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Selective inhibition of Ebola entry with selective estrogen receptor modulators by disrupting the endolysosomal calcium
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schema:ScholarlyArticle
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covidontheweb.inria.fr
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Type:
Academic Article
research paper
schema:ScholarlyArticle
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type
Academic Article
research paper
schema:ScholarlyArticle
isDefinedBy
Covid-on-the-Web dataset
has title
Selective inhibition of Ebola entry with selective estrogen receptor modulators by disrupting the endolysosomal calcium
Creator
Li, Xiangdong
Shi, Yi
Wang, Han
Zhang, Jingyuan
Du, Xiaohong
Fan, Hanlu
Gao, George
Li, Haifeng
Lu, Xiaohui
Tan, Dun-Xian
Wu, Qihui
Zheng, Han
Zhou, Zhuan
Source
PMC
abstract
The Ebola crisis occurred in West-Africa highlights the urgency for its clinical treatments. Currently, no Food and Drug Administration (FDA)-approved therapeutics are available. Several FDA-approved drugs, including selective estrogen receptor modulators (SERMs), possess selective anti-Ebola activities. However, the inhibitory mechanisms of these drugs remain elusive. By analyzing the structures of SERMs and their incidental biological activity (cholesterol accumulation), we hypothesized that this incidental biological activity induced by SERMs could be a plausible mechanism as to their inhibitory effects on Ebola infection. Herein, we demonstrated that the same dosages of SERMs which induced cholesterol accumulation also inhibited Ebola infection. SERMs reduced the cellular sphingosine and subsequently caused endolysosomal calcium accumulation, which in turn led to blocking the Ebola entry. Our study clarified the specific anti-Ebola mechanism of SERMs, even the cationic amphiphilic drugs (CADs), this mechanism led to the endolysosomal calcium as a critical target for development of anti-Ebola drugs.
has issue date
2017-01-24
(
xsd:dateTime
)
bibo:doi
10.1038/srep41226
bibo:pmid
28117364
has license
cc-by
sha1sum (hex)
62641fdbeeff7b487788b42b59a3d1ca66bdb978
schema:url
https://doi.org/10.1038/srep41226
resource representing a document's title
Selective inhibition of Ebola entry with selective estrogen receptor modulators by disrupting the endolysosomal calcium
has PubMed Central identifier
PMC5259750
has PubMed identifier
28117364
schema:publication
Sci Rep
resource representing a document's body
covid:62641fdbeeff7b487788b42b59a3d1ca66bdb978#body_text
is
schema:about
of
named entity 'effects'
named entity 'dosages'
named entity 'estrogen receptor'
named entity 'WEST'
named entity 'STUDY'
named entity 'MECHANISM'
named entity 'THEIR'
named entity 'ACCUMULATION'
named entity 'BLOCKING'
named entity 'AMPHIPHILIC'
named entity 'URGENCY'
named entity 'SPECIFIC'
named entity 'AVAILABLE'
named entity 'CALCIUM'
named entity 'CLARIFIED'
named entity 'TURN'
named entity 'THERAPEUTICS'
named entity 'OPEN'
named entity 'SELECTIVE'
named entity 'CRISIS'
named entity 'FOOD AND DRUG ADMINISTRATION'
named entity 'CRITICAL'
named entity 'ENTRY'
named entity 'EBOLA'
named entity 'CALCIUM'
named entity 'INHIBITION'
named entity 'ENTRY'
named entity 'DISRUPTING'
named entity 'SELECTIVE ESTROGEN RECEPTOR MODULATORS'
named entity 'EFFECTS'
named entity 'APPROVED'
named entity 'CHOLESTEROL'
named entity 'DEVELOPMENT'
named entity 'INCIDENTAL'
named entity 'OCCURRED'
named entity 'AFRICA'
named entity 'POSSESS'
named entity 'OUR'
named entity 'SERMS'
named entity 'CELLULAR'
named entity 'EBOLA'
named entity 'TREATMENTS'
named entity 'ITS'
named entity 'INHIBITORY MECHANISMS'
named entity 'TARGET'
named entity 'SELECTIVE'
named entity 'INHIBITED'
named entity 'CLINICAL'
named entity 'REDUCED'
named entity 'COULD BE'
named entity 'DRUGS'
named entity 'CURRENTLY'
named entity 'ACTIVITIES'
named entity 'DOSAGES'
named entity 'THESE'
named entity 'STRUCTURES'
named entity 'CAUSED'
named entity 'INDUCED'
named entity 'BIOLOGICAL ACTIVITY'
named entity 'INCLUDING'
named entity 'LED'
named entity 'DEMONSTRATED'
named entity 'SPHINGOSINE'
named entity 'INHIBITORY'
named entity 'FDA'
named entity 'INFECTION'
named entity 'ANALYZING'
named entity 'SELECTIVE ESTROGEN RECEPTOR MODULATORS'
covid:arg/62641fdbeeff7b487788b42b59a3d1ca66bdb978
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