Matches in SemOpenAlex for { <https://semopenalex.org/work/W3199211350> ?p ?o ?g. }
- W3199211350 endingPage "14357" @default.
- W3199211350 startingPage "14344" @default.
- W3199211350 abstract "Transthyretin (TTR) is a causative protein of TTR amyloidosis (ATTR amyloidosis), a general term for diseases characterized by deposition of TTR amyloid fibrils in specific organs. ATTR amyloidosis can be ameliorated by stabilization of the TTR tetramer through the binding of small molecules. Here, we show that the clinical anthelmintic drugs bithionol (42) and triclabendazole (43) potently inhibit aggregation of the amyloidogenic variant V30M-TTR. A competitive binding assay using a fluorescence probe showed that the binding affinity of 42 with V30M-TTR was significantly higher than that of the first-in-class drug tafamidis (1), and the binding affinity of 43 was similar to that of 1. The crystallographic and thermodynamic analysis revealed that 42 efficiently occupied the halogen-binding grooves of TTR, resulting in the favorable binding entropy. Multifaceted in vitro studies of anthelmintic drugs have the potential to reposition these drugs as ATTR amyloidosis inhibitors." @default.
- W3199211350 created "2021-09-27" @default.
- W3199211350 creator A5004614177 @default.
- W3199211350 creator A5011533166 @default.
- W3199211350 creator A5060229439 @default.
- W3199211350 date "2021-09-22" @default.
- W3199211350 modified "2023-10-06" @default.
- W3199211350 title "Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors" @default.
- W3199211350 cites W1560285331 @default.
- W3199211350 cites W1561744371 @default.
- W3199211350 cites W1964598017 @default.
- W3199211350 cites W1966765667 @default.
- W3199211350 cites W1971840315 @default.
- W3199211350 cites W1973152349 @default.
- W3199211350 cites W1977970084 @default.
- W3199211350 cites W1984089286 @default.
- W3199211350 cites W1984543278 @default.
- W3199211350 cites W1987063515 @default.
- W3199211350 cites W1987093238 @default.
- W3199211350 cites W1990422630 @default.
- W3199211350 cites W1995860001 @default.
- W3199211350 cites W2005974273 @default.
- W3199211350 cites W2009292577 @default.
- W3199211350 cites W2010515933 @default.
- W3199211350 cites W2012531419 @default.
- W3199211350 cites W2014056881 @default.
- W3199211350 cites W2019284374 @default.
- W3199211350 cites W2022948223 @default.
- W3199211350 cites W2025021056 @default.
- W3199211350 cites W2025125596 @default.
- W3199211350 cites W2033886756 @default.
- W3199211350 cites W2054186628 @default.
- W3199211350 cites W2058829301 @default.
- W3199211350 cites W2068287368 @default.
- W3199211350 cites W2069160027 @default.
- W3199211350 cites W2079055683 @default.
- W3199211350 cites W2080914865 @default.
- W3199211350 cites W2087039355 @default.
- W3199211350 cites W2090907772 @default.
- W3199211350 cites W2097074036 @default.
- W3199211350 cites W2102465370 @default.
- W3199211350 cites W2105872266 @default.
- W3199211350 cites W2114367386 @default.
- W3199211350 cites W2115845634 @default.
- W3199211350 cites W2132690375 @default.
- W3199211350 cites W2142822529 @default.
- W3199211350 cites W2144081223 @default.
- W3199211350 cites W2147131374 @default.
- W3199211350 cites W2148373528 @default.
- W3199211350 cites W2158907165 @default.
- W3199211350 cites W2169280166 @default.
- W3199211350 cites W2180229411 @default.
- W3199211350 cites W2206807299 @default.
- W3199211350 cites W2261131592 @default.
- W3199211350 cites W2284643705 @default.
- W3199211350 cites W2591961714 @default.
- W3199211350 cites W2809989268 @default.
- W3199211350 cites W2810909862 @default.
- W3199211350 cites W2888616781 @default.
- W3199211350 cites W2982179446 @default.
- W3199211350 cites W2990828374 @default.
- W3199211350 cites W3026714212 @default.
- W3199211350 cites W3035904866 @default.
- W3199211350 cites W3086559466 @default.
- W3199211350 cites W3087982963 @default.
- W3199211350 cites W4248872320 @default.
- W3199211350 cites W84005282 @default.
- W3199211350 doi "https://doi.org/10.1021/acs.jmedchem.1c00823" @default.
- W3199211350 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/34547896" @default.
- W3199211350 hasPublicationYear "2021" @default.
- W3199211350 type Work @default.
- W3199211350 sameAs 3199211350 @default.
- W3199211350 citedByCount "7" @default.
- W3199211350 countsByYear W31992113502022 @default.
- W3199211350 countsByYear W31992113502023 @default.
- W3199211350 crossrefType "journal-article" @default.
- W3199211350 hasAuthorship W3199211350A5004614177 @default.
- W3199211350 hasAuthorship W3199211350A5011533166 @default.
- W3199211350 hasAuthorship W3199211350A5060229439 @default.
- W3199211350 hasConcept C107824862 @default.
- W3199211350 hasConcept C121157162 @default.
- W3199211350 hasConcept C126322002 @default.
- W3199211350 hasConcept C161624437 @default.
- W3199211350 hasConcept C170493617 @default.
- W3199211350 hasConcept C179104552 @default.
- W3199211350 hasConcept C181199279 @default.
- W3199211350 hasConcept C185592680 @default.
- W3199211350 hasConcept C2776908094 @default.
- W3199211350 hasConcept C2777633098 @default.
- W3199211350 hasConcept C2778201750 @default.
- W3199211350 hasConcept C2778886173 @default.
- W3199211350 hasConcept C2779951007 @default.
- W3199211350 hasConcept C2780035454 @default.
- W3199211350 hasConcept C42972112 @default.
- W3199211350 hasConcept C51639874 @default.
- W3199211350 hasConcept C55493867 @default.
- W3199211350 hasConcept C71924100 @default.
- W3199211350 hasConcept C85196483 @default.