Matches in SemOpenAlex for { <https://semopenalex.org/work/W4224881982> ?p ?o ?g. }
- W4224881982 endingPage "114406" @default.
- W4224881982 startingPage "114406" @default.
- W4224881982 abstract "Mutation-induced resistance to targeted drug treatment poses a serious threat to successful chemotherapy. Multiple mutations underlying drug resistance remain a largely unsolved scientific issue. Tropomyosin receptor kinases (TRKs) are promising therapeutic targets for several malignant human cancers, but they have become less effective due to multiple resistance mutations. Thus, TRKs are representative cases to explore the problem of multiple resistance mutations. Here, we proposed a conformational adjustment strategy of drug design to overcome multiple resistance mutations in cancer treatments. A representative inhibitor, TIY-7, exhibited remarkable inhibitory activity against five TRK mutants, showing an IC50 value of 1.1 nM against the most severe mutant TRKA-G595R. Moreover, it displayed superior tumor growth inhibitory activity compared with the clinically used drug selitrectinib. These results validated our strategy to design a new inhibitor structure to overcome multiple resistance mutations." @default.
- W4224881982 created "2022-04-27" @default.
- W4224881982 creator A5031161501 @default.
- W4224881982 creator A5048461054 @default.
- W4224881982 creator A5053115128 @default.
- W4224881982 creator A5062292971 @default.
- W4224881982 creator A5065694184 @default.
- W4224881982 creator A5068847247 @default.
- W4224881982 date "2022-07-01" @default.
- W4224881982 modified "2023-10-15" @default.
- W4224881982 title "Conformational adjustment overcomes multiple drug-resistance mutants of tropomyosin receptor kinase" @default.
- W4224881982 cites W1581731557 @default.
- W4224881982 cites W1970573493 @default.
- W4224881982 cites W2007705382 @default.
- W4224881982 cites W2015616444 @default.
- W4224881982 cites W2038532826 @default.
- W4224881982 cites W2042619042 @default.
- W4224881982 cites W2061343703 @default.
- W4224881982 cites W2067174909 @default.
- W4224881982 cites W2105668062 @default.
- W4224881982 cites W2109269285 @default.
- W4224881982 cites W2111017461 @default.
- W4224881982 cites W2118233996 @default.
- W4224881982 cites W2125894112 @default.
- W4224881982 cites W2132629607 @default.
- W4224881982 cites W2147993766 @default.
- W4224881982 cites W2156283242 @default.
- W4224881982 cites W2194998434 @default.
- W4224881982 cites W2274032786 @default.
- W4224881982 cites W2335155752 @default.
- W4224881982 cites W2404280981 @default.
- W4224881982 cites W2474117933 @default.
- W4224881982 cites W2560663272 @default.
- W4224881982 cites W2620626563 @default.
- W4224881982 cites W2740079646 @default.
- W4224881982 cites W2790254562 @default.
- W4224881982 cites W2885875860 @default.
- W4224881982 cites W2888845108 @default.
- W4224881982 cites W2890056766 @default.
- W4224881982 cites W2896424462 @default.
- W4224881982 cites W2923683745 @default.
- W4224881982 cites W2954094311 @default.
- W4224881982 cites W2981643996 @default.
- W4224881982 cites W2988707913 @default.
- W4224881982 cites W3026064383 @default.
- W4224881982 cites W3026620415 @default.
- W4224881982 cites W3040693736 @default.
- W4224881982 cites W3045740089 @default.
- W4224881982 cites W3046078147 @default.
- W4224881982 cites W3093535367 @default.
- W4224881982 cites W3096333766 @default.
- W4224881982 cites W3112317452 @default.
- W4224881982 cites W3160965520 @default.
- W4224881982 cites W4241901990 @default.
- W4224881982 cites W950232622 @default.
- W4224881982 doi "https://doi.org/10.1016/j.ejmech.2022.114406" @default.
- W4224881982 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/35486994" @default.
- W4224881982 hasPublicationYear "2022" @default.
- W4224881982 type Work @default.
- W4224881982 citedByCount "3" @default.
- W4224881982 countsByYear W42248819822022 @default.
- W4224881982 countsByYear W42248819822023 @default.
- W4224881982 crossrefType "journal-article" @default.
- W4224881982 hasAuthorship W4224881982A5031161501 @default.
- W4224881982 hasAuthorship W4224881982A5048461054 @default.
- W4224881982 hasAuthorship W4224881982A5053115128 @default.
- W4224881982 hasAuthorship W4224881982A5062292971 @default.
- W4224881982 hasAuthorship W4224881982A5065694184 @default.
- W4224881982 hasAuthorship W4224881982A5068847247 @default.
- W4224881982 hasConcept C104317684 @default.
- W4224881982 hasConcept C114851261 @default.
- W4224881982 hasConcept C134139212 @default.
- W4224881982 hasConcept C143065580 @default.
- W4224881982 hasConcept C169760540 @default.
- W4224881982 hasConcept C170493617 @default.
- W4224881982 hasConcept C17077164 @default.
- W4224881982 hasConcept C171034665 @default.
- W4224881982 hasConcept C184235292 @default.
- W4224881982 hasConcept C185592680 @default.
- W4224881982 hasConcept C205875245 @default.
- W4224881982 hasConcept C2778423431 @default.
- W4224881982 hasConcept C2780035454 @default.
- W4224881982 hasConcept C501734568 @default.
- W4224881982 hasConcept C502942594 @default.
- W4224881982 hasConcept C54355233 @default.
- W4224881982 hasConcept C55493867 @default.
- W4224881982 hasConcept C6997183 @default.
- W4224881982 hasConcept C86803240 @default.
- W4224881982 hasConcept C98274493 @default.
- W4224881982 hasConceptScore W4224881982C104317684 @default.
- W4224881982 hasConceptScore W4224881982C114851261 @default.
- W4224881982 hasConceptScore W4224881982C134139212 @default.
- W4224881982 hasConceptScore W4224881982C143065580 @default.
- W4224881982 hasConceptScore W4224881982C169760540 @default.
- W4224881982 hasConceptScore W4224881982C170493617 @default.
- W4224881982 hasConceptScore W4224881982C17077164 @default.
- W4224881982 hasConceptScore W4224881982C171034665 @default.
- W4224881982 hasConceptScore W4224881982C184235292 @default.