Characterizing ligands for farnesoid X receptor – availablein vitrotest systems for farnesoid X receptor modulator development

Activation of the nuclear receptor FXR enhances hepatocyte chemoprotection and liver tumor chemoresistance against genotoxic compounds

(2013) Javier Vaquero et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery

(2013) Donna D. Yu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Asymmetric synthesis of the four diastereoisomers of a novel non-steroidal farnesoid X receptor (FXR) agonist: Role of the chirality on the biological activity

(2013) Maura Marinozzi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Binding Mechanism of the Farnesoid X Receptor Marine Antagonist Suvanine Reveals a Strategy To Forestall Drug Modulation on Nuclear Receptors. Design, Synthesis, and Biological Evaluation of Novel Ligands

(2013) Francesco Saverio Di Leva et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Bile Acid Sensor FXR Is Required for Immune-Regulatory Activities of TLR-9 in Intestinal Inflammation

(2013) Barbara Renga et al.   PLoS One

Pyrazole[3,4-e][1,4]thiazepin-7-one derivatives as a novel class of Farnesoid X Receptor (FXR) agonists

(2012) Maura Marinozzi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Sesquiterpenoids from Atractylodes macrocephala act as farnesoid X receptor and progesterone receptor modulators

(2012) Chia-Jui Tsai et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Bile Acids Acutely Stimulate Insulin Secretion of Mouse  -Cells via Farnesoid X Receptor Activation and KATP Channel Inhibition

(2012) M. Dufer et al.   DIABETES

Medicinal chemistry of farnesoid X receptor ligands: from agonists and antagonists to modulators

(2012) Daniel Merk et al.   Future Medicinal Chemistry

Discovery and Optimization of 1,3,4-Trisubstituted-pyrazolone Derivatives as Novel, Potent, and Nonsteroidal Farnesoid X Receptor (FXR) Selective Antagonists

(2012) Huang Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Preliminary Structure-Activity Relationship on Theonellasterol, a New Chemotype of FXR Antagonist, from the Marine Sponge Theonella swinhoei

(2012) Valentina Sepe et al.   Marine Drugs

Identification of liver X receptor and farnesoid X receptor dual agonists from Tithonia diversifolia

(2012) Hsiang-Ru Lin   MEDICINAL CHEMISTRY RESEARCH

Discovery That Theonellasterol a Marine Sponge Sterol Is a Highly Selective FXR Antagonist That Protects against Liver Injury in Cholestasis

(2012) Barbara Renga et al.   PLoS One

Polyhydroxylated sterols from the Indonesian soft coral Sinularia sp. and their effect on farnesoid X-activated receptor

(2012) Masteria Yunovilsa Putra et al.   STEROIDS

4-Methylenesterols from Theonella swinhoei sponge are natural pregnane-X-receptor agonists and farnesoid-X-receptor antagonists that modulate innate immunity

(2012) Simona De Marino et al.   STEROIDS

The significance of the nuclear farnesoid X receptor (FXR) in β cell function

(2012) Martina Düfer et al.   Islets

Pharmacophore-based discovery of FXR-agonists. Part II: Identification of bioactive triterpenes from Ganoderma lucidum

(2011) Ulrike Grienke et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Pharmacophore-based discovery of FXR agonists. Part I: Model development and experimental validation

(2011) Daniela Schuster et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Extending SAR of bile acids as FXR ligands: Discovery of 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-amine

(2011) Antimo Gioiello et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Optimization of a novel class of benzimidazole-based farnesoid X receptor (FXR) agonists to improve physicochemical and ADME properties

(2011) Hans G.F. Richter et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

FXR activation inhibits inflammation and preserves the intestinal barrier in IBD

(2011) M. E. Wildenberg et al.   GUT

Theonellasterols and Conicasterols fromTheonella swinhoei. Novel Marine Natural Ligands for Human Nuclear Receptors

(2011) Simona De Marino et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Sulfated Sterols from Marine Invertebrates as a New Class of Marine Natural Antagonists of Farnesoid-X-Receptor

(2011) Valentina Sepe et al.   JOURNAL OF MEDICINAL CHEMISTRY

Antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation

(2011) Jang Hyun Choi et al.   NATURE

Farnesoid X Receptor (FXR) Activation and FXR Genetic Variation in Inflammatory Bowel Disease

(2011) Rian M. Nijmeijer et al.   PLoS One

A tea catechin, epigallocatechin-3-gallate, is a unique modulator of the farnesoid X receptor

(2011) Guodong Li et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Regulation of FXR transcriptional activity in health and disease: Emerging roles of FXR cofactors and post-translational modifications

(2010) Jongsook Kim Kemper   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists

(2010) Ulrich Abel et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Conformationally constrained farnesoid X receptor (FXR) agonists: Heteroaryl replacements of the naphthalene

(2010) Jonathan Y. Bass et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of novel and orally active FXR agonists for the potential treatment of dyslipidemia & diabetes

(2010) Hans G.F. Richter et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Improvement of Physiochemical Properties of the Tetrahydroazepinoindole Series of Farnesoid X Receptor (FXR) Agonists: Beneficial Modulation of Lipids in Primates

(2010) Joseph T. Lundquist et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tuberatolides, Potent FXR Antagonists from the Korean Marine TunicateBotryllus tuberatus

(2010) Hyukjae Choi et al.   JOURNAL OF NATURAL PRODUCTS

Functional Characterization of the Semisynthetic Bile Acid Derivative INT-767, a Dual Farnesoid X Receptor and TGR5 Agonist

(2010) G. Rizzo et al.   MOLECULAR PHARMACOLOGY

Identification of farnesoid X receptor modulators by a fluorescence polarization-based interaction assay

(2009) Ki-Cheol Han et al.   ANALYTICAL BIOCHEMISTRY

Pyrrole[2,3-d]azepino compounds as agonists of the farnesoid X receptor (FXR)

(2009) John F. Mehlmann et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064

(2009) Jonathan Y. Bass et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

FXR agonist activity of conformationally constrained analogs of GW 4064

(2009) Adwoa Akwabi-Ameyaw et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of an N-oxide pyridine GW4064 analog as a potent FXR agonist

(2009) Song Feng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

FXR Acetylation Is Normally Dynamically Regulated by p300 and SIRT1 but Constitutively Elevated in Metabolic Disease States

(2009) Jongsook Kim Kemper et al.   Cell Metabolism

Targeting Farnesoid-X-Receptor: From Medicinal Chemistry to Disease Treatment

(2009) S. Fiorucci et al.   CURRENT MEDICINAL CHEMISTRY

Identification of Novel Pathways That Control Farnesoid X Receptor-mediated Hypocholesterolemia

(2009) Yanqiao Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

FXR activation reverses insulin resistance and lipid abnormalities and protects against liver steatosis in Zucker (fa/fa) obese rats

(2009) Sabrina Cipriani et al.   JOURNAL OF LIPID RESEARCH

Discovery of XL335 (WAY-362450), a Highly Potent, Selective, and Orally Active Agonist of the Farnesoid X Receptor (FXR)

(2009) Brenton Flatt et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure–activity relationship of bile alcohols as human farnesoid X receptor agonist

(2009) Yusuke Iguchi et al.   STEROIDS

Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064

(2008) Adwoa Akwabi-Ameyaw et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

FXR: a metabolic regulator and cell protector

(2008) Yan-Dong Wang et al.   CELL RESEARCH

Phosphorylation of Farnesoid X Receptor by Protein Kinase C Promotes Its Transcriptional Activity

(2008) Romain Gineste et al.   MOLECULAR ENDOCRINOLOGY

Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation

(2008) S. M. Soisson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA