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Isoenzyme-Selective Inhibitors of Human Neuraminidases Reveal Distinct Effects on Cell Migration
Download2020-04-20
Howlader, Md. Amran, Guo, Tianlin, Chakraberty, Radhika, Cairo, Christopher W.
The human neuraminidase enzymes (NEU1, NEU2, NEU3, and NEU4) are a class of enzymes implicated in pathologies including cancer and diabetes. Several reports have linked neuraminidase activity to the regulation of cell migration in cancer cells. Using an in vitro cell migration assay on...
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Human neuraminidase isoenzymes show variable activities for 9-O-acetyl-sialoside substrates
Download2018-01-16
Hunter, Carmanah D, Khanna, Neha, Richards, Michele R, Darestani, Reza Rezaei, Zou, Chunxia, Klassen, John S, Cairo, Christopher W.
Recognition of terminal sialic acids is central to many cellular processes, and structural modification of sialic acid can disrupt these interactions. A prominent, naturally occuring, modification of sialic acid is 9-O-acetylation (9-O-Ac). Study of this modification through generation and...
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Molecular dynamics simulations of viral neuraminidase inhibitors with the human neuraminidase enzymes: Insights into isoenzyme selectivity
Download2018-05-16
Richards, Michele R, Guo, Tianlin, Hunter, Carmanah D, Cairo, Christopher W.
Inhibitors of viral neuraminidase enzymes have been previously developed as therapeutics. Humans can express multiple forms of neuraminidase enzymes (NEU1, NEU2, NEU3, NEU4) that share a similar active site and enzymatic mechanism with their viral counterparts. Using a panel of purified human...
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2018-05-24
Hunter, Carmanah D, Guo, Tianlin, Daskhan, Gour, Richards, Michele R, Cairo, Christopher W.
The plasma membrane of cells contains a diverse array of lipids that provide important structural and biological features. Glycolipids are typically a minor component of the cell membrane and consist primarily of glycosphingolipids (GSLs). GSLs in vertebrates contain a multifarious assortment of...
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2018-11-16
Guo, Tianlin, Heon-Roberts, Rachel, Zou, Chunxia, Zheng, Ruixiang, Pshezhetsky, Alexey V, Cairo, Christopher W.
Inhibitors of human neuraminidase enzymes (NEU) are recognized as important tools for the study of the biological functions of NEU and will be potent tools for elucidating the role of these enzymes in regulating the repertoire of cellular glycans. Here we report the discovery of selective...
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2018-01-05
Guo, Tianlin, Datwyler, Philipp, Demina, Ekaterina, Richards, Michele R, Ge, Peng, Zou, Chunxia, Zheng, Ruixiang Blake, Fougerat, Anne, Pshezhetsky, Alexey V, Ernst, Beat, Cairo, Christopher W.
Human neuraminidases (NEU) are associated with human diseases including cancer, atherosclerosis, and diabetes. To obtain small molecule inhibitors as research tools for the study of their biological functions, we designed a library of 2-deoxy-2,3-didehydro-N-acetylneuraminic acid (DANA) analogues...
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Construction of multivalent homo- and hetero-functional ABO blood group glycoconjugates using a trifunctional linker strategy
Download2017-12-12
Daskhan, Gour, Tran, Hanh-Thuc, Meloncelli, Peter J, Lowary, Todd L, West, Lori J, Cairo, Christopher W.
The design and synthesis of multivalent ligands displaying complex oligosaccharides is necessary for the development of therapeutics, diagnostics, and research tools. Here, we report an efficient conjugation strategy to prepare complex glycoconjugates with four copies of one or two separate...
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Screening anti-cancer drugs against tubulin using catch-and-release electrospray ionization mass spectrometry
Download2016
Kitova, Elena N., Klassen, John S., Winter, Philip, Tuszynski, Jack A., Darestani, Reza R.
Tubulin, which is the building block of microtubules, plays an important role in cell division. This critical role makes tubulin an attractive target for the development of chemotherapeutic drugs to treat cancer. Currently, there is no general binding assay for tubulin–drug interactions. The...
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2016
Klassen, John S., Yao, Yuyu, Kitova, Elena N., Richards, Michele R.
The results of an investigation into the influence of sulfolane, a commonly used supercharging agent, on electrospray ionization mass spectrometry (ESI-MS) measurements of protein–ligand affinities are described. Binding measurements carried out on four protein–carbohydrate complexes, lysozyme...