Matches in SemOpenAlex for { <https://semopenalex.org/work/W2917877802> ?p ?o ?g. }
- W2917877802 endingPage "2597" @default.
- W2917877802 startingPage "2582" @default.
- W2917877802 abstract "Lysine acetyltransferases (KATs, also termed histone acetyltransferases, HATs) catalyze the acetylation of substrate lysine residues by employing the cofactor acetyl-coenzyme A (AcCoA), thereby providing a dynamic control mechanism of protein function. Because of their major involvement in cell development and homeostasis, small-molecule modulators of KAT activity are urgently needed to assess their therapeutic potential and for probing their underlying biology. Recent advances in the field suggest that targeting the cofactor binding site represents a promising strategy for identifying potent and selective ligands. Here, we present the synthesis of two functional cofactor-based chemical probes and their usage as mechanistic tools in a broadly applicable assay platform. A fluorescence polarization (FP)-based binding assay was combined with biolayer interferometry competition analysis and a FP competition activity immunoassay to enable easy, reliable, and profound evaluation of ligands that target the KAT cofactor binding site." @default.
- W2917877802 created "2019-03-02" @default.
- W2917877802 creator A5002842623 @default.
- W2917877802 creator A5016266091 @default.
- W2917877802 creator A5049150899 @default.
- W2917877802 creator A5067082313 @default.
- W2917877802 creator A5069953531 @default.
- W2917877802 creator A5070043395 @default.
- W2917877802 date "2019-02-20" @default.
- W2917877802 modified "2023-10-18" @default.
- W2917877802 title "Cofactor Analogues as Active Site Probes in Lysine Acetyltransferases" @default.
- W2917877802 cites W1607852746 @default.
- W2917877802 cites W1778910787 @default.
- W2917877802 cites W1967404701 @default.
- W2917877802 cites W1974384304 @default.
- W2917877802 cites W1981022538 @default.
- W2917877802 cites W1981259598 @default.
- W2917877802 cites W1982497845 @default.
- W2917877802 cites W1984246427 @default.
- W2917877802 cites W1987861824 @default.
- W2917877802 cites W1991001144 @default.
- W2917877802 cites W1992902970 @default.
- W2917877802 cites W2007884336 @default.
- W2917877802 cites W2009775964 @default.
- W2917877802 cites W2009826707 @default.
- W2917877802 cites W2015398239 @default.
- W2917877802 cites W2024587296 @default.
- W2917877802 cites W2024626861 @default.
- W2917877802 cites W2027496067 @default.
- W2917877802 cites W2029002395 @default.
- W2917877802 cites W2029130907 @default.
- W2917877802 cites W2031228008 @default.
- W2917877802 cites W2033529039 @default.
- W2917877802 cites W2035705084 @default.
- W2917877802 cites W2042302040 @default.
- W2917877802 cites W2042956459 @default.
- W2917877802 cites W2043238909 @default.
- W2917877802 cites W2051278797 @default.
- W2917877802 cites W2052296178 @default.
- W2917877802 cites W2054613755 @default.
- W2917877802 cites W2055423985 @default.
- W2917877802 cites W2066061693 @default.
- W2917877802 cites W2074631079 @default.
- W2917877802 cites W2087714970 @default.
- W2917877802 cites W2093655203 @default.
- W2917877802 cites W2095217266 @default.
- W2917877802 cites W2117514345 @default.
- W2917877802 cites W2132200096 @default.
- W2917877802 cites W2140450002 @default.
- W2917877802 cites W2142428986 @default.
- W2917877802 cites W2150044225 @default.
- W2917877802 cites W2179930594 @default.
- W2917877802 cites W2198034775 @default.
- W2917877802 cites W2345852749 @default.
- W2917877802 cites W2473834862 @default.
- W2917877802 cites W2540545429 @default.
- W2917877802 cites W2606624207 @default.
- W2917877802 cites W2742666770 @default.
- W2917877802 cites W2758743773 @default.
- W2917877802 cites W2767512731 @default.
- W2917877802 cites W2767773409 @default.
- W2917877802 cites W2783301628 @default.
- W2917877802 cites W2786527187 @default.
- W2917877802 cites W2887443702 @default.
- W2917877802 cites W4240977092 @default.
- W2917877802 cites W56939234 @default.
- W2917877802 doi "https://doi.org/10.1021/acs.jmedchem.8b01887" @default.
- W2917877802 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30785747" @default.
- W2917877802 hasPublicationYear "2019" @default.
- W2917877802 type Work @default.
- W2917877802 sameAs 2917877802 @default.
- W2917877802 citedByCount "8" @default.
- W2917877802 countsByYear W29178778022020 @default.
- W2917877802 countsByYear W29178778022022 @default.
- W2917877802 countsByYear W29178778022023 @default.
- W2917877802 crossrefType "journal-article" @default.
- W2917877802 hasAuthorship W2917877802A5002842623 @default.
- W2917877802 hasAuthorship W2917877802A5016266091 @default.
- W2917877802 hasAuthorship W2917877802A5049150899 @default.
- W2917877802 hasAuthorship W2917877802A5067082313 @default.
- W2917877802 hasAuthorship W2917877802A5069953531 @default.
- W2917877802 hasAuthorship W2917877802A5070043395 @default.
- W2917877802 hasBestOaLocation W29178778022 @default.
- W2917877802 hasConcept C104317684 @default.
- W2917877802 hasConcept C107824862 @default.
- W2917877802 hasConcept C119157956 @default.
- W2917877802 hasConcept C181199279 @default.
- W2917877802 hasConcept C185592680 @default.
- W2917877802 hasConcept C197957613 @default.
- W2917877802 hasConcept C2776016237 @default.
- W2917877802 hasConcept C2910274206 @default.
- W2917877802 hasConcept C2910921701 @default.
- W2917877802 hasConcept C41183919 @default.
- W2917877802 hasConcept C515207424 @default.
- W2917877802 hasConcept C55493867 @default.
- W2917877802 hasConcept C64927066 @default.
- W2917877802 hasConceptScore W2917877802C104317684 @default.
- W2917877802 hasConceptScore W2917877802C107824862 @default.