Crystal structures of the SH2 domain of Grb2: Highlight on the binding of a new high-affinity inhibitor

Journal of Molecular Biology

Volumn 315, Issue 5, 2002, Pages 1167-1177

  Nioche, Pierre ^a   Liu, Wang Qing ^a   Broutin, Isabelle ^a   Charbonnier, Franck ^a   Latreille, Marie Thérèse ^a   Vidal, Michel ^a   Roques, Bernard ^a   Garbay, Christiane ^a   Ducruix, Arnaud ^a  

^a UNIVERSITÉ PARIS DESCARTES   (France)

Author keywords

Drug design; Grb2; Inhibitor; SH2; X ray structure

Indexed keywords

GROWTH FACTOR RECEPTOR BOUND PROTEIN 2; PEPTIDE; PROTEIN GRB2 INHIBITOR; PROTEIN INHIBITOR; PSEUDOPEPTIDE; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; COMPLEX FORMATION; CRYSTAL STRUCTURE; DRUG DESIGN; DRUG SYNTHESIS; PHOSPHORYLATION; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN BINDING; PROTEIN DOMAIN; PROTEIN PROTEIN INTERACTION; PROTEIN STRUCTURE; SIGNAL TRANSDUCTION;

EID: 0036304080     PISSN: 00222836     EISSN: None     Source Type: Journal    
DOI: 10.1006/jmbi.2001.5299     Document Type: Article

References (42)

1. SH2/SH3 signaling proteins
2. Overexpression of Grb2 in inflammatory lesions and preneoplastic foci and tumors induced by N-nitrosodimethylamine in Helicobacter hepaticus-infected and non-infected A/J mice
3. Up-regulation of the protein tyrosine phosphatase SHP-1 in human breast cancer and correlation with GRB2 expression
4. SH2 and SH3 domains as targets for anti-proliferative agents
5. Progress in the development of inhibitors of SH2 domains
6. Inhibitors of Ras signal transduction as anti-tumor agents
7. SH2 and SH3 domains: Elements that control interactions of cytoplasmic signaling proteins
8. Modular peptide recognition domains in eukaryotic signaling
9. Structural basis for specificity of Grb2-SH2 revealed by a novel ligand binding mode
10. Solution structure of the SH2 domain of Grb2 complexed with the Shc-derived phosphotyrosine-containing peptide
11. Association of the Shc and Grb2/Sem5 SH2-containing proteins is implicated in activation of the Ras pathway by tyrosine kinases
12. Formation of Shc-Grb2 complexes is necessary to induce neoplastic transformation by overexpression of Shc proteins
13. Shc contains two Grb2 binding sites needed for efficient formation of complexes with SOS in B lymphocytes
14. Structure-based design of compounds inhibiting Grb2-SH2 mediated protein-protein interactions in signal transduction pathways
15. Selective Grb2 SH2 inhibitors as anti-ras therapy
16. Potent antagonists of the SH2 domain of Grb2: Optimization of the X + 1 position of 3-Amino-Z-Tyr (PO3H2)-X + 1-Asn-NH2
17. Structure-based design of a non-peptidic antagonist of the SH2 domain of Grb2
18. Nonphosphorylated peptide ligands for the Grb2 Src homology 2 domain
19. Structural and conformational requirements for high-affinity binding to the SH2 domain of Grb2
20. Crystal structure of the mammalian Grb2 adaptor
21. Small peptides containing phosphotyrosine and adjacent alpha Me-phosphotyrosine or its mimetics as highly potent inhibitors of Grb2 SH2 domain
22. Peptide conformation and biological activity
23. Structure of the regulatory domains of the Src-family tyrosine kinase Lck
24. Dimer formation through domain swapping in the crystal structure of the Grb2-SH2-Ac-pYVNV complex
25. The SH3 domain of Eps8 exists as a novel intertwined dimer
26. Nuclear magnetic resonance solution structure of the growth factor receptor-bound protein 2 Src homology 2 domain
27. The three-dimensional solution structure of the Src homology domain-2 of the growth factor receptor-bound protein-2
28. Binding of the Grb2 SH2 domain to phosphotyrosine motifs does not change the affinity of its SH3 domains for Sos proline-rich motifs
29. SH2 domain specificity and activity modified by a single residue
30. Discovery of 3-aminobenzyloxycarbonyl as an N-terminal group conferring high affinity to the minimal phosphopeptide sequence recognized by the Grb2-SH2 domain
31. Dual specificity of src homology 2 domains for phosphotyrosine peptide ligands
32. Structure-based design, synthesis, and X-ray crystallography of a high-affinity antagonist of the Grb2-SH2 domain containing an asparagine mimetic
33. Mapping the X(+1) binding site of the Grb2-SH2 domain with alpha,alpha-disubstituted cyclic alpha-amino acids
34. Purification, stabilization, and crystallization of a modular protein: Grb2
35. Synthesis of phosphotyrosine-containing peptides and their use as substrates for protein tyrosine phosphatases
36. Synthesis and application of bis-silylethyl-derived phosphate-protected Fmoc-phosphotyrosine derivatives for peptide synthesis
37. Tetramethyl-fluoroformamidinium hexafluorophosphate: A rapid-acting reagent for solution and solid phase peptide synthesis
38. Processing of X-ray diffraction data collected in oscillation mode
39. AMoRe: A new package for molecular replacement
40. Crystallography & NMR system: A new software suite for macromolecular structure determination
41. Structural basis for the high affinity of amino-aromatic SH2 phosphopeptide ligands