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PDBsum entry 2gs6

Go to PDB code: 
protein ligands metals links
Transferase PDB id
2gs6
Jmol
Contents
Protein chain
311 a.a. *
Ligands
GLU-ILE-TYR-GLY-
GLU
112
Metals
_CL
Waters ×74
* Residue conservation analysis
PDB id:
2gs6
Name: Transferase
Title: Crystal structure of the active egfr kinase domain in complex with an atp analog-peptide conjugate
Structure: Epidermal growth factor receptor. Chain: a. Fragment: kinase domain, residues 696-1022. Synonym: receptor tyrosine-protein kinase erbb-1. Engineered: yes. Peptide. Chain: b. Engineered: yes
Source: Homo sapiens. Human. Organism_taxid: 9606. Gene: egfr, erbb1. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108. Synthetic: yes
Biol. unit: Dimer (from PDB file)
Resolution:
2.60Å     R-factor:   0.206     R-free:   0.257
Authors: X.Zhang,J.Gureasko,K.Shen,P.A.Cole,J.Kuriyan
Key ref:
X.Zhang et al. (2006). An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor. Cell, 125, 1137-1149. PubMed id: 16777603 DOI: 10.1016/j.cell.2006.05.013
Date:
25-Apr-06     Release date:   20-Jun-06    
PROCHECK
Go to PROCHECK summary
 Headers
 References

Protein chain
Pfam   ArchSchema ?
P00533  (EGFR_HUMAN) -  Epidermal growth factor receptor
Seq:
Struc:
 
Seq:
Struc:
 
Seq:
Struc:
1210 a.a.
311 a.a.*
Key:    PfamA domain  Secondary structure  CATH domain
* PDB and UniProt seqs differ at 3 residue positions (black crosses)

 Enzyme reactions 
   Enzyme class: E.C.2.7.10.1  - Receptor protein-tyrosine kinase.
[IntEnz]   [ExPASy]   [KEGG]   [BRENDA]
      Reaction: ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
ATP
Bound ligand (Het Group name = 112)
matches with 83.00% similarity
+
[protein]-L-tyrosine
Bound ligand (Het Group name = TYR)
matches with 64.00% similarity
= ADP
+ [protein]-L-tyrosine phosphate
Molecule diagrams generated from .mol files obtained from the KEGG ftp site
 Gene Ontology (GO) functional annotation 
  GO annot!
  Biological process     regulation of signal transduction   2 terms 
  Biochemical function     transferase activity, transferring phosphorus-containing groups     5 terms  

 

 
    reference    
 
 
DOI no: 10.1016/j.cell.2006.05.013 Cell 125:1137-1149 (2006)
PubMed id: 16777603  
 
 
An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor.
X.Zhang, J.Gureasko, K.Shen, P.A.Cole, J.Kuriyan.
 
  ABSTRACT  
 
The mechanism by which the epidermal growth factor receptor (EGFR) is activated upon dimerization has eluded definition. We find that the EGFR kinase domain can be activated by increasing its local concentration or by mutating a leucine (L834R) in the activation loop, the phosphorylation of which is not required for activation. This suggests that the kinase domain is intrinsically autoinhibited, and an intermolecular interaction promotes its activation. Using further mutational analysis and crystallography we demonstrate that the autoinhibited conformation of the EGFR kinase domain resembles that of Src and cyclin-dependent kinases (CDKs). EGFR activation results from the formation of an asymmetric dimer in which the C-terminal lobe of one kinase domain plays a role analogous to that of cyclin in activated CDK/cyclin complexes. The CDK/cyclin-like complex formed by two kinase domains thus explains the activation of EGFR-family receptors by homo- or heterodimerization.
 
  Selected figure(s)  
 
Figure 1.
Figure 1. Ligand-Induced Dimerization of EGFR and Active and Inactive States of Its Kinase Domain
Figure 4.
Figure 4. The Asymmetric CDK/Cyclin-like Crystallographic Dimer of the EGFR Kinase Domain
 
  The above figures are reprinted by permission from Cell Press: Cell (2006, 125, 1137-1149) copyright 2006.  
  Figures were selected by an automated process.  

Literature references that cite this PDB file's key reference

  PubMed id Reference
22218287 N.J.Bessman, and M.A.Lemmon (2012).
Finding the missing links in EGFR.
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22785351 Y.Yarden, and G.Pines (2012).
The ERBB network: at last, cancer therapy meets systems biology.
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21549910 A.M.Ruppert, M.Wislez, V.Poulot, R.Lacave, M.Antoine, and J.Cadranel (2011).
[A simple view on lung cancer biology: The EGFR pathway.]
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21423148 B.M.Filippi, P.de Los Heros, Y.Mehellou, I.Navratilova, R.Gourlay, M.Deak, L.Plater, R.Toth, E.Zeqiraj, and D.R.Alessi (2011).
MO25 is a master regulator of SPAK/OSR1 and MST3/MST4/YSK1 protein kinases.
  EMBO J, 30, 1730-1741.  
21457523 C.L.Arteaga (2011).
ERBB receptors in cancer: signaling from the inside.
  Breast Cancer Res, 13, 304.  
21532939 D.J.Riese (2011).
Ligand-based receptor tyrosine kinase partial agonists: New paradigm for cancer drug discovery?
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21320329 G.V.Meirelles, J.C.Silva, Y.d.e. .A.Mendonça, C.H.Ramos, I.L.Torriani, and J.Kobarg (2011).
Human Nek6 is a monomeric mostly globular kinase with an unfolded short N-terminal domain.
  BMC Struct Biol, 11, 12.  
20887192 G.da Cunha Santos, F.A.Shepherd, and M.S.Tsao (2011).
EGFR mutations and lung cancer.
  Annu Rev Pathol, 6, 49-69.  
21107857 I.E.Michailidis, R.Rusinova, A.Georgakopoulos, Y.Chen, R.Iyengar, N.K.Robakis, D.E.Logothetis, and L.Baki (2011).
Phosphatidylinositol-4,5-bisphosphate regulates epidermal growth factor receptor activation.
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21430264 J.D.Sadowsky, M.A.Burlingame, D.W.Wolan, C.L.McClendon, M.P.Jacobson, and J.A.Wells (2011).
Turning a protein kinase on or off from a single allosteric site via disulfide trapping.
  Proc Natl Acad Sci U S A, 108, 6056-6061.
PDB codes: 3orx 3orz 3otu
21822280 L.Z.Mi, C.Lu, Z.Li, N.Nishida, T.Walz, and T.A.Springer (2011).
Simultaneous visualization of the extracellular and cytoplasmic domains of the epidermal growth factor receptor.
  Nat Struct Mol Biol, 18, 984-989.  
20938978 M.Mustafa, A.Mirza, and N.Kannan (2011).
Conformational regulation of the EGFR kinase core by the juxtamembrane and C-terminal tail: a molecular dynamics study.
  Proteins, 79, 99.  
  21332718 M.V.Georgieva, Y.de Pablo, D.Sanchis, J.X.Comella, and M.Llovera (2011).
Ubiquitination of TrkA by Nedd4-2 regulates receptor lysosomal targeting and mediates receptor signaling.
  J Neurochem, 117, 479-493.  
21474065 N.Jura, X.Zhang, N.F.Endres, M.A.Seeliger, T.Schindler, and J.Kuriyan (2011).
Catalytic control in the EGF receptor and its connection to general kinase regulatory mechanisms.
  Mol Cell, 42, 9.  
22020299 S.T.Low-Nam, K.A.Lidke, P.J.Cutler, R.C.Roovers, P.M.van Bergen en Henegouwen, B.S.Wilson, and D.S.Lidke (2011).
ErbB1 dimerization is promoted by domain co-confinement and stabilized by ligand binding.
  Nat Struct Mol Biol, 18, 1244-1249.  
21251949 T.B.Knudsen, K.A.Houck, N.S.Sipes, A.V.Singh, R.S.Judson, M.T.Martin, A.Weissman, N.C.Kleinstreuer, H.M.Mortensen, D.M.Reif, J.R.Rabinowitz, R.W.Setzer, A.M.Richard, D.J.Dix, and R.J.Kavlock (2011).
Activity profiles of 309 ToxCastâ„¢ chemicals evaluated across 292 biochemical targets.
  Toxicology, 282, 1.  
21132006 T.Harada, A.Lopez-Chavez, L.Xi, M.Raffeld, Y.Wang, and G.Giaccone (2011).
Characterization of epidermal growth factor receptor mutations in non-small-cell lung cancer patients of African-American ancestry.
  Oncogene, 30, 1744-1752.  
22101934 Z.Wang, P.A.Longo, M.K.Tarrant, K.Kim, S.Head, D.J.Leahy, and P.A.Cole (2011).
Mechanistic insights into the activation of oncogenic forms of EGF receptor.
  Nat Struct Mol Biol, 18, 1388-1393.  
  20519929 A.B.Sigalov (2010).
New therapeutic strategies targeting transmembrane signal transduction in the immune system.
  Cell Adh Migr, 4, 255-267.  
20946980 A.Bill, A.Schmitz, B.Albertoni, J.N.Song, L.C.Heukamp, D.Walrafen, F.Thorwirth, P.J.Verveer, S.Zimmer, L.Meffert, A.Schreiber, S.Chatterjee, R.K.Thomas, R.T.Ullrich, T.Lang, and M.Famulok (2010).
Cytohesins are cytoplasmic ErbB receptor activators.
  Cell, 143, 201-211.  
19915609 B.H.Ozer, G.J.Wiepz, and P.J.Bertics (2010).
Activity and cellular localization of an oncogenic glioblastoma multiforme-associated EGF receptor mutant possessing a duplicated kinase domain.
  Oncogene, 29, 855-864.  
20946975 B.Z.Shilo (2010).
Insider influence on ErbB activity.
  Cell, 143, 181-182.  
20005866 C.B.McDonald, K.L.Seldeen, B.J.Deegan, V.Bhat, and A.Farooq (2010).
Assembly of the Sos1-Grb2-Gab1 ternary signaling complex is under allosteric control.
  Arch Biochem Biophys, 494, 216-225.  
20084478 C.S.Gerbin, and R.Landgraf (2010).
Geldanamycin selectively targets the nascent form of ERBB3 for degradation.
  Cell Stress Chaperones, 15, 529-544.  
20970513 D.F.Stern (2010).
EGFs and ERBBs--brief history and prospects.
  Semin Cell Dev Biol, 21, 917-921.  
19937092 D.Guo, J.J.Zhang, and X.Y.Huang (2010).
A new Rac/PAK/GC/cGMP signaling pathway.
  Mol Cell Biochem, 334, 99.  
20723751 D.J.Leahy (2010).
The ins and outs of EGFR asymmetry.
  Cell, 142, 513-515.  
19774589 D.Lavogina, E.Enkvist, and A.Uri (2010).
Bisubstrate inhibitors of protein kinases: from principle to practical applications.
  ChemMedChem, 5, 23-34.  
20816829 D.N.Amin, M.R.Campbell, and M.M.Moasser (2010).
The role of HER3, the unpretentious member of the HER family, in cancer biology and cancer therapeutics.
  Semin Cell Dev Biol, 21, 944-950.  
  20371474 D.N.Amin, N.Sergina, D.Ahuja, M.McMahon, J.A.Blair, D.Wang, B.Hann, K.M.Koch, K.M.Shokat, and M.M.Moasser (2010).
Resiliency and vulnerability in the HER2-HER3 tumorigenic driver.
  Sci Transl Med, 2, 16ra7.  
  20168077 E.Li, and K.Hristova (2010).
Receptor tyrosine kinase transmembrane domains: Function, dimer structure and dimerization energetics.
  Cell Adh Migr, 4, 249-254.  
20430953 E.Witsch, M.Sela, and Y.Yarden (2010).
Roles for growth factors in cancer progression.
  Physiology (Bethesda), 25, 85.  
21074407 E.Zeqiraj, and D.M.van Aalten (2010).
Pseudokinases-remnants of evolution or key allosteric regulators?
  Curr Opin Struct Biol, 20, 772-781.  
  20212358 F.Cymer, and D.Schneider (2010).
Transmembrane helix-helix interactions involved in ErbB receptor signaling.
  Cell Adh Migr, 4, 299-312.  
20459566 F.F.Barros, D.G.Powe, I.O.Ellis, and A.R.Green (2010).
Understanding the HER family in breast cancer: interaction with ligands, dimerization and treatments.
  Histopathology, 56, 560-572.  
20351256 F.Shi, S.E.Telesco, Y.Liu, R.Radhakrishnan, and M.A.Lemmon (2010).
ErbB3/HER3 intracellular domain is competent to bind ATP and catalyze autophosphorylation.
  Proc Natl Acad Sci U S A, 107, 7692-7697.
PDB code: 3lmg
20432461 G.A.Kozloski, C.A.Carraway, and K.L.Carraway (2010).
Mechanistic and signaling analysis of Muc4-ErbB2 signaling module: new insights into the mechanism of ligand-independent ErbB2 activity.
  J Cell Physiol, 224, 649-657.  
21129606 G.Bronte, S.Rizzo, L.La Paglia, V.Adamo, S.Siragusa, C.Ficorella, D.Santini, V.Bazan, G.Colucci, N.Gebbia, and A.Russo (2010).
Driver mutations and differential sensitivity to targeted therapies: a new approach to the treatment of lung adenocarcinoma.
  Cancer Treat Rev, 36, S21-S29.  
20836684 G.M.Higa, V.Singh, and J.Abraham (2010).
Biological considerations and clinical applications of new HER2-targeted agents.
  Expert Rev Anticancer Ther, 10, 1497-1509.  
20676128 G.Pines, P.H.Huang, Y.Zwang, F.M.White, and Y.Yarden (2010).
EGFRvIV: a previously uncharacterized oncogenic mutant reveals a kinase autoinhibitory mechanism.
  Oncogene, 29, 5850-5860.  
20208517 I.Chung, R.Akita, R.Vandlen, D.Toomre, J.Schlessinger, and I.Mellman (2010).
Spatial control of EGF receptor activation by reversible dimerization on living cells.
  Nature, 464, 783-787.  
20071509 J.A.Bartos, J.D.Ulrich, H.Li, M.A.Beazely, Y.Chen, J.F.Macdonald, and J.W.Hell (2010).
Postsynaptic clustering and activation of Pyk2 by PSD-95.
  J Neurosci, 30, 449-463.  
20432069 J.H.Bae, and J.Schlessinger (2010).
Asymmetric tyrosine kinase arrangements in activation or autophosphorylation of receptor tyrosine kinases.
  Mol Cells, 29, 443-448.  
20022944 J.Monsey, W.Shen, P.Schlesinger, and R.Bose (2010).
Her4 and Her2/neu tyrosine kinase domains dimerize and activate in a reconstituted in vitro system.
  J Biol Chem, 285, 7035-7044.  
21119106 L.Chen, J.Placone, L.Novicky, and K.Hristova (2010).
The extracellular domain of fibroblast growth factor receptor 3 inhibits ligand-independent dimerization.
  Sci Signal, 3, ra86.  
20962278 L.Ma, J.S.Gao, Y.Guan, X.Shi, H.Zhang, M.K.Ayrapetov, Z.Zhang, L.Xu, Y.M.Hyun, M.Kim, S.Zhuang, and Y.E.Chin (2010).
Acetylation modulates prolactin receptor dimerization.
  Proc Natl Acad Sci U S A, 107, 19314-19319.  
20015198 L.Paz-Ares, D.Soulières, I.Melezínek, J.Moecks, L.Keil, T.Mok, R.Rosell, and B.Klughammer (2010).
Clinical outcomes in non-small-cell lung cancer patients with EGFR mutations: pooled analysis.
  J Cell Mol Med, 14, 51-69.  
20049516 M.Choura, F.Frikha, N.Kharrat, S.Aifa, and A.Rebaï (2010).
Investigating the function of three non-synonymous SNPs in EGFR gene: structural modelling and association with breast cancer.
  Protein J, 29, 50-54.  
21134635 M.E.Call, and J.J.Chou (2010).
A view into the blind spot: solution NMR provides new insights into signal transduction across the lipid bilayer.
  Structure, 18, 1559-1569.  
20026433 M.J.Eck, and C.H.Yun (2010).
Structural and mechanistic underpinnings of the differential drug sensitivity of EGFR mutations in non-small cell lung cancer.
  Biochim Biophys Acta, 1804, 559-566.  
20406974 M.J.Lazzara, K.Lane, R.Chan, P.J.Jasper, M.B.Yaffe, P.K.Sorger, T.Jacks, B.G.Neel, and D.A.Lauffenburger (2010).
Impaired SHP2-mediated extracellular signal-regulated kinase activation contributes to gefitinib sensitivity of lung cancer cells with epidermal growth factor receptor-activating mutations.
  Cancer Res, 70, 3843-3850.  
20179223 M.R.Campbell, D.Amin, and M.M.Moasser (2010).
HER3 comes of age: new insights into its functions and role in signaling, tumor biology, and cancer therapy.
  Clin Cancer Res, 16, 1373-1383.  
20336692 M.Rabiller, M.Getlik, S.Klüter, A.Richters, S.Tückmantel, J.R.Simard, and D.Rauh (2010).
Proteus in the world of proteins: conformational changes in protein kinases.
  Arch Pharm (Weinheim), 343, 193-206.  
20531426 M.Taipale, D.F.Jarosz, and S.Lindquist (2010).
HSP90 at the hub of protein homeostasis: emerging mechanistic insights.
  Nat Rev Mol Cell Biol, 11, 515-528.  
20459599 M.Y.Hsieh, S.Yang, M.A.Raymond-Stinz, J.S.Edwards, and B.S.Wilson (2010).
Spatio-temporal modeling of signaling protein recruitment to EGFR.
  BMC Syst Biol, 4, 57.  
20813958 P.Nagy, J.Claus, T.M.Jovin, and D.J.Arndt-Jovin (2010).
Distribution of resting and ligand-bound ErbB1 and ErbB2 receptor tyrosine kinases in living cells using number and brightness analysis.
  Proc Natl Acad Sci U S A, 107, 16524-16529.  
19951361 P.Sánchez-González, K.Jellali, and A.Villalobo (2010).
Calmodulin-mediated regulation of the epidermal growth factor receptor.
  FEBS J, 277, 327-342.  
20933094 P.Sanchez-Soria, and T.D.Camenisch (2010).
ErbB signaling in cardiac development and disease.
  Semin Cell Dev Biol, 21, 929-935.  
20421461 S.S.Taylor, and A.P.Kornev (2010).
Yet another "active" pseudokinase, Erb3.
  Proc Natl Acad Sci U S A, 107, 8047-8048.  
19922469 T.Mitsudomi, and Y.Yatabe (2010).
Epidermal growth factor receptor in relation to tumor development: EGFR gene and cancer.
  FEBS J, 277, 301-308.  
21134645 T.N.Lombana, N.Echols, M.C.Good, N.D.Thomsen, H.L.Ng, A.E.Greenstein, A.M.Falick, D.S.King, and T.Alber (2010).
Allosteric activation mechanism of the Mycobacterium tuberculosis receptor Ser/Thr protein kinase, PknB.
  Structure, 18, 1667-1677.
PDB code: 3orm
20493519 T.Nakakuki, M.R.Birtwistle, Y.Saeki, N.Yumoto, K.Ide, T.Nagashima, L.Brusch, B.A.Ogunnaike, M.Okada-Hatakeyama, and B.N.Kholodenko (2010).
Ligand-specific c-Fos expression emerges from the spatiotemporal control of ErbB network dynamics.
  Cell, 141, 884-896.  
20979614 V.Prieto-Echagüe, A.Gucwa, D.A.Brown, and W.T.Miller (2010).
Regulation of Ack1 localization and activity by the amino-terminal SAM domain.
  BMC Biochem, 11, 42.  
20421427 Y.Frosi, S.Anastasi, C.Ballarò, G.Varsano, L.Castellani, E.Maspero, S.Polo, S.Alemà, and O.Segatto (2010).
A two-tiered mechanism of EGFR inhibition by RALT/MIG6 via kinase suppression and receptor degradation.
  J Cell Biol, 189, 557-571.  
19186126 A.Dixit, A.Torkamani, N.J.Schork, and G.Verkhivker (2009).
Computational modeling of structurally conserved cancer mutations in the RET and MET kinases: the impact on protein structure, dynamics, and stability.
  Biophys J, 96, 858-874.  
19714203 A.Dixit, and G.M.Verkhivker (2009).
Hierarchical modeling of activation mechanisms in the ABL and EGFR kinase domains: thermodynamic and mechanistic catalysts of kinase activation by cancer mutations.
  PLoS Comput Biol, 5, e1000487.  
19834613 A.Dixit, L.Yi, R.Gowthaman, A.Torkamani, N.J.Schork, and G.M.Verkhivker (2009).
Sequence and structure signatures of cancer mutation hotspots in protein kinases.
  PLoS One, 4, e7485.  
19680293 A.F.Gazdar (2009).
Activating and resistance mutations of EGFR in non-small-cell lung cancer: role in clinical response to EGFR tyrosine kinase inhibitors.
  Oncogene, 28, S24-S31.  
19114556 A.Gárriz, H.Qiu, M.Dey, E.J.Seo, T.E.Dever, and A.G.Hinnebusch (2009).
A network of hydrophobic residues impeding helix alphaC rotation maintains latency of kinase Gcn2, which phosphorylates the alpha subunit of translation initiation factor 2.
  Mol Cell Biol, 29, 1592-1607.  
19173306 A.Papakyriakou, D.Vourloumis, F.Tzortzatou-Stathopoulou, and M.Karpusas (2009).
Conformational dynamics of the EGFR kinase domain reveals structural features involved in activation.
  Proteins, 76, 375-386.  
19081671 A.Torkamani, G.Verkhivker, and N.J.Schork (2009).
Cancer driver mutations in protein kinase genes.
  Cancer Lett, 281, 117-127.  
19079236 A.V.Korennykh, P.F.Egea, A.A.Korostelev, J.Finer-Moore, C.Zhang, K.M.Shokat, R.M.Stroud, and P.Walter (2009).
The unfolded protein response signals through high-order assembly of Ire1.
  Nature, 457, 687-693.
PDB code: 3fbv
19305428 B.M.Chung, M.Dimri, M.George, A.L.Reddi, G.Chen, V.Band, and H.Band (2009).
The role of cooperativity with Src in oncogenic transformation mediated by non-small cell lung cancer-associated EGF receptor mutants.
  Oncogene, 28, 1821-1832.  
19948031 B.M.Chung, S.M.Raja, R.J.Clubb, C.Tu, M.George, V.Band, and H.Band (2009).
Aberrant trafficking of NSCLC-associated EGFR mutants through the endocytic recycling pathway promotes interaction with Src.
  BMC Cell Biol, 10, 84.  
19334696 B.Zhou, and C.F.Wong (2009).
A computational study of the phosphorylation mechanism of the insulin receptor tyrosine kinase.
  J Phys Chem A, 113, 5144-5150.  
19518076 C.Qiu, M.K.Tarrant, T.Boronina, P.A.Longo, J.M.Kavran, R.N.Cole, P.A.Cole, and D.J.Leahy (2009).
In vitro enzymatic characterization of near full length EGFR in activated and inhibited states.
  Biochemistry, 48, 6624-6632.  
19098003 D.Tvorogov, M.Sundvall, K.Kurppa, M.Hollmén, S.Repo, M.S.Johnson, and K.Elenius (2009).
Somatic mutations of ErbB4: selective loss-of-function phenotype affecting signal transduction pathways in cancer.
  J Biol Chem, 284, 5582-5591.  
19236156 E.A.Hopper-Borge, R.E.Nasto, V.Ratushny, L.M.Weiner, E.A.Golemis, and I.Astsaturov (2009).
Mechanisms of tumor resistance to EGFR-targeted therapies.
  Expert Opin Ther Targets, 13, 339-362.  
19610074 E.E.Thompson, A.P.Kornev, N.Kannan, C.Kim, L.F.Ten Eyck, and S.S.Taylor (2009).
Comparative surface geometry of the protein kinase family.
  Protein Sci, 18, 2016-2026.
PDB code: 3fjq
19941624 E.Santos Macedo, H.G.Cardoso, A.Hernández, A.A.Peixe, A.Polidoros, A.Ferreira, A.Cordeiro, and B.Arnholdt-Schmitt (2009).
Physiologic responses and gene diversity indicate olive alternative oxidase as a potential source for markers involved in efficient adventitious root induction.
  Physiol Plant, 137, 532-552.  
19658168 E.Stuttfeld, and K.Ballmer-Hofer (2009).
Structure and function of VEGF receptors.
  IUBMB Life, 61, 915-922.  
19513107 E.Zeqiraj, B.M.Filippi, S.Goldie, I.Navratilova, J.Boudeau, M.Deak, D.R.Alessi, and D.M.van Aalten (2009).
ATP and MO25alpha regulate the conformational state of the STRADalpha pseudokinase and activation of the LKB1 tumour suppressor.
  PLoS Biol, 7, e1000126.
PDB code: 3gni
19717441 H.He, T.Yang, J.R.Terman, and X.Zhang (2009).
Crystal structure of the plexin A3 intracellular region reveals an autoinhibited conformation through active site sequestration.
  Proc Natl Acad Sci U S A, 106, 15610-15615.
PDB code: 3ig3
19536107 J.Baselga, and S.M.Swain (2009).
Novel anticancer targets: revisiting ERBB2 and discovering ERBB3.
  Nat Rev Cancer, 9, 463-475.  
19564486 J.Dackor, K.M.Caron, and D.W.Threadgill (2009).
Placental and embryonic growth restriction in mice with reduced function epidermal growth factor receptor alleles.
  Genetics, 183, 207-218.  
19336395 J.L.Macdonald-Obermann, and L.J.Pike (2009).
The intracellular juxtamembrane domain of the epidermal growth factor (EGF) receptor is responsible for the allosteric regulation of EGF binding.
  J Biol Chem, 284, 13570-13576.  
19196031 J.L.Macdonald-Obermann, and L.J.Pike (2009).
Palmitoylation of the EGF receptor impairs signal transduction and abolishes high-affinity ligand binding.
  Biochemistry, 48, 2505-2513.  
19531499 J.Tong, P.Taylor, S.M.Peterman, A.Prakash, and M.F.Moran (2009).
Epidermal growth factor receptor phosphorylation sites Ser991 and Tyr998 are implicated in the regulation of receptor endocytosis and phosphorylations at Ser1039 and Thr1041.
  Mol Cell Proteomics, 8, 2131-2144.  
19394300 J.Zhu, B.H.Luo, P.Barth, J.Schonbrun, D.Baker, and T.A.Springer (2009).
The structure of a receptor with two associating transmembrane domains on the cell surface: integrin alphaIIbbeta3.
  Mol Cell, 34, 234-249.  
19244618 K.Huang, Y.H.Wang, A.Brown, and G.Sun (2009).
Identification of N-terminal lobe motifs that determine the kinase activity of the catalytic domains and regulatory strategies of Src and Csk protein tyrosine kinases.
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19135477 K.J.Wilson, J.L.Gilmore, J.Foley, M.A.Lemmon, and D.J.Riese (2009).
Functional selectivity of EGF family peptide growth factors: implications for cancer.
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  20357902 K.L.Carraway, and G.A.Kozloski (2009).
Conformational changes in receptor tyrosine kinase signaling: an ErbB garden of delights.
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19171934 K.S.Yang, M.X.Ilagan, D.Piwnica-Worms, and L.J.Pike (2009).
Luciferase fragment complementation imaging of conformational changes in the epidermal growth factor receptor.
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19296866 L.N.Johnson (2009).
Protein kinase inhibitors: contributions from structure to clinical compounds.
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19759520 L.Regales, Y.Gong, R.Shen, E.de Stanchina, I.Vivanco, A.Goel, J.A.Koutcher, M.Spassova, O.Ouerfelli, I.K.Mellinghoff, M.F.Zakowski, K.A.Politi, and W.Pao (2009).
Dual targeting of EGFR can overcome a major drug resistance mutation in mouse models of EGFR mutant lung cancer.
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19360175 L.Tao, C.S.Kaddis, R.R.Ogorzalek Loo, G.N.Grover, J.A.Loo, and H.D.Maynard (2009).
Synthetic approach to homodimeric protein-polymer conjugates.
  Chem Commun (Camb), (), 2148-2150.  
19038249 M.A.Lemmon (2009).
Ligand-induced ErbB receptor dimerization.
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19489734 M.K.Tarrant, and P.A.Cole (2009).
The chemical biology of protein phosphorylation.
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19687304 M.Nishimura, M.S.Shin, P.Singhirunnusorn, S.Suzuki, M.Kawanishi, K.Koizumi, I.Saiki, and H.Sakurai (2009).
TAK1-mediated serine/threonine phosphorylation of epidermal growth factor receptor via p38/extracellular signal-regulated kinase: NF-{kappa}B-independent survival pathways in tumor necrosis factor alpha signaling.
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19560417 M.Red Brewer, S.H.Choi, D.Alvarado, K.Moravcevic, A.Pozzi, M.A.Lemmon, and G.Carpenter (2009).
The juxtamembrane region of the EGF receptor functions as an activation domain.
  Mol Cell, 34, 641-651.
PDB code: 3gop
19060928 M.Scaltriti, C.Verma, M.Guzman, J.Jimenez, J.L.Parra, K.Pedersen, D.J.Smith, S.Landolfi, S.Ramon y Cajal, J.Arribas, and J.Baselga (2009).
Lapatinib, a HER2 tyrosine kinase inhibitor, induces stabilization and accumulation of HER2 and potentiates trastuzumab-dependent cell cytotoxicity.
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19563760 N.Jura, N.F.Endres, K.Engel, S.Deindl, R.Das, M.H.Lamers, D.E.Wemmer, X.Zhang, and J.Kuriyan (2009).
Mechanism for activation of the EGF receptor catalytic domain by the juxtamembrane segment.
  Cell, 137, 1293-1307.
PDB code: 3gt8
20007378 N.Jura, Y.Shan, X.Cao, D.E.Shaw, and J.Kuriyan (2009).
Structural analysis of the catalytically inactive kinase domain of the human EGF receptor 3.
  Proc Natl Acad Sci U S A, 106, 21608-21613.
PDB code: 3kex
19527647 P.Sengupta, E.Bosis, E.Nachliel, M.Gutman, S.O.Smith, G.Mihályné, I.Zaitseva, and S.McLaughlin (2009).
EGFR juxtamembrane domain, membranes, and calmodulin: kinetics of their interaction.
  Biophys J, 96, 4887-4895.  
18761339 R.Bose, and X.Zhang (2009).
The ErbB kinase domain: structural perspectives into kinase activation and inhibition.
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19289058 S.E.Telesco, and R.Radhakrishnan (2009).
Atomistic insights into regulatory mechanisms of the HER2 tyrosine kinase domain: a molecular dynamics study.
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19762468 S.Mahapatra, H.Mehta, S.B.Woo, and K.E.Neet (2009).
Identification of critical residues within the conserved and specificity patches of nerve growth factor leading to survival or differentiation.
  J Biol Chem, 284, 33600-33613.  
19009236 S.Y.Zhao, Y.Sun, Z.S.Lai, Q.Z.Nan, K.Li, and Z.S.Zhang (2009).
Inhibition of migration and invasion of colorectal cancer cells via deletion of Rac1 with RNA interference.
  Mol Cell Biochem, 322, 179-184.  
19627157 T.E.Balius, and R.C.Rizzo (2009).
Quantitative prediction of fold resistance for inhibitors of EGFR.
  Biochemistry, 48, 8435-8448.  
19727074 T.Rajakulendran, M.Sahmi, M.Lefrançois, F.Sicheri, and M.Therrien (2009).
A dimerization-dependent mechanism drives RAF catalytic activation.
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19237555 T.Takaki, A.Echalier, N.R.Brown, T.Hunt, J.A.Endicott, and M.E.Noble (2009).
The structure of CDK4/cyclin D3 has implications for models of CDK activation.
  Proc Natl Acad Sci U S A, 106, 4171-4176.
PDB code: 3g33
19718043 V.Hindie, A.Stroba, H.Zhang, L.A.Lopez-Garcia, L.Idrissova, S.Zeuzem, D.Hirschberg, F.Schaeffer, T.J.Jørgensen, M.Engel, P.M.Alzari, and R.M.Biondi (2009).
Structure and allosteric effects of low-molecular-weight activators on the protein kinase PDK1.
  Nat Chem Biol, 5, 758-764.
PDB codes: 3hrc 3hrf
18990695 X.Gao, M.Lorinczi, K.S.Hill, N.C.Brooks, H.Dokainish, K.Ireton, and L.A.Elferink (2009).
Met receptor tyrosine kinase degradation is altered in response to the leucine-rich repeat of the Listeria invasion protein internalin B.
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19028587 X.Huang, P.Finerty, J.R.Walker, C.Butler-Cole, M.Vedadi, M.Schapira, S.A.Parker, B.E.Turk, D.A.Thompson, and S.Dhe-Paganon (2009).
Structural insights into the inhibited states of the Mer receptor tyrosine kinase.
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PDB codes: 2p0c 3bpr 3brb
19141286 X.Min, R.Akella, H.He, J.M.Humphreys, S.E.Tsutakawa, S.J.Lee, J.A.Tainer, M.H.Cobb, and E.J.Goldsmith (2009).
The structure of the MAP2K MEK6 reveals an autoinhibitory dimer.
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PDB code: 3enm
19357077 Y.J.Xu, and T.J.Kelly (2009).
Autoinhibition and autoactivation of the DNA replication checkpoint kinase cds1.
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19015641 Z.Tang, S.Jiang, R.Du, E.T.Petri, A.El-Telbany, P.S.Chan, T.Kijima, S.Dietrich, K.Matsui, M.Kobayashi, S.Sasada, N.Okamoto, H.Suzuki, K.Kawahara, T.Iwasaki, K.Nakagawa, I.Kawase, J.G.Christensen, T.Hirashima, B.Halmos, R.Salgia, T.J.Boggon, J.A.Kern, and P.C.Ma (2009).
Disruption of the EGFR E884-R958 ion pair conserved in the human kinome differentially alters signaling and inhibitor sensitivity.
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19396377 A.J.Shih, J.Purvis, and R.Radhakrishnan (2008).
Molecular systems biology of ErbB1 signaling: bridging the gap through multiscale modeling and high-performance computing.
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18221311 A.L.Shrout, E.A.Esposito, and R.M.Weis (2008).
Template-directed assembly of signaling proteins: a novel drug screening and research tool.
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18570899 A.Whitty, and T.V.Riera (2008).
New ways to target old receptors.
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18282484 B.E.Turk (2008).
Understanding and exploiting substrate recognition by protein kinases.
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18227510 C.H.Yun, K.E.Mengwasser, A.V.Toms, M.S.Woo, H.Greulich, K.K.Wong, M.Meyerson, and M.J.Eck (2008).
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP.
  Proc Natl Acad Sci U S A, 105, 2070-2075.
PDB codes: 2jit 2jiu 2jiv
18193092 C.Q.Cai, Y.Peng, M.T.Buckley, J.Wei, F.Chen, L.Liebes, W.L.Gerald, M.R.Pincus, I.Osman, and P.Lee (2008).
Epidermal growth factor receptor activation in prostate cancer by three novel missense mutations.
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18334220 C.Qiu, M.K.Tarrant, S.H.Choi, A.Sathyamurthy, R.Bose, S.Banjade, A.Pal, W.G.Bornmann, M.A.Lemmon, P.A.Cole, and D.J.Leahy (2008).
Mechanism of activation and inhibition of the HER4/ErbB4 kinase.
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PDB codes: 3bbt 3bbw 3bce
18454306 D.F.Stern (2008).
ERBB3/HER3 and ERBB2/HER2 duet in mammary development and breast cancer.
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18287036 E.R.Wood, L.M.Shewchuk, B.Ellis, P.Brignola, R.L.Brashear, T.R.Caferro, S.H.Dickerson, H.D.Dickson, K.H.Donaldson, M.Gaul, R.J.Griffin, A.M.Hassell, B.Keith, R.Mullin, K.G.Petrov, M.J.Reno, D.W.Rusnak, S.M.Tadepalli, J.C.Ulrich, C.D.Wagner, D.E.Vanderwall, A.G.Waterson, J.D.Williams, W.L.White, and D.E.Uehling (2008).
6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases.
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PDB code: 2r4b
19111661 E.W.Debler, Y.Ma, H.S.Seo, K.C.Hsia, T.R.Noriega, G.Blobel, and A.Hoelz (2008).
A fence-like coat for the nuclear pore membrane.
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PDB codes: 3f3f 3f3g 3f3p
18404164 G.Sithanandam, and L.M.Anderson (2008).
The ERBB3 receptor in cancer and cancer gene therapy.
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19060208 H.Chen, C.F.Xu, J.Ma, A.V.Eliseenkova, W.Li, P.M.Pollock, N.Pitteloud, W.T.Miller, T.A.Neubert, and M.Mohammadi (2008).
A crystallographic snapshot of tyrosine trans-phosphorylation in action.
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PDB code: 3cly
18427122 J.J.Lammerts van Bueren, W.K.Bleeker, A.Brännström, A.von Euler, M.Jansson, M.Peipp, T.Schneider-Merck, T.Valerius, J.G.van de Winkel, and P.W.Parren (2008).
The antibody zalutumumab inhibits epidermal growth factor receptor signaling by limiting intra- and intermolecular flexibility.
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18165319 J.L.Macdonald, and L.J.Pike (2008).
Heterogeneity in EGF-binding affinities arises from negative cooperativity in an aggregating system.
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18412405 J.Purvis, V.Ilango, and R.Radhakrishnan (2008).
Role of network branching in eliciting differential short-term signaling responses in the hypersensitive epidermal growth factor receptor mutants implicated in lung cancer.
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18394559 J.Schmiedel, A.Blaukat, S.Li, T.Knöchel, and K.M.Ferguson (2008).
Matuzumab binding to EGFR prevents the conformational rearrangement required for dimerization.
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PDB codes: 3c08 3c09
18573086 K.M.Ferguson (2008).
Structure-based view of epidermal growth factor receptor regulation.
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18771282 L.Z.Mi, M.J.Grey, N.Nishida, T.Walz, C.Lu, and T.A.Springer (2008).
Functional and structural stability of the epidermal growth factor receptor in detergent micelles and phospholipid nanodiscs.
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HER-2-directed, small-molecule antagonists.
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18794843 M.Azam, M.A.Seeliger, N.S.Gray, J.Kuriyan, and G.Q.Daley (2008).
Activation of tyrosine kinases by mutation of the gatekeeper threonine.
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PDB codes: 3dqw 3dqx
18259690 M.J.Wieduwilt, and M.M.Moasser (2008).
The epidermal growth factor receptor family: biology driving targeted therapeutics.
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18031935 M.Landau, and N.Ben-Tal (2008).
Dynamic equilibrium between multiple active and inactive conformations explains regulation and oncogenic mutations in ErbB receptors.
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18585454 M.Peipp, M.Dechant, and T.Valerius (2008).
Effector mechanisms of therapeutic antibodies against ErbB receptors.
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18728635 O.Acuto, V.D.Bartolo, and F.Michel (2008).
Tailoring T-cell receptor signals by proximal negative feedback mechanisms.
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18365190 O.Samna Soumana, N.Garnier, and M.Genest (2008).
Insight into the recognition patterns of the ErbB receptor family transmembrane domains: heterodimerization models through molecular dynamics search.
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18775312 P.Filippakopoulos, M.Kofler, O.Hantschel, G.D.Gish, F.Grebien, E.Salah, P.Neudecker, L.E.Kay, B.E.Turk, G.Superti-Furga, T.Pawson, and S.Knapp (2008).
Structural coupling of SH2-kinase domains links Fes and Abl substrate recognition and kinase activation.
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PDB codes: 3bkb 3cbl 3cd3
18065762 R.Abdulhussein, D.H.Koo, and W.F.Vogel (2008).
Identification of disulfide-linked dimers of the receptor tyrosine kinase DDR1.
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18566585 S.Baumli, G.Lolli, E.D.Lowe, S.Troiani, L.Rusconi, A.N.Bullock, J.E.Debreczeni, S.Knapp, and L.N.Johnson (2008).
The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation.
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PDB codes: 2ivx 3blh 3blq 3blr
17890389 S.E.Webb, S.K.Roberts, S.R.Needham, C.J.Tynan, D.J.Rolfe, M.D.Winn, D.T.Clarke, R.Barraclough, and M.L.Martin-Fernandez (2008).
Single-molecule imaging and fluorescence lifetime imaging microscopy show different structures for high- and low-affinity epidermal growth factor receptors in A431 cells.
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18275813 S.Li, P.Kussie, and K.M.Ferguson (2008).
Structural basis for EGF receptor inhibition by the therapeutic antibody IMC-11F8.
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PDB codes: 3b2u 3b2v
18762250 X.Li, Y.Huang, J.Jiang, and S.J.Frank (2008).
ERK-dependent threonine phosphorylation of EGF receptor modulates receptor downregulation and signaling.
  Cell Signal, 20, 2145-2155.  
17653080 Y.N.Fu, C.L.Yeh, H.H.Cheng, C.H.Yang, S.F.Tsai, S.F.Huang, and Y.R.Chen (2008).
EGFR mutants found in non-small cell lung cancer show different levels of sensitivity to suppression of Src: implications in targeting therapy.
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18039657 Y.X.Fan, L.Wong, J.Ding, N.A.Spiridonov, R.C.Johnson, and G.R.Johnson (2008).
Mutational activation of ErbB2 reveals a new protein kinase autoinhibition mechanism.
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17496912 A.Clapéron, and M.Therrien (2007).
KSR and CNK: two scaffolds regulating RAS-mediated RAF activation.
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17242402 A.E.Greenstein, N.Echols, T.N.Lombana, D.S.King, and T.Alber (2007).
Allosteric activation by dimerization of the PknD receptor Ser/Thr protein kinase from Mycobacterium tuberculosis.
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17199039 A.E.Kelly, S.C.Sampath, T.A.Maniar, E.M.Woo, B.T.Chait, and H.Funabiki (2007).
Chromosomal enrichment and activation of the aurora B pathway are coupled to spatially regulate spindle assembly.
  Dev Cell, 12, 31-43.  
17349580 C.H.Yun, T.J.Boggon, Y.Li, M.S.Woo, H.Greulich, M.Meyerson, and M.J.Eck (2007).
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity.
  Cancer Cell, 11, 217-227.
PDB codes: 2itn 2ito 2itp 2itq 2itt 2itu 2itv 2itw 2itx 2ity 2itz 2j6m
17280834 C.W.Ward, M.C.Lawrence, V.A.Streltsov, T.E.Adams, and N.M.McKern (2007).
The insulin and EGF receptor structures: new insights into ligand-induced receptor activation.
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17339316 D.F.McCole, A.Truong, M.Bunz, and K.E.Barrett (2007).
Consequences of direct versus indirect activation of epidermal growth factor receptor in intestinal epithelial cells are dictated by protein-tyrosine phosphatase 1B.
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17254971 D.Guo, Y.C.Tan, D.Wang, K.S.Madhusoodanan, Y.Zheng, T.Maack, J.J.Zhang, and X.Y.Huang (2007).
A Rac-cGMP signaling pathway.
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18059449 D.J.Leahy (2007).
A monkey wrench in the kinase machine.
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Mutational activation of ErbB family receptor tyrosine kinases: insights into mechanisms of signal transduction and tumorigenesis.
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17613438 D.Li, T.Shimamura, H.Ji, L.Chen, H.J.Haringsma, K.McNamara, M.C.Liang, S.A.Perera, S.Zaghlul, C.L.Borgman, S.Kubo, M.Takahashi, Y.Sun, L.R.Chirieac, R.F.Padera, N.I.Lindeman, P.A.Jänne, R.K.Thomas, M.L.Meyerson, M.J.Eck, J.A.Engelman, G.I.Shapiro, and K.K.Wong (2007).
Bronchial and peripheral murine lung carcinomas induced by T790M-L858R mutant EGFR respond to HKI-272 and rapamycin combination therapy.
  Cancer Cell, 12, 81-93.  
17314037 E.M.Bublil, and Y.Yarden (2007).
The EGF receptor family: spearheading a merger of signaling and therapeutics.
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17167796 G.M.Verkhivker (2007).
In silico profiling of tyrosine kinases binding specificity and drug resistance using Monte Carlo simulations with the ensembles of protein kinase crystal structures.
  Biopolymers, 85, 333-348.  
17173284 G.M.Verkhivker (2007).
Computational proteomics of biomolecular interactions in the sequence and structure space of the tyrosine kinome: deciphering the molecular basis of the kinase inhibitors selectivity.
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17537753 G.M.Verkhivker (2007).
Exploring sequence-structure relationships in the tyrosine kinome space: functional classification of the binding specificity mechanisms for cancer therapeutics.
  Bioinformatics, 23, 1919-1926.  
18059446 I.Amit, R.Wides, and Y.Yarden (2007).
Evolvable signaling networks of receptor tyrosine kinases: relevance of robustness to malignancy and to cancer therapy.
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18075577 J.Kuriyan, and D.Eisenberg (2007).
The origin of protein interactions and allostery in colocalization.
  Nature, 450, 983-990.  
17373877 J.L.Nakamura (2007).
The epidermal growth factor receptor in malignant gliomas: pathogenesis and therapeutic implications.
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17697999 J.P.Dawson, Z.Bu, and M.A.Lemmon (2007).
Ligand-induced structural transitions in ErbB receptor extracellular domains.
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17254961 J.Settleman (2007).
PAK-in' up cGMP for the move.
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18042729 K.W.Thiel, and G.Carpenter (2007).
Epidermal growth factor receptor juxtamembrane region regulates allosteric tyrosine kinase activation.
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17355866 M.A.Seeliger, B.Nagar, F.Frank, X.Cao, M.N.Henderson, and J.Kuriyan (2007).
c-Src binds to the cancer drug imatinib with an inactive Abl/c-Kit conformation and a distributed thermodynamic penalty.
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PDB code: 2oiq
17306385 M.Katz, I.Amit, and Y.Yarden (2007).
Regulation of MAPKs by growth factors and receptor tyrosine kinases.
  Biochim Biophys Acta, 1773, 1161-1176.  
17877814 M.M.de Gunst, M.I.Gallegos-Ruiz, G.Giaccone, and J.A.Rodriguez (2007).
Functional analysis of cancer-associated EGFR mutants using a cellular assay with YFP-tagged EGFR intracellular domain.
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17920260 M.Mapelli, and A.Musacchio (2007).
MAD contortions: conformational dimerization boosts spindle checkpoint signaling.
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17529991 M.Yang, J.C.Culhane, L.M.Szewczuk, C.B.Gocke, C.A.Brautigam, D.R.Tomchick, M.Machius, P.A.Cole, and H.Yu (2007).
Structural basis of histone demethylation by LSD1 revealed by suicide inactivation.
  Nat Struct Mol Biol, 14, 535-539.
PDB code: 2uxn
17981505 N.V.Sergina, and M.M.Moasser (2007).
The HER family and cancer: emerging molecular mechanisms and therapeutic targets.
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17468161 P.Liu, T.Sudhaharan, R.M.Koh, L.C.Hwang, S.Ahmed, I.N.Maruyama, and T.Wohland (2007).
Investigation of the dimerization of proteins from the epidermal growth factor receptor family by single wavelength fluorescence cross-correlation spectroscopy.
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17197699 P.Rellos, F.J.Ivins, J.E.Baxter, A.Pike, T.J.Nott, D.M.Parkinson, S.Das, S.Howell, O.Fedorov, Q.Y.Shen, A.M.Fry, S.Knapp, and S.J.Smerdon (2007).
Structure and regulation of the human Nek2 centrosomal kinase.
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PDB code: 2jav
17227773 P.Sengupta, M.J.Ruano, F.Tebar, U.Golebiewska, I.Zaitseva, C.Enrich, S.McLaughlin, and A.Villalobo (2007).
Membrane-permeable calmodulin inhibitors (e.g. W-7/W-13) bind to membranes, changing the electrostatic surface potential: dual effect of W-13 on epidermal growth factor receptor activation.
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17274834 R.Landgraf (2007).
HER2 therapy. HER2 (ERBB2): functional diversity from structurally conserved building blocks.
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17599051 S.Anastasi, M.F.Baietti, Y.Frosi, S.Alemà, and O.Segatto (2007).
The evolutionarily conserved EBR module of RALT/MIG6 mediates suppression of the EGFR catalytic activity.
  Oncogene, 26, 7833-7846.  
17512407 S.Deindl, T.A.Kadlecek, T.Brdicka, X.Cao, A.Weiss, and J.Kuriyan (2007).
Structural basis for the inhibition of tyrosine kinase activity of ZAP-70.
  Cell, 129, 735-746.
PDB code: 2ozo
16953218 S.H.Choi, J.M.Mendrola, and M.A.Lemmon (2007).
EGF-independent activation of cell-surface EGF receptors harboring mutations found in gefitinib-sensitive lung cancer.
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17306972 S.R.Hubbard, and W.T.Miller (2007).
Receptor tyrosine kinases: mechanisms of activation and signaling.
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18046415 X.Zhang, K.A.Pickin, R.Bose, N.Jura, P.A.Cole, and J.Kuriyan (2007).
Inhibition of the EGF receptor by binding of MIG6 to an activating kinase domain interface.
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PDB codes: 2rf9 2rfd 2rfe
17273938 Y.Liu, J.Purvis, A.Shih, J.Weinstein, N.Agrawal, and R.Radhakrishnan (2007).
A multiscale computational approach to dissect early events in the Erb family receptor mediated activation, differential signaling, and relevance to oncogenic transformations.
  Ann Biomed Eng, 35, 1012-1025.  
17081964 E.E.Matthews, M.Zoonens, and D.M.Engelman (2006).
Dynamic helix interactions in transmembrane signaling.
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16879967 J.Boudeau, D.Miranda-Saavedra, G.J.Barton, and D.R.Alessi (2006).
Emerging roles of pseudokinases.
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17084073 M.G.Gold, D.Barford, and D.Komander (2006).
Lining the pockets of kinases and phosphatases.
  Curr Opin Struct Biol, 16, 693-701.  
16843261 N.E.Hynes, and T.Schlange (2006).
Targeting ADAMS and ERBBs in lung cancer.
  Cancer Cell, 10, 7.  
16928683 P.P.Knowles, J.Murray-Rust, S.Kjaer, R.P.Scott, S.Hanrahan, M.Santoro, C.F.Ibáñez, and N.Q.McDonald (2006).
Structure and chemical inhibition of the RET tyrosine kinase domain.
  J Biol Chem, 281, 33577-33587.
PDB codes: 2ivs 2ivt 2ivu 2ivv
17079130 P.Pellicena, and J.Kuriyan (2006).
Protein-protein interactions in the allosteric regulation of protein kinases.
  Curr Opin Struct Biol, 16, 702-709.  
17026767 R.A.Stein, and J.V.Staros (2006).
Insights into the evolution of the ErbB receptor family and their ligands from sequence analysis.
  BMC Evol Biol, 6, 79.  
17085043 R.Bose, M.A.Holbert, K.A.Pickin, and P.A.Cole (2006).
Protein tyrosine kinase-substrate interactions.
  Curr Opin Struct Biol, 16, 668-675.  
17085044 Z.Shi, K.A.Resing, and N.G.Ahn (2006).
Networks for the allosteric control of protein kinases.
  Curr Opin Struct Biol, 16, 686-692.  
The most recent references are shown first. Citation data come partly from CiteXplore and partly from an automated harvesting procedure. Note that this is likely to be only a partial list as not all journals are covered by either method. However, we are continually building up the citation data so more and more references will be included with time. Where a reference describes a PDB structure, the PDB codes are shown on the right.