Structure-based design of novel bicyclic nonpeptide inhibitors for the Src SH2 domain [1]

Journal of Medicinal Chemistry

Volumn 43, Issue 21, 2000, Pages 3815-3819

  Shakespeare, W C ^a   Bohacek, R S ^a   Azimioara, M D ^a   Macek, K J ^a   Luke, G P ^a   Dalgarno, D C ^a   Hatada, M H ^a   Lu, X ^a   Violette, S M ^a   Bartlett, C ^a   Sawyer, T K ^a  

^a ARIAD PHARMACEUTICALS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

PROTEIN TYROSINE KINASE; PROTEIN TYROSINE KINASE INHIBITOR;

CHEMICAL ANALYSIS; DRUG DESIGN; DRUG STRUCTURE; DRUG SYNTHESIS; LETTER; STRUCTURE ANALYSIS;

BICYCLO COMPOUNDS; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; FLUORESCENCE POLARIZATION; MODELS, MOLECULAR; SRC HOMOLOGY DOMAINS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0034687218     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0003337     Document Type: Letter

References (32)

1. Protein tyrosine kinase inhibitors as novel therapeutic agents
2. Protein tyrosine phosphatases and the control of cellular signaling responses
3. Modular binding domains in signal transduction proteins
4. Cellular functions regulated by Src family kinases
5. Requirement of phosphatidylinositol-3 kinase modification for its association with p60(src)
6. Autophosphorylation of the focal adhesion kinase, pp125 (FAK), directs SH2-dependent binding of pp60(src)
7. An RNA-binding protein associated with Src through its SH2 and SH3 domains in mitosis
8. Adhesion-induced tyrosine phosphorylation of the p130(src) substrate
9. Characterization of protein tyrosine kinases from human breast cancer: Involvement of the c-src oncogene product
10. Different pp60c-src activity in well and poorly differentiated human colon carcinomas and cell lines
11. Targeted disruption of the c-src proto-oncogene leads to osteoporosis in mice
12. Binding of a high affinity phosphotyrosyl peptide to the Src SH2 domain: Crystal structures of the complexed and peptide-free forms
13. Peptide inhibitors of Src SH3-SH2-phosphoprotein interactions
14. Recognition of a high affinity phosphotyrosyl peptide by the Src homology-2 domain of p561ck
15. Crystal structure of the phosphotyrosine recognition domain (SH2) of the v·src tyrosine kinase complexed with tyrosine phosphorylated peptides
16. Recognition of a high affinity phosphotyrosyl peptide by the Src homology 2 domain of p561ck
17. Definition and display of steric, hydrophobic and hydrogen-bonding properties of ligand binding sites in proteins using Lee and Richards accessible surface: Validation of a high-resolution graphical tool for drug design
18. Aromatic-aromatic interaction: A mechanism of protein structure stabilization
19. Weakly polar interactions in proteins
20. Structure-based design and synthesis of a novel class of Src SH2 inhibitors
21. Crystal structures of the human p561ck SH2 domain in complex with two short phosphotyrosyl peptides at 1.0 ANG. and 1.8 ANG. resolution
22. QXP: Powerful, rapid computer algorithms for structure-based design
23. Structure-based design of a novel series of nonpeptide ligands that bind to the pp60(src) SH2 domain
24. Compounds, compositions and methods for inhibiting the binding of proteins containing an SH2 domain to cognate phosphorylated proteins
25. Direct conversion of activated alcohols to azides using diphenyl phosphorazidate. A practical alternative to Mitsunobu conditions
26. Zur kenntnis des kohlenstoffringes. Uber cis-3,4-polymethylen-cyclohexanone
27. Regiospecific oxidation of methyl groups in dimethylanisoles
28. Directive effects in the bromination of bicyclic phenols
29. A fluoresence polarization based Src-SH2 binding assay
30. A Src SH2 selective binding compound inhibits osteoclast-mediated resorption
31. Structure-based design of a novel, osteoclastselective, nonpeptide Src SH2 inhibitor with in vivo antiresorptive activity