Discovery of an inhibitor of insulin-like growth factor 1 receptor activation: implications for cellular potency and selectivity over insulin receptor.

[1]  I. Puzanov,et al.  Phase I dose escalation study of continuous oral dosing of OSI-906, an insulin like growth factor-1 receptor (IGF-1R) tyrosine kinase inhibitor, in patients with advanced solid tumors. , 2016, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[2]  A. Gualberto,et al.  Emerging role of insulin-like growth factor receptor inhibitors in oncology: early clinical trial results and future directions , 2009, Oncogene.

[3]  Brian J. Wilson,et al.  Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R). , 2009, Bioorganic & medicinal chemistry letters.

[4]  G. Müller,et al.  Small-molecule inhibitors binding to protein kinase. Part II: the novel pharmacophore approach of type II and type III inhibition , 2008, Expert opinion on drug discovery.

[5]  J. Góra‐Tybor,et al.  Targeted drugs in chronic myeloid leukemia. , 2008, Current medicinal chemistry.

[6]  R. Kurzrock,et al.  Early drug development of inhibitors of the insulin-like growth factor-I receptor pathway: Lessons from the first clinical trials , 2008, Molecular Cancer Therapeutics.

[7]  Wolfgang Jahnke,et al.  Solution Conformations and Dynamics of ABL Kinase-Inhibitor Complexes Determined by NMR Substantiate the Different Binding Modes of Imatinib/Nilotinib and Dasatinib*♦ , 2008, Journal of Biological Chemistry.

[8]  V. Macaulay,et al.  Targeting the type 1 insulin-like growth factor receptor as a treatment for cancer , 2008 .

[9]  F. Shepherd,et al.  Epidermal growth factor receptor inhibitors in the treatment of lung cancer: reality and hopes , 2008, Current opinion in oncology.

[10]  L. Shewchuk,et al.  Impact of common epidermal growth factor receptor and HER2 variants on receptor activity and inhibition by lapatinib. , 2008, Cancer research.

[11]  A. Mukherjee,et al.  Lapatinib: a tyrosine kinase inhibitor with a clinical role in breast cancer , 2007, Expert opinion on pharmacotherapy.

[12]  N. Gibson,et al.  A novel, potent, and selective insulin-like growth factor-I receptor kinase inhibitor blocks insulin-like growth factor-I receptor signaling in vitro and inhibits insulin-like growth factor-I receptor–dependent tumor growth in vivo , 2007, Molecular Cancer Therapeutics.

[13]  Lewis C. Cantley,et al.  AKT/PKB Signaling: Navigating Downstream , 2007, Cell.

[14]  R. Angell,et al.  N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3. , 2007, Bioorganic & medicinal chemistry letters.

[15]  W. Miller,et al.  Role of the Activation Loop Tyrosines in Regulation of the Insulin-like Growth Factor I Receptor-tyrosine Kinase* , 2006, Journal of Biological Chemistry.

[16]  D. Yee,et al.  Type I insulin-like growth factor receptor as a therapeutic target in cancer. , 2005, Cancer research.

[17]  S. Stirdivant,et al.  Biochemical and structural characterization of a novel class of inhibitors of the type 1 insulin-like growth factor and insulin receptor kinases. , 2005, Biochemistry.

[18]  L. Wodicka,et al.  A small molecule–kinase interaction map for clinical kinase inhibitors , 2005, Nature Biotechnology.

[19]  Krystal J Alligood,et al.  A Unique Structure for Epidermal Growth Factor Receptor Bound to GW572016 (Lapatinib) , 2004, Cancer Research.

[20]  E. Glezer,et al.  Clinical and Biological Applications of ECL , 2004 .

[21]  L. Johnson,et al.  Protein Kinase Inhibitors: Insights into Drug Design from Structure , 2004, Science.

[22]  D. Fabbro,et al.  In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase. , 2004, Cancer cell.

[23]  L. Kuo,et al.  Structure of apo, unactivated insulin-like growth factor-1 receptor kinase at 1.5 A resolution. , 2003, Acta crystallographica. Section D, Biological crystallography.

[24]  E. Sausville,et al.  Issues and progress with protein kinase inhibitors for cancer treatment , 2003, Nature Reviews Drug Discovery.

[25]  J. Sportsman,et al.  A Homogeneous Fluorescence Polarization Assay Adaptable for a Range of Protein Serine/Threonine and Tyrosine Kinases , 2003, Journal of biomolecular screening.

[26]  S. Stirdivant,et al.  Crystal Structure of the Apo, Unactivated Insulin-like Growth Factor-1 Receptor Kinase , 2002, The Journal of Biological Chemistry.

[27]  D. Hanahan,et al.  Elevated levels of IGF-1 receptor convey invasive and metastatic capability in a mouse model of pancreatic islet tumorigenesis. , 2002, Cancer cell.

[28]  K. Lackey,et al.  Comparison of the Biochemical and Kinetic Properties of the Type 1 Receptor Tyrosine Kinase Intracellular Domains , 2002, The Journal of Biological Chemistry.

[29]  Stevan R. Hubbard,et al.  Structure and autoregulation of the insulin-like growth factor 1 receptor kinase , 2001, Nature Structural Biology.

[30]  A. Rufer,et al.  Dimerization-induced activation of soluble insulin/IGF-1 receptor kinases: an alternative mechanism of activation. , 2001, Biochemistry.

[31]  B. Calabretta,et al.  Multiple Signaling Pathways of the Insulin-Like Growth Factor 1 Receptor in Protection from Apoptosis , 1999, Molecular and Cellular Biology.

[32]  A. Woods,et al.  Homogeneous proximity tyrosine kinase assays: scintillation proximity assay versus homogeneous time-resolved fluorescence. , 1999, Analytical biochemistry.

[33]  A. Smith,et al.  A scintillation proximity assay for the Raf/MEK/ERK kinase cascade: high-throughput screening and identification of selective enzyme inhibitors. , 1999, Analytical biochemistry.

[34]  S. Hubbard.  Crystal structure of the activated insulin receptor tyrosine kinase in complex with peptide substrate and ATP analog , 1997, The EMBO journal.

[35]  M. Rubini,et al.  The IGF-I receptor in cell growth, transformation and apoptosis. , 1997, Biochimica et biophysica acta.

[36]  D. Le Roith,et al.  Signaling via the insulin-like growth factor-I receptor: does it differ from insulin receptor signaling? , 1996, Cytokine & growth factor reviews.

[37]  K. Lipson,et al.  Measurement of the protein tyrosine kinase activity of c-src using time-resolved fluorometry of europium chelates. , 1996, Analytical biochemistry.

[38]  S. Hubbard,et al.  Expression, Characterization, and Crystallization of the Catalytic Core of the Human Insulin Receptor Protein-tyrosine Kinase Domain (*) , 1995, The Journal of Biological Chemistry.

[39]  Charis Eng,et al.  Catalytic specificity of protein-tyrosine kinases is critical for selective signalling , 1995, Nature.

[40]  S. Hubbard,et al.  Crystal structure of the tyrosine kinase domain of the human insulin receptor , 1994, Nature.

[41]  W. Rutter,et al.  Overexpression of the human insulinlike growth factor I receptor promotes ligand-dependent neoplastic transformation , 1990, Molecular and cellular biology.

[42]  A. Ullrich,et al.  Molecular analysis of signal transduction by growth factors. , 1988, Biochemistry.

[43]  S. Jacobs,et al.  An antibody to the receptor for insulin-like growth factor I inhibits the growth of MCF-7 cells in tissue culture. , 1987, Biochemical and biophysical research communications.

[44]  C Collins,et al.  Insulin‐like growth factor I receptor primary structure: comparison with insulin receptor suggests structural determinants that define functional specificity. , 1986, The EMBO journal.

[45]  C. Conover,et al.  In vitro and in vivo antitumor effects of the dual insulin-like growth factor-I/insulin receptor inhibitor, BMS-554417. , 2006, Cancer research.

[46]  Z. Otwinowski,et al.  [20] Processing of X-ray diffraction data collected in oscillation mode. , 1997, Methods in enzymology.

[47]  Robert A. Copeland,et al.  Enzymes: A Practical Introduction to Structure, Mechanism, and Data Analysis , 1996 .