标题
FXR: structures, biology, and drug development for NASH and fibrosis diseases
作者
关键词
-
出版物
ACTA PHARMACOLOGICA SINICA
Volume 43, Issue 5, Pages 1120-1132
出版商
Springer Science and Business Media LLC
发表日期
2022-02-25
DOI
10.1038/s41401-021-00849-4
参考文献
相关参考文献
注意:仅列出部分参考文献,下载原文获取全部文献信息。- A structurally optimized FXR agonist, MET409, reduced liver fat content over 12 weeks in patients with non-alcoholic steatohepatitis
- (2021) Stephen A. Harrison et al. JOURNAL OF HEPATOLOGY
- Intestine-specific FXR agonists as potential therapeutic agents for colorectal cancer
- (2021) Yiming Yin et al. BIOCHEMICAL PHARMACOLOGY
- Safety, Pharmacokinetics, Pharmacodynamics, and Formulation of Liver‐Distributed Farnesoid X‐Receptor Agonist TERN‐101 in Healthy Volunteers
- (2021) Yujin Wang et al. Clinical Pharmacology in Drug Development
- Cilofexor, a Nonsteroidal FXR Agonist, in Non‐Cirrhotic Patients with Nonalcoholic Steatohepatitis: A Phase 2 Randomized Controlled Trial
- (2020) Keyur Patel et al. HEPATOLOGY
- Emerging drugs for the treatment of non-alcoholic steatohepatitis: a focused review of farnesoid X receptor agonists
- (2020) Raj A. Shah et al. EXPERT OPINION ON EMERGING DRUGS
- Bile acid modulators for the treatment of nonalcoholic steatohepatitis (NASH)
- (2020) Stefano Fiorucci et al. EXPERT OPINION ON INVESTIGATIONAL DRUGS
- Structural basis of tropifexor as a potent and selective agonist of farnesoid X receptor
- (2020) Longying Jiang et al. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
- Combination Therapies Including Cilofexor and Firsocostat for Bridging Fibrosis and Cirrhosis Attributable to NASH
- (2020) Rohit Loomba et al. HEPATOLOGY
- Molecular tuning of farnesoid X receptor partial agonism
- (2019) Daniel Merk et al. Nature Communications
- REGENERATE: Design of a pivotal, randomised, phase 3 study evaluating the safety and efficacy of obeticholic acid in patients with fibrosis due to nonalcoholic steatohepatitis
- (2019) Vlad Ratziu et al. Contemporary Clinical Trials
- Obeticholic acid for the treatment of non-alcoholic steatohepatitis: interim analysis from a multicentre, randomised, placebo-controlled phase 3 trial
- (2019) Zobair M Younossi et al. LANCET
- Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel Non–Bile Acid FXR Agonist Tropifexor (LJN452) in Healthy Volunteers
- (2019) Michael K. Badman et al. Clinical Pharmacology in Drug Development
- Anti-NASH Drug Development Hitches a Lift on PPAR Agonism
- (2019) Joost Boeckmans et al. Cells
- Farnesoid X receptor modulators 2014-present: a patent review
- (2018) Valentina Sepe et al. EXPERT OPINION ON THERAPEUTIC PATENTS
- Update on FXR Biology: Promising Therapeutic Target?
- (2018) Chang Han INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
- Structural insights into the heterodimeric complex of the nuclear receptors FXR and RXR
- (2018) Weili Zheng et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Future trends in the treatment of non-alcoholic steatohepatitis
- (2018) Stefano Fiorucci et al. PHARMACOLOGICAL RESEARCH
- Progress and challenges of selective Farnesoid X Receptor modulation
- (2018) Vittoria Massafra et al. PHARMACOLOGY & THERAPEUTICS
- Farnesoid X receptor agonist INT-767 attenuates liver steatosis and inflammation in rat model of nonalcoholic steatohepatitis
- (2018) Ying-Bin Hu et al. Drug Design Development and Therapy
- FXR modulators for enterohepatic and metabolic diseases
- (2018) Hong Wang et al. EXPERT OPINION ON THERAPEUTIC PATENTS
- Ligand binding and heterodimerization with retinoid X receptor α (RXRα) induce farnesoid X receptor (FXR) conformational changes affecting coactivator binding
- (2018) Na Wang et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Current and future pharmacological therapies for NAFLD/NASH
- (2017) Yoshio Sumida et al. JOURNAL OF GASTROENTEROLOGY
- Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH)
- (2017) David C. Tully et al. JOURNAL OF MEDICINAL CHEMISTRY
- Dual PPARα/γ agonist saroglitazar improves liver histopathology and biochemistry in experimental NASH models
- (2017) Mukul R. Jain et al. LIVER INTERNATIONAL
- Targeting nuclear receptors for the treatment of fatty liver disease
- (2017) Naoki Tanaka et al. PHARMACOLOGY & THERAPEUTICS
- Synthesis and Biological Evaluation of a Series of Bile Acid Derivatives as FXR Agonists for Treatment of NASH
- (2017) Hualing Xiao et al. ACS Medicinal Chemistry Letters
- Nuclear receptors and nonalcoholic fatty liver disease 1 1This article is part of a Special Issue entitled: Xenobiotic nuclear receptors: New Tricks for An Old Dog, edited by Dr. Wen Xie.
- (2016) Matthew C. Cave et al. Biochimica et Biophysica Acta-Gene Regulatory Mechanisms
- Novel substituted isoxazole FXR agonists with cyclopropyl, hydroxycyclobutyl and hydroxyazetidinyl linkers: Understanding and improving key determinants of pharmacological properties
- (2016) Olaf Kinzel et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Farnesoid X Receptor Agonists and Other Bile Acid Signaling Strategies for Treatment of Liver Disease
- (2016) Emina Halilbasic et al. DIGESTIVE DISEASES
- Novel Pharmacotherapy Options for NASH
- (2016) Vlad Ratziu DIGESTIVE DISEASES AND SCIENCES
- Recent Progress on Bile Acid Receptor Modulators for Treatment of Metabolic Diseases
- (2016) Yanping Xu JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders
- (2016) Roberto Pellicciari et al. JOURNAL OF MEDICINAL CHEMISTRY
- Fatty liver diseases, bile acids, and FXR
- (2016) Yan Zhu et al. Acta Pharmaceutica Sinica B
- Insights on FXR selective modulation. Speculation on bile acid chemical space in the discovery of potent and selective agonists
- (2016) Valentina Sepe et al. Scientific Reports
- FXR Agonists as Therapeutic Agents for Non-alcoholic Fatty Liver Disease
- (2015) Rotonya M. Carr et al. Current Atherosclerosis Reports
- Structural Basis for Small Molecule NDB (N-Benzyl-N-(3-(tert-butyl)-4-hydroxyphenyl)-2,6-dichloro-4-(dimethylamino) Benzamide) as a Selective Antagonist of Farnesoid X Receptor α (FXRα) in Stabilizing the Homodimerization of the Receptor
- (2015) Xing Xu et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: A Novel FXR Agonist for the Treatment of Dyslipidemia
- (2015) Michael J. Genin et al. JOURNAL OF MEDICINAL CHEMISTRY
- Farnesoid X nuclear receptor ligand obeticholic acid for non-cirrhotic, non-alcoholic steatohepatitis (FLINT): a multicentre, randomised, placebo-controlled trial
- (2015) Brent A Neuschwander-Tetri et al. LANCET
- Intestinal FXR agonism promotes adipose tissue browning and reduces obesity and insulin resistance
- (2015) Sungsoon Fang et al. NATURE MEDICINE
- Intestine-selective farnesoid X receptor inhibition improves obesity-related metabolic dysfunction
- (2015) Changtao Jiang et al. Nature Communications
- Gut Microbiota Regulates Bile Acid Metabolism by Reducing the Levels of Tauro-beta-muricholic Acid, a Naturally Occurring FXR Antagonist
- (2013) Sama I. Sayin et al. Cell Metabolism
- The antiparasitic drug ivermectin is a novel FXR ligand that regulates metabolism
- (2013) Lihua Jin et al. Nature Communications
- Transcriptional integration of metabolism by the nuclear sterol-activated receptors LXR and FXR
- (2012) Anna C. Calkin et al. NATURE REVIEWS MOLECULAR CELL BIOLOGY
- 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
- Selective Activation of Nuclear Bile Acid Receptor FXR in the Intestine Protects Mice Against Cholestasis
- (2011) Salvatore Modica et al. GASTROENTEROLOGY
- Structural and functional insights into nuclear receptor signaling
- (2010) Lihua Jin et al. ADVANCED DRUG DELIVERY REVIEWS
- 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
- 2 FARNESOID-X RECEPTOR AGONISTS: A NEW CLASS OF DRUGS FOR THE TREATMENT OF PBC? AN INTERNATIONAL STUDY EVALUATING THE ADDITION OF INT-747 TO URSODEOXYCHOLIC ACID
- (2010) A. Mason et al. JOURNAL OF HEPATOLOGY
- 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
- Farnesoid X receptor agonist WAY-362450 attenuates liver inflammation and fibrosis in murine model of non-alcoholic steatohepatitis
- (2009) Songwen Zhang et al. JOURNAL OF HEPATOLOGY
- 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
- Role of Bile Acids and Bile Acid Receptors in Metabolic Regulation
- (2009) Philippe Lefebvre et al. PHYSIOLOGICAL REVIEWS
- 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
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