Development of heterodimeric estrogen receptor alpha antagonists to target simultaneously the ligand and coactivator binding site.
Sign Up to like & getrecommendations! Published in 2023 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200638
Abstract: One-third of breast cancer patients will develop recurrent cancer within 15 years of endocrine treatment. Notably, tumor growth in a hormone-refractory state still relies on the interaction between estrogen receptor alpha (ERĪ±) and upregulated coactivators.… read more here.
Keywords: binding site; site; estrogen receptor; coactivator binding ... See more keywords
Steroid receptor/coactivator binding inhibitors: An update
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DOI: 10.1016/j.mce.2019.110471
Abstract: The purpose of this review is to highlight recent developments in small molecules and peptides that block the binding of coactivators to steroid receptors. These coactivator binding inhibitors bind at the coregulator binding groove, also… read more here.
Keywords: receptor coactivator; binding inhibitors; steroid receptors; coactivator binding ... See more keywords
The dynamic properties of a nuclear coactivator binding domain are evolutionarily conserved.
Sign Up to like & getrecommendations! Published in 2022 at "Communications biology"
DOI: 10.1038/s42003-022-03217-y
Abstract: Evolution of proteins is constrained by their structure and function. While there is a consensus that the plasticity of intrinsically disordered proteins relaxes the structural constraints on evolution there is a paucity of data on… read more here.
Keywords: dynamic properties; binding domain; domain; coactivator binding ... See more keywords