FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2897316441> ?p ?o ?g. }

• W2897316441 endingPage "14925" @default.
• W2897316441 startingPage "14915" @default.
• W2897316441 abstract "Glycan-binding proteins are key components of central physiological and cellular processes such as self-/non-self-recognition, cellular tissue homing, and protein homeostasis. Herein, C-type lectins are a diverse protein family that play important roles in the immune system, rendering them attractive drug targets. To evaluate C-type lectin receptors as target proteins for small-molecule effectors, chemical probes are required, which are, however, still lacking. To overcome the supposedly poor druggability of C-type lectin receptors and to identify starting points for chemical probe development, we screened murine langerin using 1H and 19F NMR against a library of 871 drug-like fragments. Subsequently, hits were validated by surface plasmon resonance and enzyme-linked lectin assay. Using structure–activity relationship studies and chemical synthesis, we identified thiazolopyrimidine derivatives with double-digit micromolar activity that displayed langerin selectivity. Based on 1H–15N HSQC NMR and competitive binding and inhibition experiments, we demonstrate that thiazolopyrimidines allosterically inhibit langerin. To the best of our knowledge, this is the first report of drug-like allosteric inhibitors of a mammalian lectin." @default.
• W2897316441 created "2018-10-26" @default.
• W2897316441 creator A5015580284 @default.
• W2897316441 creator A5043627681 @default.
• W2897316441 creator A5049855471 @default.
• W2897316441 creator A5051100505 @default.
• W2897316441 creator A5060935979 @default.
• W2897316441 creator A5063220607 @default.
• W2897316441 creator A5084604517 @default.
• W2897316441 creator A5090253001 @default.
• W2897316441 date "2018-10-10" @default.
• W2897316441 modified "2023-10-15" @default.
• W2897316441 title "Allosteric Inhibition of a Mammalian Lectin" @default.
• W2897316441 cites W1516646538 @default.
• W2897316441 cites W1557759563 @default.
• W2897316441 cites W1955707222 @default.
• W2897316441 cites W1983004361 @default.
• W2897316441 cites W1984275656 @default.
• W2897316441 cites W1985580893 @default.
• W2897316441 cites W2005474992 @default.
• W2897316441 cites W2011138994 @default.
• W2897316441 cites W2013600324 @default.
• W2897316441 cites W2043509228 @default.
• W2897316441 cites W2046258407 @default.
• W2897316441 cites W2050871885 @default.
• W2897316441 cites W2062038341 @default.
• W2897316441 cites W2063756289 @default.
• W2897316441 cites W2073661736 @default.
• W2897316441 cites W2074370114 @default.
• W2897316441 cites W2079671002 @default.
• W2897316441 cites W2081075664 @default.
• W2897316441 cites W2101994976 @default.
• W2897316441 cites W2127057372 @default.
• W2897316441 cites W2129374849 @default.
• W2897316441 cites W2138545185 @default.
• W2897316441 cites W2139066193 @default.
• W2897316441 cites W2149170824 @default.
• W2897316441 cites W2158988272 @default.
• W2897316441 cites W2165980525 @default.
• W2897316441 cites W2169864898 @default.
• W2897316441 cites W2177899781 @default.
• W2897316441 cites W2190199357 @default.
• W2897316441 cites W2255897055 @default.
• W2897316441 cites W2259272450 @default.
• W2897316441 cites W2320453739 @default.
• W2897316441 cites W2324415260 @default.
• W2897316441 cites W2325716909 @default.
• W2897316441 cites W2342485871 @default.
• W2897316441 cites W2397609778 @default.
• W2897316441 cites W2463036497 @default.
• W2897316441 cites W2516930383 @default.
• W2897316441 cites W2558064835 @default.
• W2897316441 cites W2588523817 @default.
• W2897316441 cites W2615305549 @default.
• W2897316441 doi "https://doi.org/10.1021/jacs.8b08644" @default.
• W2897316441 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30303367" @default.
• W2897316441 hasPublicationYear "2018" @default.
• W2897316441 type Work @default.
• W2897316441 sameAs 2897316441 @default.
• W2897316441 citedByCount "31" @default.
• W2897316441 countsByYear W28973164412019 @default.
• W2897316441 countsByYear W28973164412020 @default.
• W2897316441 countsByYear W28973164412021 @default.
• W2897316441 countsByYear W28973164412022 @default.
• W2897316441 countsByYear W28973164412023 @default.
• W2897316441 crossrefType "journal-article" @default.
• W2897316441 hasAuthorship W2897316441A5015580284 @default.
• W2897316441 hasAuthorship W2897316441A5043627681 @default.
• W2897316441 hasAuthorship W2897316441A5049855471 @default.
• W2897316441 hasAuthorship W2897316441A5051100505 @default.
• W2897316441 hasAuthorship W2897316441A5060935979 @default.
• W2897316441 hasAuthorship W2897316441A5063220607 @default.
• W2897316441 hasAuthorship W2897316441A5084604517 @default.
• W2897316441 hasAuthorship W2897316441A5090253001 @default.
• W2897316441 hasConcept C106257327 @default.
• W2897316441 hasConcept C106847996 @default.
• W2897316441 hasConcept C108625454 @default.
• W2897316441 hasConcept C119765067 @default.
• W2897316441 hasConcept C155672457 @default.
• W2897316441 hasConcept C161624437 @default.
• W2897316441 hasConcept C166342909 @default.
• W2897316441 hasConcept C170493617 @default.
• W2897316441 hasConcept C171250308 @default.
• W2897316441 hasConcept C171852809 @default.
• W2897316441 hasConcept C185592680 @default.
• W2897316441 hasConcept C192562407 @default.
• W2897316441 hasConcept C203014093 @default.
• W2897316441 hasConcept C206212055 @default.
• W2897316441 hasConcept C2778170410 @default.
• W2897316441 hasConcept C2780758401 @default.
• W2897316441 hasConcept C51785407 @default.
• W2897316441 hasConcept C55493867 @default.
• W2897316441 hasConcept C74187038 @default.
• W2897316441 hasConcept C86803240 @default.
• W2897316441 hasConcept C8891405 @default.
• W2897316441 hasConceptScore W2897316441C106257327 @default.
• W2897316441 hasConceptScore W2897316441C106847996 @default.
• W2897316441 hasConceptScore W2897316441C108625454 @default.

• next