Insulin and epidermal growth factor receptor structures publications

The following publications detail the work involved in the development of CSIRO’s Insulin and epidermal growth factor receptor structures.

Patents

Adams TE, Burgess AW, Elleman TC, Garrett TPJ, Jorissen RN, Lou M, McKern NM, Lovrecz GO, Nice EC, Ward CW, 2008, ‘Methods of screening based on the EGF receptor crystal structure’, U.S. Patent Number 2008/0025983 A1 – Publication Number WO/2003/014159.

Garrett TPJ, Adams TE, Lovrecz G, McKern NM, Lawrence MC, Sparrow LG, Ward CW, Lou M, Streltsov V, 2007, ‘Structure of the insulin receptor ectodomain’, Publication Number WO/2007/147213.

Garrett TPJ, Elleman TC, Adams TE, Burgess AW, Jorissen RN, Lou M, Lovrecz GO, McKern NM, Ward CW, 2007, ‘Crystal structure of ErbB2 and uses thereof’, U.S. Patent Number 2007/0281365 A1 – Publication Number WO/2004/031232.

Bentley JD, Tulloch PA, Cosgrove LJ, Frenkel MJ, Garrett TPJ, Lawrence LJ, Lou M, Lovrecz GO, Ward CW, 2006, ‘Method of designing agonists and antagonists to IGF receptor’, U.S. Patent Number 7,020,563 B1 – Patent Number EP1034188 B1 – Publication Number WO99/28347.

Johns TG, Scott AM, Burgess AW, Old LJ, Adams TE, Wittrup KD, Chao G, 2005, ‘EGF receptor epitope peptides and uses thereof’, U.S. Patent Number 2005/0255555 A1.

Jorissen RN, Burgess AW, Elleman TC, Epa VC, Garrett TPJ, Lou M, McKern NM, Treutlin HR, Ward CW, 2005, ‘Method of designing agonists and antagonists to EGF receptor family’, U.S. Patent Number 6,941,229 B1 – Publication Number WO99/62955.

Ward CW, McKern NM, Lovrecz GO, Jorissen RN, Garrett TPJ, Elleman TC, Burgess AW, Adams TE, Domagala T, Nice EC, 2005, ‘Truncated EGF receptor’, U.S. Patent Number 6,946,543 B2 – Publication Number WO/2002/000876.

Key publications

Smith BJ, Huang K, Kong G, Chan SJ, Nakagawa S, Menting J, Hu S-Q, Whittaker J, Steiner D, Katsoyannis P, Ward CW, Weiss MA, Lawrence MC, 2010, ‘Structural resolution of a tandem hormone-binding element in the insulin receptor: implication for design of peptide agonists’, Proc Natl Acad Sci USA, 107: 6771-6776.

Ward CW, Lawrence MC, 2009, ‘Ligand-induced activation of the insulin receptor: a multi-step process involving structural changes in both the ligand and the receptor’, Bioessays, 31: 422-434.

Sparrow LG, Lawrence MC, Gorman JJ, Strike PM, Robinson CP, McKern NM, Ward CW, 2008, ‘N-linked glycans of the human insulin receptor and their distribution over the crystal structure’, Proteins: Structure, Function and Bioinformatics, 71: 426-439.

Lawrence MC, McKern NM, Ward CW, 2007, ‘Insulin receptor structure and its implications for the IGF-1 receptor’, Current Opinion in Structural Biology, 17: 1-7.

Ward CW, Lawrence MC, Streltsov VA, Lou M-Z, McKern NM, 2007, ‘The insulin and epidermal growth factor receptor structures: new insights into ligand-induced signal transduction’, Trends in Biological Sciences, 32: 129-137.

Lou M-Z, Garrett TPJ, Epa VC, McKern NM, Hoyne PA, Bentley JD, Lovrecz GO, Cosgrove LJ, Ward CW, 2006, ‘Crystal structure of the first three domains of the human insulin receptor: comparison with the insulin-like growth factor receptor’, _Proc. of the National Academy of Sciences, USA, 103: 12429-12434.

McKern NM, Lawrence MC, Streltsov VA, Lou M-Z, Adams TE, Lovrecz GO, Elleman TC, Richards KM, Bentley JD, Pilling PA, Hoyne PA, Cartledge KA, Pham TM, Lewis JL, Sankovich SE, Stoichevska V, Da Silva E, Robinson CP, Frenkel MJ, Sparrow LG, Fernley RT, Epa VC, Ward CW, 2006, ‘Structure of the insulin receptor ectodomain homodimer reveals an unexpected folded-over arrangement of the N- and C-terminal halves’, Nature, 443: 218-221.

Burgess AW, Cho H-S, Eigenbrot C, Ferguson KM, Garrett TPJ, Leahy DJ, Lemmon MA, Sliwkowski MX, Ward CW, Yokoyama S, 2003, ‘An open-and-shut case ? Recent insights into the activation of EGF/ErbB Receptors’, Molecular Cell, 12: 541-552.

Garrett TPJ, McKern NM, Lou M, Elleman TC, Adams TE, Lovrecz GO, Kofler M, Jorissen RN, Nice EC, Burgess AW, Ward CW, 2003, ‘The crystal structure of a truncated ErbB2 ectodomain reveals an active conformation, poised to interact with other ErbB receptors’, Molecular Cell, 11: 495-505.

Jorissen RN, Walker F, Pouliot N, Garrett TPJ, Ward CW, Burgess AW, 2003, ‘Epidermal growth factor receptor: mechanisms of activation and signalling’, Exp. Cell Res, 284: 31-53.

Garrett TPJ, McKern NM, Lou M, Elleman TC, Adams TE, Lovrecz GO, Zhu HJ, Walker F, Hoyne PA, Jorissen RN, Nice EC, Burgess AW, Ward CW, 2002, ‘Crystal Structure of a Truncated Epidermal Growth Factor Receptor Extracellular Domain Bound to Transforming Growth Factor’, Cell, 110: 763-773.

Elleman TC, Domagala T, McKern NM, Nerrie M, Lönnqvist B, Adams TE, Lewis J, Lovrecz GO, Hoyne PA, Richards KM, Howlett GJ, Rothaker J, Jorrisen R, Lou M, Garrett TPJ, Burgess AW, Nice EC, Ward CW, 2001, ‘Identification of a determinant of epidermal growth factor receptor ligand binding specificity using a truncated, high affinity form of the ectodomain’, Biochemistry, 40: 8930-8939.

Adams TE, Epa VC, Garrett TPJ, Ward CW, 2000, ‘Structure and function of the type I insulin-like growth factor receptor’, Cellular and Molecular Life Sciences, 57: 1050-1093.

Ward CW, 1999, ‘Members of the insulin receptor family contain three fibronectin type III domains’, Growth Factors, 16: 315-322.

Garrett TPJ, McKern NM, Lou M, Frenkel MJ, Bentley JD, Lovrecz GL, Elleman TC, Cosgrove L, Ward CW, 1998, ‘The structure of the first three domains of the type 1 insulin-like growth factor receptor’, Nature, 394: 395-399.

Sparrow LG, McKern NM, Gorman JJ, Strike PM, Robinson CP, Bentley JD, Ward CW, 1997, ‘The disulfide bonds in the C-terminal domains of the human insulin receptor ectodomain’, Journal of Biological Chemistry, 272: 29460-29467.

Ward CW, Hoyne PA, Flegg RH, 1995, ‘Insulin and epidermal growth factor receptors contain the cysteine repeat motif found in the tumour necrosis factor receptor’, Proteins: Structure, Function and Genetics, 22: 141-153.

Reviews

Ward CW, Lawrence MC, Streltsov VA, Garrett TPJ, McKern NM, Lou M-Z, Lovrecz GO, Adams TE, 2008, ‘Structural insights into ligand-induced activation of the insulin receptor’, Acta Physiologica, 192: 3-9, (including the cover).

Ward CW, Lawrence MC, McKern NM, 2006, ‘Landmarks in insulin research – the determination of the crystal structure of the human insulin receptor’, Chemistry in Australia, pp.5-7.

Adams TE, Ward CW, 2004, ‘Signalling by the type-1 insulin-like growth factor receptor: interplay with the epidermal growth factor receptor’, Growth Factors, 22: 89-95.

Ward CW, Garrett TPJ, 2004, ‘Structural relationships between the insulin receptor and the epidermal growth factor receptor families’, Current Opinion in Drug Development and Discovery, 7: 630-638.

Nice EC, Garrett TPJ, Ward CW, Lou M-Z, McKern NM, Lovrecz GO, Ellman TC, Adams TE, Jorissen RN, Rothacker J, Zhu H-J, Walker F, Burgess AW, 2003, ‘Structure-function studies on the EGF/EGFR family: towards the clinic’, Proc Chinese Peptide Conference, Dalian, China, July 2002, pp.110-115.

Nice EC, Catimel B, Rothacker J, Burgess, AW, Garrett, TPJ, Ward CW, 2003, ‘Applications of optical biosensors to structure-function studies on the EGF/EGF receptor’, In: Methods in Proteome and Protein Analysis, Kamp RM, Calvete J, Choli-Papadopoulou T (eds), Proc. 14th Meeting Methods of Protein Structure Analysis, Valencia, Spain , September 8th-12th, 2002, pp.133-164.

Ward CW, Garrett TPJ, Lou M, McKern NM, Adams TE, Elleman TC, Hoyne PA, Frenkel MJ, Cosgrove LJ, Lovrecz GO, Sparrow LG, Lawrence LJ, Epa VC, 2003, ‘The structure of the type-I insulin like growth factor receptor’, In: Insulin-like growth factors, LeRoith D, Zumkeller W, Baxter R (eds), Eurekah.com and Kluwer Academic / Plenum Publishers, pp.1-21.

Ward CW, Garrett TPJ, McKern NM, Lou M, Cosgrove LJ, Sparrow LG, Frenkel MJ, Hoyne PA, Elleman TC, Adams TE, Lovrecz GO, Lawrence LJ, Tulloch PA, 2001, ‘The 3D structure of the type I IGF receptor’, Molecular Pathology, 54: 125-132.

Ward CW, Garrett TPJ, McKern NM, Sparrow LG, Frenkel MJ, Lou M, 2001, ‘Structural relationships between members of the insulin receptor family’, In: Alcuin Symposium on Insulin and Related Proteins – From Structure to Function and Pharmacology, Federwisch M (ed), Kluwer Academic Publishers, pp.151-164.

Ward CW, Garrett TPJ, McKern NM, Lawrence LJ, 1999, ‘Structure of the insulin receptor family: unexpected relationships with other proteins’, Today’s Life Sciences, 11: 26-32.

Original papers

Adams TE, Koziolek EJ, Hoyne PH, Bentley JD, Lu L, Lovrecz G, Ward CW, Lee FT, Scott AM, Nash AD, Rothacker J, Nice EC, Burgess AW, Johns TG, 2009, ‘A truncated soluble epidermal growth factor receptor-Fc fusion ligand trap displays anti-tumour activity in vivo‘, Growth Factors, 27: 141-154.

Menting JG, Ward CW, Margetts MB, Lawrence MC, 2009, ‘A thermodynamic study of ligand binding to the first three domains of the human insulin receptor: relationship between the receptor alpha-chain C-terminal peptide and the site 1 insulin mimetic peptides’, Biochemistry, 48: 5492-5500.

Garrett TP, Burgess AW, Gan HK, Luwor RB, Cartwright G, Walker F, Orchard SG, Clayton AH, Nice EC, Rothacker J, Catimel B, Cavenee WK, Old LJ, Stockert E, Ritter G, Adams TE, Hoyne PA, Wittrup D, Chao G, Cochran JR, Luo C, Lou M, Huyton T, Xu Y, Fairlie WD, Yao S, Scott AM, Johns TG, 2009, ‘Antibodies specifically targeting a locally misfolded region of tumor associated EGFR’, Proc. Natl Acad Sci USA, 106: 5082-5087.

Whitten AE, Smith BJ, Menting JG, Margetts MB, McKern NM, Lovrecz GO, Adams TE Richards K, Bentley JD, Trewhella J, Ward CW, Lawrence MC, 2009, ‘Solution structure of ectodomains of the insulin receptor family: the ectodomain of the type 1 insulin-like growth factor receptor displays asymmetry of ligand binding accompanied by limited conformational change’, J Mol Biol, 394: 878-892.

Konstantopoulos N, Marcuccio S, Kyi S, Stoichevska V, Castelli LA, Ward CW, Macaulay SL, 2007, ‘A purine analogue kinase inhibitor, CK59, reveals a role for CaMKII in insulin-stimulated glucose transport’, Endocrinology, 148: 374-385.

Sparrow LG, Gorman JJ, Strike PM, Robinson CP, McKern NM, Epa VC, Ward CW, 2007, ‘The location and characterisation of the O-linked glycans of the human insulin receptor’, Proteins: Structure, Function and Bioinformatics, 66: 261-265.

Zahnd C, Wyler E, Schwenk JM, Steiner D, Lawrence MC, McKern NM, Pecorari F, Ward CW, Joos TO, Plückthun A, 2007, ‘A designed ankyrin repeat protein evolved to picomolar affinity to Her2′, J Mol Biol, 369: 1015-1028.

Epa VC, Ward CW, 2006, ‘Model for the complex between the type-1 insulin-like growth factor and its receptor: towards designing antagonists for the IGF-1 receptor’, Protein Engineering Design and Selection, 19: 377-384.

Denley A, Bonython ER, Booker GW, Cosgrove LJ, Forbes BE, Ward CW, Wallace JC, 2004, ‘The insulin and IGF-I receptor binding specificity of IGF-I and IGF-II lies within their C and D domains’, Molecular Endocrinology, 18: 2502-2512.

Johns TG, Adams TE, Cochran JR, Hall NE, Hoyne PA, Olsen MJ, Kim Y-S, Rothaker J, Nice EC, Walker F, Old LJ, Ward CW, Burgess AW, Wittrup KD, Scott AM, 2004, ‘Identification of the epitope for the EGFR-specific monoclonal antibody 806 reveals that it preferentially recognizes an untethered form of the receptor’, J Biol Chem, 279: 30375-30384.

Walker F, Orchard S, Jorissen RN, Hall N, Zhang H-H, Hoyne PA, Adams TE, Johns TG, Ward CW, Garrett TPJ, Zhu HJ, Nerrie M, Scott AM, Nice EC, Burgess AW, 2004, ‘Analysis of CR1/CR2 domain interactions on the function of the cell-surface epidermal growth factor receptor’, J Biol Chem, 279: 22387-22398.

Macaulay SL, Stoichevska V, Grusovin J, Gough KH, Castelli LA, Ward CW, 2003, ‘Insulin stimulates movement of sorting nexin 9 between cellular compartments: a putative role mediating cell surface receptor expression and insulin action’, Biochemical Journal, 376: 123-134.

Macaulay SL, Grusovin J, Stoichevska V, Ryan JM, Castelli LA, Ward CW, 2002, ‘Cellular munc 18c levels can modulate glucose transport rate and GLUT4 translocation in 3T3L1 cells’, FEBS Letters, 528: 154-160.

Ward CW, Garrett TPJ, 2001, ‘The relationship between the L1 and L2 domains of the insulin and epidermal growth factor receptors to leucine-rich repeat modules’, BMC Bioinformatics, 2: 4.

Elleman TC, Frenkel MJ, Hoyne PA, McKern NM, Cosgrove L, Jachno KM, Bentley JD, Sankovich SE, Ward CW, 2000, ‘Mutational analysis of the N-linked glycosylation-sites of the human insulin receptor’, Biochemical Journal, 347: 771-779.

Grusovin J, Stoichevska V, Gough KH, Nunan K, Ward CW, Macaulay SL, 2000, ‘Definition of a minimal Munc18c domain that interacts with syntaxin 4′, Biochemical Journal, 350: 741-746.

Hoyne PA, Cosgrove LJ, McKern NM, Bentley JD, Ivancic N, Elleman TC, Ward CW, 2000, ‘High affinity insulin binding by soluble insulin receptor extracellular domain fused to a leucine zipper’, FEBS Letters, 479: 15-18.

Hoyne PA, Elleman TC, Adams TE, Richards KM, Ward CW, 2000, ‘Ligand binding and antibody binding properties of a cys-rich loop exchange chimera of insulin receptor and insulin-like growth factor receptor’, FEBS Letters, 469: 57-60.

Jorissen RN, Epa VC, Treutlein HR, Garrett TPJ, Ward CW, Burgess AW, 2000, ‘Characterization of a comparative model of the extracellular domain of the epidermal growth factor receptor’, Protein Sci., 9: 310-324.

Rouard M, Bass J, Grigorescu F, Garrett TPJ, Ward CW, Lipkind G, Jaffiole C, Steiner DF, Bell GI, 1999, ‘Congenital insulin resistance associated with a conformational alteration in a conserved beta-sheet in the insulin receptor L1 domain’, Journal of Biological Chemistry, 274: 18487-18491.

Tulloch PA, Lawrence L, McKern NM, Bentley JD, Cosgrove L, Robinson CP, Ivancic N, Siddle K, Ward CW, 1999, ‘Single-molecule imaging of human insulin receptor ectodomain and its Fab complexes’, Journal of Structural Biology, 125: 11-18.

Jagadish MN, Tellam JT, Macaulay SL, Gough KH, James DE, Ward CW, 1997, ‘A novel isoform of syntaxin 1 is expressed in mammalian cells’, Biochemical Journal, 321: 151-156.

Macaulay SL, Hewish DR, Gough KH, Stoichesvska V, Macpherson SF, Jagadish MN, Ward CW, 1997, ‘Functional studies in 3T3-L1 cells support a role for SNARE proteins in insulin stimulation of GLUT4 translocation’, Biochemical Journal, 324: 217-224.

Macaulay SL, Rea S, Gough KH, Baldini G, Niemann H, Ward CW, James DE, 1997, ‘Botulinum E toxin light chain does not cleave SNAP-23 and does not impair GLUT4 translocation in 3T3-L1 cells’, Biochemical and Biophysical Research Communications, 237: 388-393.

McKern NM, Lou M, Frenkel MJ, Verkuylen A, Bentley JD, Lovrecz GO, Ivancic N, Elleman TC, Garrett TPJ, Cosgrove L, Ward CW, 1997, ‘Crystallization of the first three domains of the human insulin-like growth factor-1 receptor’, Protein Science, 6: 2663-2666.

Tellam JT, Macaulay SL, McIntosh S, Hewish DR, Ward CW, James DE, 1997, ‘Characterization of Munc-18c and syntaxin-4 in 3T3-L1 adipocytes. Putative role in insulin-dependent movement of GLUT4′, Journal of Biological Chemistry, 272: 6179-6186.

Jagadish MN, Fernandez CS, Hewish DR, Macaulay SL, Gough KH, Grusovin J, Verkuylen A, Cosgrove L, Alafaci A, Frenkel ML, Ward CW, 1996, ‘Insulin-responsive tissues contain the core complex protein SNAP-25 A and B isoforms in addition to syntaxin 4 and synaptobrevins 1 and 2′, Biochemical Journal, 317: 945-954.

Ward CW, Gough KH, Rashke M, Wan SS, Tribbick G, Wang JX, 1996, ‘Systematic mapping of potential binding sites for Shc and Grb2 SH2 domains on insulin receptor substrate-1 and the receptors for insulin, epidermal growth factor, platelet-derived growth factor, and fibroblast growth factor’, Journal of Biological Chemistry, 271: 5603-5609.

Cosgrove L, McKern NM, Lovrecz GO, Verkuylen A, Cavaleri L, Black LA, Bentley JD, Howlett GJ, Gray P, Ward CW, 1995, ‘Purification and properties of insulin receptor ectodomain from large-scale mammalian cell culture’, Protein Expression and Purification, 6: 789-798.

Macauley SL, Polites M, Frenkel MJ, Hewish DR, Ward CW, 1995, ‘Mutagenic structure/function analysis of the cytoplasmic cysteines of the insulin receptor’, Biochemical Journal, 306: 811-820.

Macaulay SL, Polites M, Hewish DR, Ward CW, 1994, ‘Cysteine-524 is not the only residue involved in the formation of disulfide-bonded dimers of the insulin receptor’, Biochemical Journal, 303: 575-581.