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Molecular Wipes: Application to Epidemic Keratoconjuctivitis

Aplander, Karolina LU ; Marttila, Marko; Manner, Sophie LU ; Arnberg, Niklas; Sterner, Olov LU and Ellervik, Ulf LU (2011) In Journal of Medicinal Chemistry 54(19). p.6670-6675
Abstract
Epidemic keratoconjunctivitis (EKC) is a severe disease of the eye, caused by members of the Adenoviridae (Ad) family, with symptoms such as keratitis, conjunctivitis, pain, edema, and reduced vision that may last for months or years. There are no vaccines or antiviral drugs available to prevent or treat EKC. It was found previously that EKC-causing Ads use sialic acid as a cellular receptor and demonstrated that soluble, sialic acid-containing molecules can prevent infection. In this study, multivalent sialic acid constructs based on 10,12-pentacosadiynoic acid (PDA) have been synthesized, and these constructs are shown to be efficient inhibitors of Ad binding (IC50 = 0.9 mu M) and Ad infectivity (IC50 = 0.7 mu M). The mechanism of action... (More)
Epidemic keratoconjunctivitis (EKC) is a severe disease of the eye, caused by members of the Adenoviridae (Ad) family, with symptoms such as keratitis, conjunctivitis, pain, edema, and reduced vision that may last for months or years. There are no vaccines or antiviral drugs available to prevent or treat EKC. It was found previously that EKC-causing Ads use sialic acid as a cellular receptor and demonstrated that soluble, sialic acid-containing molecules can prevent infection. In this study, multivalent sialic acid constructs based on 10,12-pentacosadiynoic acid (PDA) have been synthesized, and these constructs are shown to be efficient inhibitors of Ad binding (IC50 = 0.9 mu M) and Ad infectivity (IC50 = 0.7 mu M). The mechanism of action is to aggregate virus particles and thereby prevent them from binding to ocular cells. Such formulations may be used for topical treatment of adenovirus-caused EKC. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Journal of Medicinal Chemistry
volume
54
issue
19
pages
6670 - 6675
publisher
American Chemical Society (ACS)
external identifiers
  • wos:000295546200022
  • scopus:80053900761
ISSN
1520-4804
DOI
10.1021/jm200545m
language
English
LU publication?
yes
id
ed8ef3c4-3820-45b8-8c2b-7e9f33649d6b (old id 2211798)
date added to LUP
2011-11-29 15:26:13
date last changed
2017-11-12 03:06:47
@article{ed8ef3c4-3820-45b8-8c2b-7e9f33649d6b,
  abstract     = {Epidemic keratoconjunctivitis (EKC) is a severe disease of the eye, caused by members of the Adenoviridae (Ad) family, with symptoms such as keratitis, conjunctivitis, pain, edema, and reduced vision that may last for months or years. There are no vaccines or antiviral drugs available to prevent or treat EKC. It was found previously that EKC-causing Ads use sialic acid as a cellular receptor and demonstrated that soluble, sialic acid-containing molecules can prevent infection. In this study, multivalent sialic acid constructs based on 10,12-pentacosadiynoic acid (PDA) have been synthesized, and these constructs are shown to be efficient inhibitors of Ad binding (IC50 = 0.9 mu M) and Ad infectivity (IC50 = 0.7 mu M). The mechanism of action is to aggregate virus particles and thereby prevent them from binding to ocular cells. Such formulations may be used for topical treatment of adenovirus-caused EKC.},
  author       = {Aplander, Karolina and Marttila, Marko and Manner, Sophie and Arnberg, Niklas and Sterner, Olov and Ellervik, Ulf},
  issn         = {1520-4804},
  language     = {eng},
  number       = {19},
  pages        = {6670--6675},
  publisher    = {American Chemical Society (ACS)},
  series       = {Journal of Medicinal Chemistry},
  title        = {Molecular Wipes: Application to Epidemic Keratoconjuctivitis},
  url          = {http://dx.doi.org/10.1021/jm200545m},
  volume       = {54},
  year         = {2011},
}