10.1021/acsmedchemlett.8b00361.s001
Autumn
R. Flynn
Autumn
R.
Flynn
Suzanne G. Mays
Suzanne G.
Mays
Eric A. Ortlund
Eric
A. Ortlund
Nathan T. Jui
Nathan T.
Jui
Development of Hybrid Phospholipid Mimics as Effective
Agonists for Liver Receptor Homologue‑1
American Chemical Society
2018
receptor Liver Receptor Homologue
micromolar efficacy
Effective Agonists
ligand classes
Hybrid Phospholipid Mimics
drug target
LRH
hexahydropentalene compounds
ligand binding pocket
2018-09-04 00:00:00
Journal contribution
https://acs.figshare.com/articles/journal_contribution/Development_of_Hybrid_Phospholipid_Mimics_as_Effective_Agonists_for_Liver_Receptor_Homologue_1/7063742
The
orphan nuclear receptor Liver Receptor Homologue-1 (LRH-1)
is an emerging drug target for metabolic disorders. The most effective
known LRH-1 modulators are phospholipids or synthetic hexahydropentalene
compounds. While both classes have micromolar efficacy, they target
different portions of the ligand binding pocket and activate LRH-1
through different mechanisms. Guided by crystallographic data, we
combined aspects of both ligand classes into a single scaffold, resulting
in the most potent and efficacious LRH-1 agonists to date.