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Title: An S116R Phosphorylation Site Mutation in Human Fibroblast Growth Factor-1 Differentially Affects Mitogenic and Glucose-Lowering Activities

Authors:
; ; ; ; ; ; ; ; ; ; ; ;
Publication Date:
Sponsoring Org.:
USDOE Office of Science (SC), Basic Energy Sciences (BES)
OSTI Identifier:
1396844
Grant/Contract Number:  
W-31-109-Eng-38
Resource Type:
Publisher's Accepted Manuscript
Journal Name:
Journal of Pharmaceutical Sciences
Additional Journal Information:
Journal Name: Journal of Pharmaceutical Sciences Journal Volume: 105 Journal Issue: 12; Journal ID: ISSN 0022-3549
Publisher:
Elsevier
Country of Publication:
United States
Language:
English

Citation Formats

Xia, Xue, Kumru, Ozan S., Blaber, Sachiko I., Middaugh, C. Russell, Li, Ling, Ornitz, David M., Suh, Jae Myoung, Atkins, Annette R., Downes, Michael, Evans, Ronald M., Tenorio, Connie A., Bienkiewicz, Ewa, and Blaber, Michael. An S116R Phosphorylation Site Mutation in Human Fibroblast Growth Factor-1 Differentially Affects Mitogenic and Glucose-Lowering Activities. United States: N. p., 2016. Web. doi:10.1016/j.xphs.2016.09.005.
Xia, Xue, Kumru, Ozan S., Blaber, Sachiko I., Middaugh, C. Russell, Li, Ling, Ornitz, David M., Suh, Jae Myoung, Atkins, Annette R., Downes, Michael, Evans, Ronald M., Tenorio, Connie A., Bienkiewicz, Ewa, & Blaber, Michael. An S116R Phosphorylation Site Mutation in Human Fibroblast Growth Factor-1 Differentially Affects Mitogenic and Glucose-Lowering Activities. United States. https://doi.org/10.1016/j.xphs.2016.09.005
Xia, Xue, Kumru, Ozan S., Blaber, Sachiko I., Middaugh, C. Russell, Li, Ling, Ornitz, David M., Suh, Jae Myoung, Atkins, Annette R., Downes, Michael, Evans, Ronald M., Tenorio, Connie A., Bienkiewicz, Ewa, and Blaber, Michael. Thu . "An S116R Phosphorylation Site Mutation in Human Fibroblast Growth Factor-1 Differentially Affects Mitogenic and Glucose-Lowering Activities". United States. https://doi.org/10.1016/j.xphs.2016.09.005.
@article{osti_1396844,
title = {An S116R Phosphorylation Site Mutation in Human Fibroblast Growth Factor-1 Differentially Affects Mitogenic and Glucose-Lowering Activities},
author = {Xia, Xue and Kumru, Ozan S. and Blaber, Sachiko I. and Middaugh, C. Russell and Li, Ling and Ornitz, David M. and Suh, Jae Myoung and Atkins, Annette R. and Downes, Michael and Evans, Ronald M. and Tenorio, Connie A. and Bienkiewicz, Ewa and Blaber, Michael},
abstractNote = {},
doi = {10.1016/j.xphs.2016.09.005},
journal = {Journal of Pharmaceutical Sciences},
number = 12,
volume = 105,
place = {United States},
year = {Thu Dec 01 00:00:00 EST 2016},
month = {Thu Dec 01 00:00:00 EST 2016}
}

Journal Article:
Free Publicly Available Full Text
Publisher's Version of Record
https://doi.org/10.1016/j.xphs.2016.09.005

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Works referenced in this record:

Endocrine FGFs and Klothos: emerging concepts
journal, September 2008


Structural Basis for FGF Receptor Dimerization and Activation
journal, September 1999


Iterative model building, structure refinement and density modification with the PHENIX AutoBuild wizard
journal, December 2007

  • Terwilliger, Thomas C.; Grosse-Kunstleve, Ralf W.; Afonine, Pavel V.
  • Acta Crystallographica Section D Biological Crystallography, Vol. 64, Issue 1
  • DOI: 10.1107/S090744490705024X

FGF1 C-terminal domain and phosphorylation regulate intracrine FGF1 signaling for its neurotrophic and anti-apoptotic activities
journal, February 2016


Different abilities of the four FGFRs to mediate FGF-1 translocation are linked to differences in the receptor C-terminal tail
journal, October 2006

  • Sorensen, V.; Wiedlocha, A.; Haugsten, E. M.
  • Journal of Cell Science, Vol. 119, Issue 20
  • DOI: 10.1242/jcs.03209

Effects of Solutes on Empirical Phase Diagrams of Human Fibroblast Growth Factor 1
journal, June 2007

  • Fan, Haihong; Li, Huaina; Zhang, Mingyu
  • Journal of Pharmaceutical Sciences, Vol. 96, Issue 6
  • DOI: 10.1002/jps.20796

The complete amino acid sequence of human brain-derived acidic fibroblast growth factor
journal, July 1986

  • Gimenez-Gallego, Guillermo; Conn, Greg; Hatcher, Victor B.
  • Biochemical and Biophysical Research Communications, Vol. 138, Issue 2
  • DOI: 10.1016/S0006-291X(86)80540-X

Genome-Wide Gene Expression Analysis of NIH 3T3 Cell Line Under Mechanical Stimulation
journal, November 2010

  • Kurulgan Demirci, E.; Demirci, T.; Trzewik, J.
  • Cellular and Molecular Bioengineering, Vol. 4, Issue 1
  • DOI: 10.1007/s12195-010-0149-4

Alternative type I and I′ turn conformations in the β8/β9 β-hairpin of human acidic fibroblast growth factor
journal, March 2002

  • Kim, Jaewon; Blaber, Sachiko I.; Blaber, Michael
  • Protein Science, Vol. 11, Issue 3
  • DOI: 10.1110/ps.43802

Receptor Specificity of the Fibroblast Growth Factor Family: THE COMPLETE MAMMALIAN FGF FAMILY
journal, April 2006

  • Zhang, Xiuqin; Ibrahimi, Omar A.; Olsen, Shaun K.
  • Journal of Biological Chemistry, Vol. 281, Issue 23
  • DOI: 10.1074/jbc.M601252200

Phosphorylation-regulated Nucleocytoplasmic Trafficking of Internalized Fibroblast Growth Factor-1
journal, February 2005

  • Więdłocha, Antoni; Nilsen, Trine; Wesche, Jørgen
  • Molecular Biology of the Cell, Vol. 16, Issue 2
  • DOI: 10.1091/mbc.e04-05-0389

Unliganded Fibroblast Growth Factor Receptor 1 Forms Density-independent Dimers
journal, October 2015

  • Comps-Agrar, Laëtitia; Dunshee, Diana Ronai; Eaton, Dan L.
  • Journal of Biological Chemistry, Vol. 290, Issue 40
  • DOI: 10.1074/jbc.M115.681395

The use of fluorescence methods to monitor unfolding transitions in proteins
journal, February 1994


Receptor Specificity of the Fibroblast Growth Factor Family
journal, June 1996

  • Ornitz, David M.; Xu, Jingsong; Colvin, Jennifer S.
  • Journal of Biological Chemistry, Vol. 271, Issue 25
  • DOI: 10.1074/jbc.271.25.15292

Quantitative export of FGF-2 occurs through an alternative, energy-dependent, non-ER/Golgi pathway
journal, March 1995

  • Florkiewicz, Robert Z.; Majack, Richard A.; Buechler, Robbie D.
  • Journal of Cellular Physiology, Vol. 162, Issue 3
  • DOI: 10.1002/jcp.1041620311

Regulation of FGF receptor-2 expression by transcription factor E2F-1
journal, August 2003


The Fibroblast Growth Factor signaling pathway
journal, March 2015

  • Ornitz, David M.; Itoh, Nobuyuki
  • Wiley Interdisciplinary Reviews: Developmental Biology, Vol. 4, Issue 3
  • DOI: 10.1002/wdev.176

Role of the Nuclear Localization Sequence in Fibroblast Growth Factor-1-stimulated Mitogenic Pathways
journal, March 1996

  • Lin, Yao-Zhong; Yao, SongYi; Hawiger, Jacek
  • Journal of Biological Chemistry, Vol. 271, Issue 10
  • DOI: 10.1074/jbc.271.10.5305

Endocrinization of FGF1 produces a neomorphic and potent insulin sensitizer
journal, July 2014

  • Suh, Jae Myoung; Jonker, Johan W.; Ahmadian, Maryam
  • Nature, Vol. 513, Issue 7518
  • DOI: 10.1038/nature13540

Solution NMR structure of a human FGF-1 monomer, activated by a hexasaccharide heparin-analogue: Solution NMR structure of hexasaccharide-FGF-1
journal, September 2006


Receptor Binding and Mitogenic Properties of Mouse Fibroblast Growth Factor 3
journal, October 1995

  • Mathieu, Marc; Chatelain, Eric; Ornitz, David
  • Journal of Biological Chemistry, Vol. 270, Issue 41
  • DOI: 10.1074/jbc.270.41.24197

Spackling the Crack: Stabilizing Human Fibroblast Growth Factor-1 by Targeting the N and C terminus β-Strand Interactions
journal, August 2007

  • Dubey, Vikash Kumar; Lee, Jihun; Somasundaram, Thayumana
  • Journal of Molecular Biology, Vol. 371, Issue 1
  • DOI: 10.1016/j.jmb.2007.05.065

Pharmacokinetic Properties of 2nd-Generation Fibroblast Growth Factor-1 Mutants for Therapeutic Application
journal, November 2012


Fibroblast growth factor receptors have different signaling and mitogenic potentials.
journal, January 1994

  • Wang, J. K.; Gao, G.; Goldfarb, M.
  • Molecular and Cellular Biology, Vol. 14, Issue 1
  • DOI: 10.1128/MCB.14.1.181

Effective treatment of steatosis and steatohepatitis by fibroblast growth factor 1 in mouse models of nonalcoholic fatty liver disease
journal, February 2016

  • Liu, Weilin; Struik, Dicky; Nies, Vera J. M.
  • Proceedings of the National Academy of Sciences, Vol. 113, Issue 8
  • DOI: 10.1073/pnas.1525093113

Transfer of functional EGF receptors to an IL3-dependent cell line
journal, November 1988

  • Collins, Mary K. L.; Downward, Julian; Miyajima, Atsushi
  • Journal of Cellular Physiology, Vol. 137, Issue 2
  • DOI: 10.1002/jcp.1041370212

X-ray Crystal Structure of Human Acidic Fibroblast Growth Factor ,
journal, January 1996

  • Blaber, Michael; DiSalvo, Jerry; Thomas, Kenneth A.
  • Biochemistry, Vol. 35, Issue 7
  • DOI: 10.1021/bi9521755

Divergent Synthesis of 48 Heparan Sulfate-Based Disaccharides and Probing the Specific Sugar–Fibroblast Growth Factor-1 Interaction
journal, December 2012

  • Hu, Yu-Peng; Zhong, Yong-Qing; Chen, Zhi-Geng
  • Journal of the American Chemical Society, Vol. 134, Issue 51
  • DOI: 10.1021/ja3090065

FGF signaling in the developing endochondral skeleton
journal, April 2005


Symmetric Primary and Tertiary Structure Mutations within a Symmetric Superfold: A Solution, not a Constraint, to Achieve a Foldable Polypeptide
journal, November 2004

  • Brych, Stephen R.; Dubey, Vikash K.; Bienkiewicz, Ewa
  • Journal of Molecular Biology, Vol. 344, Issue 3
  • DOI: 10.1016/j.jmb.2004.09.060

Identification of a Key Structural Element for Protein Folding Within β-Hairpin Turns
journal, May 2003


Fibroblast growth factor signalling: from development to cancer
journal, February 2010

  • Turner, Nicholas; Grose, Richard
  • Nature Reviews Cancer, Vol. 10, Issue 2
  • DOI: 10.1038/nrc2780

Inability of the Acidic Fibroblast Growth Factor Mutant K132E to Stimulate DNA Synthesis after Translocation into Cells
journal, May 1998

  • Klingenberg, Olav; Wiedlocha, Antoni; Rapak, Andrzej
  • Journal of Biological Chemistry, Vol. 273, Issue 18
  • DOI: 10.1074/jbc.273.18.11164

Structure of a heparin-linked biologically active dimer of fibroblast growth factor
journal, June 1998

  • DiGabriele, Anna D.; Lax, Irit; Chen, Denise I.
  • Nature, Vol. 393, Issue 6687
  • DOI: 10.1038/31741

FGF1 nuclear translocation is required for both its neurotrophic activity and its p53-dependent apoptosis protection
journal, November 2009

  • Rodriguez-Enfedaque, Aida; Bouleau, Sylvina; Laurent, Maryvonne
  • Biochimica et Biophysica Acta (BBA) - Molecular Cell Research, Vol. 1793, Issue 11
  • DOI: 10.1016/j.bbamcr.2009.09.010

A PPARγ–FGF1 axis is required for adaptive adipose remodelling and metabolic homeostasis
journal, April 2012

  • Jonker, Johan W.; Suh, Jae Myoung; Atkins, Annette R.
  • Nature, Vol. 485, Issue 7398
  • DOI: 10.1038/nature10998

β-Trefoil fold
journal, January 1992


Two Nuclear Localization Signals Required for Transport from the Cytosol to the Nucleus of Externally Added FGF-1 Translocated into Cells
journal, April 2005

  • Wesche, Jørgen; Małecki, Jȩdrzej; Wiȩdłocha, Antoni
  • Biochemistry, Vol. 44, Issue 16
  • DOI: 10.1021/bi047403m

Basic fibroblast growth factor, a protein devoid of secretory signal sequence, is released by cells via a pathway independent of the endoplasmic reticulum-Golgi complex
journal, April 1992

  • Mignatti, Paolo; Morimoto, Takashi; Rifkin, Daniel B.
  • Journal of Cellular Physiology, Vol. 151, Issue 1
  • DOI: 10.1002/jcp.1041510113

Molecular regionalization of the neocortex is disrupted in Fgf8 hypomorphic mutants
journal, May 2003


Heparin is required for cell-free binding of basic fibroblast growth factor to a soluble receptor and for mitogenesis in whole cells.
journal, January 1992

  • Ornitz, D. M.; Yayon, A.; Flanagan, J. G.
  • Molecular and Cellular Biology, Vol. 12, Issue 1
  • DOI: 10.1128/MCB.12.1.240

Mode of action of soybean trypsin inhibitor (Kunitz) as a model for specific protein–protein interactions
journal, May 1974

  • Blow, D. M.; Janin, J.; Sweet, R. M.
  • Nature, Vol. 249, Issue 5452
  • DOI: 10.1038/249054a0

Nucleolin Regulates Phosphorylation and Nuclear Export of Fibroblast Growth Factor 1 (FGF1)
journal, March 2014


Reversible Thermal Denaturation of Human FGF-1 Induced by Low Concentrations of Guanidine Hydrochloride
journal, July 1999


The structure of human acidic fibroblast growth factor and its interaction with heparin
journal, August 1991

  • Copeland, Robert A.; Ji, Hanlee; Halfpenny, Anne J.
  • Archives of Biochemistry and Biophysics, Vol. 289, Issue 1
  • DOI: 10.1016/0003-9861(91)90441-K

An atomic resolution structure for human fibroblast growth factor 1
journal, July 2004

  • Bernett, Matthew J.; Somasundaram, Thayumanasamy; Blaber, Michael
  • Proteins: Structure, Function, and Bioinformatics, Vol. 57, Issue 3
  • DOI: 10.1002/prot.20239

Coot model-building tools for molecular graphics
journal, November 2004

  • Emsley, Paul; Cowtan, Kevin
  • Acta Crystallographica Section D Biological Crystallography, Vol. 60, Issue 12, p. 2126-2132
  • DOI: 10.1107/S0907444904019158

Imaging Tc-99m-labeled FGF-1 targeting in rats
journal, May 2000


Analysis Tool Web Services from the EMBL-EBI
journal, May 2013

  • McWilliam, Hamish; Li, Weizhong; Uludag, Mahmut
  • Nucleic Acids Research, Vol. 41, Issue W1
  • DOI: 10.1093/nar/gkt376

FGF signaling inhibits chondrocyte proliferation and regulates bone development through the STAT-1 pathway
journal, June 1999

  • Sahni, M.; Ambrosetti, D. -C.; Mansukhani, A.
  • Genes & Development, Vol. 13, Issue 11
  • DOI: 10.1101/gad.13.11.1361

Plasticity in Interactions of Fibroblast Growth Factor 1 (FGF1) N Terminus with FGF Receptors Underlies Promiscuity of FGF1
journal, November 2011

  • Beenken, Andrew; Eliseenkova, Anna V.; Ibrahimi, Omar A.
  • Journal of Biological Chemistry, Vol. 287, Issue 5
  • DOI: 10.1074/jbc.M111.275891

Cell surface, heparin-like molecules are required for binding of basic fibroblast growth factor to its high affinity receptor
journal, February 1991


Improved data visualization techniques for analyzing macromolecule structural changes: Techniques for Analyzing Macromolecule Structure
journal, September 2012

  • Kim, Jae Hyun; Iyer, Vidyashankara; Joshi, Sangeeta B.
  • Protein Science, Vol. 21, Issue 10
  • DOI: 10.1002/pro.2144

Distribution of intravenously administered acidic and basic fibroblast growth factors in the mouse
journal, September 1990

  • Hondermarck, H.; Courty, J.; Thomas, D.
  • Experientia, Vol. 46, Issue 9
  • DOI: 10.1007/BF01939392

Structure and stability effects of mutations designed to increase the primary sequence symmetry within the core region of a β-trefoil
journal, December 2001

  • Brych, Stephen R.; Blaber, Sachiko I.; Logan, Timothy M.
  • Protein Science, Vol. 10, Issue 12
  • DOI: 10.1110/ps.ps.34701

Diversification of the Structural Determinants of Fibroblast Growth Factor-Heparin Interactions
journal, November 2012

  • Xu, Ruoyan; Ori, Alessandro; Rudd, Timothy R.
  • Journal of Biological Chemistry, Vol. 287, Issue 47
  • DOI: 10.1074/jbc.M112.398826

Pharmacokinetics and distribution of heparin-binding growth factor I (endothelial cell growth factor) in the rat.
journal, February 1989

  • Rosengart, T. K.; Kuperschmid, J. P.; Maciag, T.
  • Circulation Research, Vol. 64, Issue 2
  • DOI: 10.1161/01.RES.64.2.227

Amelioration of Type 2 Diabetes by Antibody-Mediated Activation of Fibroblast Growth Factor Receptor 1
journal, December 2011


Requirement of heparan sulfate for bFGF-mediated fibroblast growth and myoblast differentiation
journal, June 1991


Paracrine Effects of Phosphorylated and Excreted FGF1 by Retinal Pigmented Epithelial Cells
journal, January 1998

  • Guillonneau, Xavier; Régnier-Ricard, Fabienne; Dupuis, Colette
  • Growth Factors, Vol. 15, Issue 2
  • DOI: 10.3109/08977199809117186

The FGF family: biology, pathophysiology and therapy
journal, March 2009

  • Beenken, Andrew; Mohammadi, Moosa
  • Nature Reviews Drug Discovery, Vol. 8, Issue 3
  • DOI: 10.1038/nrd2792

Acidic Fibroblast Growth Factor Accelerates Dermal Wound Healing
journal, January 1992


Effects of Mutations of a Phosphorylation Site in an Exposed Loop in Acidic Fibroblast Growth Factor
journal, June 1999

  • Klingenberg, Olav; Wi IJdłocha, Antoni; Olsnes, Sjur
  • Journal of Biological Chemistry, Vol. 274, Issue 25
  • DOI: 10.1074/jbc.274.25.18081

Neocortex Patterning by the Secreted Signaling Molecule FGF8
journal, September 2001


Transport of Exogenous Growth Factors and Cytokines to the Cytosol and to the Nucleus
journal, January 2003


Free R value: a novel statistical quantity for assessing the accuracy of crystal structures
journal, January 1992


Three-dimensional structures of acidic and basic fibroblast growth factors
journal, January 1991


Dual mode of signal transduction by externally added acidic fibroblast growth factor
journal, March 1994


Release of basic fibroblast growth factor, an angiogenic factor devoid of secretory signal sequence: A trivial phenomenon or a novel secretion mechanism?
journal, November 1991

  • Mignatti, Paolo; Rifkin, Daniel B.
  • Journal of Cellular Biochemistry, Vol. 47, Issue 3
  • DOI: 10.1002/jcb.240470303

[20] Processing of X-ray diffraction data collected in oscillation mode
book, January 1997


Automated Structure Solution with the PHENIX Suite
book, January 2008


Towards a Resolution of the Stoichiometry of the Fibroblast Growth Factor (FGF)–FGF Receptor–Heparin Complex
journal, June 2004

  • Harmer, Nicholas J.; Ilag, Leopold L.; Mulloy, Barbara
  • Journal of Molecular Biology, Vol. 339, Issue 4
  • DOI: 10.1016/j.jmb.2004.04.031

Interaction of Partially Structured States of Acidic Fibroblast Growth Factor with Phospholipid Membranes
journal, August 1995


Crystal structure of fibroblast growth factor receptor ectodomain bound to ligand and heparin
journal, October 2000

  • Pellegrini, Luca; Burke, David F.; von Delft, Frank
  • Nature, Vol. 407, Issue 6807
  • DOI: 10.1038/35039551