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Title: Isoform-specific inhibition of FGFR signaling achieved by a de-novo-designed mini-protein

Journal Article · · Cell Reports

Research Organization:
Argonne National Laboratory (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
DOE - Office Of Science; NCI; National Institutes of Health (NIH)
OSTI ID:
1902361
Journal Information:
Cell Reports, Vol. 41, Issue (4)
Country of Publication:
United States
Language:
ENGLISH

References (50)

PHENIX: a comprehensive Python-based system for macromolecular structure solution journal January 2010
Towards automated crystallographic structure refinement with phenix.refine journal March 2012
Plasticity in Interactions of Fibroblast Growth Factor 1 (FGF1) N Terminus with FGF Receptors Underlies Promiscuity of FGF1 journal November 2011
Design of protein-binding proteins from the target structure alone journal March 2022
α-Klotho is a non-enzymatic molecular scaffold for FGF23 hormone signalling journal January 2018
MolProbity : all-atom structure validation for macromolecular crystallography journal December 2009
Heparan Sulfate-Dependent Signaling of Fibroblast Growth Factor 18 by Chondrocyte-Derived Perlecan journal June 2010
Receptor subtype discrimination using extensive shape complementary designed interfaces journal May 2019
Targeting FGF19 inhibits tumor growth in colon cancer xenograft and FGF19 transgenic hepatocellular carcinoma models journal June 2007
Features and development of Coot journal March 2010
Cellular signaling by fibroblast growth factor receptors journal April 2005
Targeting FGFR4 Inhibits Hepatocellular Carcinoma in Preclinical Mouse Models journal May 2012
First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway journal March 2015
Acquired On-Target Clinical Resistance Validates FGFR4 as a Driver of Hepatocellular Carcinoma journal December 2019
Structural basis for fibroblast growth factor receptor 2 activation in Apert syndrome journal June 2001
Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis journal October 2005
H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma journal December 2017
XDS journal January 2010
First-in-Human Phase I Study of Fisogatinib (BLU-554) Validates Aberrant FGF19 Signaling as a Driver Event in Hepatocellular Carcinoma journal October 2019
Roles of FGF19 in Liver Metabolism journal January 2011
NMR structure of the first Ig module of mouse FGFR1 journal June 2006
Inference of Macromolecular Assemblies from Crystalline State journal September 2007
Tissue-specific Expression of βKlotho and Fibroblast Growth Factor (FGF) Receptor Isoforms Determines Metabolic Activity of FGF19 and FGF21 journal July 2007
Structures of ligand-occupied β-Klotho complexes reveal a molecular mechanism underlying endocrine FGF specificity and activity journal April 2019
Shape Complementarity at Protein/Protein Interfaces journal December 1993
Structures of β-klotho reveal a ‘zip code’-like mechanism for endocrine FGF signalling journal January 2018
Cell Signaling by Receptor Tyrosine Kinases journal June 2010
FGF19 and Cancer book January 2012
Heparin/Heparan Sulfate Domains in Binding and Signaling of Fibroblast Growth Factor 8b journal September 2002
Lenvatinib inhibits angiogenesis and tumor fibroblast growth factor signaling pathways in human hepatocellular carcinoma models journal May 2018
Phaser crystallographic software journal July 2007
A Mouse Model of Hepatocellular Carcinoma journal June 2002
Insights into the molecular basis for fibroblast growth factor receptor autoinhibition and ligand-binding promiscuity journal January 2004
Structural basis by which alternative splicing modulates the organizer activity of FGF8 in the brain journal January 2006
The Fibroblast Growth Factor signaling pathway journal March 2015
Ligand specificity and heparin dependence of fibroblast growth factor receptors 1 and 3. journal August 1992
Receptor Specificity of the Fibroblast Growth Factor Family journal June 1996
[20] Processing of X-ray diffraction data collected in oscillation mode book January 1997
Crystal Structures of Two FGF-FGFR Complexes Reveal the Determinants of Ligand-Receptor Specificity journal May 2000
Structural Basis for FGF Receptor Dimerization and Activation journal September 1999
Antibody-based targeting of FGFR3 in bladder carcinoma and t(4;14)-positive multiple myeloma in mice journal May 2009
Identification of a Therapeutic Strategy Targeting Amplified FGF19 in Liver Cancer by Oncogenomic Screening journal March 2011
Cell Signaling by Receptor Tyrosine Kinases journal October 2000
Crystal Structure of a Ternary FGF-FGFR-Heparin Complex Reveals a Dual Role for Heparin in FGFR Binding and Dimerization journal September 2000
Indirect recruitment of the signalling adaptor Shc to the fibroblast growth factor receptor 2 (FGFR2) journal November 2008
Heparin-induced oligomerization of FGF molecules is responsible for FGF receptor dimerization, activation, and cell proliferation journal December 1994
FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer journal August 2019
Co-receptor Requirements for Fibroblast Growth Factor-19 Signaling journal October 2007
Novel Recognition Motif on Fibroblast Growth Factor Receptor Mediates Direct Association and Activation of SNT Adapter Proteins journal July 1998
Receptor Specificity of the Fibroblast Growth Factor Family: THE COMPLETE MAMMALIAN FGF FAMILY journal April 2006