FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2330508045> ?p ?o ?g. }

• W2330508045 endingPage "822" @default.
• W2330508045 startingPage "810" @default.
• W2330508045 abstract "Alzheimer's disease (AD) is the most frequent form of neurodegenerative disorder in elderly people. Involvement of several pathogenic events and their interconnections make this disease a complex disorder. Therefore, designing compounds that can inhibit multiple toxic pathways is the most attractive therapeutic strategy in complex disorders like AD. Here, we have designed a multi-tier screening protocol combining ensemble docking to mine BACE1 inhibitor, as well as 2-D QSAR models for anti-amyloidogenic and antioxidant activities. An in house developed phytochemical library of 200 phytochemicals has been screened through this multi-target procedure which mine hesperidin, a flavanone glycoside commonly found in citrus food items, as a multi-potent phytochemical in AD therapeutics. Steady-state and time-resolved fluorescence spectroscopy reveal that binding of hesperidin to the active site of BACE1 induces a conformational transition of the protein from open to closed form. Hesperidin docks close to the catalytic aspartate residues and orients itself in a way that blocks the cavity opening thereby precluding substrate binding. Hesperidin is a high affinity BACE1 inhibitor and only 500 nM of the compound shows complete inhibition of the enzyme activity. Furthermore, ANS and Thioflavin-T binding assay show that hesperidin completely inhibits the amyloid fibril formation which is further supported by atomic force microscopy. Hesperidin exhibits moderate ABTS(+) radical scavenging assay but strong hydroxyl radical scavenging ability, as evident from DNA nicking assay. Present study demonstrates the applicability of a novel multi-target screening procedure to mine multi-potent agents from natural origin for AD therapeutics." @default.
• W2330508045 created "2016-06-24" @default.
• W2330508045 creator A5048341540 @default.
• W2330508045 creator A5050152302 @default.
• W2330508045 creator A5055974130 @default.
• W2330508045 creator A5075781286 @default.
• W2330508045 date "2016-10-01" @default.
• W2330508045 modified "2023-10-16" @default.
• W2330508045 title "Multi-target screening mines hesperidin as a multi-potent inhibitor: Implication in Alzheimer's disease therapeutics" @default.
• W2330508045 cites W1481000570 @default.
• W2330508045 cites W1487727801 @default.
• W2330508045 cites W1824652155 @default.
• W2330508045 cites W1966312971 @default.
• W2330508045 cites W1967881385 @default.
• W2330508045 cites W1968249511 @default.
• W2330508045 cites W1968900405 @default.
• W2330508045 cites W1968986912 @default.
• W2330508045 cites W1969249329 @default.
• W2330508045 cites W1972278713 @default.
• W2330508045 cites W1974888479 @default.
• W2330508045 cites W1981458288 @default.
• W2330508045 cites W1983789627 @default.
• W2330508045 cites W1986168235 @default.
• W2330508045 cites W1990755847 @default.
• W2330508045 cites W1992185682 @default.
• W2330508045 cites W1996917933 @default.
• W2330508045 cites W2000899341 @default.
• W2330508045 cites W2008649582 @default.
• W2330508045 cites W2012991711 @default.
• W2330508045 cites W2016332054 @default.
• W2330508045 cites W2017044298 @default.
• W2330508045 cites W2025628659 @default.
• W2330508045 cites W2026053103 @default.
• W2330508045 cites W2036288989 @default.
• W2330508045 cites W2041573170 @default.
• W2330508045 cites W2049466195 @default.
• W2330508045 cites W2059136988 @default.
• W2330508045 cites W2059412214 @default.
• W2330508045 cites W2063789588 @default.
• W2330508045 cites W2067133013 @default.
• W2330508045 cites W2068871047 @default.
• W2330508045 cites W2076585724 @default.
• W2330508045 cites W2078658743 @default.
• W2330508045 cites W2078832316 @default.
• W2330508045 cites W2081571747 @default.
• W2330508045 cites W2090778647 @default.
• W2330508045 cites W2094411486 @default.
• W2330508045 cites W2096584150 @default.
• W2330508045 cites W2100307248 @default.
• W2330508045 cites W2114779636 @default.
• W2330508045 cites W2134193762 @default.
• W2330508045 cites W2155237226 @default.
• W2330508045 cites W2159879659 @default.
• W2330508045 cites W2175225119 @default.
• W2330508045 cites W2324445849 @default.
• W2330508045 cites W255205693 @default.
• W2330508045 doi "https://doi.org/10.1016/j.ejmech.2016.03.057" @default.
• W2330508045 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/27068363" @default.
• W2330508045 hasPublicationYear "2016" @default.
• W2330508045 type Work @default.
• W2330508045 sameAs 2330508045 @default.
• W2330508045 citedByCount "35" @default.
• W2330508045 countsByYear W23305080452016 @default.
• W2330508045 countsByYear W23305080452017 @default.
• W2330508045 countsByYear W23305080452018 @default.
• W2330508045 countsByYear W23305080452019 @default.
• W2330508045 countsByYear W23305080452020 @default.
• W2330508045 countsByYear W23305080452021 @default.
• W2330508045 countsByYear W23305080452022 @default.
• W2330508045 countsByYear W23305080452023 @default.
• W2330508045 crossrefType "journal-article" @default.
• W2330508045 hasAuthorship W2330508045A5048341540 @default.
• W2330508045 hasAuthorship W2330508045A5050152302 @default.
• W2330508045 hasAuthorship W2330508045A5055974130 @default.
• W2330508045 hasAuthorship W2330508045A5075781286 @default.
• W2330508045 hasBestOaLocation W23305080451 @default.
• W2330508045 hasConcept C142724271 @default.
• W2330508045 hasConcept C159110408 @default.
• W2330508045 hasConcept C185592680 @default.
• W2330508045 hasConcept C195475562 @default.
• W2330508045 hasConcept C204787440 @default.
• W2330508045 hasConcept C2776128092 @default.
• W2330508045 hasConcept C2776816829 @default.
• W2330508045 hasConcept C2777252647 @default.
• W2330508045 hasConcept C2778004101 @default.
• W2330508045 hasConcept C2779054382 @default.
• W2330508045 hasConcept C2779396153 @default.
• W2330508045 hasConcept C41685203 @default.
• W2330508045 hasConcept C55493867 @default.
• W2330508045 hasConcept C56173144 @default.
• W2330508045 hasConcept C71240020 @default.
• W2330508045 hasConcept C71924100 @default.
• W2330508045 hasConcept C98274493 @default.
• W2330508045 hasConceptScore W2330508045C142724271 @default.
• W2330508045 hasConceptScore W2330508045C159110408 @default.
• W2330508045 hasConceptScore W2330508045C185592680 @default.
• W2330508045 hasConceptScore W2330508045C195475562 @default.
• W2330508045 hasConceptScore W2330508045C204787440 @default.

• next