SH2 domain inhibition: A problem solved?

Current Opinion in Chemical Biology

Volumn 5, Issue 4, 2001, Pages 409-415

  Shakespeare, William C ^a  

^a ARIAD PHARMACEUTICALS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4' (DIPHOSPHONOMETHYL)PHENYLALANINE; ADAPTOR PROTEIN; ANTINEOPLASTIC AGENT; GROWTH FACTOR RECEPTOR BOUND PROTEIN 2; PHOSPHOTYROSINE; PROTEIN INHIBITOR; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; BINDING AFFINITY; CELL ACTIVITY; DNA TEMPLATE; DRUG DESIGN; IC 50; PROTEIN BINDING; PROTEIN STRUCTURE; REVIEW; SEQUENCE HOMOLOGY;

EID: 0035415663     PISSN: 13675931     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1367-5931(00)00222-2     Document Type: Review

References (41)

1. Targeted disruption of the c-Src proto-oncogene leads to osteopetrosis in mice
2. c-Src, receptor tyrosine kinases, and human cancer
3. Src homology-2 domains: Structure, mechanisms, and discovery
4. Recent advances in the design and synthesis of SH2 inhibitors of Src, Grb2, and ZAP-70
5. Peptidomimetic SH2 domain antagonists for targeting signal transduction
6. Progress in the development of inhibitors of SH2 domains
7. Signal transduction drug discovery: Targets, mechanisms and structure-based design
8. SH2 domains recognize specific phosphopeptide sequences
9. Structure-based design and synthesis of a novel class of Src SH2 inhibitors
10. Structure-activity relationships of a novel class of Src SH2 inhibitors
11. src SH2 domain
12. Structure-based design and solid-phase parallel synthesis of phosphorylated nonpeptides to explore hydrophobic binding at the Src SH2 domain
13. Structure-based design of novel bicyclic nonpeptide inhibitors for the Src SH2 domain
14. Synthesis of new amino acids mimicking sulfated and phosphorylated tyrosine residues
15. Preparation of fluoro- and hydroxy-4-phosphonomethyl-D,L-phenylalanine suitably protected for solid-phase synthesis of peptides containing hydrolytically stable analogues of O-phosotyrosine
16. SH2 and SH3 domains: Choreographers of multiple signaling pathways
17. c-src SH2 domains: A thermodynamic and structural study
18. The formation of a covalent complex between a dipeptide ligand and the Src SH2 domain
19. An efficient synthesis of a 4′-phosphonodifluoromethyl-3′-formyl-phenylalanine containing Src SH2 ligand
20. A Src SH2 selective binding compound inhibits osteoclast-mediated resorption
21. X-ray structure of citrate bound to Src SH2 leads to a high-affinity, bone-targeted Src SH2 inhibitor
22. Bone targeted drugs 2. Synthesis of estrogens with hydroxyapatite affinity
23. 2-bisphosphonate conjugates: Potential agents for treatment of osteoporosis
24. Bone-targeted Src SH2 inhibitors block Src cellular activity and osteoclast-mediated resorption
25. Structure-based design of a novel, osteoclast-selective, nonpeptide Src SH2 inhibitor with in vivo anti-resorptive activity
26. The SH2 and SH3 domain-containing protein Grb2 links receptor tyrosine kinases to Ras signalling
27. SH2 and SH3 domains: Potential targets for anti-cancer drug design
28. Structure-based design of compounds inhibiting Grb2-SH2 mediated protein-protein interactions in signal transduction pathways
29. SH2/SH3 signaling proteins
30. Signal transduction through MAP kinase cascades
31. 2
32. Discovery of 3-aminobenzyloxycarbonyl as an N-terminal group conferring high affinity to the minimal phosphopeptide sequence recognized by the Grb2-SH2 domian
33. Structure-based design and synthesis of high affinity tripeptide ligands of the Grb2-SH2 domain
34. Highly potent inhibitors of the Grb2-SH2 domain
35. Selective Grb2 inhibitors as anti-RAS therapy
36. Effect of potent and selective inhibitors of the Grb2 SH2 domain on cell motility
37. Phosphotyrosyl-based motifs in the structure-based design of protein-tyrosine kinase dependent signal transduction inhibitors
38. Monocarboxylic-based phosphotyrosyl mimetics in the design of Grb2 SH2 domain inhibitors
39. Synthesis of Fmoc-protected 4-carboxydifluoromethyl-L-phenylalanine: A phosphotyrosyl mimetic of potential use for signal transduction studies
40. Potent inhibition of Grb2 SH2 domain binding by non-phosphate-containing ligands
41. Inhibition of Grb2 SH2 domain binding by non-phosphate-containing ligands. 2. 4-(2-malonyl)phenylalanine as a potent phosphotyrosyl mimetic