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

Nuclear receptors in renal disease

(2011) Moshe Levi   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

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

Conformationally constrained farnesoid X receptor (FXR) agonists: Alternative replacements of the stilbene

(2011) Adwoa Akwabi-Ameyaw et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

Farnesoid X receptor agonists for primary biliary cirrhosis

(2011) Keith D Lindor   CURRENT OPINION IN GASTROENTEROLOGY

Farnesoid X Receptor Deficiency Improves Glucose Homeostasis in Mouse Models of Obesity

(2011) J. Prawitt et al.   DIABETES

Lowering Bile Acid Pool Size with a Synthetic Farnesoid X Receptor (FXR) Agonist Induces Obesity and Diabetes through Reduced Energy Expenditure

(2011) Mitsuhiro Watanabe et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Impact of bile acids on the growth of human cholangiocarcinoma via FXR

(2011) Jiaqi Dai et al.   Journal of Hematology & Oncology

Aldo-keto reductase 1B7 is a target gene of FXR and regulates lipid and glucose homeostasis

(2011) Xuemei Ge et al.   JOURNAL OF LIPID RESEARCH

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

A formulation‐enabled preclinical efficacy assessment of a farnesoid X receptor agonist, GW4064, in hamsters and cynomolgus monkeys

(2011) Po‐Chang Chiang et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Farnesoid X receptor inhibits tamoxifen-resistant MCF-7 breast cancer cell growth through downregulation of HER2 expression

(2011) C Giordano et al.   ONCOGENE

The statin class of HMG-CoA reductase inhibitors demonstrate differential activation of the nuclear receptors PXR, CAR and FXR, as well as their downstream target genes

(2011) Katharine Howe et al.   XENOBIOTICA

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

(2010) Ulrich Abel 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

Diabetic Nephropathy Is Accelerated by Farnesoid X Receptor Deficiency and Inhibited by Farnesoid X Receptor Activation in a Type 1 Diabetes Model

(2010) X. X. Wang et al.   DIABETES

Antidiabetic sulfonylureas modulate farnesoid X receptor activation and target gene transcription

(2010) Ramona Steri et al.   Future Medicinal Chemistry

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

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

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

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

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

FXR an emerging therapeutic target for the treatment of atherosclerosis

(2009) Andrea Mencarelli et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Activation of farnesoid X receptor prevents atherosclerotic lesion formation in LDLR−/−and apoE−/−mice

(2009) Helen B. Hartman 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

Differential Modulation of Farnesoid X Receptor Signaling Pathway by the Thiazolidinediones

(2009) R. Kaimal et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Exposure to the synthetic FXR agonist GW4064 causes alterations in gene expression and sublethal hepatotoxicity in eleutheroembryo medaka (Oryzias latipes)

(2009) Deanna L. Howarth et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Pyrazolidine-3,5-dione derivatives as potent non-steroidal agonists of farnesoid X receptor: Virtual screening, synthesis, and biological evaluation

(2008) Guanghui Deng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

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

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