FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2124444513> ?p ?o ?g. }

• W2124444513 endingPage "1438" @default.
• W2124444513 startingPage "1430" @default.
• W2124444513 abstract "The deletion of Phe-508 (DeltaPhe508) constitutes the most prevalent of a number of mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) that cause cystic fibrosis (CF). This mutation leads to CFTR misfolding and retention in the endoplasmic reticulum, as well as impaired channel activity. The biosynthetic defect can be partially overcome by small-molecule correctors; once at the cell surface, small-molecule potentiators enhance the channel activity of DeltaPhe508-CFTR. Certain compounds, such as VRT-532, exhibit both corrector and potentiator functions. In the current studies, we confirmed that the inherent chloride channel activity of DeltaPhe508-CFTR (after biosynthetic rescue) is potentiated in studies of intact cells and membrane vesicles. It is noteworthy that we showed that the ATPase activity of the purified and reconstituted mutant protein is directly modulated by binding of VRT-532 [4-methyl-2-(5-phenyl-1H-pyrazol-3-yl)-phenol] ATP turnover by reconstituted DeltaPhe508-CFTR is decreased by VRT-532 treatment, an effect that may account for the increase in channel open time induced by this compound. To determine whether the modification of DeltaPhe508-CFTR function caused by direct VRT-532 binding is associated with structural changes, we evaluated the effect of VRT-532 binding on the protease susceptibility of the major mutant. We found that binding of VRT-532 to DeltaPhe508-CFTR led to a minor but significant decrease in the trypsin susceptibility of the full-length mutant protein and a fragment encompassing the second half of the protein. These findings suggest that direct binding of this small molecule induces and/or stabilizes a structure that promotes the channel open state and may underlie its efficacy as a corrector of DeltaPhe508-CFTR." @default.
• W2124444513 created "2016-06-24" @default.
• W2124444513 creator A5002189140 @default.
• W2124444513 creator A5017237506 @default.
• W2124444513 creator A5033878654 @default.
• W2124444513 creator A5072698271 @default.
• W2124444513 creator A5085540478 @default.
• W2124444513 creator A5085975282 @default.
• W2124444513 date "2009-04-01" @default.
• W2124444513 modified "2023-09-27" @default.
• W2124444513 title "A Small-Molecule Modulator Interacts Directly with ΔPhe508-CFTR to Modify Its ATPase Activity and Conformational Stability" @default.
• W2124444513 cites W1559483365 @default.
• W2124444513 cites W1606430679 @default.
• W2124444513 cites W1637411575 @default.
• W2124444513 cites W1855293480 @default.
• W2124444513 cites W1966528069 @default.
• W2124444513 cites W1971736406 @default.
• W2124444513 cites W1975971473 @default.
• W2124444513 cites W1976507289 @default.
• W2124444513 cites W1982625622 @default.
• W2124444513 cites W1985018756 @default.
• W2124444513 cites W1996779865 @default.
• W2124444513 cites W2004844038 @default.
• W2124444513 cites W2015199039 @default.
• W2124444513 cites W2016362105 @default.
• W2124444513 cites W2020518757 @default.
• W2124444513 cites W2022612600 @default.
• W2124444513 cites W2025546802 @default.
• W2124444513 cites W2034872994 @default.
• W2124444513 cites W2039599894 @default.
• W2124444513 cites W2040690917 @default.
• W2124444513 cites W2044594872 @default.
• W2124444513 cites W2047198892 @default.
• W2124444513 cites W2047384616 @default.
• W2124444513 cites W2050662826 @default.
• W2124444513 cites W2058530636 @default.
• W2124444513 cites W2066266956 @default.
• W2124444513 cites W2067308664 @default.
• W2124444513 cites W2079234445 @default.
• W2124444513 cites W2083493906 @default.
• W2124444513 cites W2093391043 @default.
• W2124444513 cites W2107156397 @default.
• W2124444513 cites W2114007446 @default.
• W2124444513 cites W2125460059 @default.
• W2124444513 cites W2127402429 @default.
• W2124444513 cites W2129528064 @default.
• W2124444513 cites W2130807253 @default.
• W2124444513 cites W2131881430 @default.
• W2124444513 cites W2137704498 @default.
• W2124444513 cites W2148964640 @default.
• W2124444513 cites W2149142984 @default.
• W2124444513 cites W2161849629 @default.
• W2124444513 cites W2161983628 @default.
• W2124444513 cites W2308269884 @default.
• W2124444513 cites W2413441002 @default.
• W2124444513 cites W2789633529 @default.
• W2124444513 cites W4248239529 @default.
• W2124444513 doi "https://doi.org/10.1124/mol.109.055608" @default.
• W2124444513 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/19339490" @default.
• W2124444513 hasPublicationYear "2009" @default.
• W2124444513 type Work @default.
• W2124444513 sameAs 2124444513 @default.
• W2124444513 citedByCount "68" @default.
• W2124444513 countsByYear W21244445132012 @default.
• W2124444513 countsByYear W21244445132013 @default.
• W2124444513 countsByYear W21244445132014 @default.
• W2124444513 countsByYear W21244445132015 @default.
• W2124444513 countsByYear W21244445132016 @default.
• W2124444513 countsByYear W21244445132017 @default.
• W2124444513 countsByYear W21244445132018 @default.
• W2124444513 countsByYear W21244445132019 @default.
• W2124444513 countsByYear W21244445132020 @default.
• W2124444513 countsByYear W21244445132021 @default.
• W2124444513 countsByYear W21244445132022 @default.
• W2124444513 crossrefType "journal-article" @default.
• W2124444513 hasAuthorship W2124444513A5002189140 @default.
• W2124444513 hasAuthorship W2124444513A5017237506 @default.
• W2124444513 hasAuthorship W2124444513A5033878654 @default.
• W2124444513 hasAuthorship W2124444513A5072698271 @default.
• W2124444513 hasAuthorship W2124444513A5085540478 @default.
• W2124444513 hasAuthorship W2124444513A5085975282 @default.
• W2124444513 hasConcept C104317684 @default.
• W2124444513 hasConcept C12554922 @default.
• W2124444513 hasConcept C143065580 @default.
• W2124444513 hasConcept C145822097 @default.
• W2124444513 hasConcept C158617107 @default.
• W2124444513 hasConcept C164718446 @default.
• W2124444513 hasConcept C170493617 @default.
• W2124444513 hasConcept C181199279 @default.
• W2124444513 hasConcept C185592680 @default.
• W2124444513 hasConcept C203014093 @default.
• W2124444513 hasConcept C24530287 @default.
• W2124444513 hasConcept C2776714187 @default.
• W2124444513 hasConcept C2776938444 @default.
• W2124444513 hasConcept C2778428886 @default.
• W2124444513 hasConcept C2780340462 @default.
• W2124444513 hasConcept C501734568 @default.
• W2124444513 hasConcept C54355233 @default.

• next