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Triazole linker-bas...
Triazole linker-based trivalent sialic acid inhibitors of adenovirus type 37 infection of human corneal epithelial cells
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- Caraballo, Rémi (author)
- Umeå universitet,Kemiska institutionen,Umeå Centre for Microbial Research (UCMR)
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- Saleeb, Michael (author)
- Umeå universitet,Kemiska institutionen,Umeå Centre for Microbial Research (UCMR)
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- Bauer, Johannes (author)
- Interfaculty Institute of Biochemistry, University of Tübingen, Germany
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- Liaci, Antonio-Manuel (author)
- Interfaculty Institute of Biochemistry, University of Tübingen, Germany
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- Chandra, Naresh (author)
- Umeå universitet,Virologi,Umeå Centre for Microbial Research (UCMR),Molekylär Infektionsmedicin, Sverige (MIMS)
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- Storm, Rickard J (author)
- Umeå universitet,Virologi,Umeå Centre for Microbial Research (UCMR),Molekylär Infektionsmedicin, Sverige (MIMS)
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- Frängsmyr, Lars (author)
- Umeå universitet,Virologi,Umeå Centre for Microbial Research (UCMR),Molekylär Infektionsmedicin, Sverige (MIMS)
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- Qian, Weixing (author)
- Umeå universitet,Kemiska institutionen
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- Stehle, Thilo (author)
- Interfaculty Institute of Biochemistry, University of Tübingen, Germany ; Department of Pediatrics, Vanderbilt University School of Medicine, USA
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- Arnberg, Niklas (author)
- Umeå universitet,Virologi,Umeå Centre for Microbial Research (UCMR),Molekylär Infektionsmedicin, Sverige (MIMS)
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- Elofsson, Mikael (author)
- Umeå universitet,Kemiska institutionen,Umeå Centre for Microbial Research (UCMR)
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(creator_code:org_t)
- 2015
- 2015
- English.
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In: Organic and biomolecular chemistry. - 1477-0520 .- 1477-0539. ; 13:35, s. 9194-9205
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- Adenovirus type 37 (Ad37) is one of the principal agents responsible for epidemic keratoconjunctivitis (EKC), a severe ocular infection that remains without any available treatment. Recently, a trivalent sialic acid derivative (ME0322, Angew. Chem. Int. Ed., 2011, 50, 6519) was shown to function as a highly potent inhibitor of Ad37, efficiently preventing the attachment of the virion to the host cells and subsequent infection. Here, new trivalent sialic acid derivatives were designed, synthesized and their inhibitory properties against Ad37 infection of the human corneal epithelial cells were investigated. In comparison to ME0322, the best compound (17a) was found to be over three orders of magnitude more potent in a cell-attachment assay (IC50 = 1.4 nM) and about 140 times more potent in a cell-infection assay (IC50 = 2.9nM). X-ray crystallographic analysis demonstrated a trivalent binding mode of all compounds to the Ad37 fiber knob. For the most potent compound ophthalmic toxicity in rabbits was investigated and it was concluded that repeated eye administration did not cause any adverse effects.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Mikrobiologi inom det medicinska området (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Microbiology in the medical area (hsv//eng)
Publication and Content Type
- ref (subject category)
- art (subject category)
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- By the author/editor
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Caraballo, Rémi
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Saleeb, Michael
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Bauer, Johannes
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Liaci, Antonio-M ...
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Chandra, Naresh
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Storm, Rickard J
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show more...
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Frängsmyr, Lars
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Qian, Weixing
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Stehle, Thilo
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Arnberg, Niklas
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Elofsson, Mikael
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show less...
- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Microbiology in ...
- Articles in the publication
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Organic and biom ...
- By the university
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Umeå University