Mechanism of Activation and Inhibition of the HER4/ErbB4 Kinase

Structure

Volumn 16, Issue 3, 2008, Pages 460-467

  Qiu, Chen ^a   Tarrant, Mary K ^a   Choi, Sung Hee ^b   Sathyamurthy, Aruna ^a   Bose, Ron ^a   Banjade, Sudeep ^a   Pal, Ashutosh ^c   Bornmann, William G ^c   Lemmon, Mark A ^b   Cole, Philip A ^a   Leahy, Daniel J ^a  

^a JOHNS HOPKINS UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b UNIVERSITY OF PENNSYLVANIA   (United States)

^c UNIVERSITY OF TEXAS MD ANDERSON CANCER CENTER   (United States)

Author keywords

SIGNALING

Indexed keywords

EPIDERMAL GROWTH FACTOR RECEPTOR 4; LAPATINIB;

ARTICLE; BINDING SITE; CHEMICAL STRUCTURE; CRYSTAL STRUCTURE; DRUG ACTIVATION; DRUG BINDING; DRUG INHIBITION; DRUG MECHANISM; HUMAN; MUTAGENESIS; PRIORITY JOURNAL;

ANIMALS; CELLS, CULTURED; CONSERVED SEQUENCE; ENZYME ACTIVATION; HUMANS; MODELS, BIOLOGICAL; MODELS, MOLECULAR; PROTEIN BINDING; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, QUATERNARY; PROTEIN STRUCTURE, SECONDARY; QUINAZOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR; RECEPTOR, ERBB-2; SPODOPTERA;

EID: 40049099848     PISSN: 09692126     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.str.2007.12.016     Document Type: Article

References (43)

1. Ballotti R., Lammers R., Scimeca J.C., Dull T., Schlessinger J., Ullrich A., and Van Obberghen E. Intermolecular transphosphorylation between insulin receptors and EGF-insulin receptor chimerae. EMBO J. 8 (1989) 3303-3309
2. Berger M.B., Mendrola J.M., and Lemmon M.A. ErbB3/HER3 does not homodimerize upon neuregulin binding at the cell surface. FEBS Lett. 569 (2004) 332-336
3. Bouyain S., Longo P.A., Li S., Ferguson K.M., and Leahy D.J. The extracellular region of ErbB4 adopts a tethered conformation in the absence of ligand. Proc. Natl. Acad. Sci. USA 102 (2005) 15024-15029
4. Brignola P.S., Lackey K., Kadwell S.H., Hoffman C., Horne E., Carter H.L., Stuart J.D., Blackburn K., Moyer M.B., Alligood K.J., et al. Comparison of the biochemical and kinetic properties of the type 1 receptor tyrosine kinase intracellular domains. Demonstration of differential sensitivity to kinase inhibitors. J. Biol. Chem. 277 (2002) 1576-1585
5. Brunger A.T., Adams P.D., Clore G.M., DeLano W.L., Gros P., Grosse-Kunstleve R.W., Jiang J.S., Kuszewski J., Nilges M., Pannu N.S., et al. Crystallography & NMR system: a new software suite for macromolecular structure determination. Acta Crystallogr. D Biol. Crystallogr. 54 (1998) 905-921
6. Burgess A.W., Cho H.S., Eigenbrot C., Ferguson K.M., Garrett T.P., Leahy D.J., Lemmon M.A., Sliwkowski M.X., Ward C.W., and Yokoyama S. An open-and-shut case? Recent insights into the activation of EGF/ErbB receptors. Mol. Cell 12 (2003) 541-552
7. Carpenter G. ErbB-4: mechanism of action and biology. Exp. Cell Res. 284 (2003) 66-77
8. Cho H.S., and Leahy D.J. Structure of the extracellular region of HER3 reveals an interdomain tether. Science 297 (2002) 1330-1333
9. Cho H.S., Mason K., Ramyar K.X., Stanley A.M., Gabelli S.B., Denney Jr. D.W., and Leahy D.J. Structure of the extracellular region of HER2 alone and in complex with the Herceptin Fab. Nature 421 (2003) 756-760
10. Denny W.A. The 4-anilinoquinazoline class of inhibitors of the erbB family of receptor tyrosine kinases. Farmaco 56 (2001) 51-56
11. Emsley P., and Cowtan K. Coot: model-building tools for molecular graphics. Acta Crystallogr. D Biol. Crystallogr. 60 (2004) 2126-2132
12. Ferguson K.M., Darling P.J., Mohan M.J., Macatee T.L., and Lemmon M.A. Extracellular domains drive homo- but not hetero-dimerization of erbB receptors. EMBO J. 19 (2000) 4632-4643
13. Ferguson K.M., Berger M.B., Mendrola J.M., Cho H.S., Leahy D.J., and Lemmon M.A. EGF activates its receptor by removing interactions that autoinhibit ectodomain dimerization. Mol. Cell 11 (2003) 507-517
14. Garrett T.P., McKern N.M., Lou M., Elleman T.C., Adams T.E., Lovrecz G.O., Zhu H.J., Walker F., Frenkel M.J., Hoyne P.A., et al. Crystal structure of a truncated epidermal growth factor receptor extracellular domain bound to transforming growth factor alpha. Cell 110 (2002) 763-773
15. Garrett T.P., McKern N.M., Lou M., Elleman T.C., Adams T.E., Lovrecz G.O., Kofler M., Jorissen R.N., Nice E.C., Burgess A.W., and Ward C.W. The crystal structure of a truncated ErbB2 ectodomain reveals an active conformation, poised to interact with other ErbB receptors. Mol. Cell 11 (2003) 495-505
16. Gassmann M., Casagranda F., Orioli D., Simon H., Lai C., Klein R., and Lemke G. Aberrant neural and cardiac development in mice lacking the ErbB4 neuregulin receptor. Nature 378 (1995) 390-394
17. Holbro T., and Hynes N.E. ErbB receptors: directing key signaling networks throughout life. Annu. Rev. Pharmacol. Toxicol. 44 (2004) 195-217
18. Huse M., and Kuriyan J. The conformational plasticity of protein kinases. Cell 109 (2002) 275-282
19. Hynes N.E., and Lane H.A. ERBB receptors and cancer: the complexity of targeted inhibitors. Nat. Rev. Cancer 5 (2005) 341-354
20. Jeffrey P.D., Russo A.A., Polyak K., Gibbs E., Hurwitz J., Massague J., and Pavletich N.P. Mechanism of CDK activation revealed by the structure of a cyclinA-CDK2 complex. Nature 376 (1995) 313-320
21. Johnston J.B., Navaratnam S., Pitz M.W., Maniate J.M., Wiechec E., Baust H., Gingerich J., Skliris G.P., Murphy L.C., and Los M. Targeting the EGFR pathway for cancer therapy. Curr. Med. Chem. 13 (2006) 3483-3492
22. Karamouzis M.V., Badra F.A., and Papavassiliou A.G. Breast cancer: the upgraded role of HER-3 and HER-4. Int. J. Biochem. Cell Biol. 39 (2007) 851-856
23. Karunagaran D., Tzahar E., Beerli R.R., Chen X., Graus-Porta D., Ratzkin B.J., Seger R., Hynes N.E., and Yarden Y. ErbB-2 is a common auxiliary subunit of NDF and EGF receptors: implications for breast cancer. EMBO J. 15 (1996) 254-264
24. Klapper L.N., Glathe S., Vaisman N., Hynes N.E., Andrews G.C., Sela M., and Yarden Y. The ErbB-2/HER2 oncoprotein of human carcinomas may function solely as a shared coreceptor for multiple stroma-derived growth factors. Proc. Natl. Acad. Sci. USA 96 (1999) 4995-5000
25. Lammers R., Van Obberghen E., Ballotti R., Schlessinger J., and Ullrich A. Transphosphorylation as a possible mechanism for insulin and epidermal growth factor receptor activation. J. Biol. Chem. 265 (1990) 16886-16890
26. Lawrence M.C., and Colman P.M. Shape complementarity at protein/protein interfaces. J. Mol. Biol. 234 (1993) 946-950
27. Levinson N.M., Kuchment O., Shen K., Young M.A., Koldobskiy M., Karplus M., Cole P.A., and Kuriyan J. A Src-like inactive conformation in the abl tyrosine kinase domain. PLoS Biol. 4 (2006) e144
28. Murshudov G.N., Vagin A.A., and Dodson E.J. Refinement of macromolecular structures by the maximum-likelihood method. Acta Crystallogr. D Biol. Crystallogr. 53 (1997) 240-255
29. Ogiso H., Ishitani R., Nureki O., Fukai S., Yamanaka M., Kim J.H., Saito K., Sakamoto A., Inoue M., Shirouzu M., et al. Crystal structure of the complex of human epidermal growth factor and receptor extracellular domains. Cell 110 (2002) 775-787
30. Olayioye M.A., Neve R.M., Lane H.A., and Hynes N.E. The ErbB signaling network: receptor heterodimerization in development and cancer. EMBO J. 19 (2000) 3159-3167
31. Otwinowski Z., and Minor W. Processing of X-ray diffraction data collected in oscillation mode. Methods Enzymol. 276 (1997) 307-326
32. Petrov K.G., Zhang Y.M., Carter M., Cockerill G.S., Dickerson S., Gauthier C.A., Guo Y., Mook Jr. R.A., Rusnak D.W., Walker A.L., et al. Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series. Bioorg. Med. Chem. Lett. 16 (2006) 4686-4691
33. Plowman G.D., Culouscou J.M., Whitney G.S., Green J.M., Carlton G.W., Foy L., Neubauer M.G., and Shoyab M. Ligand-specific activation of HER4/p180erbB4, a fourth member of the epidermal growth factor receptor family. Proc. Natl. Acad. Sci. USA 90 (1993) 1746-1750
34. Sierke S.L., Cheng K., Kim H.H., and Koland J.G. Biochemical characterization of the protein tyrosine kinase homology domain of the ErbB3 (HER3) receptor protein. Biochem. J. 322 (1997) 757-763
35. Stamos J., Sliwkowski M.X., and Eigenbrot C. Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor. J. Biol. Chem. 277 (2002) 46265-46272
36. Storoni L.C., McCoy A.J., and Read R.J. Likelihood-enhanced fast rotation functions. Acta Crystallogr. D Biol. Crystallogr. 60 (2004) 432-438
37. Tidcombe H., Jackson-Fisher A., Mathers K., Stern D.F., Gassmann M., and Golding J.P. Neural and mammary gland defects in ErbB4 knockout mice genetically rescued from embryonic lethality. Proc. Natl. Acad. Sci. USA 100 (2003) 8281-8286
38. Wilson K.J., Mill C.P., Cameron E.M., Hobbs S.S., Hammer R.P., and Riese II D.J. Inter-conversion of neuregulin2 full and partial agonists for ErbB4. Biochem. Biophys. Res. Commun. 364 (2007) 351-357
39. Winn M.D., Isupov M.N., and Murshudov G.N. Use of TLS parameters to model anisotropic displacements in macromolecular refinement. Acta Crystallogr. D Biol. Crystallogr. 57 (2001) 122-133
40. Wood E.R., Truesdale A.T., McDonald O.B., Yuan D., Hassell A., Dickerson S.H., Ellis B., Pennisi C., Horne E., Lackey K., et al. A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells. Cancer Res. 64 (2004) 6652-6659
41. Yarden Y., and Sliwkowski M.X. Untangling the ErbB signalling network. Nat. Rev. Mol. Cell Biol. 2 (2001) 127-137
42. Zhang X., Gureasko J., Shen K., Cole P.A., and Kuriyan J. An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor. Cell 125 (2006) 1137-1149
43. Zhang X., Pickin K.A., Bose R., Jura N., Cole P.A., and Kuriyan J. Inhibition of the EGF receptor by binding of MIG6 to an activating kinase domain interface. Nature 450 (2007) 741-744