Ontology highlight
ABSTRACT:
SUBMITTER: Kick EK
PROVIDER: S-EPMC5150697 | biostudies-literature | 2016 Dec
REPOSITORIES: biostudies-literature
Kick Ellen K EK Busch Brett B BB Martin Richard R Stevens William C WC Bollu Venkataiah V Xie Yinong Y Boren Brant C BC Nyman Michael C MC Nanao Max H MH Nguyen Lam L Plonowski Artur A Schulman Ira G IG Yan Grace G Zhang Huiping H Hou Xiaoping X Valente Meriah N MN Narayanan Rangaraj R Behnia Kamelia K Rodrigues A David AD Brock Barry B Smalley James J Cantor Glenn H GH Lupisella John J Sleph Paul P Grimm Denise D Ostrowski Jacek J Wexler Ruth R RR Kirchgessner Todd T Mohan Raju R
ACS medicinal chemistry letters 20161023 12
Introducing a uniquely substituted phenyl sulfone into a series of biphenyl imidazole liver X receptor (LXR) agonists afforded a dramatic potency improvement for induction of ATP binding cassette transporters, ABCA1 and ABCG1, in human whole blood. The agonist series demonstrated robust LXRβ activity (>70%) with low partial LXRα agonist activity (<25%) in cell assays, providing a window between desired blood cell ABCG1 gene induction in cynomolgus monkeys and modest elevation of plasma triglycer ...[more]