Development of Hybrid Phospholipid Mimics as Effective Agonists for Liver Receptor Homologue-1
Year: 2018
Type: article
Abstract: 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.
Source: ACS Medicinal Chemistry Letters
Institutions: Emory University, Winship Cancer Institute
Language: English
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: green
Awards: Targeting LRH-1 - Phospholipid Signaling in Metabolic Pathways, Regulation of LRH-1 by small molecules, A pilot study to target out-of-dialysis-unit versus dialysis-unit blood pressure, G8062246797, Targeting the orphan nuclear receptor LRH-1 with small molecules, Graduate Training in the Pharmacological Sciences
OpenAlex ID: W2891588020