Publications by authors named "Joseph Schlessinger"

100Publications

FGF23 contains two distinct high-affinity binding sites enabling bivalent interactions with α-Klotho.

Proc Natl Acad Sci U S A 2020 12 30;117(50):31800-31807. Epub 2020 Nov 30.

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06510;

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December 2020

Selective Janus Kinase 2 (JAK2) Pseudokinase Ligands with a Diaminotriazole Core.

J Med Chem 2020 05 8;63(10):5324-5340. Epub 2020 May 8.

Department of Chemistry, Yale University, New Haven, Connecticut 06520-8107, United States.

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May 2020

Reminiscences on the "Classic" 1976 FRAP Article in Biophysical Journal.

Biophys J 2018 10 4;115(7):1156-1159. Epub 2018 Sep 4.

Department of Biochemistry, University of Connecticut Health Center, Farmington, Connecticut.

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October 2018

Structures of β-klotho reveal a 'zip code'-like mechanism for endocrine FGF signalling.

Nature 2018 01 17;553(7689):501-505. Epub 2018 Jan 17.

Department of Pharmacology and Yale Cancer Biology Institute, Yale School of Medicine, 333 Cedar Street, New Haven, Connecticut 06520, USA.

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January 2018

Alk and Ltk ligands are essential for iridophore development in zebrafish mediated by the receptor tyrosine kinase Ltk.

Proc Natl Acad Sci U S A 2017 11 23;114(45):12027-12032. Epub 2017 Oct 23.

Department of Pharmacology, Yale School of Medicine, New Haven, CT 06520;

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November 2017

Identification and Characterization of JAK2 Pseudokinase Domain Small Molecule Binders.

ACS Med Chem Lett 2017 Jun 17;8(6):618-621. Epub 2017 May 17.

Department of Pharmacology and Department of Chemistry, Yale University, New Haven, Connecticut 06520, United States.

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June 2017

JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules.

ACS Med Chem Lett 2017 Jun 17;8(6):614-617. Epub 2017 May 17.

Department of Chemistry, Yale University, New Haven, Connecticut 06520-8107, United States.

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June 2017

Regression of Chemotherapy-Resistant Polymerase ε (POLE) Ultra-Mutated and MSH6 Hyper-Mutated Endometrial Tumors with Nivolumab.

Clin Cancer Res 2016 Dec 2;22(23):5682-5687. Epub 2016 Aug 2.

Department of Genetics, Howard Hughes Medical Institute, Yale University School of Medicine, New Haven, Connecticut.

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December 2016

Loss of TRIM33 causes resistance to BET bromodomain inhibitors through MYC- and TGF-β-dependent mechanisms.

Proc Natl Acad Sci U S A 2016 08 18;113(31):E4558-66. Epub 2016 Jul 18.

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520; Department of Cell Biology, Yale University School of Medicine, New Haven, CT 06520

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August 2016

The Dark Side of Cell Signaling: Positive Roles for Negative Regulators.

Cell 2016 Mar;164(6):1172-1184

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA; Yale Cancer Biology Institute, West Haven, CT 06516, USA.

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March 2016

Early and multiple origins of metastatic lineages within primary tumors.

Proc Natl Acad Sci U S A 2016 Feb 8;113(8):2140-5. Epub 2016 Feb 8.

Department of Biostatistics, Yale School of Public Health, New Haven, CT 06510; Department of Ecology and Evolutionary Biology, Yale University, New Haven, CT 06520; Program in Computational Biology and Bioinformatics, Yale University, New Haven, CT 06511

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February 2016

Structural analysis of the mechanism of phosphorylation of a critical autoregulatory tyrosine residue in FGFR1 kinase domain.

Genes Cells 2015 Oct 24;20(10):860-70. Epub 2015 Aug 24.

Department of Structural Biology, Faculty of Advanced Life Science, Hokkaido University, Sapporo, Hokkaido, 060-0810, Japan.

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October 2015

FGF1 and FGF19 reverse diabetes by suppression of the hypothalamic-pituitary-adrenal axis.

Nat Commun 2015 Apr 28;6:6980. Epub 2015 Apr 28.

1] Howard Hughes Medical Institute, Yale University School of Medicine, New Haven, Connecticut 06536-8012, USA [2] Department of Internal Medicine, Yale University School of Medicine, New Haven, Connecticut 06536-8012, USA [3] Department of Cellular &Molecular Physiology, Yale University School of Medicine, New Haven, Connecticut 06536-8012, USA.

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April 2015

The strength and cooperativity of KIT ectodomain contacts determine normal ligand-dependent stimulation or oncogenic activation in cancer.

Mol Cell 2015 Jan 24;57(1):191-201. Epub 2014 Dec 24.

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA. Electronic address:

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January 2015

Whole-exome sequencing characterizes the landscape of somatic mutations and copy number alterations in adrenocortical carcinoma.

J Clin Endocrinol Metab 2015 Mar 9;100(3):E493-502. Epub 2014 Dec 9.

Yale Endocrine Neoplasia Laboratory (C.C.J., J.M.H., A.L.F., J.W.K., T.C.B., R.K., T.C.), Yale School of Medicine, New Haven, Connecticut 06520; Department of Surgery (C.C.J., J.M.H., A.L.F., J.W.K., T.C.B., R.K., T.C.), Yale School of Medicine, New Haven, Connecticut, 06520; Department of Genetics (G.G., C.N.W., M.C., R.P.L.), Yale School of Medicine and Howard Hughes Medical Institute, New Haven, Connecticut, 06520; Department of Oncology-Pathology (C.C.J., A.S., A.H., C.L.), Karolinska Institutet, Karolinska University Hospital, CCK, SE-171 76 Stockholm, Sweden; Yale Center for Genome Analysis (JDO, SMM), Orange, Connecticut, 06477; Department of Pathology (D.L.R., M.L.P.), Yale School of Medicine, New Haven, Connecticut, 06520; Department of Pharmacology (J.S.), Yale School of Medicine, New Haven, Connecticut 06520; Department of Molecular Medicine and Surgery (M.B.), Karolinska Institutet, Karolinska University Hospital, SE-171 76 Stockholm, Sweden; Division of Nephrology (U.I.S.), University Hospital Düsseldorf, 40225 Düsseldorf, Germany; Department of Pathology (A.C.S.), University Hospital Düsseldorf, 40225 Düsseldorf, Germany; and Division of Endocrinology and Diabetology (M.H.), University Hospital Düsseldorf, 40225 Düsseldorf, Germany.

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March 2015

Differential TAM receptor-ligand-phospholipid interactions delimit differential TAM bioactivities.

Elife 2014 Sep 29;3. Epub 2014 Sep 29.

Molecular Neurobiology Laboratory, The Salk Institute for Biological Studies, La Jolla, United States.

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September 2014

The docking protein FRS2α is a critical regulator of VEGF receptors signaling.

Proc Natl Acad Sci U S A 2014 Apr 2;111(15):5514-9. Epub 2014 Apr 2.

Yale Cardiovascular Research Center, Department of Internal Medicine, and Departments of Surgery, Pharmacology, and Cell Biology, Yale University School of Medicine, New Haven, CT 06520.

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April 2014

The EGFR family: not so prototypical receptor tyrosine kinases.

Cold Spring Harb Perspect Biol 2014 Apr 1;6(4):a020768. Epub 2014 Apr 1.

Department of Biochemistry and Biophysics, University of Pennsylvania Perelman School of Medicine, Philadelphia, Pennsylvania 19104.

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April 2014

Receptor tyrosine kinases: legacy of the first two decades.

Cold Spring Harb Perspect Biol 2014 Mar 1;6(3). Epub 2014 Mar 1.

Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06520.

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March 2014

Structure, domain organization, and different conformational states of stem cell factor-induced intact KIT dimers.

Proc Natl Acad Sci U S A 2014 Feb 21;111(5):1772-7. Epub 2014 Jan 21.

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520.

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February 2014

Tony Pawson (1952-2013).

Cancer Cell 2013 Sep;24(3):273-4

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September 2013

RAC1P29S is a spontaneously activating cancer-associated GTPase.

Proc Natl Acad Sci U S A 2013 Jan 2;110(3):912-7. Epub 2013 Jan 2.

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA.

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January 2013

A step towards treating KRAS-mutant NSCLC.

Lancet Oncol 2013 Jan 28;14(1):3-5. Epub 2012 Nov 28.

Yale Comprehensive Cancer Center, Yale University School of Medicine, New Haven, CT 06520, USA.

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January 2013

The genesis of Zelboraf: targeting mutant B-Raf in melanoma.

J Cell Biol 2012 Oct;199(1):15-9

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA.

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October 2012

Type II p21-activated kinases (PAKs) are regulated by an autoinhibitory pseudosubstrate.

Proc Natl Acad Sci U S A 2012 Oct 17;109(40):16107-12. Epub 2012 Sep 17.

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA.

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October 2012

Suppression of EGFR endocytosis by dynamin depletion reveals that EGFR signaling occurs primarily at the plasma membrane.

Proc Natl Acad Sci U S A 2012 Mar 27;109(12):4419-24. Epub 2012 Feb 27.

Departments of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA.

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March 2012

Pyk2 is required for neutrophil degranulation and host defense responses to bacterial infection.

J Immunol 2011 Feb 27;186(3):1656-65. Epub 2010 Dec 27.

Program in Immunology, Department of Laboratory Medicine, University of California, San Francisco, San Francisco, CA 94143, USA.

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February 2011

Constitutive activated Cdc42-associated kinase (Ack) phosphorylation at arrested endocytic clathrin-coated pits of cells that lack dynamin.

Mol Biol Cell 2011 Feb 17;22(4):493-502. Epub 2010 Dec 17.

Department of Cell Biology, Howard Hughes Medical Institute, Program in Cellular Neuroscience, Neurodegeneration and Repair, and Kavli Institute for Neuroscience, Yale University School of Medicine, New Haven, CT 06510, USA.

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February 2011

Proline-rich tyrosine kinase-2 is critical for CD8 T-cell short-lived effector fate.

Proc Natl Acad Sci U S A 2010 Sep 30;107(37):16234-9. Epub 2010 Aug 30.

Department of Medicine, Division of Rheumatology, The Howard Hughes Medical Institute, Rosalind Russell Medical Research Center for Arthritis, and Graduate Program in Biomedical Sciences, University of California, San Francisco, CA 94143-0795, USA.

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September 2010

Cell signaling by receptor tyrosine kinases.

Cell 2010 Jun;141(7):1117-34

Department of Biochemistry and Biophysics, University of Pennsylvania School of Medicine, Philadelphia, PA 19104-6059, USA.

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June 2010

Asymmetric tyrosine kinase arrangements in activation or autophosphorylation of receptor tyrosine kinases.

Mol Cells 2010 May 28;29(5):443-8. Epub 2010 Apr 28.

Department of Pharmacology, Yale University School of Medicine, 333 Cedar St., New Haven, CT 06520-8066, USA.

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May 2010

Spatial control of EGF receptor activation by reversible dimerization on living cells.

Nature 2010 Apr 7;464(7289):783-7. Epub 2010 Mar 7.

Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, USA.

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April 2010

Asymmetric receptor contact is required for tyrosine autophosphorylation of fibroblast growth factor receptor in living cells.

Proc Natl Acad Sci U S A 2010 Feb 26;107(7):2866-71. Epub 2010 Jan 26.

Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA.

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February 2010

Direct contacts between extracellular membrane-proximal domains are required for VEGF receptor activation and cell signaling.

Proc Natl Acad Sci U S A 2010 Feb 11;107(5):1906-11. Epub 2010 Jan 11.

Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA.

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February 2010

The selectivity of receptor tyrosine kinase signaling is controlled by a secondary SH2 domain binding site.

Cell 2009 Aug;138(3):514-24

Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA.

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August 2009

FGFR3-targeted mAb therapy for bladder cancer and multiple myeloma.

J Clin Invest 2009 May;119(5):1077-9

Kolltan Pharmaceuticals Inc., New Haven, Connecticut, USA.

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May 2009

Crystal structures of free and ligand-bound focal adhesion targeting domain of Pyk2.

Biochem Biophys Res Commun 2009 Jun 7;383(3):347-52. Epub 2009 Apr 7.

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA.

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June 2009

The precise sequence of FGF receptor autophosphorylation is kinetically driven and is disrupted by oncogenic mutations.

Sci Signal 2009 Feb 17;2(58):ra6. Epub 2009 Feb 17.

Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA.

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February 2009

Contacts between membrane proximal regions of the PDGF receptor ectodomain are required for receptor activation but not for receptor dimerization.

Proc Natl Acad Sci U S A 2008 Jun 27;105(22):7681-6. Epub 2008 May 27.

Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA.

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June 2008

[Structural biology of receptor tyrosine kinase kit].

Seikagaku 2008 Feb;80(2):94-104

Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA.

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February 2008

'Tuning' of type I interferon-induced Jak-STAT1 signaling by calcium-dependent kinases in macrophages.

Nat Immunol 2008 Feb 16;9(2):186-93. Epub 2007 Dec 16.

Arthritis and Tissue Degeneration Program, Hospital for Special Surgery, New York, New York 10021, USA.

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February 2008

Structural basis for reduced FGFR2 activity in LADD syndrome: Implications for FGFR autoinhibition and activation.

Proc Natl Acad Sci U S A 2007 Dec 3;104(50):19802-7. Epub 2007 Dec 3.

Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06510, USA.

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December 2007

Structural basis for activation of the receptor tyrosine kinase KIT by stem cell factor.

Cell 2007 Jul;130(2):323-34

Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA.

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July 2007

Skeletal overgrowth is mediated by deficiency in a specific isoform of fibroblast growth factor receptor 3.

Proc Natl Acad Sci U S A 2007 Mar 23;104(10):3937-42. Epub 2007 Feb 23.

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA.

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March 2007

Nuclear signaling by receptor tyrosine kinases: the first robin of spring.

Cell 2006 Oct;127(1):45-8

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA.

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October 2006

Activation of the nonreceptor protein tyrosine kinase Ack by multiple extracellular stimuli.

Proc Natl Acad Sci U S A 2006 Jun 15;103(26):9796-801. Epub 2006 Jun 15.

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA.

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June 2006

On the nature of low- and high-affinity EGF receptors on living cells.

Proc Natl Acad Sci U S A 2006 Apr 29;103(15):5735-40. Epub 2006 Mar 29.

Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA.

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April 2006

Autophosphorylation of FGFR1 kinase is mediated by a sequential and precisely ordered reaction.

Mol Cell 2006 Mar;21(5):711-7

Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06520, USA.

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March 2006

Trans-activation of EphA4 and FGF receptors mediated by direct interactions between their cytoplasmic domains.

Proc Natl Acad Sci U S A 2005 Dec 19;102(52):18866-71. Epub 2005 Dec 19.

Department of Molecular Cell Biology, Institute of Advanced Medicine, Wakayama Medical University, 811-1 Kimiidera, Wakayama 641-8509, Japan.

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December 2005

Epidermal growth factor receptor dimerization and activation require ligand-induced conformational changes in the dimer interface.

Mol Cell Biol 2005 Sep;25(17):7734-42

Department of Biochemistry and Biophysics, University of Pennsylvania School of Medicine, Philadelphia, 19104-6059, USA.

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September 2005

Common and distinct elements in cellular signaling via EGF and FGF receptors.

Science 2004 Nov;306(5701):1506-7

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA.

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November 2004

The docking protein Gab1 is the primary mediator of EGF-stimulated activation of the PI-3K/Akt cell survival pathway.

BMC Biol 2004 Nov 18;2:24. Epub 2004 Nov 18.

Department of Pharmacology, Yale University School of Medicine, PO Box 208066, New Haven, CT 06520-8066, USA.

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November 2004

The biochemical response of the heart to hypertension and exercise.

Trends Biochem Sci 2004 Nov;29(11):609-17

Department of Biochemistry and Molecular Biophysics, Washington University School of Medicine, Washington University Medical Center, Campus Box 8231, 660 South Euclid Avenue, St Louis, MI 63110-1093, USA.

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November 2004

FRS2 family docking proteins with overlapping roles in activation of MAP kinase have distinct spatial-temporal patterns of expression of their transcripts.

FEBS Lett 2004 Apr;564(1-2):14-8

Department of Pharmacology, Yale University School of Medicine, Sterling Hall of Medicine, 333 Cedar Street, B-204, New Haven, CT 06520, USA.

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April 2004

Scanning electron microscopy of cells and tissues under fully hydrated conditions.

Proc Natl Acad Sci U S A 2004 Mar 26;101(10):3346-51. Epub 2004 Feb 26.

Department of Physics of Complex Systems, The Weizmann Institute of Science, Rehovot 76100, Israel.

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March 2004

A structure-based model for ligand binding and dimerization of EGF receptors.

Proc Natl Acad Sci U S A 2004 Jan 19;101(4):929-34. Epub 2004 Jan 19.

Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA.

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January 2004

The tethered configuration of the EGF receptor extracellular domain exerts only a limited control of receptor function.

Proc Natl Acad Sci U S A 2004 Jan 19;101(4):923-8. Epub 2004 Jan 19.

Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA.

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January 2004

Insights into the molecular basis for fibroblast growth factor receptor autoinhibition and ligand-binding promiscuity.

Proc Natl Acad Sci U S A 2004 Jan 19;101(4):935-40. Epub 2004 Jan 19.

Departments of Pharmacology and Microbiology, New York University School of Medicine, New York, NY 10016, USA.

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January 2004

SH2 and PTB domains in tyrosine kinase signaling.

Sci STKE 2003 Jul 15;2003(191):RE12. Epub 2003 Jul 15.

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA.

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July 2003

Signal transduction. Autoinhibition control.

Science 2003 May;300(5620):750-2

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA.

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May 2003

A putative molecular-activation switch in the transmembrane domain of erbB2.

Proc Natl Acad Sci U S A 2002 Dec 2;99(25):15937-40. Epub 2002 Dec 2.

Department of Biochemistry, The George S. Wise Faculty of Life Sciences, Tel-Aviv University, Ramat-Aviv 69987, Israel Middle East.

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December 2002

A critical role for the protein tyrosine phosphatase receptor type Z in functional recovery from demyelinating lesions.

Nat Genet 2002 Nov 30;32(3):411-4. Epub 2002 Sep 30.

Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06520, USA.

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November 2002

Ligand-induced, receptor-mediated dimerization and activation of EGF receptor.

Cell 2002 Sep;110(6):669-72

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA.

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September 2002

All signaling is local?

Mol Cell 2002 Aug;10(2):218-9

Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06510, USA.

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August 2002