FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2088431330> ?p ?o ?g. }

• W2088431330 endingPage "8075" @default.
• W2088431330 startingPage "8061" @default.
• W2088431330 abstract "Compound A (CpdA), a dissociated glucocorticoid receptor modulator, decreases corticosteroid-binding globulin (CBG), adrenocorticotropic hormone (ACTH), and luteneinizing hormone levels in rats. Whether this is due to transcriptional regulation by CpdA is not known. Using promoter reporter assays we show that CpdA, like dexamethasone (Dex), directly transrepresses these genes. Results using a rat Cbg proximal-promoter reporter construct in BWTG3 and HepG2 cell lines support a glucocorticoid receptor (GR)-dependent transrepression mechanism for CpdA. However, CpdA, unlike Dex, does not result in transactivation via glucocorticoid-responsive elements within a promoter reporter construct even when GR is co-transfected. The inability of CpdA to result in transactivation via glucocorticoid-responsive elements is confirmed on the endogenous tyrosine aminotransferase gene, whereas transrepression ability is confirmed on the endogenous CBG gene. Consistent with a role for CpdA in modulating GR activity, whole cell binding assays revealed that CpdA binds reversibly to the GR, but with lower affinity than Dex, and influences association of [(3)H]Dex, but has no effect on dissociation. In addition, like Dex, CpdA causes nuclear translocation of the GR, albeit to a lesser degree. Several lines of evidence, including fluorescence resonance energy transfer, co-immunoprecipitation, and nuclear immunofluorescence studies of nuclear localization-deficient GR show that CpdA, unlike Dex, does not elicit ligand-induced GR dimerization. Comparison of the behavior of CpdA in the presence of wild type GR to that of Dex with a dimerization-deficient GR mutant (GR(dim)) strongly supports the conclusion that loss of dimerization is responsible for the dissociated behavior of CpdA." @default.
• W2088431330 created "2016-06-24" @default.
• W2088431330 creator A5013916475 @default.
• W2088431330 creator A5018162918 @default.
• W2088431330 creator A5018767436 @default.
• W2088431330 creator A5022369864 @default.
• W2088431330 creator A5039693984 @default.
• W2088431330 creator A5040777054 @default.
• W2088431330 creator A5046462982 @default.
• W2088431330 creator A5052226197 @default.
• W2088431330 creator A5058466834 @default.
• W2088431330 creator A5079718410 @default.
• W2088431330 creator A5091781730 @default.
• W2088431330 date "2010-03-01" @default.
• W2088431330 modified "2023-10-15" @default.
• W2088431330 title "Abrogation of Glucocorticoid Receptor Dimerization Correlates with Dissociated Glucocorticoid Behavior of Compound A" @default.
• W2088431330 cites W1549679997 @default.
• W2088431330 cites W1582124530 @default.
• W2088431330 cites W1598886839 @default.
• W2088431330 cites W1747846752 @default.
• W2088431330 cites W1835342283 @default.
• W2088431330 cites W1909262944 @default.
• W2088431330 cites W1964051577 @default.
• W2088431330 cites W1965674955 @default.
• W2088431330 cites W1970259819 @default.
• W2088431330 cites W1977176665 @default.
• W2088431330 cites W1981067651 @default.
• W2088431330 cites W1983695933 @default.
• W2088431330 cites W1985341596 @default.
• W2088431330 cites W1990157223 @default.
• W2088431330 cites W1993057625 @default.
• W2088431330 cites W1997103341 @default.
• W2088431330 cites W2000328498 @default.
• W2088431330 cites W2001034975 @default.
• W2088431330 cites W2001449831 @default.
• W2088431330 cites W2012462612 @default.
• W2088431330 cites W2021789739 @default.
• W2088431330 cites W2026938521 @default.
• W2088431330 cites W2043382313 @default.
• W2088431330 cites W2043703663 @default.
• W2088431330 cites W2052500168 @default.
• W2088431330 cites W2053125671 @default.
• W2088431330 cites W2056582616 @default.
• W2088431330 cites W2066441538 @default.
• W2088431330 cites W2068281228 @default.
• W2088431330 cites W2070754236 @default.
• W2088431330 cites W2072049431 @default.
• W2088431330 cites W2072300954 @default.
• W2088431330 cites W2074631079 @default.
• W2088431330 cites W2076764916 @default.
• W2088431330 cites W2077993951 @default.
• W2088431330 cites W2078084967 @default.
• W2088431330 cites W2078111498 @default.
• W2088431330 cites W2081776165 @default.
• W2088431330 cites W2081794745 @default.
• W2088431330 cites W2082755088 @default.
• W2088431330 cites W2084219713 @default.
• W2088431330 cites W2092603902 @default.
• W2088431330 cites W2092900546 @default.
• W2088431330 cites W2095060581 @default.
• W2088431330 cites W2097221860 @default.
• W2088431330 cites W2099297532 @default.
• W2088431330 cites W2107529851 @default.
• W2088431330 cites W2110114520 @default.
• W2088431330 cites W2110244387 @default.
• W2088431330 cites W2117556333 @default.
• W2088431330 cites W2135268524 @default.
• W2088431330 cites W2142090085 @default.
• W2088431330 cites W2143103923 @default.
• W2088431330 cites W2143734001 @default.
• W2088431330 cites W2147277158 @default.
• W2088431330 cites W2156056701 @default.
• W2088431330 cites W2158526972 @default.
• W2088431330 cites W2165718181 @default.
• W2088431330 cites W2168006710 @default.
• W2088431330 cites W2168789122 @default.
• W2088431330 cites W2169457085 @default.
• W2088431330 cites W2169753137 @default.
• W2088431330 cites W4249742297 @default.
• W2088431330 cites W6483477 @default.
• W2088431330 doi "https://doi.org/10.1074/jbc.m109.087866" @default.
• W2088431330 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2832957" @default.
• W2088431330 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/20037160" @default.
• W2088431330 hasPublicationYear "2010" @default.
• W2088431330 type Work @default.
• W2088431330 sameAs 2088431330 @default.
• W2088431330 citedByCount "71" @default.
• W2088431330 countsByYear W20884313302012 @default.
• W2088431330 countsByYear W20884313302013 @default.
• W2088431330 countsByYear W20884313302014 @default.
• W2088431330 countsByYear W20884313302015 @default.
• W2088431330 countsByYear W20884313302016 @default.
• W2088431330 countsByYear W20884313302017 @default.
• W2088431330 countsByYear W20884313302018 @default.
• W2088431330 countsByYear W20884313302019 @default.
• W2088431330 countsByYear W20884313302020 @default.
• W2088431330 countsByYear W20884313302021 @default.
• W2088431330 countsByYear W20884313302022 @default.

• next