4.7 Review

Development of bile acid activated receptors hybrid molecules for the treatment of inflammatory and metabolic disorders

Related references

Note: Only part of the references are listed.
Article Multidisciplinary Sciences

Combinatorial therapy with BAR502 and UDCA resets FXR and GPBAR1 signaling and reverses liver histopathology in a model of NASH

Silvia Marchiano et al.

Summary: BAR502 and UDCA combination therapy showed better efficacy than individual therapy in treating NAFLD/NASH, by improving liver damage, steatosis, inflammation, and fibrosis. The combination also increased insulin sensitivity and bile acid signaling, modulated gene expression, reduced expression of inflammatory markers, and redirected bile acid metabolism.

SCIENTIFIC REPORTS (2023)

Article Chemistry, Multidisciplinary

Discovery of a Novel Class of Dual GPBAR1 Agonists-RORγt Inverse Agonists for the Treatment of IL-17-Mediated Disorders

Bianca Fiorillo et al.

Summary: Researchers designed and synthesized bile acid-derived ligands with potent dual activity, and compound 7 showed excellent pharmacokinetic properties and robust anti-inflammatory activity.

ACS OMEGA (2023)

Article Biochemistry & Molecular Biology

Discovery of FXR/PPAR? dual partial agonist

Yukiko Yamashita et al.

Summary: This study identified a benzimidazole compound 18 with dual partial agonistic activity for FXR and PPAR gamma, which could be a novel candidate for treating NAFLD associated with type 2 diabetes mellitus.

BIOORGANIC & MEDICINAL CHEMISTRY (2023)

Review Pharmacology & Pharmacy

Structures of Leukotriene Biosynthetic Enzymes and Development of New Therapeutics

Jesper Z. Haeggstrom et al.

Summary: Leukotrienes are potent immune-regulating lipid mediators involved in inflammatory and allergic diseases. They also contribute to low-grade inflammation in various diseases. Their biosynthesis involves specific enzymes in cells of the immune system, which assemble to form a biosynthetic complex. This article discusses recent advances in understanding the protein components of this enzyme machinery, as well as the potential for pharmacological intervention and development of new therapeutics.

ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY (2023)

Article Gastroenterology & Hepatology

Combinatorial targeting of G-protein-coupled bile acid receptor 1 and cysteinyl leukotriene receptor 1 reveals a mechanistic role for bile acids and leukotrienes in drug-induced liver injury

Michele Biagioli et al.

Summary: This study investigated the mutual interaction between GPBAR1 and CYSLTR1 in the development of drug-induced liver injury (DILI). The results showed that a small molecule called CHIN117, which functions as a GPBAR1 agonist and CYSLTR1 antagonist, could reverse liver damage caused by APAP and modulate multiple genes. This suggests that CHIN117 has potential therapeutic value for DILI.

HEPATOLOGY (2023)

Article Gastroenterology & Hepatology

A multisociety Delphi consensus statement on new fatty liver disease nomenclature

Mary E. Rinella et al.

Summary: This study aimed to determine if there was a need to change the nomenclature and definition of NAFLD and NASH. Through a Delphi process involving content experts and patient advocates, a consensus was reached to replace NAFLD with metabolic dysfunction-associated steatotic liver disease (MetALD) and modify the diagnostic criteria. The new nomenclature and criteria are widely supported, nonstigmatizing, and can improve awareness and patient identification.

HEPATOLOGY (2023)

Article Chemistry, Medicinal

Discovery of the First-in-Class Intestinal Restricted FXR and FABP1 Dual Modulator ZLY28 for the Treatment of Nonalcoholic Fatty Liver Disease

Qiang Ren et al.

Summary: The prevalence of nonalcoholic steatohepatitis (NASH) is rapidly increasing worldwide, posing a serious health problem. Selective activation of the intestinal farnesoid X receptor (FXR) is considered a promising strategy for NASH treatment with reduced side effects. Inhibition of intestinal fatty acid binding protein 1 (FABP1) also alleviates obesity and NASH. This study discovered ZLY28, a dual-target modulator of FXR and FABP1, which demonstrated strong anti-NASH effects and reduced systemic exposure, making it a potential novel anti-NASH agent.

JOURNAL OF MEDICINAL CHEMISTRY (2023)

Article Endocrinology & Metabolism

A time- and space-resolved nuclear receptor atlas in mouse liver

Francesco Paolo Zummo et al.

Summary: The liver plays a crucial role in maintaining organismal homeostasis through the function of nuclear receptors (NRs), which are transcription factors sensitive to external signals and regulated by intracellular signaling pathways. However, the understanding of NR functions in different liver cell populations is still limited. This study characterized the expression levels of NRs in the entire liver of mice under different time and diet conditions, and identified their cyclic expression patterns and cell-type specificity. Single-cell RNA sequencing analysis further revealed a zonation pattern of NRs in hepatocytes, liver sinusoidal cells, and stellate cells, highlighting the link between NR localization and liver functional specialization.

JOURNAL OF MOLECULAR ENDOCRINOLOGY (2023)

Article Biochemistry & Molecular Biology

Expanding the Library of 1,2,4-Oxadiazole Derivatives: Discovery of New Farnesoid X Receptor (FXR) Antagonists/Pregnane X Receptor (PXR) Agonists

Claudia Finamore et al.

Summary: A series of novel 1,2,4-oxadiazole derivatives were synthesized and their pharmacological and in vitro pharmacokinetic properties were evaluated. Compounds 5 and 11 were identified as the first examples of nonsteroidal dual FXR/PXR modulators, showing potential in the treatment of inflammatory disorders.

MOLECULES (2023)

Article Pharmacology & Pharmacy

The ameliorating effect of withaferin A on high-fat diet-induced non-alcoholic fatty liver disease by acting as an LXR/FXR dual receptor activator

Varsha D. D. Shiragannavar et al.

Summary: The incidence of non-alcoholic fatty liver disease (NAFLD) is rapidly increasing and has become a major disease in the modern world. Withaferin A, a natural dietary compound, shows potential as a therapeutic agent for the treatment of NAFLD due to its anti-inflammatory properties and its ability to regulate metabolism-associated gene expressions.

FRONTIERS IN PHARMACOLOGY (2023)

Article Oncology

Discovery of BAR502, as potent steroidal antagonist of leukemia inhibitory factor receptor for the treatment of pancreatic adenocarcinoma

Cristina Di Giorgio et al.

Summary: This study found that bile acids have a weak antagonistic effect on LIF/LIFR pathway in PDAC cells, while BAR502, a non-bile acid dual FXR and GPBAR1 ligand, can effectively inhibit the binding of LIF to LIFR, indicating its potential use in the treatment of LIFR overexpressing-PDAC.

FRONTIERS IN ONCOLOGY (2023)

Article Endocrinology & Metabolism

Gut hormone co-agonists for the treatment of obesity: from bench to bedside

Ruben Nogueiras et al.

Summary: The discovery and development of gut hormone co-agonists have revolutionized the treatment of diabetes and obesity. These therapeutics combine multiple gastrointestinal hormones into a single molecule, resulting in synergistic metabolic benefits. The GLP-1-GIP co-agonist tirzepatide, approved in 2022, has shown superior HbA1c reduction and significant weight loss in non-diabetic individuals with obesity.

NATURE METABOLISM (2023)

Review Pharmacology & Pharmacy

Epoxylipids and soluble epoxide hydrolase in heart diseases

John D. Imig et al.

Summary: Coronary artery dysfunction, inflammation, and mitochondrial dysfunction contribute to the progression of heart diseases, and genetic and pharmacological manipulation of epoxylipids has therapeutic benefits.

BIOCHEMICAL PHARMACOLOGY (2022)

Review Pharmacology & Pharmacy

Withaferin A in the Treatment of Liver Diseases: Progress and Pharmacokinetic Insights

Yangliu Xia et al.

Summary: This review summarizes the effects of Withaferin A (WA) in the treatment of liver injury, systematic inflammation, and liver cancer. It also discusses the toxicity, metabolism, and pharmacological potentials of WA and other extracts from Withania somnifera (W. somnifera). The pharmacokinetic behaviors of WA are summarized and highlighted for future studies in the treatment of liver diseases.

DRUG METABOLISM AND DISPOSITION (2022)

Review Biochemistry & Molecular Biology

Linking liver metabolic and vascular disease via bile acid signaling

Stefano Fiorucci et al.

Summary: NAFLD is a metabolic disorder affecting over one quarter of the global population, primarily caused by liver fat accumulation leading to the development of atherosclerotic cardiovascular disease. Developing dual FXR/GPBAR1 ligands or other therapies is a potential treatment approach for this issue.

TRENDS IN MOLECULAR MEDICINE (2022)

Review Pharmacology & Pharmacy

Therapeutic Opportunities of GPBAR1 in Cholestatic Diseases

Fangling Zhang et al.

Summary: This review summarizes the function and mechanisms of GPBAR1 in cholestatic liver disease. GPBAR1 regulates cholestasis through various pathways and plays an important role in protecting against diseases and injuries. However, its proliferative properties also increase the risk of cholangiocarcinoma.

FRONTIERS IN PHARMACOLOGY (2022)

Article Multidisciplinary Sciences

Human gut bacteria produce TH17-modulating bile acid metabolites

Donggi Paik et al.

Summary: This study identifies bile acids produced by gut bacteria that inhibit the differentiation of T(H)17 cells, a key immune cell type involved in inflammatory disorders such as inflammatory bowel disease. The levels of these bile acids are reduced in patients with inflammatory bowel disease and are inversely correlated with the expression of T(H)17-cell-associated genes.

NATURE (2022)

Article Pharmacology & Pharmacy

Discovery of a Potent and Orally Active Dual GPBAR1/CysLT1R Modulator for the Treatment of Metabolic Fatty Liver Disease

Stefano Fiorucci et al.

Summary: This study reported the discovery of a novel class of hybrid molecules for the treatment of NAFLD/NASH. These compounds, acting as both CysLT(1)R antagonists and GPBAR1 agonists, showed efficacy in reversing liver histopathology features in a preclinical model of NASH, indicating their potential for further development.

FRONTIERS IN PHARMACOLOGY (2022)

Article Biochemistry & Molecular Biology

The role of FXR and TGR5 in reversing and preventing progression of Western diet-induced hepatic steatosis, inflammation, and fibrosis in mice

Xiaoxin X. Wang et al.

Summary: The dual FXR-TGR5 agonist INT-767 can prevent the progression of Western diet-induced NASH in mice by modulating bile acid composition, improving liver fatty acid synthesis and uptake, reducing inflammation, and maintaining mitochondrial function.

JOURNAL OF BIOLOGICAL CHEMISTRY (2022)

Review Pharmacology & Pharmacy

Bile acid metabolism and signaling, the microbiota, and metabolic disease

Jingwei Cai et al.

Summary: The diversity, composition, and function of the bacterial community in the human gastrointestinal tract play a crucial role in host health. Bile acids, as potent metabolic and immune signaling molecules, have significant impacts on host metabolic and immunological functions. Manipulating the microbiota-bile acid-bile acid receptor axis has emerged as a novel therapeutic approach for human health.

PHARMACOLOGY & THERAPEUTICS (2022)

Article Chemistry, Medicinal

Structural Basis for Developing Multitarget Compounds Acting on Cysteinyl Leukotriene Receptor 1 and G-Protein-Coupled Bile Acid Receptor

Bianca Fiorillo et al.

Summary: GPCRs are important molecular targets for drug development, with potential for multitarget drugs. Compounds with dual activity towards CysLT(1)R and GPBAR1 show promise in treating inflammatory diseases such as colitis. The binding mode of these compounds reveals structural basis for future drug design studies.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Biochemistry & Molecular Biology

Liver X receptors and liver physiology

Lillian Russo-Savage et al.

Summary: Liver X receptors are ligand-dependent transcription factors that regulate transcription by directly binding cholesterol derivatives, playing important roles in lipid homeostasis throughout the body. In the liver, LXR controls cholesterol and fatty acid metabolism, and modifying LXR activity can influence the pathology of liver diseases.

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE (2021)

Review Pharmacology & Pharmacy

Therapy for Nonalcoholic Fatty Liver Disease: Current Options and Future Directions

Patrick Campbell et al.

Summary: NAFLD, a highly prevalent chronic liver disease driven by metabolic syndrome, currently relies on risk factor control and lifestyle changes for weight loss. Due to difficulty in sustained weight loss for many patients, there is a critical need for pharmacotherapy to treat NAFLD, especially NASH, to prevent cirrhosis.

CLINICAL THERAPEUTICS (2021)

Article Gastroenterology & Hepatology

Lanifibranor and NASH resolution

Eleni Kotsiliti

Nature Reviews Gastroenterology & Hepatology (2021)

Article Medicine, General & Internal

A Randomized, Controlled Trial of the Pan-PPAR Agonist Lanifibranor in NASH

Sven M. Francque et al.

Summary: In a randomized trial, the pan-PPAR agonist Lanifibranor showed significant improvement in histologic features of NASH at a dose of 1200 mg. However, adverse events such as weight gain, anemia, peripheral edema, diarrhea, and nausea were more common with Lanifibranor compared to placebo.

NEW ENGLAND JOURNAL OF MEDICINE (2021)

Review Endocrinology & Metabolism

DPP4 Activity, Hyperinsulinemia, and Atherosclerosis

Kaitlin M. Love et al.

Summary: The relationship between hyperinsulinemia, DPP4 activity, and diseases like atherosclerosis has been studied, but the exact mechanisms remain unclear. While some research suggests that DPP4 inhibitors may be beneficial in improving cardiovascular outcomes, their effectiveness in clinical settings is still not fully confirmed.

JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM (2021)

Review Endocrinology & Metabolism

PPARgamma in Metabolism, Immunity, and Cancer: Unified and Diverse Mechanisms of Action

Miguel Hernandez-Quiles et al.

Summary: PPARγ, a member of the nuclear receptor superfamily, plays crucial roles in adipocyte differentiation, immune system cells maturation, and cell proliferation in various tissues. Dysregulation of PPARγ signaling is associated with tumor development, and understanding its molecular mechanism may help develop novel therapeutic strategies for obesity, diabetes, and cancer.

FRONTIERS IN ENDOCRINOLOGY (2021)

Article Chemistry, Medicinal

Development and in vitro Profiling of Dual FXR/LTA4H Modulators

Simone Schierle et al.

Summary: Designed polypharmacology is an attractive strategy to increase therapeutic efficacy in multi-factorial diseases by targeting multiple involved targets with a single molecule. Activation of FXRa and inhibition of LTA4Hi show promise in counteracting NASH, and dual FXR/LTA4H modulators have been developed as pharmacological tools for further evaluation.

CHEMMEDCHEM (2021)

Review Pharmacology & Pharmacy

The identification of farnesoid X receptor modulators as treatment options for nonalcoholic fatty liver disease

Stefano Fiorucci et al.

Summary: FXR agonists show potential in treating nonalcoholic fatty liver disease, but side effects such as elevated cholesterol levels and pruritus are common. Studies are underway to evaluate the benefits and safety of combination therapies.

EXPERT OPINION ON DRUG DISCOVERY (2021)

Review Biochemistry & Molecular Biology

Bile acids and their receptors in metabolic disorders

Stefano Fiorucci et al.

Summary: Bile acids play a crucial role in regulating metabolic processes by integrating their signaling with other receptors in a time-ordered manner synchronized by circadian rhythm. The last decade has seen challenges in developing systemic FXR agonists, with the emergence of intestinal-restricted and dual FXR/GPBAR1 agonists as potential alternatives.

PROGRESS IN LIPID RESEARCH (2021)

Article Chemistry, Medicinal

Second-Generation Dual FXR/sEH Modulators with Optimized Pharmacokinetics

Moritz Helmstadter et al.

Summary: NASH is a chronic liver disease with no effective pharmacological interventions. Researchers have developed a second-generation drug with improved pharmacokinetic parameters, aiming to enhance therapeutic efficacy for NASH treatment.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Pharmacology & Pharmacy

(E)-7-Ethylidene-lithocholic Acid (7-ELCA) Is a Potent Dual Farnesoid X Receptor (FXR) Antagonist and GPBAR1 Agonist Inhibiting FXR-Induced Gene Expression in Hepatocytes and Stimulating Glucagon-like Peptide-1 Secretion From Enteroendocrine Cells

Alzbeta Stefela et al.

Summary: The study identified 7-ethylidene-lithocholic acid (7-ELCA) as a novel combined FXR antagonist/GPBAR1 agonist, which can regulate glucose, lipid, and energy homeostasis as well as stimulate the production of GLP-1 to improve postprandial glucose utilization. The dual modulation of GPBAR1 and FXR by 7-ELCA may offer a promising approach for the treatment of type II diabetes.

FRONTIERS IN PHARMACOLOGY (2021)

Article Gastroenterology & Hepatology

Meta-analysis and Consolidation of Farnesoid X Receptor Chromatin Immunoprecipitation Sequencing Data Across Different Species and Conditions

Emilian Jungwirth et al.

Summary: The FXR receptor plays an important role in controlling gene regulation in metabolic pathways and is a potential drug target for liver diseases. A meta-analysis of FXR binding data across species revealed modest overlap, with a consolidated murine FXR binding atlas enhancing understanding of FXR signaling capabilities. This could provide a basis for developing new drugs targeting FXR in liver diseases.

HEPATOLOGY COMMUNICATIONS (2021)

Article Gastroenterology & Hepatology

Impact of Obeticholic acid Exposure on Decompensation and Mortality in Primary Biliary Cholangitis and Cirrhosis

Binu V. John et al.

Summary: This study investigated the effects of OCA treatment on hepatic decompensation and liver-related mortality or transplantation in patients with compensated PBC cirrhosis. The results showed that OCA use was associated with an increase in hepatic decompensation risk, but not with liver-related mortality or transplantation. Additional studies are recommended to further explore these findings.

HEPATOLOGY COMMUNICATIONS (2021)

Article Chemistry, Medicinal

Differential Therapeutic Effects of FXR Activation, sEH Inhibition, and Dual FXR/sEH Modulation in NASH in Diet-Induced Obese Mice

Moritz Helmstadter et al.

Summary: The study found that while full FXR activation can provide anti-steatosis effects, it can worsen ballooning degeneration and fibrosis. On the other hand, sEH inhibition and dual FXR/sEH modulation, despite lacking anti-steatosis activity, have anti-inflammatory effects and efficiently counteract hepatic fibrosis.

ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE (2021)

Review Peripheral Vascular Disease

Pemafibrate, a New Selective PPARα Modulator: Drug Concept and Its Clinical Applications for Dyslipidemia and Metabolic Diseases

Shizuya Yamashita et al.

CURRENT ATHEROSCLEROSIS REPORTS (2020)

Article Gastroenterology & Hepatology

Burden of Illness and Economic Model for Patients With Nonalcoholic Steatohepatitis in the United States

Zobair M. Younossi et al.

HEPATOLOGY (2019)

Article Pharmacology & Pharmacy

A dual farnesoid X receptor/soluble epoxide hydrolase modulator treats non-alcoholic steatohepatitis in mice

Md. Abdul Hye Khan et al.

BIOCHEMICAL PHARMACOLOGY (2019)

Article Multidisciplinary Sciences

MRGPRX4 is a G protein-coupled receptor activated by bile acids that may contribute to cholestatic pruritus

James Meixiong et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2019)

Review Endocrinology & Metabolism

Glucagon-like peptide 1 (GLP-1)

T. D. Mueller et al.

MOLECULAR METABOLISM (2019)

Article Multidisciplinary Sciences

Bile acid metabolites control TH17 and Treg cell differentiation

Saiyu Hang et al.

NATURE (2019)

Article Urology & Nephrology

FXR/TGR5 Dual Agonist Prevents Progression of Nephropathy in Diabetes and Obesity

Xiaoxin X. Wang et al.

JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY (2018)

Review Endocrinology & Metabolism

Molecular Actions of PPARα in Lipid Metabolism and Inflammation

Nadia Bougarne et al.

ENDOCRINE REVIEWS (2018)

Article Chemistry, Medicinal

Farnesoid X receptor modulators 2014-present: a patent review

Valentina Sepe et al.

EXPERT OPINION ON THERAPEUTIC PATENTS (2018)

Review Biochemistry & Molecular Biology

Insights into the Role of PPARβ/δ in NAFLD

Jiapeng Chen et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2018)

Article Chemistry, Medicinal

Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology

Simone Schierle et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

Review Biochemistry & Molecular Biology

Mechanisms of NAFLD development and therapeutic strategies

Scott L. Friedman et al.

NATURE MEDICINE (2018)

Review Chemistry, Medicinal

RORγ antagonists and inverse agonists: a patent review

Sarah M. Bronner et al.

EXPERT OPINION ON THERAPEUTIC PATENTS (2017)

Article Chemistry, Medicinal

A Dual Modulator of Farnesoid X Receptor and Soluble Epoxide Hydrolase To Counter Nonalcoholic Steatohepatitis

Jurema Schmidt et al.

JOURNAL OF MEDICINAL CHEMISTRY (2017)

Article Multidisciplinary Sciences

Hyodeoxycholic acid derivatives as liver X receptor α and G-protein-coupled bile acid receptor agonists

Simona De Marino et al.

SCIENTIFIC REPORTS (2017)

Review Biochemistry & Molecular Biology

The role and regulation of the peroxisome proliferator activated receptor alpha in human liver

Sander Kersten et al.

BIOCHIMIE (2017)

Article Biochemistry & Molecular Biology

Activation of Transmembrane Bile Acid Receptor TGR5 Modulates Pancreatic Islet Cells to Promote Glucose Homeostasis

Divya P. Kumar et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2016)

Review Biochemistry & Molecular Biology

Transcriptional control of physiological and pathological processes by the nuclear receptor PPARβ/δ

Nguan Soon Tan et al.

PROGRESS IN LIPID RESEARCH (2016)

Article Biochemistry & Molecular Biology

Anthranilic acid derivatives as nuclear receptor modulators-Development of novel PPAR selective and dual PPAR/FXR ligands

Daniel Merk et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2015)

Article Endocrinology & Metabolism

The LXR inverse agonist SR9238 suppresses fibrosis in a model of non-alcoholic steatohepatitis

Kristine Griffett et al.

MOLECULAR METABOLISM (2015)

Review Endocrinology & Metabolism

Saroglitazar for the treatment of hypertriglyceridemia in patients with type 2 diabetes: current evidence

Aravind Sosale et al.

DIABETES METABOLIC SYNDROME AND OBESITY-TARGETS AND THERAPY (2015)

Article Multidisciplinary Sciences

Inhibition of soluble epoxide hydrolase modulates inflammation and autophagy in obese adipose tissue and liver: Role for omega-3 epoxides

Cristina Lopez-Vicario et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2015)

Article Pharmacology & Pharmacy

The First Approved Agent in the Glitazar's Class: Saroglitazar

Ritesh Agrawal

CURRENT DRUG TARGETS (2014)

Article Chemistry, Medicinal

Design, Synthesis, and Biological Evaluation of Potent Dual Agonists of Nuclear and Membrane Bile Acid Receptors

Claudio D'Amore et al.

JOURNAL OF MEDICINAL CHEMISTRY (2014)

Review Physiology

PHYSIOLOGICAL FUNCTIONS OF PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR β

Jaap G. Neels et al.

PHYSIOLOGICAL REVIEWS (2014)

Article Gastroenterology & Hepatology

Cysteinyl leukotrienes and their receptors: Bridging inflammation and colorectal cancer

Sayeh Savari et al.

WORLD JOURNAL OF GASTROENTEROLOGY (2014)

Article Pharmacology & Pharmacy

Semisynthetic Bile Acid FXR and TGR5 Agonists: Physicochemical Properties, Pharmacokinetics, and Metabolism in the Rat

Aldo Roda et al.

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2014)

Article Biochemistry & Molecular Biology

Identification of GPR99 Protein as a Potential Third Cysteinyl Leukotriene Receptor with a Preference for Leukotriene E4 Ligand

Yoshihide Kanaoka et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2013)

Article Biochemistry & Molecular Biology

Decoding Signaling and Function of the Orphan G Protein-Coupled Receptor GPR17 with a Small-Molecule Agonist

Stephanie Hennen et al.

SCIENCE SIGNALING (2013)

Review Biochemistry & Molecular Biology

Targeting Orphan Nuclear Receptors for Treatment of Metabolic Diseases and Autoimmunity

Thomas P. Burris et al.

CHEMISTRY & BIOLOGY (2012)

Article Endocrinology & Metabolism

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

Janne Prawitt et al.

DIABETES (2011)

Article Chemistry, Medicinal

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

Simona De Marino et al.

JOURNAL OF MEDICINAL CHEMISTRY (2011)

Article Biochemistry & Molecular Biology

Identification of a Physiologically Relevant Endogenous Ligand for PPARα in Liver

Manu V. Chakravarthy et al.

Review Biotechnology & Applied Microbiology

Fatty acid-binding proteins: role in metabolic diseases and potential as drug targets

Masato Furuhashi et al.

NATURE REVIEWS DRUG DISCOVERY (2008)

Article Biochemistry & Molecular Biology

Signaling by the cysteinyl-leukotriene receptor 2 -: Involvement in chemokine gene transcription

Charles Thompson et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2008)

Article Biochemistry & Molecular Biology

T0901317 is a potent PXR ligand: Implications for the biology ascribed to LXR

Nico Mitro et al.

FEBS LETTERS (2007)

Article Biochemistry & Molecular Biology

20-Carboxy-arachidonic acid is a dual activator of peroxisome proliferator-activated receptors alpha and gamma

Xiang Fang et al.

PROSTAGLANDINS & OTHER LIPID MEDIATORS (2007)

Review Environmental Sciences

Cysteinyl-leukotriene receptors and cellular signals

G. Enrico Rovati et al.

THESCIENTIFICWORLDJOURNAL (2007)

Article Biochemistry & Molecular Biology

Anatomical profiling of nuclear receptor expression reveals a hierarchical transcriptional network

Angie L. Bookout et al.

Article Endocrinology & Metabolism

T0901317 is a dual LXR/FXR agonist

KA Houck et al.

MOLECULAR GENETICS AND METABOLISM (2004)

Article Biochemistry & Molecular Biology

A G protein-coupled receptor responsive to bile acids

Y Kawamata et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2003)

Article Pharmacology & Pharmacy

Selective interaction of bile acids with muscarinic receptors: a case of molecular mimicry

JP Raufman et al.

EUROPEAN JOURNAL OF PHARMACOLOGY (2002)

Article Pharmacology & Pharmacy

Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist

KR Cheng et al.

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2002)

Article Pharmacology & Pharmacy

Deoxycholic acid conjugates are muscarinic cholinergic receptor antagonists

JP Raufman et al.

PHARMACOLOGY (2002)

Article Multidisciplinary Sciences

Vitamin D receptor as an intestinal bile acid sensor

M Makishima et al.

SCIENCE (2002)

Article Pharmacology & Pharmacy

Dual inhibitors of cyclooxygenase and 5-lipoxygenase. A new avenue in anti-inflammatory therapy?

S Fiorucci et al.

BIOCHEMICAL PHARMACOLOGY (2001)

Article Multidisciplinary Sciences

The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity

JL Staudinger et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2001)