Discovery and structure–activity relationship studies of indole derivatives as liver X receptor (LXR) agonists

Autor:	Ila Sircar, Chiaki Fukushima, Lisa Schneider, James Zapf, Madhavi Pannala, Lisa Morera, Trang Nguyen, Jie-Fei Cheng, Rick Jack, Norma Wilson, Shao-Hui Zhang, Kui Xu, Farid Bakir, Juping Liu, Kei Takedomi, Naoki Sakurai, Sunil Kher
Rok vydání:	2007
Předmět:	Agonist Indoles medicine.drug_class Clinical Biochemistry Receptors Cytoplasmic and Nuclear Pharmaceutical Science Biochemistry Monocytes Cell Line Structure-Activity Relationship Transactivation Drug Discovery Gene expression medicine ABCA1 Gene Humans Structure–activity relationship Liver X receptor Molecular Biology Liver X Receptors Chemistry Macrophages Organic Chemistry Orphan Nuclear Receptors DNA-Binding Proteins Gene Expression Regulation Models Chemical Nuclear receptor Molecular Medicine ATP-Binding Cassette Transporters lipids (amino acids peptides and proteins) Signal transduction Sterol Regulatory Element Binding Protein 1 ATP Binding Cassette Transporter 1
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 17:3473-3479
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2007.03.076
Popis:	A structurally novel liver X receptor (LXR) agonist (1) was identified from internal compound collection utilizing the combination of structure-based virtual screening and high-throughput gene profiling. Compound 1 increased ABCA1 gene expression by eightfold and SREBP1c by threefold in differentiated THP-1 macrophage cell lines. Confirmation of its agonistic activity against LXR was obtained in the co-factor recruitment and reporter transactivation assays. Structure-activity relationship studies on compound 1 are described.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f7eb508e31f7c0f8a1fb69a6abab291c https://doi.org/10.1016/j.bmcl.2007.03.076 Zobrazit plný text záznamu Full Text from ScienceDirect