Abstract
In this paper, we report the first evidence of 4-methylenesterols, isolated from the marine sponge Theonella swinhoei, as antagonists of Estrogen Related Receptors (ERRs). The interactions of 4-methylenesterols with ERRs were investigated through a multi-parametric approach involving biological assays and molecular modelling. Here the first homology model of active and inactive conformations of the Estrogen Related Receptor β (ERRβ) is also reported, benchmarked with the well known agonists gsk4716 and genistein, and the antagonists 4-hydroxytamoxifen and diethylstilbestrol. Our proposed model could contribute to the clarification of small molecule interaction mode in the ERRβ and, notably, to the rational design of new potential and selective modulators of this emerging therapeutic target.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.