides Enhance Binding to Siglec-2 (CD22): Towards Potent Siglec Inhibitors for ImmunoglycotherapySørge Kelm
Centre for Biomolecular Interactions Bremen, Department of Biology and Chemistry, University of Bremen, 28334 Bremen Germany http www cbib uni bremen de Institute for Glycomics, Gold Coast Campus, Griffith University, Queensland, 4222 Australia http www griffith edu au glycomics
Angew Chem Int Ed Engl 52:3616-20. 2013..This approach gives a lead compound that has sub-micromolar affinity for Siglec-2 and may provide a pathway for immunoglycotherapy strategies for autoimmune diseases and B cell derived non-Hodgkin's lymphoma... - Novel sialic acid derivatives lock open the 150-loop of an influenza A virus group-1 sialidaseSantosh Rudrawar
Institute for Glycomics, Gold Coast Campus, Griffith University, Queensland 4222, Australia
Nat Commun 1:113. 2010..This is the first direct proof that compounds may be developed to selectively target the pandemic A/H1N1, avian A/H5N1 and other group-1 sialidase-containing viruses, based on an open 150-loop conformation of the enzyme... - Functional expression of the CMP-sialic acid transporter in Escherichia coli and its identification as a simple mobile carrierJoe Tiralongo
Institute for Glycomics, Griffith University (Gold Coast Campus, PMB 50 Gold Coast Mail Centre, Queensland 9726, Australia
Glycobiology 16:73-81. 2006..Kinetic studies carried out with CMP-Neu5Ac and established CMP-Neu5Ac antagonist's evaluated natural conformation of the reconstituted protein and clearly demonstrate that the transporter acts as a simple mobile carrier... - Probing a CMP-Kdn synthetase by 1H, 31P, and STD NMR spectroscopyThomas Haselhorst
Institute for Glycomics, Griffith University (Gold Coast Campus, PMB 60 Gold Coast Mail Centre, Queensland 9726, Australia
Biochem Biophys Res Commun 327:565-70. 2005..Furthermore, proton-decoupled (31)P NMR spectroscopy was successfully used to follow the enzyme reaction and clearly confirmed the appearance of CMP-Sia and the inorganic pyrophosphate by-product... - Uronosyl phosphonate-based sialidase inhibitor synthesis and conformational analysisBeenu Bhatt
Institute for Glycomics, Griffith University, Gold Coast Campus, Queensland 4222, Australia
Bioorg Med Chem Lett 22:7623-6. 2012..For the α-L-threo-hex-4-en derivative this conformation is equivalent to that of Neu5Ac2en, and opposite to that seen for alkyl O-glycosides with the same overall stereochemistry... - Accessing C-1 phosphonylated 2-acylamino uronic acids via 2-nitro-glycalsBeenu Bhatt
Institute for Glycomics, Griffith University, Gold Coast Campus, Queensland 4222, Australia
J Org Chem 76:4099-104. 2011..Reversing the reaction order resulted in the exclusive formation of the β-D-gluco-configured phosphonate. In both cases the thermodynamic 1,2-trans-di-equatorial phosphonylation product is obtained... - NMR spectroscopic and molecular modeling investigations of the trans-sialidase from Trypanosoma cruziThomas Haselhorst
Institute for Glycomics, Griffith University (Gold Coast Campus, PMB 50 Gold Coast Mail Centre, Queensland, 9726, Australia
Glycobiology 14:895-907. 2004..The association of the asialo acceptor with the active site is an absolute requirement for the transfer reaction to proceed... - Towards the synthesis of aryl glucuronides as potential heparanase probes. An interesting outcome in the glycosidation of glucuronic acid with 4-hydroxycinnamic acidAndrew G Pearson
Institute for Glycomics, Griffith University (Gold Coast Campus, PMB 50, Gold Coast Mail Centre, Australia
Carbohydr Res 340:2077-85. 2005..This paper rationalises the formation of each of these products, and reports our efforts in trying to optimise the formation of the alpha-fluoride 16... - Carbohydrates as inhibitors of rotaviral infectionMilton J Kiefel
Centre for Biomolecular Science and Drug Discovery, Griffith University (Gold Coast Campus, PMB 50, Gold Coast Mail Centre, Queensland 9726, Australia
Methods Enzymol 363:395-412. 2003 - Second sialic acid binding site in Newcastle disease virus hemagglutinin-neuraminidase: implications for fusionViatcheslav Zaitsev
Centre for Biomolecular Sciences, University of St. Andrews, St. Andrews, Fife KY16 9ST, United Kingdom
J Virol 78:3733-41. 2004..Three different crystal forms of NDV HN now reveal identical tetrameric arrangements of HN monomers, perhaps indicative of the tetramer association found on the viral surface... - Sialic acid recognition by Vibrio cholerae neuraminidaseIbrahim Moustafa
Centre for Biomolecular Sciences, University of St Andrews, St Andrews, Fife KY16 9ST, Scotland
J Biol Chem 279:40819-26. 2004..The discovery of the sialic acid binding site in the N-lectin-like domain suggests that this might help target VCNA to sialic acid-rich environments, thereby enhancing the catalytic efficiency of the enzyme... - An investigation of the activity of recombinant rat skeletal muscle cytosolic sialidaseSamia Albouz-Abo
Department of Medicinal Chemistry, Monash University Parkville Campus, 381 Royal Parade, Parkville, VIC 3052, Australia
FEBS Lett 579:1034-8. 2005..This result further supports the notion that all sialidases appear to be retaining enzymes... - A convenient synthesis of C-galactofuranosylic compounds (C-galactofuranosides)David J Owen
Department of Medicinal Chemistry, Monash University (Parkville Campus, 381 Royal Parade, Parkville, Victoria 3052, Australia
Carbohydr Res 337:2017-22. 2002..A procedure for the efficient hydrolysis of the introduced nitrile group to produce the methyl ester is reported, along with procedures for the synthesis of both the corresponding alpha,beta-unsaturated, and 3-deoxy ester derivatives... - Lysosomal sialidase (neuraminidase-1) is targeted to the cell surface in a multiprotein complex that facilitates elastic fiber assemblyAleksander Hinek
Cardiovascular Research Program, The Hospital for Sick Children, University of Toronto, Ontario, Canada
J Biol Chem 281:3698-710. 2006..In turn, the exposed galactosugars interact with the galectin domain of EBP, thereby inducing the release of transported tropoelastin molecules and facilitating their subsequent assembly into elastic fibers... - Structural analysis of a designed inhibitor complexed with the hemagglutinin-neuraminidase of Newcastle disease virusCharlotte Ryan
Centre for Biomolecular Sciences, University of St Andrews, St Andrews, Fife, KY16 9ST, Scotland, UK
Glycoconj J 23:135-41. 2006..These results highlight the striking difference between the influenza neuraminidase and paramyxovirus HN active sites, and provide a platform for the development of improved HN inhibitors...