Matches in SemOpenAlex for { <https://semopenalex.org/work/W2009805364> ?p ?o ?g. }
Showing items 1 to 84 of
84
with 100 items per page.
- W2009805364 endingPage "15" @default.
- W2009805364 startingPage "3" @default.
- W2009805364 abstract "Stimulation of CXC-type chemokine receptor 2 (CXCR2)-transfected cells by Gro-α or IL-8 induced (i) CXCR2 internalization, (ii) phosphorylation of ERK1/2 (pERK) and (iii) translocation of nuclear factor of activated T-cells (NFAT) into the nucleus. Employing high content screening (HCS; i.e. fluorimetric imaging combined with image analysis) these three ligand-induced events were quantified by using a CXCR2-specific antibody, an antibody recognizing phosphorylated ERK1/2 (pERK) and a red fluorescent protein (RFP) in fusion to transiently overexpressed NFAT, respectively. As an RFP, we applied a recently developed mutant of an Entacmaea quadricolor fluorescent protein with favorable properties for HCS, such as high fluorescence brightness, photostability, large Stokes shift, and stability with regard to formaldehyde. Receptor internalization was closely coupled with ERK signalling both when analyzed in regard of stimulation by physiological CXCR2 ligands and when observed in the presence of antagonistic test compounds. A means of increasing the throughput or of broadening the pharmacological characterization of test compounds is the use of multiplexed imaging. Indeed, CXCR2 internalization could be multiplexed with the NFAT nuclear translocation by fixation at ˜ 45 min after Gro-α stimulation. This multiplexing demonstrated that Gro-α-induced CXCR2 internalization was tightly correlated with Gro-α-induced NFAT translocation, also on the single cell level. The analysis of ERK phosphorylation, NFAT translocation and receptor internalization enabled the profiling of antagonistic test compounds with respect to G-protein signalling and possible receptor desensitization liabilities. Keywords: High content screening, CXCR2, ERK, NFAT, high throughput screening" @default.
- W2009805364 created "2016-06-24" @default.
- W2009805364 creator A5002103266 @default.
- W2009805364 creator A5004168852 @default.
- W2009805364 creator A5036296217 @default.
- W2009805364 creator A5039209878 @default.
- W2009805364 creator A5041416404 @default.
- W2009805364 creator A5055339113 @default.
- W2009805364 creator A5079879196 @default.
- W2009805364 creator A5080297071 @default.
- W2009805364 date "2010-01-01" @default.
- W2009805364 modified "2023-10-16" @default.
- W2009805364 title "High Content Screening of CXCR2-Dependent Signalling Pathways" @default.
- W2009805364 doi "https://doi.org/10.2174/138620710790218249" @default.
- W2009805364 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/20214572" @default.
- W2009805364 hasPublicationYear "2010" @default.
- W2009805364 type Work @default.
- W2009805364 sameAs 2009805364 @default.
- W2009805364 citedByCount "11" @default.
- W2009805364 countsByYear W20098053642012 @default.
- W2009805364 countsByYear W20098053642013 @default.
- W2009805364 countsByYear W20098053642014 @default.
- W2009805364 countsByYear W20098053642015 @default.
- W2009805364 crossrefType "journal-article" @default.
- W2009805364 hasAuthorship W2009805364A5002103266 @default.
- W2009805364 hasAuthorship W2009805364A5004168852 @default.
- W2009805364 hasAuthorship W2009805364A5036296217 @default.
- W2009805364 hasAuthorship W2009805364A5039209878 @default.
- W2009805364 hasAuthorship W2009805364A5041416404 @default.
- W2009805364 hasAuthorship W2009805364A5055339113 @default.
- W2009805364 hasAuthorship W2009805364A5079879196 @default.
- W2009805364 hasAuthorship W2009805364A5080297071 @default.
- W2009805364 hasConcept C104317684 @default.
- W2009805364 hasConcept C11960822 @default.
- W2009805364 hasConcept C12823836 @default.
- W2009805364 hasConcept C13373296 @default.
- W2009805364 hasConcept C139770010 @default.
- W2009805364 hasConcept C153911025 @default.
- W2009805364 hasConcept C170493617 @default.
- W2009805364 hasConcept C185592680 @default.
- W2009805364 hasConcept C189938988 @default.
- W2009805364 hasConcept C55493867 @default.
- W2009805364 hasConcept C57074206 @default.
- W2009805364 hasConcept C84913492 @default.
- W2009805364 hasConcept C86339819 @default.
- W2009805364 hasConcept C86803240 @default.
- W2009805364 hasConcept C95444343 @default.
- W2009805364 hasConceptScore W2009805364C104317684 @default.
- W2009805364 hasConceptScore W2009805364C11960822 @default.
- W2009805364 hasConceptScore W2009805364C12823836 @default.
- W2009805364 hasConceptScore W2009805364C13373296 @default.
- W2009805364 hasConceptScore W2009805364C139770010 @default.
- W2009805364 hasConceptScore W2009805364C153911025 @default.
- W2009805364 hasConceptScore W2009805364C170493617 @default.
- W2009805364 hasConceptScore W2009805364C185592680 @default.
- W2009805364 hasConceptScore W2009805364C189938988 @default.
- W2009805364 hasConceptScore W2009805364C55493867 @default.
- W2009805364 hasConceptScore W2009805364C57074206 @default.
- W2009805364 hasConceptScore W2009805364C84913492 @default.
- W2009805364 hasConceptScore W2009805364C86339819 @default.
- W2009805364 hasConceptScore W2009805364C86803240 @default.
- W2009805364 hasConceptScore W2009805364C95444343 @default.
- W2009805364 hasIssue "1" @default.
- W2009805364 hasLocation W20098053641 @default.
- W2009805364 hasLocation W20098053642 @default.
- W2009805364 hasOpenAccess W2009805364 @default.
- W2009805364 hasPrimaryLocation W20098053641 @default.
- W2009805364 hasRelatedWork W1498784784 @default.
- W2009805364 hasRelatedWork W1512080499 @default.
- W2009805364 hasRelatedWork W1667563338 @default.
- W2009805364 hasRelatedWork W2009805364 @default.
- W2009805364 hasRelatedWork W2016146739 @default.
- W2009805364 hasRelatedWork W2036548518 @default.
- W2009805364 hasRelatedWork W2106969175 @default.
- W2009805364 hasRelatedWork W2142925367 @default.
- W2009805364 hasRelatedWork W2317452501 @default.
- W2009805364 hasRelatedWork W2336184425 @default.
- W2009805364 hasVolume "13" @default.
- W2009805364 isParatext "false" @default.
- W2009805364 isRetracted "false" @default.
- W2009805364 magId "2009805364" @default.
- W2009805364 workType "article" @default.