Title : Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool.

Pub. Date : 2019 Aug 1

PMID : 31673308






3 Functional Relationships(s)
Download
Sentence
Compound Name
Protein Name
Organism
1 Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. pregna-4,17-diene-3,16-dione nuclear receptor subfamily 1 group H member 4 Homo sapiens
2 Although relatively weak, its activity at the farnesoid X receptor (FXR) is particularly intriguing as guggulsterone acts as an antagonist with a peculiar ability of gene selective modulation. pregna-4,17-diene-3,16-dione nuclear receptor subfamily 1 group H member 4 Homo sapiens
3 We report here a chemical biology study with the aim to further characterize the biological action of guggulsterone at the FXR and to obtain further insights into the functional role played by noncanonical FXR binding pockets S2 and S3. pregna-4,17-diene-3,16-dione nuclear receptor subfamily 1 group H member 4 Homo sapiens