About: Discovery of Small-Molecule HIV-1 Fusion and Integrase Inhibitors Oleuropein and Hydroxytyrosol: I. Fusion Inhibition

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About: Discovery of Small-Molecule HIV-1 Fusion and Integrase Inhibitors Oleuropein and Hydroxytyrosol: I. Fusion Inhibition Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Discovery of Small-Molecule HIV-1 Fusion and Integrase Inhibitors Oleuropein and Hydroxytyrosol: I. Fusion Inhibition
Creator	Bao, Ju Chang, Young-Tae Lee-Huang, Sylvia Sun, Yongtao Zhang, Dawei Zhang, John Lee, Jae Huang, Paul Lin Huang, Philip
topic	covid:1eb6b055ab21fcc5051ab645e25d1e8ac53d29d7#this
Source	Medline; PMC
abstract	We have identified oleuropein (Ole) and hydroxytyrosol (HT) as a unique class of HIV-1 inhibitors from olive leaf extracts effective against viral fusion and integration. We used molecular docking simulation to study the interactions of Ole and HT with viral targets. We find that Ole and HT bind to the conserved hydrophobic pocket on the surface of the HIV-gp41 fusion domain by hydrogen bonds with Q577 and hydrophobic interactions with I573, G572, and L568 on the gp41 N-terminal heptad repeat peptide N36, interfering with formation of the gp41 fusion-active core. To test and confirm modeling predications, we examined the effect of Ole and HT on HIV-1 fusion complex formation using native polyacrylamide gel electrophoresis and circular dichroism spectroscopy. Ole and HT exhibit dose dependent inhibition on HIV-1 fusion core formation with EC(50)s of 66–58 nM, with no detectable toxicity. Our findings on effects on HIV-1 integrase are reported separately.
has issue date	2007-03-01(xsd:dateTime)
bibo:doi	10.1016/j.bbrc.2007.01.071
bibo:pmid	17275783
has license	green-oa
sha1sum (hex)	1eb6b055ab21fcc5051ab645e25d1e8ac53d29d7
schema:url	https://doi.org/10.1016/j.bbrc.2007.01.071
resource representing a document's title	Discovery of Small-Molecule HIV-1 Fusion and Integrase Inhibitors Oleuropein and Hydroxytyrosol: I. Fusion Inhibition
has PubMed Central identifier	PMC2790717
has PubMed identifier	17275783
schema:publication	Biochemical and Biophysical Research Communications
resource representing a document's body	covid:1eb6b055ab21fcc5051ab645e25d1e8ac53d29d7#body_text
is http://vocab.deri.ie/void#inDataset of	proxy:http/ns.inria.fr/covid19/1eb6b055ab21fcc5051ab645e25d1e8ac53d29d7
is schema:about of	named entity 'MOLECULE' named entity 'HIV-1' named entity 'pocket' named entity 'Oleuropein' named entity 'CORE' named entity 'DOSE' named entity 'USING' named entity 'BIND' named entity 'FUSION COMPLEX' named entity 'HYDROGEN BONDS' named entity 'DETECTABLE' named entity 'OLE' named entity 'EXAMINED' named entity 'HAVE' named entity 'EFFECT' named entity 'HYDROPHOBIC' named entity 'COMPLEX FORMATION' named entity 'INHIBITION' named entity 'OLEUROPEIN' named entity 'OUR' named entity 'CLASS' named entity 'VIRAL' named entity 'INTERACTIONS' named entity 'TOXICITY' named entity 'FUSION' named entity 'CONFIRM' named entity 'HYDROXYTYROSOL' named entity 'STUDY' named entity 'EXTRACTS' named entity 'EXHIBIT' named entity 'CONSERVED' named entity 'SURFACE' named entity 'NATIVE POLYACRYLAMIDE GEL ELECTROPHORESIS' named entity 'OLIVE LEAF' named entity 'HIV' named entity 'REPEAT' named entity 'PEPTIDE N36' named entity 'INTEGRATION' named entity 'DOMAIN' named entity 'SMALL' named entity 'HYDROXYTYROSOL' named entity 'TARGETS' named entity 'USED' named entity 'FINDINGS' named entity 'OLEUROPEIN' named entity 'INTEGRASE INHIBITORS' named entity 'IDENTIFIED' named entity 'ACTIVE' named entity 'FORMATION' named entity 'INTERFERING' named entity 'DISCOVERY' named entity 'MODELING' named entity 'MOLECULAR DOCKING SIMULATION' named entity 'N-TERMINAL ' named entity 'INTEGRASE' named entity 'INHIBITORS' named entity 'REPORTED' named entity 'INHIBITION' named entity 'HIV-1' named entity 'CIRCULAR DICHROISM SPECTROSCOPY' named entity 'TO TEST' named entity 'EFFECTIVE' named entity 'FUSION' named entity 'GP41' named entity 'UNIQUE' named entity 'DEPENDENT' covid:arg/1eb6b055ab21fcc5051ab645e25d1e8ac53d29d7 named entity 'integration' named entity 'inhibitors' named entity 'interactions' named entity 'dose'

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