DARK AND BRIGHT SIDE OF TARGETING THE FIBROBLAST GROWTH FACTOR RECEPTOR 4 IN THE LIVER

Global cancer statistics 2020: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries

(2021) Hyuna Sung et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Association Between Fibrosis Stage and Outcomes of Patients with Non-Alcoholic Fatty Liver Disease: a Systematic Review and Meta-Analysis

(2020) Rod S. Taylor et al.   GASTROENTEROLOGY

Nonalcoholic Steatohepatitis

(2020) Adam C. Sheka et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Efficacy and Safety of Aldafermin, an Engineered FGF19 Analog, in a Randomized, Double-Blind, Placebo-Controlled Trial of Patients With Nonalcoholic Steatohepatitis

(2020) Stephen A. Harrison et al.   GASTROENTEROLOGY

Fibroblast Growth Factor Receptor 4 Targeting in Cancer: New Insights into Mechanisms and Therapeutic Strategies

(2019) Liwei Lang et al.   Cells

Erdafitinib: First Global Approval

(2019) Anthony Markham   DRUGS

FGF19–FGFR4 Signaling in Hepatocellular Carcinoma

(2019) Aroosha Raja et al.   Cells

FGF401, a first-in-class highly selective and potent FGFR4 inhibitor for the treatment of FGF19-driven hepatocellular cancer

(2019) Andreas Weiss et al.   MOLECULAR CANCER THERAPEUTICS

First-in-Human Phase I Study of Fisogatinib (BLU-554) Validates Aberrant Fibroblast Growth Factor 19 Signaling as a Driver Event in Hepatocellular Carcinoma

(2019) Richard D Kim et al.   Cancer Discovery

Expression of FGFR1–4 in Malignant Pleural Mesothelioma Tissue and Corresponding Cell Lines and its Relationship to Patient Survival and FGFR Inhibitor Sensitivity

(2019) Gregor Vlacic et al.   Cells

Bile acids, FGF15/19 and liver regeneration: From mechanisms to clinical applications

(2018) Gloria Alvarez-Sola et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

Fibroblast growth factor 15 deficiency increases susceptibility but does not improve repair to acetaminophen-induced liver injury in mice

(2018) Mingxing Huang et al.   DIGESTIVE AND LIVER DISEASE

Expression of Fibroblast Growth Factor 21 and β-Klotho Regulates Hepatic Fibrosis through the Nuclear Factor-κB and c-Jun N-Terminal Kinase Pathways

(2018) Kyong Joo Lee et al.   Gut and Liver

Lenvatinib versus sorafenib in first-line treatment of patients with unresectable hepatocellular carcinoma: a randomised phase 3 non-inferiority trial

(2018) Masatoshi Kudo et al.   LANCET

NGM282 for treatment of non-alcoholic steatohepatitis: a multicentre, randomised, double-blind, placebo-controlled, phase 2 trial

(2018) Stephen A Harrison et al.   LANCET

Differential receptor selectivity of the FGF15/FGF19 orthologues determines distinct metabolic activities in db/db mice

(2018) Ann Maria K. Hansen et al.   BIOCHEMICAL JOURNAL

Global Perspectives on Non-alcoholic Fatty Liver Disease and Non-alcoholic Steatohepatitis

(2018) Zobair Younossi et al.   HEPATOLOGY

Epidemiology and Management of Hepatocellular Carcinoma

(2018) Laura Kulik et al.   GASTROENTEROLOGY

Infigratinib mediates vascular normalization, impairs metastasis and improves chemotherapy in hepatocellular carcinoma

(2018) Hung Huynh et al.   HEPATOLOGY

Rosuvastatin improves the FGF19 analogue NGM282-associated lipid changes in patients with non-alcoholic steatohepatitis

(2018) Mary E. Rinella et al.   JOURNAL OF HEPATOLOGY

Effect of NGM282, an FGF19 analogue, in primary sclerosing cholangitis: A multicenter, randomized, double-blind, placebo-controlled phase II trial

(2018) Gideon M. Hirschfield et al.   JOURNAL OF HEPATOLOGY

Fibroblast growth factor receptors as treatment targets in clinical oncology

(2018) Masaru Katoh   Nature Reviews Clinical Oncology

Carcinogenesis on the background of liver fibrosis: Implications for the management of hepatocellular cancer

(2018) Joanne Marie O’Rourke et al.   WORLD JOURNAL OF GASTROENTEROLOGY

Suppression of Hepatic Bile Acid Synthesis by a non-tumorigenic FGF19 analogue Protects Mice from Fibrosis and Hepatocarcinogenesis

(2018) Raffaella Maria Gadaleta et al.   Scientific Reports

Liver Cancer Cell of Origin, Molecular Class, and Effects on Patient Prognosis

(2017) Daniela Sia et al.   GASTROENTEROLOGY

Suppressed hepatic bile acid signalling despite elevated production of primary and secondary bile acids in NAFLD

(2017) Na Jiao et al.   GUT

Modeling the epidemic of nonalcoholic fatty liver disease demonstrates an exponential increase in burden of disease

(2017) Chris Estes et al.   HEPATOLOGY

Increased risk of mortality by fibrosis stage in nonalcoholic fatty liver disease: Systematic review and meta-analysis

(2017) Parambir S. Dulai et al.   HEPATOLOGY

Safety, tolerability and pharmacokinetics of the fibroblast growth factor receptor inhibitor AZD4547 in Japanese patients with advanced solid tumours: a Phase I study

(2017) Hideo Saka et al.   INVESTIGATIONAL NEW DRUGS

Safety, pharmacokinetic, and pharmacodynamics of erdafitinib, a pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor, in patients with advanced or refractory solid tumors

(2017) Tomohiro Nishina et al.   INVESTIGATIONAL NEW DRUGS

Mouse species-specific control of hepatocarcinogenesis and metabolism by FGF19/FGF15

(2017) Mei Zhou et al.   JOURNAL OF HEPATOLOGY

Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors

(2017) Ken A. Brameld et al.   JOURNAL OF MEDICINAL CHEMISTRY

Regorafenib for patients with hepatocellular carcinoma who progressed on sorafenib treatment (RESORCE): a randomised, double-blind, placebo-controlled, phase 3 trial

(2017) Jordi Bruix et al.   LANCET

Fibroblast growth factors (FGFs) in cancer: FGF traps as a new therapeutic approach

(2017) Marco Presta et al.   PHARMACOLOGY & THERAPEUTICS

Quantitative liver proteomics identifies FGF19 targets that couple metabolism and proliferation

(2017) Vittoria Massafra et al.   PLoS One

A Phase 1 Study of LY2874455, an Oral Selective pan-FGFR Inhibitor, in Patients with Advanced Cancer

(2017) Michael Michael et al.   Targeted Oncology

Mitogen-Activated Protein Kinase Regulation in Hepatic Metabolism

(2017) Ahmed Lawan et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Engineered fibroblast growth factor 19 protects from acetaminophen-induced liver injury and stimulates aged liver regeneration in mice

(2017) Gloria Alvarez-Sola et al.   Cell Death & Disease

Non-cell-autonomous activation of IL-6/STAT3 signaling mediates FGF19-driven hepatocarcinogenesis

(2017) Mei Zhou et al.   Nature Communications

Implications of FGF19 on sorafenib-mediated nitric oxide production in hepatocellular carcinoma cells - a short report

(2017) Lixia Gao et al.   CELLULAR ONCOLOGY

FGF19 genetic amplification as a potential therapeutic target in lung squamous cell carcinomas

(2017) Xiaochen Zhang et al.   Thoracic Cancer

Long-term Administration of Nuclear Bile Acid Receptor FXR Agonist Prevents Spontaneous Hepatocarcinogenesis in Abcb4−/− Mice

(2017) Marica Cariello et al.   Scientific Reports

Bile acids and nonalcoholic fatty liver disease: Molecular insights and therapeutic perspectives

(2016) Juan P. Arab et al.   HEPATOLOGY

FGFR inhibitors: Effects on cancer cells, tumor microenvironment and whole-body homeostasis (Review)

(2016) MASARU KATOH   INTERNATIONAL JOURNAL OF MOLECULAR MEDICINE

Whole-genome DNA methylation and hydroxymethylation profiling for HBV-related hepatocellular carcinoma

(2016) Chao Ye et al.   INTERNATIONAL JOURNAL OF ONCOLOGY

Postprandial Plasma Concentrations of Individual Bile Acids and FGF-19 in Patients With Type 2 Diabetes

(2016) David P. Sonne et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

ASP5878, a Novel Inhibitor of FGFR1, 2, 3, and 4, Inhibits the Growth of FGF19-Expressing Hepatocellular Carcinoma

(2016) Takashi Futami et al.   MOLECULAR CANCER THERAPEUTICS

FXR Primes the Liver for Intestinal FGF15 Signaling by Transient Induction of β-Klotho

(2016) Ting Fu et al.   MOLECULAR ENDOCRINOLOGY

Increased FGF19 copy number is frequently detected in hepatocellular carcinoma with a complete response after sorafenib treatment

(2016) Masaki Kaibori et al.   Oncotarget

Fibroblast growth factor receptor 4 (FGFR4) and fibroblast growth factor 19 (FGF19) autocrine enhance breast cancer cells survival

(2016) Kai Hung Tiong et al.   Oncotarget

Targeting FGFR Signaling in Cancer

(2015) M. Touat et al.   CLINICAL CANCER RESEARCH

The FGFR Landscape in Cancer: Analysis of 4,853 Tumors by Next-Generation Sequencing

(2015) T. Helsten et al.   CLINICAL CANCER RESEARCH

Fibroblast Growth Factor Signaling Controls Liver Size in Mice With Humanized Livers

(2015) Willscott E. Naugler et al.   GASTROENTEROLOGY

Engineered fibroblast growth factor 19 reduces liver injury and resolves sclerosing cholangitis in Mdr2 -deficient mice

(2015) Mei Zhou et al.   HEPATOLOGY

Targeting cancer with kinase inhibitors

(2015) Stefan Gross et al.   JOURNAL OF CLINICAL INVESTIGATION

Stress kinases in the modulation of metabolism and energy balance

(2015) Elisa Manieri et al.   JOURNAL OF MOLECULAR ENDOCRINOLOGY

Quantitative Proteomic Verification of Membrane Proteins as Potential Therapeutic Targets Located in the 11q13 Amplicon in Cancers

(2015) Heather Hoover et al.   JOURNAL OF PROTEOME RESEARCH

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

Exome sequencing of hepatocellular carcinomas identifies new mutational signatures and potential therapeutic targets

(2015) Kornelius Schulze et al.   NATURE GENETICS

FGFR4 Is a Potential Predictive Biomarker in Oral and Oropharyngeal Squamous Cell Carcinoma

(2015) Koos Koole et al.   PATHOBIOLOGY

Paralog-Specific Kinase Inhibition of FGFR4: Adding to the Arsenal of Anti-FGFR Agents

(2015) L. M. Packer et al.   Cancer Discovery

First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway

(2015) M. Hagel et al.   Cancer Discovery

FGF19 promotes epithelial-mesenchymal transition in hepatocellular carcinoma cells by modulating the GSK3β/β- catenin signaling cascade via FGFR4 activation

(2015) Huakan Zhao et al.   Oncotarget

Fibroblast growth factor 15 deficiency impairs liver regeneration in mice

(2014) Bo Kong et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

Separating Tumorigenicity from Bile Acid Regulatory Activity for Endocrine Hormone FGF19

(2014) M. Zhou et al.   CANCER RESEARCH

Cytoplasmic Tyrosine Phosphatase Shp2 Coordinates Hepatic Regulation of Bile Acid and FGF15/19 Signaling to Repress Bile Acid Synthesis

(2014) Shuangwei Li et al.   Cell Metabolism

Hepatocyte FRS2α is Essential for the Endocrine Fibroblast Growth Factor to Limit the Amplitude of Bile Acid Production Induced by Prandial Activity

(2014) C. Wang et al.   CURRENT MOLECULAR MEDICINE

Genomic portrait of resectable hepatocellular carcinomas: Implications ofRB1andFGF19aberrations for patient stratification

(2014) Sung-Min Ahn et al.   HEPATOLOGY

Prevention of spontaneous hepatocarcinogenesis in farnesoid X receptor-null mice by intestinal-specific farnesoid X receptor reactivation

(2014) Chiara Degirolamo et al.   HEPATOLOGY

Opposite alterations in FGF21 and FGF19 levels and disturbed expression of the receptor machinery for endocrine FGFs in obese patients

(2014) J M Gallego-Escuredo et al.   INTERNATIONAL JOURNAL OF OBESITY

Targeted inhibition of the FGF19-FGFR4 pathway in hepatocellular carcinoma; translational safety considerations

(2014) Howard R. Mellor   LIVER INTERNATIONAL

Proteogenomic characterization of human colon and rectal cancer

(2014) Bing Zhang et al.   NATURE

A nontumorigenic variant of FGF19 treats cholestatic liver diseases

(2014) J. Luo et al.   Science Translational Medicine

Upregulation of hepatic bile acid synthesis via fibroblast growth factor 19 is defective in gallstone disease but functional in overweight individuals

(2014) Olga Renner et al.   United European Gastroenterology Journal

A Role for Fibroblast Growth Factor 19 and Bile Acids in Diabetes Remission After Roux-en-Y Gastric Bypass

(2013) G. S. Gerhard et al.   DIABETES CARE

Expression of Fibroblast Growth Factor 19 Is Associated with Recurrence and Poor Prognosis of Hepatocellular Carcinoma

(2013) Jiyeon Hyeon et al.   DIGESTIVE DISEASES AND SCIENCES

Identification of fibroblast growth factor 15 as a novel mediator of liver regeneration and its application in the prevention of post-resection liver failure in mice

(2013) Iker Uriarte et al.   GUT

Genomic landscape of copy number aberrations enables the identification of oncogenic drivers in hepatocellular carcinoma

(2013) Kai Wang et al.   HEPATOLOGY

Exploring mechanisms of FGF signalling through the lens of structural biology

(2013) Regina Goetz et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Fibroblast growth factor 19 expression correlates with tumor progression and poorer prognosis of hepatocellular carcinoma

(2012) Seiki Miura et al.   BMC CANCER

Preliminary evidence of a reduced serum level of fibroblast growth factor 19 in patients with biopsy-proven nonalcoholic fatty liver disease

(2012) Fatih Eren et al.   CLINICAL BIOCHEMISTRY

Mechanism of tissue-specific farnesoid X receptor in suppressing the expression of genes in bile-acid synthesis in mice

(2012) Bo Kong et al.   HEPATOLOGY

Promotion of liver regeneration/repair by farnesoid X receptor in both liver and intestine in mice

(2012) Lisheng Zhang et al.   HEPATOLOGY

Nuclear Receptors HNF4α and LRH-1 Cooperate in RegulatingCyp7a1 in Vivo

(2012) Serkan Kir et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeting FGFR4 Inhibits Hepatocellular Carcinoma in Preclinical Mouse Models

(2012) Dorothy M. French et al.   PLoS One

Regulation of Amphiregulin Gene Expression by β-Catenin Signaling in Human Hepatocellular Carcinoma Cells: A Novel Crosstalk between FGF19 and the EGFR System

(2012) Maria U. Latasa et al.   PLoS One

Antibody-Mediated Inhibition of Fibroblast Growth Factor 19 Results in Increased Bile Acids Synthesis and Ileal Malabsorption of Bile Acids in Cynomolgus Monkeys

(2012) Rama Pai et al.   TOXICOLOGICAL SCIENCES

FGFR Genetic Alterations Predict for Sensitivity to NVP-BGJ398, a Selective Pan-FGFR Inhibitor

(2012) V. Guagnano et al.   Cancer Discovery

Antiviral therapy for prevention of hepatocellular carcinoma in chronic hepatitis C: systematic review and meta-analysis of randomised controlled trials

(2012) Nina Kimer et al.   BMJ Open

Emerging Signaling Pathways in Hepatocellular Carcinoma

(2012) Agrin Moeini et al.   Liver Cancer

Identification of a Therapeutic Strategy Targeting Amplified FGF19 in Liver Cancer by Oncogenomic Screening

(2011) Eric T. Sawey et al.   CANCER CELL

FGF15/19 Regulates Hepatic Glucose Metabolism by Inhibiting the CREB-PGC-1α Pathway

(2011) Matthew J. Potthoff et al.   Cell Metabolism

Selective Activation of Nuclear Bile Acid Receptor FXR in the Intestine Protects Mice Against Cholestasis

(2011) Salvatore Modica et al.   GASTROENTEROLOGY

Interleukin-22 promotes human hepatocellular carcinoma by activation of STAT3

(2011) Runqiu Jiang et al.   HEPATOLOGY

Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase

(2011) Vito Guagnano et al.   JOURNAL OF MEDICINAL CHEMISTRY

FGF19 as a Postprandial, Insulin-Independent Activator of Hepatic Protein and Glycogen Synthesis

(2011) S. Kir et al.   SCIENCE

Hepatocyte IKKβ/NF-κB Inhibits Tumor Promotion and Progression by Preventing Oxidative Stress-Driven STAT3 Activation

(2010) Guobin He et al.   CANCER CELL

NF-κB and STAT3 – key players in liver inflammation and cancer

(2010) Guobin He et al.   CELL RESEARCH

Research Resource: Comprehensive Expression Atlas of the Fibroblast Growth Factor System in Adult Mouse

(2010) Klementina Fon Tacer et al.   MOLECULAR ENDOCRINOLOGY

Relevant use of Klotho in FGF19 subfamily signaling system in vivo

(2010) K.-i. Tomiyama et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Hepatocellular carcinoma in non-cirrhotic liver: A reappraisal

(2009) Franco Trevisani et al.   DIGESTIVE AND LIVER DISEASE

FGF15/FGFR4 Integrates Growth Factor Signaling with Hepatic Bile Acid Metabolism and Insulin Action

(2009) Dong-Ju Shin et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Decreased Incidence of Hepatocellular Carcinoma in Hepatitis B Vaccinees: A 20-Year Follow-up Study

(2009) Mei-Hwei Chang et al.   JNCI-Journal of the National Cancer Institute

The FGF family: biology, pathophysiology and therapy

(2009) Andrew Beenken et al.   NATURE REVIEWS DRUG DISCOVERY

Fibroblast growth factor receptor 4 regulates proliferation, anti-apoptosis and alpha-fetoprotein secretion during hepatocellular carcinoma progression and represents a potential target for therapeutic intervention

(2008) Han Kiat Ho et al.   JOURNAL OF HEPATOLOGY

Liver Receptor Homolog-1 Regulates Bile Acid Homeostasis but Is Not Essential for Feedback Regulation of Bile Acid Synthesis

(2008) Youn-Kyoung Lee et al.   MOLECULAR ENDOCRINOLOGY

Sorafenib in Advanced Hepatocellular Carcinoma

(2008) Josep M. Llovet et al.   NEW ENGLAND JOURNAL OF MEDICINE

Fibroblast growth factor‐19: Development, analytical characterization and clinical evaluation of a new ELISA test

(2008) D. Stejskal et al.   SCANDINAVIAN JOURNAL OF CLINICAL & LABORATORY INVESTIGATION