Research Topics
Genomes and GenesSpecies | Hakon LefflerSummaryAffiliation: Lund University Country: Sweden Publications
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Publications
Introduction to galectinsHakon Leffler
Section MIG Microbiology, Immunology, Glycobiology, Inst Laboratory Medicine, Lund University, Sweden
Glycoconj J 19:433-40. 2004..Here we will give a brief introduction to the galectins as a protein family with some comments on nomenclature...- Dendritic cell maturation results in pronounced changes in glycan expression affecting recognition by siglecs and galectinsMarieke Bax
Department of Molecular Cell Biology and Immunology, Vrije Universiteit University Medical Center, Amsterdam, The Netherlands
J Immunol 179:8216-24. 2007..Interestingly, the binding of the LacNAc-specific lectins galectin-3 and -8 increased during maturation and up-regulation of sialic acid expression by mDC correlated with an increased binding of siglec-1, -2, and -7... 
Ligand induced galectin-3 protein self-associationAdriana Lepur
Microbiology, Immunology, and Glycobiology MIG Section, Department of Laboratory Medicine, Lund University, 223 62 Lund, Sweden
J Biol Chem 287:21751-6. 2012....- The carbohydrate-binding site in galectin-3 is preorganized to recognize a sugarlike framework of oxygens: ultra-high-resolution structures and water dynamicsKadhirvel Saraboji
Department of Biochemistry and Structural Biology, Center for Molecular Protein Science, Box 124, Lund University, SE 221 00 Lund, Sweden
Biochemistry 51:296-306. 2012..These observations make a case for protein cryo-crystallography as a valuable screening method in fragment-based drug discovery and further suggest that identification of water sites might inform inhibitor design... 
Protein subtype-targeting through ligand epimerization: talose-selectivity of galectin-4 and galectin-8Christopher T Oberg
Organic Chemistry, Lund University, PO Box 124, SE 221 00 Lund, Sweden
Bioorg Med Chem Lett 18:3691-4. 2008..Galectin-4C and 8N were found to prefer the d-talopyranose configuration to the natural ligand d-galactopyranose configuration. Derivatization at talose O2 and/or O3 provided selective submillimolar inhibitors for these two galectins...- Arginine binding motifs: design and synthesis of galactose-derived arginine tweezers as galectin-3 inhibitorsChristopher T Oberg
Organic Chemistry, Lund University, SE 221 00 Lund, Sweden
J Med Chem 51:2297-301. 2008..Modeling revealed arginine-144 being pinched by the C3 benzamide and O2 anionic substituents in that the benzamide stacked face-to-face and the anionic O2 substituent ion-paired with the guanidinium moiety... - Galectin-1-binding glycoforms of haptoglobin with altered intracellular trafficking, and increase in metastatic breast cancer patientsMichael C Carlsson
Section Microbiology, Immunology, Glycobiology, Department of Laboratory Medicine, Lund University, Lund, Sweden
PLoS ONE 6:e26560. 2011..In conclusion, galectin-1 detects a new type of functional biomarker for cancer: a specific type of glycoform of haptoglobin, and possibly other serum glycoproteins, with a different function after uptake into tissue cells... - Double affinity amplification of galectin-ligand interactions through arginine-arene interactions: synthetic, thermodynamic, and computational studies with aromatic diamido thiodigalactosidesIan Cumpstey
Organic Chemistry, Lund University, POB 124, 22100 Lund, Sweden
Chemistry 14:4233-45. 2008..Furthermore, the arginine mutants revealed distinct differences between free, flexible, and solvent-exposed arginine side chains and tightly ion-paired arginine side chains in interactions with aromatic systems... - Monovalent interactions of galectin-1Emma Salomonsson
Institute of Laboratory Medicine, Lund University, Lund, Sweden
Biochemistry 49:9518-32. 2010..It follows that such weak additional interactions must be important for the biological function of galectin-1 and also for the design of galectin-1 inhibitors... - Galectin-3 endocytosis by carbohydrate independent and dependent pathways in different macrophage like cell typesAdriana Lepur
Section MIG Microbiology, Immunology, Glycobiology, Department of Laboratory Medicine, Lund University, 223 62 Lund, Sweden
Biochim Biophys Acta 1820:804-18. 2012..We have studied endocytosis of galectin-3 as one important step relevant for its function, and compared it between variants of a macrophage like cell line, and non-macrophage cells... - The anti-angiogenic peptide anginex greatly enhances galectin-1 binding affinity for glycoproteinsEmma Salomonsson
Section Microbiology, Immunology, Glycobiology, Institute of Laboratory Medicine, Lund University, Solvegatan 23, SE 223 62 Lund, Sweden
J Biol Chem 286:13801-4. 2011..Here we show that when bound to anginex, galectin-1 binds various glycoproteins with hundred- to thousand-fold higher affinity. Anginex also interacts with galectin-2, -7, -8N, and -9N but not with galectin-3, -4, or -9C... - Galectin-inhibitory thiodigalactoside ester derivatives have antimigratory effects in cultured lung and prostate cancer cellsTamara Delaine
Organic Chemistry, Lund University, POB 124, SE 221 00 Lund, Sweden
J Med Chem 51:8109-14. 2008..Two of the compounds were selected for testing in cell culture and were shown to have potent antimigratory effects on human PC-3 prostate and human A549 nonsmall-cell lung cancer cells... - Different fractions of human serum glycoproteins bind galectin-1 or galectin-8, and their ratio may provide a refined biomarker for pathophysiological conditions in cancer and inflammatory diseaseMichael C Carlsson
Section MIG Microbiology, Immunology, Glycobiology, Department of Laboratory Medicine, Lund University, Lund, Sweden
Biochim Biophys Acta 1820:1366-72. 2012..Now we have explored the use of a combination of two galectins with different specificities, to further increase biomarker sensitivity and specificity... - Fragment-based development of triazole-substituted O-galactosyl aldoximes with fragment-induced affinity and selectivity for galectin-3Johan Tejler
Organic Chemistry, Lund University, POB 124, SE 22100, Lund, Sweden
Org Biomol Chem 7:3982-90. 2009..Galectin-7, 8 N-terminal CRD, and 9 N-terminal CRD bound the inhibitors only weakly. The galectin-3 selectivity was hypothesized to stem from interaction of the aldoxime moiety with a site not present in the other galectins... - Mutational tuning of galectin-3 specificity and biological functionEmma Salomonsson
Section MIG, Department of Laboratory Medicine, Lund University, 223 62 Lund, Sweden
J Biol Chem 285:35079-91. 2010..Finally, the mutants have helped to define the differences in fine specificity shown by Xenopus, mouse, and human galectin-3 and, as such, the evidence for adaptive change during evolution... - Synthesis of a 3'-naphthamido-LacNAc fluorescein conjugate with high selectivity and affinity for galectin-3Karolina Aplander
Organic Chemistry, Lund University, P.O. Box 124, SE-221 00 Lund, Sweden
Carbohydr Res 341:1363-9. 2006..Its use as a selective and sensitive galectin-3 probe is demonstrated with fluorescence polarization measurements... - Arene-anion based arginine-binding motif on a galactose scaffold: structure-activity relationships of interactions with arginine-rich galectinsChristopher T Oberg
Organic Chemistry, Lund University, PO Box 124, SE 221 00 Lund, Sweden
Chemistry 17:8139-44. 2011..In the second series, the electron-donating capacity of the 4-substituent of the C3-benzamides correlated positively with the magnitude of the affinity enhancement by the 2O-sulfate... - Different affinity of galectins for human serum glycoproteins: galectin-3 binds many protease inhibitors and acute phase proteinsCecilia Cederfur
Department of Laboratory Medicine, Section MIG Microbiology, Immunology, Glycobiology, Lund University, 223 62 Lund, Sweden
Glycobiology 18:384-94. 2008.... - Synthesis of galactose-mimicking 1H-(1,2,3-triazol-1-yl)-mannosides as selective galectin-3 and 9N inhibitorsJohan Tejler
Organic Chemistry, Lund University, PO Box 124, SE 221 00 Lund, Sweden
Carbohydr Res 342:1869-75. 2007.... - C2-symmetrical thiodigalactoside bis-benzamido derivatives as high-affinity inhibitors of galectin-3: efficient lectin inhibition through double arginine-arene interactionsIan Cumpstey
Organic Chemistry, Lund University, Box 124, 221 00 Lund, Sweden
Angew Chem Int Ed Engl 44:5110-2. 2005 - Galectin-8 in IgA nephritis: decreased binding of IgA by galectin-8 affinity chromatography and associated increased binding in non-IgA serum glycoproteinsMichael C Carlsson
Section MIG Microbiology, Immunology, Glycobiology, Department of Laboratory Medicine, Lund University, Solvegatan 23, 223 62, Lund, Sweden
J Clin Immunol 32:246-55. 2012..It is caused by accumulation of IgA1-containing immune complexes in the kidney resulting in renal failure, which is thought to be due to altered glycosylation of IgA with a decrease of 2-3-sialylated galactosides (NeuAcα2-3Gal)... - Structural and thermodynamic studies on cation-Pi interactions in lectin-ligand complexes: high-affinity galectin-3 inhibitors through fine-tuning of an arginine-arene interactionPernilla Sörme
Organic and Bioorganic Chemistry, Lund University, P O Box 124, SE 221 00 Lund, Sweden
J Am Chem Soc 127:1737-43. 2005..The results demonstrate that protein-ligand interactions can be significantly enhanced by the fine-tuning of arginine-arene interactions... - Protein flexibility and conformational entropy in ligand design targeting the carbohydrate recognition domain of galectin-3Carl Diehl
Center for Molecular Protein Science, Biophysical Chemistry, Lund University, P O Box 124, SE 22100 Lund, Sweden
J Am Chem Soc 132:14577-89. 2010.... - 3-(1,2,3-Triazol-1-yl)-1-thio-galactosides as small, efficient, and hydrolytically stable inhibitors of galectin-3Bader A Salameh
Organic Chemistry, Lund University, PO Box 124, SE-221 00 Lund, Sweden
Bioorg Med Chem Lett 15:3344-6. 2005.... - Synthesis of O-galactosyl aldoximes as potent LacNAc-mimetic galectin-3 inhibitorsJohan Tejler
Organic Chemistry, Lund University, PO Box 124, SE-221 00 Lund, Sweden
Bioorg Med Chem Lett 15:2343-5. 2005.... - Intracellular sorting of galectin-8 based on carbohydrate fine specificitySusanne Carlsson
Institute of Laboratory Medicine, Section of Microbiology Immunology and Glycobiology, Lund University, Solvegatan 23, S 223 62 Lund, Sweden
Glycobiology 17:906-12. 2007..Moreover, the pattern of galectin-3 after endocytosis differed from that of both the wt and mutant galectin-8. These data clearly demonstrate a role of galectin fine specificity for intracellular targeting... - Studies of arginine-arene interactions through synthesis and evaluation of a series of galectin-binding aromatic lactose estersIan Cumpstey
Organic Chemistry, Lund University, P O Box 124, Lund, Sweden
Chembiochem 8:1389-98. 2007..The results provide a basis for the design of lectin inhibitors and drugs that exploit interactions with arginine side-chains via aromatic moieties, which are involved in intramolecular protein salt bridges... - Taloside inhibitors of galectin-1 and galectin-3Patrick M Collins
Institute for Glycomics, Gold Coast Campus, Griffith University, Queensland 4222, Australia Organic Chemistry, Lund University, PO Box 124, SE 22100 Lund, Sweden Department of Laboratory Medicine, Lund University, Solvegatan 23, SE 22362 Lund, Sweden
Chem Biol Drug Des 79:339-46. 2012.... - Synthesis of multivalent lactose derivatives by 1,3-dipolar cycloadditions: selective galectin-1 inhibitionJohan Tejler
Organic Chemistry, Lund University, PO Box 124, SE-221 00 Lund, Sweden
Carbohydr Res 341:1353-62. 2006..This divalent compound had at least one order of magnitude higher affinity for galectin-1 than for any of the other galectins investigated... - Synthesis of a phenyl thio-beta-D-galactopyranoside library from 1,5-difluoro-2,4-dinitrobenzene: discovery of efficient and selective monosaccharide inhibitors of galectin-7Ian Cumpstey
Organic Chemistry, Lund University, Box 124, SE-221 00, Lund, Sweden
Org Biomol Chem 3:1922-32. 2005..The best inhibitors against galectin-7 were poor against the other galectins and thus have potential as structurally simple and selective tools for dissecting biological functions of galectin-7... - Glycoproteomic identification of galectin-3 and -8 ligands in bronchoalveolar lavage of mild asthmatics and healthy subjectsCecilia Cederfur
MIG Microbiology, Immunology, Glycobiology, Dept of Laboratory Medicine Lund, Sweden
Biochim Biophys Acta 1820:1429-36. 2012..Galectins are found in cells of the airways and in airway secretions, but their glycoprotein ligands there have only been studied to a very limited extent... - Inhibition mechanism of human galectin-7 by a novel galactose-benzylphosphate inhibitorGeoffrey Masuyer
Department of Biology and Biochemistry, University of Bath, Bath, UK
FEBS J 279:193-202. 2012..This structural information will allow the design of further inhibitors with improved potency and specificity... - Galectin-3 inhibits Schwann cell proliferation in cultured sciatic nervePer Gustavsson
Department of Cell and Organism Biology, Lund University, Lund, Sweden
Neuroreport 18:669-73. 2007..We conclude that galectin-3 reduces proliferation of Schwann cells in cultured sciatic nerve segments by a mechanism which is independent of its carbohydrate-binding moiety... - Fluorescence polarization as an analytical tool to evaluate galectin-ligand interactionsPernilla Sörme
Organic and Bioorganic Chemistry, Lund University, POB 124, SE 221 00 Lund, Sweden
Anal Biochem 334:36-47. 2004..As all interaction components are known, K(d) values for galectin-inhibitor interaction can be directly calculated without approximation other than the assumption of a simple one-site competition... - Superantigen- and TLR-dependent activation of tonsillar B cells after receptor-mediated endocytosisJohan Jendholm
Department of Laboratory Medicine, University Hospital Malmo, Lund University, Malmo, Sweden
J Immunol 182:4713-20. 2009..In conclusion, our findings suggest an important role of TLRs in the adaptive immune response and reveal novel insights into the T cell-independent B cell activation induced by bacteria... - Design and synthesis of galectin inhibitorsPernilla Sörme
Department of Bioorganic Chemistry, Lund University, P O Box 124, Lund SE 22100, Sweden
Methods Enzymol 363:157-69. 2003 - Efficient and expedient two-step pyranose-retaining fluorescein conjugation of complex reducing oligosaccharides: galectin oligosaccharide specificity studies in a fluorescence polarization assayChristopher T Oberg
Department of Chemistry, University of Waterloo, 200 University Avenue West, Waterloo, Ontario N2L 3G1, Canada
Bioconjug Chem 14:1289-97. 2003..The results show that fluorescence labeling can be chemically tuned to find optimal probes for individual galectins but also probes interacting well with many galectins... - Phylogenetic analysis of the vertebrate galectin familyDenis Houzelstein
Laboratoire de Genetique et Developpement des Mammiferes, Institut Jacques Monod, Paris, France
Mol Biol Evol 21:1177-87. 2004..We show that all vertebrate mono-CRD galectins known to date belong to either the F3- or F4- subtype. A sequence of duplication and divergence events of the different galectins in chordates is proposed... - Galectin-4 in normal tissues and cancerMargaret E Huflejt
Sidney Kimmel Cancer Center, 10835 Altman Row, San Diego, CA 92121, USA
Glycoconj J 20:247-55. 2004..Because of its distinct induction in breast and other cancers, it may be a valuable diagnostic marker and target for the development of inhibitory carbohydrate-based drugs... - Affinity of galectin-8 and its carbohydrate recognition domains for ligands in solution and at the cell surfaceSusanne Carlsson
Section of Microbiology Immunology and Glycobiology MIG, Solvegatan 23, 223 62, Sweden
Glycobiology 17:663-76. 2007..Also galectin-8 binding and signaling at cell surfaces can be explained by combined binding of the two CRDs to low or medium affinity ligands, and their highest affinity ligands, such as sialylated galactosides, are not required... - Enhancement of bound-state residual dipolar couplings: conformational analysis of lactose bound to Galectin-3Tiandi Zhuang
Complex Carbohydrate Research Center, University of Georgia, Athens, GA 30602, USA
Protein Sci 15:1780-90. 2006..As an illustration, we have added a propyl chain to the C terminus of the carbohydrate recognition domain of the protein, Galectin-3, and report enhanced RDCs that prove consistent with known bound-ligand geometries for this protein... - Complex N-glycans are the major ligands for galectin-1, -3, and -8 on Chinese hamster ovary cellsSantosh Kumar Patnaik
Department of Cell Biology, Albert Einstein Collegeof Medicine, New York, NY 10461 USA
Glycobiology 16:305-17. 2006....