Matches in SemOpenAlex for { <https://semopenalex.org/work/W3119388575> ?p ?o ?g. }
- W3119388575 endingPage "391" @default.
- W3119388575 startingPage "391" @default.
- W3119388575 abstract "Mitogen- and Stress-Activated Kinase 1 (MSK1) is a nuclear kinase, taking part in the activation pathway of the pro-inflammatory transcription factor NF-kB and is demonstrating a therapeutic target potential in inflammatory diseases such as asthma, psoriasis and atherosclerosis. To date, few MSK1 inhibitors were reported. In order to identify new MSK1 inhibitors, a screening of a library of low molecular weight compounds was performed, and the results highlighted the 6-phenylpyridin-2-yl guanidine (compound 1a, IC50~18 µM) as a starting hit for structure-activity relationship study. Derivatives, homologues and rigid mimetics of 1a were designed, and all synthesized compounds were evaluated for their inhibitory activity towards MSK1. Among them, the non-cytotoxic 2-aminobenzimidazole 49d was the most potent at inhibiting significantly: (i) MSK1 activity, (ii) the release of IL-6 in inflammatory conditions in vitro (IC50~2 µM) and (iii) the inflammatory cell recruitment to the airways in a mouse model of asthma." @default.
- W3119388575 created "2021-01-18" @default.
- W3119388575 creator A5017947580 @default.
- W3119388575 creator A5020318990 @default.
- W3119388575 creator A5025683789 @default.
- W3119388575 creator A5030473981 @default.
- W3119388575 creator A5037175705 @default.
- W3119388575 creator A5041747297 @default.
- W3119388575 creator A5042039085 @default.
- W3119388575 creator A5042591341 @default.
- W3119388575 creator A5066442376 @default.
- W3119388575 creator A5082835189 @default.
- W3119388575 creator A5084036027 @default.
- W3119388575 creator A5090197451 @default.
- W3119388575 date "2021-01-13" @default.
- W3119388575 modified "2023-10-12" @default.
- W3119388575 title "Design, Synthesis and Biological Evaluation of Arylpyridin-2-yl Guanidine Derivatives and Cyclic Mimetics as Novel MSK1 Inhibitors. An Application in an Asthma Model" @default.
- W3119388575 cites W1543963511 @default.
- W3119388575 cites W1967600634 @default.
- W3119388575 cites W1977707794 @default.
- W3119388575 cites W1977759779 @default.
- W3119388575 cites W1984631082 @default.
- W3119388575 cites W1991001144 @default.
- W3119388575 cites W2002920137 @default.
- W3119388575 cites W2013269907 @default.
- W3119388575 cites W2018623979 @default.
- W3119388575 cites W2021255160 @default.
- W3119388575 cites W2023538608 @default.
- W3119388575 cites W2027425960 @default.
- W3119388575 cites W2031261247 @default.
- W3119388575 cites W2045522986 @default.
- W3119388575 cites W2045626601 @default.
- W3119388575 cites W2047152276 @default.
- W3119388575 cites W2057199361 @default.
- W3119388575 cites W2063956233 @default.
- W3119388575 cites W2064640405 @default.
- W3119388575 cites W2064678460 @default.
- W3119388575 cites W2069666032 @default.
- W3119388575 cites W2072922969 @default.
- W3119388575 cites W2075204296 @default.
- W3119388575 cites W2082069882 @default.
- W3119388575 cites W2084429276 @default.
- W3119388575 cites W2087731916 @default.
- W3119388575 cites W2091448951 @default.
- W3119388575 cites W2098482961 @default.
- W3119388575 cites W2105324106 @default.
- W3119388575 cites W2125218902 @default.
- W3119388575 cites W2125719366 @default.
- W3119388575 cites W2131162745 @default.
- W3119388575 cites W2138884788 @default.
- W3119388575 cites W2145722383 @default.
- W3119388575 cites W2156549384 @default.
- W3119388575 cites W2162830089 @default.
- W3119388575 cites W2272492043 @default.
- W3119388575 cites W2415671922 @default.
- W3119388575 cites W2560333665 @default.
- W3119388575 cites W2763897043 @default.
- W3119388575 cites W2766747008 @default.
- W3119388575 cites W2789500193 @default.
- W3119388575 cites W2793059925 @default.
- W3119388575 cites W2908698939 @default.
- W3119388575 cites W2953555477 @default.
- W3119388575 cites W4247904703 @default.
- W3119388575 doi "https://doi.org/10.3390/molecules26020391" @default.
- W3119388575 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7828447" @default.
- W3119388575 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/33450992" @default.
- W3119388575 hasPublicationYear "2021" @default.
- W3119388575 type Work @default.
- W3119388575 sameAs 3119388575 @default.
- W3119388575 citedByCount "2" @default.
- W3119388575 countsByYear W31193885752022 @default.
- W3119388575 crossrefType "journal-article" @default.
- W3119388575 hasAuthorship W3119388575A5017947580 @default.
- W3119388575 hasAuthorship W3119388575A5020318990 @default.
- W3119388575 hasAuthorship W3119388575A5025683789 @default.
- W3119388575 hasAuthorship W3119388575A5030473981 @default.
- W3119388575 hasAuthorship W3119388575A5037175705 @default.
- W3119388575 hasAuthorship W3119388575A5041747297 @default.
- W3119388575 hasAuthorship W3119388575A5042039085 @default.
- W3119388575 hasAuthorship W3119388575A5042591341 @default.
- W3119388575 hasAuthorship W3119388575A5066442376 @default.
- W3119388575 hasAuthorship W3119388575A5082835189 @default.
- W3119388575 hasAuthorship W3119388575A5084036027 @default.
- W3119388575 hasAuthorship W3119388575A5090197451 @default.
- W3119388575 hasBestOaLocation W31193885751 @default.
- W3119388575 hasConcept C184235292 @default.
- W3119388575 hasConcept C185592680 @default.
- W3119388575 hasConcept C202751555 @default.
- W3119388575 hasConcept C21951064 @default.
- W3119388575 hasConcept C2777752497 @default.
- W3119388575 hasConcept C2779463914 @default.
- W3119388575 hasConcept C55493867 @default.
- W3119388575 hasConcept C71924100 @default.
- W3119388575 hasConcept C98274493 @default.
- W3119388575 hasConceptScore W3119388575C184235292 @default.
- W3119388575 hasConceptScore W3119388575C185592680 @default.
- W3119388575 hasConceptScore W3119388575C202751555 @default.
- W3119388575 hasConceptScore W3119388575C21951064 @default.