2021
DOI: 10.1039/d0md00311e
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Microwave-assisted green synthesis of bile acid derivatives and evaluation of glucocorticoid receptor binding

Abstract: Green synthesis of bile acids derivatives and 5β-cholanic acid was achieved under microwave irradiation, and the binding affinity for the ligand binding domain of the glucocorticoid receptor was measured.

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Cited by 5 publications
(14 citation statements)
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“…For GR expression in yeast, a galactose‐inducible plasmid (pRF4‐6‐rGR‐LBD‐EYFP) encoding the ligand binding domain (LBD) of the glucocorticoid receptor (GR) fused to enhanced yellow fluorescent protein (EYFP) was used. Expression of GR‐LBD‐EYFP in yeast was detected by fluorescence microscopy, and dose‐dependent binding of a positive control GR ligand, prednisolone, was confirmed [24] . Bile acid methyl ester derivatives (5, 6, 6a, 6b, 10, 11, 14, 16, 18, 19, 19a) were then tested for affinity to the GR‐LBD by evaluation of the fold fluorescence change between ligand‐treated and estradiol‐treated (negative control) yeast cells expressing GR‐LBD‐YFP as described [24] .…”
Section: Resultsmentioning
confidence: 97%
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“…For GR expression in yeast, a galactose‐inducible plasmid (pRF4‐6‐rGR‐LBD‐EYFP) encoding the ligand binding domain (LBD) of the glucocorticoid receptor (GR) fused to enhanced yellow fluorescent protein (EYFP) was used. Expression of GR‐LBD‐EYFP in yeast was detected by fluorescence microscopy, and dose‐dependent binding of a positive control GR ligand, prednisolone, was confirmed [24] . Bile acid methyl ester derivatives (5, 6, 6a, 6b, 10, 11, 14, 16, 18, 19, 19a) were then tested for affinity to the GR‐LBD by evaluation of the fold fluorescence change between ligand‐treated and estradiol‐treated (negative control) yeast cells expressing GR‐LBD‐YFP as described [24] .…”
Section: Resultsmentioning
confidence: 97%
“…UDCA and UDCA derivatives have affinity for the glucocorticoid receptor (GR) and have been shown to be GR modulators, inducing GR translocation and activation in cell models [61] . Because of their structural similarity to UDCA and other GR ligands, we tested the potential affinity of compounds (5, 6, 6a, 6b, 10, 11, 14, 16, 18, 19, 19a) for GR using a yeast‐based fluorescence assay optimized for screening steroidal derivatives with estrogen, androgen or glucocorticoid receptor binding properties [23,24] . For GR expression in yeast, a galactose‐inducible plasmid (pRF4‐6‐rGR‐LBD‐EYFP) encoding the ligand binding domain (LBD) of the glucocorticoid receptor (GR) fused to enhanced yellow fluorescent protein (EYFP) was used.…”
Section: Resultsmentioning
confidence: 99%
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