Related Articles: FXR

ABSTRACT Although several potent bile acid Farnesoid X receptor (FXR) and Takeda G-protein-coupled receptor 5 (TGR5, GPBAR1) dual agonists such as INT-767 have been reported, no non-bile acid FXR/TGR5 dual agonist has been investigated to date. Therefore, we attempted to discover potent non-bile acid FXR/TGR5 dual agonists and identified some non-bile acid FXR/TGR5 dual agonists,Read More

ABSTRACT The invention provides compositions and methods for use in the treatment and prevention of cholestatic diseases. To read the full Patent, click HERE. Date of publication: 14 January 2021; United States Patent Application 20210008128 Inventor Information: Nandakumar, Madhumitha (Arlington, MA, US), Liou, Alice Peiyu (Somerville, MA, US), Halvorsen, Elizabeth Moritz (Malden, MA, US), Mckenzie,Read More

ABSTRACT Intestinal health relies on the immunosuppressive activity of CD4+ regulatory T (Treg) cells. Expression of the transcription factor Foxp3 defines this lineage, and can be induced extrathymically by dietary or commensal-derived antigens in a process assisted by a Foxp3 enhancer known as conserved non-coding sequence 1 (CNS1). Products of microbial fermentation including butyrate facilitate the generationRead More

ABSTRACT Non-alcoholic steatohepatitis (NASH), characterized by hepatocyte injury, inflammation, and fibrosis, is the maincause of chronic liver disease in the Western world. There are currently no approved pharmacological therapies for NASH, underscoring the urgent need for effective treatments. The farnesoid X receptor (FXR) has emerged as an attractive target for the treatment of metabolic andRead More

View Full Size Research conducted by: Koji Toyokawa (1), Ewa Maddox (1), Jack Vanden Huevel (1,2), & Bruce Sherf (1) (1) INDIGO Biosciences, Inc., 1981 Pine Hall Rd, State College, PA, USA (2) Center for Molecular Toxicology and Carcinogenesis, 325 Life Sciences Building, Penn State University, University Park, PA 16802, USA Date of Publication: 2017

ABSTRACT Chemicals that alter normal function of farnesoid X receptor (FXR) have been shown to affect the homeostasis of bile acids, glucose, and lipids. Several structural classes of environmental chemicals and drugs that modulated FXR transactivation were previously identified by quantitative high-throughput screening (qHTS) of the Tox21 10 K chemical collection. In the present study, weRead More

ABSTRACT Exposure to certain munitions compounds is know to alter physiological functions in test organisms, however little is known about their molecular and cellular effects. Several nuclear receptors are regulated by xenobiotic compounds. These nuclear receptors belong to a class of ligand-activated transcription factors that, when heterodimerized with RXRa and bound to their respective DNARead More

Meets industry demand for increased pre-clinical predictability. State College, PA (August 9, 2016) INDIGO Biosciences, the recognized industry leader in Nuclear Receptor research, announced the addition of the Mouse Farnesoid X Receptor (mFXR) assay to their FXR portfolio. This addition both complements INDIGO’s industry-leading human FXR assay and meets the demand for an expansion ofRead More

ABSTRACT The RAR-related orphan receptor gamma t (RORγt) is a nuclear receptor required for generating IL-17–producing CD4+ Th17 T cells, which are essential in host defense and may play key pathogenic roles in autoimmune diseases. Oxysterols elicit profound effects on immune and inflammatory responses as well as on cholesterol and lipid metabolism. Here, we describe the identification of several naturally occurringRead More

View Full Size Research conducted by: Jerry Thompson (1), Jun Zhang (1), & Jack Vanden Huevel (1,2) (1) Center for Nutrigenomics, Penn State University, University Park, PA 16802, USA (2) INDIGO Biosciences, Inc., 1981 Pine Hall Rd, State College, PA, USA Date of Publication: March 2010