Molecular Wipes: Application to Epidemic Keratoconjuctivitis

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Molecular Wipes: Application to Epidemic Keratoconjuctivitis. / Aplander, Karolina; Marttila, Marko; Manner, Sophie; Arnberg, Niklas; Sterner, Olov; Ellervik, Ulf.

In: Journal of Medicinal Chemistry, Vol. 54, No. 19, 2011, p. 6670-6675.

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Aplander, Karolina ; Marttila, Marko ; Manner, Sophie ; Arnberg, Niklas ; Sterner, Olov ; Ellervik, Ulf. / Molecular Wipes: Application to Epidemic Keratoconjuctivitis. In: Journal of Medicinal Chemistry. 2011 ; Vol. 54, No. 19. pp. 6670-6675.

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TY - JOUR

T1 - Molecular Wipes: Application to Epidemic Keratoconjuctivitis

AU - Aplander, Karolina

AU - Marttila, Marko

AU - Manner, Sophie

AU - Arnberg, Niklas

AU - Sterner, Olov

AU - Ellervik, Ulf

N1 - The information about affiliations in this record was updated in December 2015. The record was previously connected to the following departments: Organic chemistry (S/LTH) (011001240)

PY - 2011

Y1 - 2011

N2 - 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.

AB - 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.

U2 - 10.1021/jm200545m

DO - 10.1021/jm200545m

M3 - Article

VL - 54

SP - 6670

EP - 6675

JO - Journal of Medicinal and Pharmaceutical Chemistry

T2 - Journal of Medicinal and Pharmaceutical Chemistry

JF - Journal of Medicinal and Pharmaceutical Chemistry

SN - 1520-4804

IS - 19

ER -