FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W3028462022> ?p ?o ?g. }

• W3028462022 endingPage "516" @default.
• W3028462022 startingPage "505" @default.
• W3028462022 abstract "Aims: TNF receptor-associated protein 1 (TRAP1), the mitochondrial paralog of the heat shock protein 90 (Hsp90) family of molecular chaperones, is required for neoplastic growth in several tumor cell models, where it inhibits succinate dehydrogenase (SDH) activity, thus favoring bioenergetic rewiring, maintenance of redox homeostasis, and orchestration of a hypoxia-inducible factor 1-alpha (HIF1α)-mediated pseudohypoxic program. Development of selective TRAP1 inhibitors is instrumental for targeted development of antineoplastic drugs, but it has been hampered up to now by the high degree of homology among catalytic pockets of Hsp90 family members. The vegetal derivative honokiol and its lipophilic bis-dichloroacetate ester, honokiol DCA (HDCA), are small-molecule compounds with antineoplastic activity. HDCA leads to oxidative stress and apoptosis in in vivo tumor models and displays an action that is functionally opposed to that of TRAP1, as it induces both SDH and the mitochondrial deacetylase sirtuin-3 (SIRT3), which further enhances SDH activity. We investigated whether HDCA could interact with TRAP1, inhibiting its chaperone function, and the effects of HDCA on tumor cells harboring TRAP1. Results: An allosteric binding site in TRAP1 is able to host HDCA, which inhibits TRAP1 but not Hsp90 ATPase activity. In neoplastic cells, HDCA reverts TRAP1-dependent downregulation of SDH, decreases proliferation rate, increases mitochondrial superoxide levels, and abolishes tumorigenic growth. Innovation: HDCA is a potential lead compound for the generation of antineoplastic approaches based on the allosteric inhibition of TRAP1 chaperone activity. Conclusions: We have identified a selective TRAP1 inhibitor that can be used to better dissect TRAP1 biochemical functions and to tailor novel tumor-targeting strategies." @default.
• W3028462022 created "2020-05-29" @default.
• W3028462022 creator A5004887935 @default.
• W3028462022 creator A5029969206 @default.
• W3028462022 creator A5041224543 @default.
• W3028462022 creator A5045827300 @default.
• W3028462022 creator A5046491394 @default.
• W3028462022 creator A5067982591 @default.
• W3028462022 creator A5069152410 @default.
• W3028462022 creator A5082483947 @default.
• W3028462022 creator A5083786119 @default.
• W3028462022 date "2021-03-01" @default.
• W3028462022 modified "2023-10-12" @default.
• W3028462022 title "Honokiol Bis-Dichloroacetate Is a Selective Allosteric Inhibitor of the Mitochondrial Chaperone TRAP1" @default.
• W3028462022 cites W1522859997 @default.
• W3028462022 cites W1569584260 @default.
• W3028462022 cites W1841393598 @default.
• W3028462022 cites W1969128168 @default.
• W3028462022 cites W1972616589 @default.
• W3028462022 cites W1979815517 @default.
• W3028462022 cites W1985458442 @default.
• W3028462022 cites W2000690172 @default.
• W3028462022 cites W2000980220 @default.
• W3028462022 cites W2004349079 @default.
• W3028462022 cites W2010105281 @default.
• W3028462022 cites W2014880001 @default.
• W3028462022 cites W2021440731 @default.
• W3028462022 cites W2025772881 @default.
• W3028462022 cites W2029103952 @default.
• W3028462022 cites W2031047333 @default.
• W3028462022 cites W2037316279 @default.
• W3028462022 cites W2043061500 @default.
• W3028462022 cites W2052543023 @default.
• W3028462022 cites W2058666198 @default.
• W3028462022 cites W2094143445 @default.
• W3028462022 cites W2096745022 @default.
• W3028462022 cites W2098215141 @default.
• W3028462022 cites W2100215915 @default.
• W3028462022 cites W2115527176 @default.
• W3028462022 cites W2122127456 @default.
• W3028462022 cites W2156113012 @default.
• W3028462022 cites W2202366653 @default.
• W3028462022 cites W2264038168 @default.
• W3028462022 cites W2327305889 @default.
• W3028462022 cites W2481421684 @default.
• W3028462022 cites W2520817237 @default.
• W3028462022 cites W2524612188 @default.
• W3028462022 cites W2549856864 @default.
• W3028462022 cites W2573185154 @default.
• W3028462022 cites W2594013466 @default.
• W3028462022 cites W2598147689 @default.
• W3028462022 cites W2603218564 @default.
• W3028462022 cites W2606824156 @default.
• W3028462022 cites W2751651288 @default.
• W3028462022 cites W2783607048 @default.
• W3028462022 cites W2791440475 @default.
• W3028462022 cites W2883741152 @default.
• W3028462022 cites W2888230031 @default.
• W3028462022 cites W2890326186 @default.
• W3028462022 cites W2906326387 @default.
• W3028462022 cites W2912834637 @default.
• W3028462022 cites W2937524633 @default.
• W3028462022 cites W3016857825 @default.
• W3028462022 cites W3165449168 @default.
• W3028462022 doi "https://doi.org/10.1089/ars.2019.7972" @default.
• W3028462022 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/8020504" @default.
• W3028462022 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32438819" @default.
• W3028462022 hasPublicationYear "2021" @default.
• W3028462022 type Work @default.
• W3028462022 sameAs 3028462022 @default.
• W3028462022 citedByCount "23" @default.
• W3028462022 countsByYear W30284620222020 @default.
• W3028462022 countsByYear W30284620222021 @default.
• W3028462022 countsByYear W30284620222022 @default.
• W3028462022 countsByYear W30284620222023 @default.
• W3028462022 crossrefType "journal-article" @default.
• W3028462022 hasAuthorship W3028462022A5004887935 @default.
• W3028462022 hasAuthorship W3028462022A5029969206 @default.
• W3028462022 hasAuthorship W3028462022A5041224543 @default.
• W3028462022 hasAuthorship W3028462022A5045827300 @default.
• W3028462022 hasAuthorship W3028462022A5046491394 @default.
• W3028462022 hasAuthorship W3028462022A5067982591 @default.
• W3028462022 hasAuthorship W3028462022A5069152410 @default.
• W3028462022 hasAuthorship W3028462022A5082483947 @default.
• W3028462022 hasAuthorship W3028462022A5083786119 @default.
• W3028462022 hasBestOaLocation W30284620222 @default.
• W3028462022 hasConcept C104317684 @default.
• W3028462022 hasConcept C138488276 @default.
• W3028462022 hasConcept C142724271 @default.
• W3028462022 hasConcept C166342909 @default.
• W3028462022 hasConcept C170493617 @default.
• W3028462022 hasConcept C181199279 @default.
• W3028462022 hasConcept C185592680 @default.
• W3028462022 hasConcept C205260736 @default.
• W3028462022 hasConcept C2775932338 @default.
• W3028462022 hasConcept C2775962898 @default.
• W3028462022 hasConcept C2780561631 @default.
• W3028462022 hasConcept C2781334404 @default.

• next