Matches in SemOpenAlex for { <https://semopenalex.org/work/W4319843503> ?p ?o ?g. }
- W4319843503 abstract "Abstract Casein kinases 1 (CK1) are key signaling molecules that have emerged recently as attractive therapeutic targets in particular for the treatment of hematological malignancies. Herein, we report the identification of a new class of potent and highly selective inhibitors of CK1α, δ and ϵ. Based on their optimal in vitro and in vivo profiles and their exclusive selectivity, MU1250, MU1500 and MU1742 were selected as quality chemical probes for those CK1 isoforms. At proper concentrations, MU1250 and MU1500 allow for specific targeting of CK1δ or dual inhibition of CK1δ/ϵ in cells. The compound MU1742 also efficiently inhibits CK1α and, to our knowledge, represents the first potent and highly selective inhibitor of this enzyme. In addition, we demonstrate that the central 1 H ‐pyrrolo[2,3‐ b ]pyridine‐imidazole pharmacophore can be used as the basis of highly selective inhibitors of other therapeutically relevant protein kinases, e.g. p38α, as exemplified by the compound MU1299." @default.
- W4319843503 created "2023-02-11" @default.
- W4319843503 creator A5015963505 @default.
- W4319843503 creator A5017132592 @default.
- W4319843503 creator A5029000240 @default.
- W4319843503 creator A5030788329 @default.
- W4319843503 creator A5031637705 @default.
- W4319843503 creator A5043616644 @default.
- W4319843503 creator A5058082024 @default.
- W4319843503 creator A5059929737 @default.
- W4319843503 creator A5062075072 @default.
- W4319843503 creator A5068116960 @default.
- W4319843503 creator A5075097409 @default.
- W4319843503 creator A5078288323 @default.
- W4319843503 creator A5078295432 @default.
- W4319843503 creator A5081132581 @default.
- W4319843503 creator A5087347408 @default.
- W4319843503 date "2023-02-02" @default.
- W4319843503 modified "2023-10-14" @default.
- W4319843503 title "Discovery of Potent and Exquisitely Selective Inhibitors of Kinase CK1 with Tunable Isoform Selectivity" @default.
- W4319843503 cites W1191502296 @default.
- W4319843503 cites W1971590501 @default.
- W4319843503 cites W1985577180 @default.
- W4319843503 cites W1987190270 @default.
- W4319843503 cites W2013273979 @default.
- W4319843503 cites W2039661168 @default.
- W4319843503 cites W2040942754 @default.
- W4319843503 cites W2062239697 @default.
- W4319843503 cites W2077433574 @default.
- W4319843503 cites W2086286404 @default.
- W4319843503 cites W2171943005 @default.
- W4319843503 cites W2253992243 @default.
- W4319843503 cites W2280676615 @default.
- W4319843503 cites W2559012455 @default.
- W4319843503 cites W2635415917 @default.
- W4319843503 cites W2739895575 @default.
- W4319843503 cites W2766504508 @default.
- W4319843503 cites W2783191314 @default.
- W4319843503 cites W2805025185 @default.
- W4319843503 cites W2888415936 @default.
- W4319843503 cites W2900073034 @default.
- W4319843503 cites W2925605044 @default.
- W4319843503 cites W3094568106 @default.
- W4319843503 cites W3108703095 @default.
- W4319843503 cites W3120212778 @default.
- W4319843503 cites W3189949217 @default.
- W4319843503 cites W3197240335 @default.
- W4319843503 cites W3211017623 @default.
- W4319843503 cites W4237482149 @default.
- W4319843503 doi "https://doi.org/10.1002/ange.202217532" @default.
- W4319843503 hasPublicationYear "2023" @default.
- W4319843503 type Work @default.
- W4319843503 citedByCount "1" @default.
- W4319843503 countsByYear W43198435032023 @default.
- W4319843503 crossrefType "journal-article" @default.
- W4319843503 hasAuthorship W4319843503A5015963505 @default.
- W4319843503 hasAuthorship W4319843503A5017132592 @default.
- W4319843503 hasAuthorship W4319843503A5029000240 @default.
- W4319843503 hasAuthorship W4319843503A5030788329 @default.
- W4319843503 hasAuthorship W4319843503A5031637705 @default.
- W4319843503 hasAuthorship W4319843503A5043616644 @default.
- W4319843503 hasAuthorship W4319843503A5058082024 @default.
- W4319843503 hasAuthorship W4319843503A5059929737 @default.
- W4319843503 hasAuthorship W4319843503A5062075072 @default.
- W4319843503 hasAuthorship W4319843503A5068116960 @default.
- W4319843503 hasAuthorship W4319843503A5075097409 @default.
- W4319843503 hasAuthorship W4319843503A5078288323 @default.
- W4319843503 hasAuthorship W4319843503A5078295432 @default.
- W4319843503 hasAuthorship W4319843503A5081132581 @default.
- W4319843503 hasAuthorship W4319843503A5087347408 @default.
- W4319843503 hasConcept C104317684 @default.
- W4319843503 hasConcept C118792377 @default.
- W4319843503 hasConcept C160110348 @default.
- W4319843503 hasConcept C161790260 @default.
- W4319843503 hasConcept C184235292 @default.
- W4319843503 hasConcept C185592680 @default.
- W4319843503 hasConcept C202751555 @default.
- W4319843503 hasConcept C207001950 @default.
- W4319843503 hasConcept C53345823 @default.
- W4319843503 hasConcept C54355233 @default.
- W4319843503 hasConcept C55493867 @default.
- W4319843503 hasConcept C56173144 @default.
- W4319843503 hasConcept C86803240 @default.
- W4319843503 hasConcept C97029542 @default.
- W4319843503 hasConceptScore W4319843503C104317684 @default.
- W4319843503 hasConceptScore W4319843503C118792377 @default.
- W4319843503 hasConceptScore W4319843503C160110348 @default.
- W4319843503 hasConceptScore W4319843503C161790260 @default.
- W4319843503 hasConceptScore W4319843503C184235292 @default.
- W4319843503 hasConceptScore W4319843503C185592680 @default.
- W4319843503 hasConceptScore W4319843503C202751555 @default.
- W4319843503 hasConceptScore W4319843503C207001950 @default.
- W4319843503 hasConceptScore W4319843503C53345823 @default.
- W4319843503 hasConceptScore W4319843503C54355233 @default.
- W4319843503 hasConceptScore W4319843503C55493867 @default.
- W4319843503 hasConceptScore W4319843503C56173144 @default.
- W4319843503 hasConceptScore W4319843503C86803240 @default.
- W4319843503 hasConceptScore W4319843503C97029542 @default.
- W4319843503 hasFunder F4320310818 @default.
- W4319843503 hasFunder F4320321005 @default.