Alexei Kharitonenkov

Alexei Kharitonenkov

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Alexei Kharitonenkov

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Molecular elements in FGF19 and FGF21 defining KLB/FGFR activity and specificity.

Mol Metab 2018 07 11;13:45-55. Epub 2018 May 11.

Department of Chemistry, Indiana University, Bloomington, IN, 47405, USA; Interdisciplinary Biochemistry Graduate Program, Indiana University, Bloomington, IN, 47405, USA; Novo Nordisk Research Center Indianapolis, Indianapolis, IN, 46241, USA. Electronic address:

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http://dx.doi.org/10.1016/j.molmet.2018.05.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6026317PMC
July 2018

The Nuclear Receptor Rev-erbα Regulates Adipose Tissue-specific FGF21 Signaling.

J Biol Chem 2016 May 21;291(20):10867-75. Epub 2016 Mar 21.

From the Division of Endocrinology, Diabetes, and Metabolism, Departments of Medicine and Genetics, and Institute for Diabetes, Obesity, and Metabolism, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104,

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http://dx.doi.org/10.1074/jbc.M116.719120DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4865931PMC
May 2016

Overexpression of β-Klotho in Adipose Tissue Sensitizes Male Mice to Endogenous FGF21 and Provides Protection From Diet-Induced Obesity.

Endocrinology 2016 Apr 22;157(4):1467-80. Epub 2016 Feb 22.

Lilly Research Laboratories (R.J.S., C.C.C., R.E.G., A.C.A.) and formerly of Lilly Research Laboratories (A.K.), Lilly Corporate Center, Indianapolis, Indiana 46285.

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http://dx.doi.org/10.1210/en.2015-1722DOI Listing
April 2016

FGF21 Revolutions: Recent Advances Illuminating FGF21 Biology and Medicinal Properties.

Trends Endocrinol Metab 2015 Nov 18;26(11):608-617. Epub 2015 Oct 18.

Chemistry Department, Indiana University, Bloomington, IN, USA.

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https://linkinghub.elsevier.com/retrieve/pii/S10432760150018
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http://dx.doi.org/10.1016/j.tem.2015.09.007DOI Listing
November 2015

Dual effects of fibroblast growth factor 21 on hepatic energy metabolism.

J Endocrinol 2015 Oct 20;227(1):37-47. Epub 2015 Aug 20.

School of Life SciencesQueen's Medical Centre, University of Nottingham, Nottingham NG7 2UH, UKLilly Research LaboratoriesIndianapolis, IN, USAChemistry DepartmentCollege of Arts and Sciences, Indiana University Bloomington, 800 East Kirkwood Avenue, Bloomington, IN 47405-7102, USA

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http://dx.doi.org/10.1530/JOE-15-0334DOI Listing
October 2015

Central Fibroblast Growth Factor 21 Browns White Fat via Sympathetic Action in Male Mice.

Endocrinology 2015 Jul 29;156(7):2470-81. Epub 2015 Apr 29.

Division of Endocrinology (N.D., D.M.S., f.M.F., T.I.C., M.J.C., J.S.F., E.M.-F.), Beth Israel Deaconess Medical Center, Department of Medicine, Harvard Medical School, Boston, Massachusetts 02215-5491; Institute of Medical Physiology (D.M.S.), School of Medicine, University of Belgrade, 11000 Belgrade, Serbia; Department of Biology and Center for Obesity Reversal (N.L.N., E.Z., T.J.B.), Georgia State University, Atlanta, Georgia 30302-4010; and Diabetes Research (A.C.A., A.K.), Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana 46285-0001.

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http://dx.doi.org/10.1210/en.2014-2001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4475718PMC
July 2015

Genetic disruption of uncoupling protein 1 in mice renders brown adipose tissue a significant source of FGF21 secretion.

Mol Metab 2015 Jul 14;4(7):537-42. Epub 2015 May 14.

Helmholtz Diabetes Center, Helmholtz Zentrum München, 85764 Neuherberg, Germany ; Department of Animal Physiology, Philipps-Universität, 35043 Marburg, Germany.

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http://dx.doi.org/10.1016/j.molmet.2015.04.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4481421PMC
July 2015

Fibroblast growth factor 21 is not required for the reductions in circulating insulin-like growth factor-1 or global cell proliferation rates in response to moderate calorie restriction in adult mice.

PLoS One 2014 4;9(11):e111418. Epub 2014 Nov 4.

Department of Nutritional Science and Toxicology, University of California, Berkeley, California, United States of America; KineMed, Inc., Emeryville, California, United States of America.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0111418PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4219748PMC
June 2015

Naringenin prevents obesity, hepatic steatosis, and glucose intolerance in male mice independent of fibroblast growth factor 21.

Endocrinology 2015 Jun 16;156(6):2087-102. Epub 2015 Mar 16.

Department of Vascular Biology (J.M.A., E.E.M., A.C.B., B.G.S., D.E.T., S.S.C., C.G.S., M.W.H.) and Imaging Research Laboratories (M.D.), Robarts Research Institute, London, Ontario, Canada N6A 5B7; Children's Health Research Institute and Departments of Paediatrics, Physiology and Pharmacology, and Oncology (C.L.P.); Departments of Biochemistry (J.M.A., E.E.M., A.C.B., S.S.C., M.W.H.), Medical Biophysics (M.D.) and Medicine (D.E.T., C.G.S., M.W.H.), The University of Western Ontario, London, Ontario, Canada N6A 5B7; and Lilly Research Laboratories (A.C.A., A.K.), Division of Eli Lilly and Company, Indianapolis, Indiana 46285.

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https://academic.oup.com/endo/article-lookup/doi/10.1210/en.
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http://dx.doi.org/10.1210/en.2014-2003DOI Listing
June 2015

Discrete Aspects of FGF21 In Vivo Pharmacology Do Not Require UCP1.

Cell Rep 2015 May 5;11(7):991-9. Epub 2015 May 5.

Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2015.04.046DOI Listing
May 2015

Thyroid hormone receptor regulates most genes independently of fibroblast growth factor 21 in liver.

J Endocrinol 2015 Mar 11;224(3):289-301. Epub 2014 Dec 11.

Houston Methodist Research InstituteGenomic Medicine Program, 6670 Bertner Ave, Houston, Texas 77030, USACollege of Arts and SciencesChemistry Department, Indiana University Bloomington, Bloomington, Indiana, USADepartments of PaediatricsOncology, and Physiology and Pharmacology, University of Western Ontario, London, Ontario, CanadaChildren's Health Research InstituteLondon, Ontario, CanadaDepartment of Molecular Physiology and BiophysicsBaylor College of Medicine, Houston, Texas, USAThe Third Affiliated Hospital of Guangzhou Medical UniversityGuangzhou, China Houston Methodist Research InstituteGenomic Medicine Program, 6670 Bertner Ave, Houston, Texas 77030, USACollege of Arts and SciencesChemistry Department, Indiana University Bloomington, Bloomington, Indiana, USADepartments of PaediatricsOncology, and Physiology and Pharmacology, University of Western Ontario, London, Ontario, CanadaChildren's Health Research InstituteLondon, Ontario, CanadaDepartment of Molecular Physiology and BiophysicsBaylor College of Medicine, Houston, Texas, USAThe Third Affiliated Hospital of Guangzhou Medical UniversityGuangzhou, China

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http://dx.doi.org/10.1530/JOE-14-0440DOI Listing
March 2015

Epigenetic reprogramming in Mist1(-/-) mice predicts the molecular response to cerulein-induced pancreatitis.

PLoS One 2014 21;9(1):e84182. Epub 2014 Jan 21.

Children's Health Research Institute, London, Ontario, Canada ; Children's Health Research Institute, Department of Paediatrics, London, Ontario, Canada ; Children's Health Research Institute, Department of Physiology & Pharmacology, London, Ontario, Canada ; Oncology, the University of Western Ontario, London, Ontario, Canada.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0084182PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3897368PMC
October 2014

Break on through to the other 1.

Cell Metab 2014 Oct;20(4):554-5

College of Arts and Sciences, Chemistry Department, Indiana University Bloomington, 800 East Kirkwood Avenue, Bloomington, IN 47405-7102, USA.

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http://dx.doi.org/10.1016/j.cmet.2014.09.009DOI Listing
October 2014

Fibroblast growth factor (Fgf) 21 is a novel target gene of the aryl hydrocarbon receptor (AhR).

Toxicol Appl Pharmacol 2014 Jul 24;278(1):65-71. Epub 2014 Apr 24.

Department of Internal Medicine, University of Kansas Medical Center, 3901 Rainbow Boulevard, Kansas City, KS 66160, USA. Electronic address:

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http://dx.doi.org/10.1016/j.taap.2014.04.013DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4090247PMC
July 2014

Inventing new medicines: The FGF21 story.

Mol Metab 2014 Jun 27;3(3):221-9. Epub 2013 Dec 27.

Eli Lilly and Company, Diabetes Research, Indianapolis, IN 46285, USA.

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http://dx.doi.org/10.1016/j.molmet.2013.12.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3986619PMC
June 2014

Photoperiodic regulation of FGF21 production in the Siberian hamster.

Horm Behav 2014 Jun;66(1):180-5

School of Life Sciences, University of Nottingham Medical School, Queen Medical Centre, Nottingham NG7 2UH, UK. Electronic address:

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http://dx.doi.org/10.1016/j.yhbeh.2014.03.013DOI Listing
June 2014

Fibroblast growth factor 21 and thyroid hormone show mutual regulatory dependency but have independent actions in vivo.

Endocrinology 2014 May 24;155(5):2031-40. Epub 2014 Feb 24.

Division of Endocrinology (E.M.D., f.M.F., I.A., E.C.F., J.S.F., A.N.H., E.M.-F.), Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts 02215; and Lilly Research Laboratories (A.K.), Indianapolis, Indiana 46225.

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http://dx.doi.org/10.1210/en.2013-1902DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3990851PMC
May 2014

Silencing of the Fibroblast growth factor 21 gene is an underlying cause of acinar cell injury in mice lacking MIST1.

Am J Physiol Endocrinol Metab 2014 Apr 18;306(8):E916-28. Epub 2014 Feb 18.

Children's Health Research Institute, London, Ontario, Canada;

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http://dx.doi.org/10.1152/ajpendo.00559.2013DOI Listing
April 2014

Hepatic SIRT1 attenuates hepatic steatosis and controls energy balance in mice by inducing fibroblast growth factor 21.

Gastroenterology 2014 Feb 1;146(2):539-49.e7. Epub 2013 Nov 1.

Department of Medicine, Boston University School of Medicine, Boston, Massachusetts. Electronic address:

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http://dx.doi.org/10.1053/j.gastro.2013.10.059DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4228483PMC
February 2014

The breadth of FGF21's metabolic actions are governed by FGFR1 in adipose tissue.

Mol Metab 2012 28;2(1):31-7. Epub 2012 Aug 28.

Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA.

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http://dx.doi.org/10.1016/j.molmet.2012.08.007DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3757657PMC
September 2013

The effects of LY2405319, an FGF21 analog, in obese human subjects with type 2 diabetes.

Cell Metab 2013 Sep;18(3):333-40

Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA.

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http://dx.doi.org/10.1016/j.cmet.2013.08.005DOI Listing
September 2013

Fibroblast growth factor 21 is not required for the antidiabetic actions of the thiazoladinediones.

Mol Metab 2013 29;2(3):205-14. Epub 2013 May 29.

Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA.

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http://dx.doi.org/10.1016/j.molmet.2013.05.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3773835PMC
September 2013

Endocrine protection of ischemic myocardium by FGF21 from the liver and adipose tissue.

Sci Rep 2013 Sep 26;3:2767. Epub 2013 Sep 26.

Biomedical Engineering Department, Northwestern University, Evanston, IL 60208, USA.

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http://dx.doi.org/10.1038/srep02767DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3783882PMC
September 2013

FGF21 requires βklotho to act in vivo.

PLoS One 2012 27;7(11):e49977. Epub 2012 Nov 27.

Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN, USA.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0049977PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3507945PMC
June 2013

Fibroblast growth factor 21 (FGF21) inhibits chondrocyte function and growth hormone action directly at the growth plate.

J Biol Chem 2012 Jul 13;287(31):26060-7. Epub 2012 Jun 13.

Department of Pediatrics, Drexel University College of Medicine, Philadelphia, Pennsylvania 19134, USA.

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http://dx.doi.org/10.1074/jbc.M112.343707DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3406689PMC
July 2012

FGF21 is increased by inflammatory stimuli and protects leptin-deficient ob/ob mice from the toxicity of sepsis.

Endocrinology 2012 Jun 2;153(6):2689-700. Epub 2012 Apr 2.

Metabolism Section, Department of Veterans Affairs Medical Center, University of California San Francisco, San Francisco, California 94121, USA.

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https://academic.oup.com/endo/article-lookup/doi/10.1210/en.
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http://dx.doi.org/10.1210/en.2011-1496DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3359613PMC
June 2012

Role of fibroblast growth factor 21 (FGF21) in undernutrition-related attenuation of growth in mice.

Endocrinology 2012 May 28;153(5):2287-95. Epub 2012 Feb 28.

Section of Endocrinology and Diabetes, St. Christopher's Hospital for Children, Drexel University College of Medicine, Philadelphia, Pennsylvania 19134, USA.

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http://dx.doi.org/10.1210/en.2011-1909DOI Listing
May 2012

FGF21 as a therapeutic reagent.

Adv Exp Med Biol 2012 ;728:214-28

Eli Lilly and Company, Indianapolis, IN, USA.

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http://dx.doi.org/10.1007/978-1-4614-0887-1_14DOI Listing
April 2012

Plasma FGF21 is elevated by the intense lipid mobilization of lactation.

Endocrinology 2011 Dec 11;152(12):4652-61. Epub 2011 Oct 11.

Department of Animal Science, Cornell University, 259 Morrison Hall, Ithaca, New York 14853, USA.

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http://dx.doi.org/10.1210/en.2011-1425DOI Listing
December 2011

Integrated regulation of hepatic metabolism by fibroblast growth factor 21 (FGF21) in vivo.

Endocrinology 2011 Aug 28;152(8):2996-3004. Epub 2011 Jun 28.

Division of Endocrinology, Beth Israel Deaconess Medical Center, Boston, Massachusetts 02215, USA.

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http://dx.doi.org/10.1210/en.2011-0281DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3138239PMC
August 2011

Hormone-like fibroblast growth factors and metabolic regulation.

Biochim Biophys Acta 2011 Jul 12;1812(7):791-5. Epub 2011 Apr 12.

Eli Lilly and company, Lilly Research Laboratory, Lilly Corporate Center, Indianapolis Indiana 46285, USA.

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http://linkinghub.elsevier.com/retrieve/pii/S092544391100076
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http://dx.doi.org/10.1016/j.bbadis.2011.04.002DOI Listing
July 2011

FGF21 reloaded: challenges of a rapidly growing field.

Trends Endocrinol Metab 2011 Mar 29;22(3):81-6. Epub 2010 Dec 29.

Eli Lilly and Company, Diabetes Research, Indianapolis, IN 46285, USA.

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http://dx.doi.org/10.1016/j.tem.2010.11.003DOI Listing
March 2011

Obesity is a fibroblast growth factor 21 (FGF21)-resistant state.

Diabetes 2010 Nov 3;59(11):2781-9. Epub 2010 Aug 3.

Department of Medicine, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts, USA.

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http://dx.doi.org/10.2337/db10-0193DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2963536PMC
November 2010

FGFs and metabolism.

Curr Opin Pharmacol 2009 Dec 14;9(6):805-10. Epub 2009 Aug 14.

Eli Lilly and Company, Lilly Research Laboratories, BioTechnology Discovery Research, Lilly Corporate Center, Indianapolis, IN 46285, USA.

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http://dx.doi.org/10.1016/j.coph.2009.07.001DOI Listing
December 2009

Fibroblast growth factor 21 reduces the severity of cerulein-induced pancreatitis in mice.

Gastroenterology 2009 Nov 5;137(5):1795-804. Epub 2009 Aug 5.

Children's Health Research Institute, London, Ontario.

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http://dx.doi.org/10.1053/j.gastro.2009.07.064DOI Listing
November 2009

Fibroblast growth factor 21-deficient mice demonstrate impaired adaptation to ketosis.

Endocrinology 2009 Nov 9;150(11):4931-40. Epub 2009 Oct 9.

Associate Professor of Medicine, Division of Endocrinology, Diabetes, and Metabolism, Beth Israel Deaconess Medical Center, Center for Life Sciences, 7th Floor, 330 Brookline Avenue, Boston, Massachusetts 02215, USA.

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https://academic.oup.com/endo/article-lookup/doi/10.1210/en.
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http://dx.doi.org/10.1210/en.2009-0532DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2775979PMC
November 2009

Fibroblast growth factor 21 controls glycemia via regulation of hepatic glucose flux and insulin sensitivity.

Endocrinology 2009 Sep 21;150(9):4084-93. Epub 2009 May 21.

Department of Molecular Physiology and Biophysics, National Institutes of Health-Vanderbilt University Mouse Metabolic Phenotyping Center, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, USA.

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http://dx.doi.org/10.1210/en.2009-0221DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2736088PMC
September 2009

Different roles of N- and C- termini in the functional activity of FGF21.

J Cell Physiol 2009 May;219(2):227-34

Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA.

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http://dx.doi.org/10.1002/jcp.21675DOI Listing
May 2009

FGF21: a novel prospect for the treatment of metabolic diseases.

Curr Opin Investig Drugs 2009 Apr;10(4):359-64

Eli Lilly & Co, Lilly Research Laboratories, Biotechnology Discovery Research, Lilly Corporate Center, Indianapolis, IN 46285, USA.

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April 2009

Fibroblast growth factor 21 corrects obesity in mice.

Endocrinology 2008 Dec 7;149(12):6018-27. Epub 2008 Aug 7.

Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana 46285, USA.

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http://dx.doi.org/10.1210/en.2008-0816DOI Listing
December 2008

FGF21 is an Akt-regulated myokine.

FEBS Lett 2008 Nov 21;582(27):3805-10. Epub 2008 Oct 21.

Molecular Cardiology, Whitaker Cardiovascular Institute, Boston University School of Medicine, 715 Albany Street, W611, Boston, MA 02118, United States.

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http://dx.doi.org/10.1016/j.febslet.2008.10.021DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2604129PMC
November 2008

The circulating metabolic regulator FGF21 is induced by prolonged fasting and PPARalpha activation in man.

Cell Metab 2008 Aug;8(2):169-74

Department of Endocrinology, Metabolism and Diabetes, Molecular Nutrition Unit, Karolinska Institutet, Karolinska University Hospital Huddinge, S-141 86 Stockholm, Sweden.

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http://dx.doi.org/10.1016/j.cmet.2008.06.014DOI Listing
August 2008

Tyrosine phosphorylation of annexin A2 regulates Rho-mediated actin rearrangement and cell adhesion.

J Cell Sci 2008 Jul;121(Pt 13):2177-85

Institute of Medical Biochemistry, Centre for Molecular Biology of Inflammation, and Interdisciplinary Clinical Research Centre, University of Muenster, 48149 Muenster, Germany.

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http://dx.doi.org/10.1242/jcs.028415DOI Listing
July 2008

Fibroblast growth factor-21 as a therapeutic agent for metabolic diseases.

BioDrugs 2008 ;22(1):37-44

BioTechology Discovery Research, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana 46285, USA.

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http://dx.doi.org/10.2165/00063030-200822010-00004DOI Listing
June 2008

FGF21 attenuates lipolysis in human adipocytes - a possible link to improved insulin sensitivity.

FEBS Lett 2008 May 5;582(12):1725-30. Epub 2008 May 5.

Department of Medicine, M63 Karolinska Institutet, Karolinska University Hospital, Huddinge, 141 86 Stockholm, Sweden.

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http://dx.doi.org/10.1016/j.febslet.2008.04.038DOI Listing
May 2008

The metabolic state of diabetic monkeys is regulated by fibroblast growth factor-21.

Endocrinology 2007 Feb 26;148(2):774-81. Epub 2006 Oct 26.

Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, Indiana 46285, USA.

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http://dx.doi.org/10.1210/en.2006-1168DOI Listing
February 2007

Molecular determinants of FGF-21 activity-synergy and cross-talk with PPARgamma signaling.

J Cell Physiol 2007 Jan;210(1):1-6

Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA.

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http://dx.doi.org/10.1002/jcp.20847DOI Listing
January 2007

Inhibition of T cell antigen receptor signaling by VHR-related MKPX (VHX), a new dual specificity phosphatase related to VH1 related (VHR).

J Biol Chem 2002 Feb 3;277(7):5524-8. Epub 2001 Dec 3.

Laboratory of Signal Transduction, La Jolla Cancer Research Center, The Burnham Institute, La Jolla, California 92037, USA.

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http://dx.doi.org/10.1074/jbc.M107653200DOI Listing
February 2002