Data analysis of the nuclear receptor activation assay: Transcriptional activation is monitored by luminescence. Data are expressed as fold activation relative to the vehicle control, following normalization of luciferase activity against cell viability. The use of 5 or more doses of test article and ...
Differential control of gene activity by isoforms A, B1 and B2 of the Drosophila ecdysone receptor. Eur. J. Biochem. 268, 1811–1819 (2001). Article CAS PubMed Google Scholar Clayton, G. M., Peak-Chew, S. Y., Evans, R. M. & Schwabe, J. W. The structure of the ultraspiracle ...
摘要: The ligand-binding domain of nuclear receptors appears to contain a common fold that generates a conserved ligand-binding pocket. Their transcriptional activity is induced by ligand through realignment of a C-terminal helix to form a novel interacting surface....
In vitro assays ?INTERACTION (BINDING) to the receptor ? competitive ligand binding assay ?Effect unknown (? Activation / suppression / no effect ?) ?Testing the effect at cellular level (interference with receptor biological activity) ? cell proliferation assay ? endogenous protein expression (or ...
In vitro assays ?INTERACTION (BINDING) to the receptor ? competitive ligand binding assay ?Effect unknown (? Activation / suppression / no effect ?) ?Testing the effect at cellular level (interference with receptor biological activity) ? cell proliferation assay ? endogenous protein expression (or ...
Identification of the tryptophan photoproduct 6-formylindolo[3,2-b]carbazole, in cell culture medium, as a factor that controls the background aryl hydrocarbon receptor activity. Toxicol Sci 2005; 85: 935–943. PubMed Google Scholar Yasui T, Kim EY, Iwata H, Franks DG, Karchner SI, Hahn...
The subsequent cloning of other receptor genes led to the unexpected discovery that there were many more nuclear receptor–like genes than previously suspected. Today, the human genome is reported to contain 48 members of this transcription factor family (1). This superfamily includes not only the...
Upon ligand binding, the androgen receptor (AR) can inhibit Nur77 activity through interaction of the N-terminal domain of Nur77 with the DBD of AR. Competition for SRC-1 binding was identified as the underlying mechanism for this inhibition of Nur77 activity, analogous to DAX1 inhibition [...
Members of the nuclear receptor superfamily are ligand-dependent transcription factors that regulate the expression of target genes via binding to specific cis-acting elements (Evans, 1988; Green and Chambon, 1988; Beato, 1989; O’Malley, 1990; Parker, 1990; Wahli and Martinez, 1991; Tsai and ...
Although nuclear hormone receptors have emerged as key therapeutic targets in breast and prostate malignancies, whose initiation and progression are intricately linked to the estrogen and testosterone sex hormones, the clinical potential of nuclearhormone receptortargeting in other solid cancers originating fr...