Src inhibitors: Drugs for the treatment of osteoporosis, cancer or both?

Trends in Pharmacological Sciences

Volumn 21, Issue 12, 2000, Pages 489-495

  Susva M ^a   Missbach, M ^a   Green, J ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

PROTEIN TYROSINE KINASE INHIBITOR;

ANTINEOPLASTIC ACTIVITY; CANCER; DRUG USE; HUMAN; ONCOGENE SRC; OSTEOPOROSIS; PRIORITY JOURNAL; PROTO ONCOGENE; REVIEW; TREATMENT INDICATION;

ANIMALS; BONE RESORPTION; CELL ADHESION; CELL DIVISION; CELL MOVEMENT; CELL SURVIVAL; HUMANS; MICE; NEOPLASMS; OSTEOPOROSIS; PROTO-ONCOGENE PROTEINS PP60(C-SRC); SRC-FAMILY KINASES;

EID: 0034424220     PISSN: 01656147     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0165-6147(00)01567-4     Document Type: Review

References (46)

1. Vertebrate non-receptor protein-tyrosine kinase families
2. Crystal structures of c-Src reveal features of its autoinhibitory mechanism
3. Cellular functions regulated by Src family kinases
4. Emerging therapies for osteoporosis
5. c-Src, receptor tyrosine kinases and human cancer
6. Activation of c-Src by receptor tyrosine kinases in human colon cancer cells with high metastatic potential
7. STAT3 activation by Src induces specific gene regulation and is required for cell transformation
8. Etk, a Btk family tyrosine kinase, mediates cellular transformation by linking Src to STAT3 activation
9. Non-transcriptional action of oestradiol and progestin triggers DNA synthesis
10. Src family kinases are required for integrin but not PDGF signal transduction
11. The catalytic activity of Src is dispensable for translocation to focal adhesions but controls the turnover of these structures during cell motility
12. Rho-A is critical for osteoclast podosome organization, motility, and bone resorption
13. Tyrosine kinase Src inhibitors: Mechanisms of action in potential therapeutic applications
14. PDGF, TGF-β and heterotypic cell-cell interactions mediate endothelial cell-induced recruitment of 10T1/2 cells and their differentiation to a smooth muscle fate
15. Trafficking of matrix collagens through bone-resorbing osteoclasts
16. EGF receptor signaling stimulates Src kinase phosphorylation of clathrin, influencing clathrin redistribution and EGF uptake
17. Src interacts with dynamin and synapsin in neuronal cells
18. Selective requirement for Src kinases during VEGF-induced angiogenesis and vascular permeability
19. The vesiculo-vacuolar organelle (VVO): A distinct endothelial cell structure that provides a transcellular pathway for macromolecular extravasation
20. New roles for Src kinases in control of cell survival and angiogenesis
21. TRANCE, a TNF family member, activates Akt/PKB through a signaling complex involving TRAF6 and c-Src
22. Herbimycin A induces the 20 S proteasome- and ubiquitin-dependent degradation of receptor tyrosine kinases
23. A Src SH2 selective binding compound inhibits osteoclast-mediated resorption
24. Structure-based design of an osteoclast-selective, nonpeptide src homology 2 inhibitor with in vivo antiresorptive activity
25. Design, synthesis and cocrystal structure of a nonpeptide Src SH2 domain ligand
26. Exploring the leucine-proline binding pocket of the Src SH3 domain
27. Discovery of a novel series of potent and selective substrate-based inhibitors of p60(c-Src) protein tyrosine kinase: Conformational and topographical constraints in peptide design
28. Discovery of a novel, potent and Src family selective tyrosine kinase inhibitor
29. 2-Substituted aminopyrido[2,3d]pyrimidin-7(OH)ones. Structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity
30. Substituted 5,7-diphenyl-pyrrolo(2,3d)pyrimidines: Potent inhibitors of the tyrosine kinase pp60 c-Src
31. Combinatorial target-guided ligand assembly: Identification of potent subtype-selective c-Src inhibitors
32. A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellular substrates and reduces bone resorption in vitro and in rodent models in vivo
33. Crystal structure of the Src family tyrosine kinase Hck
34. Decreased c-Src expression enhances osteoblast differentiation and bone formation
35. c-Cbl is downstream of c-Src in a signalling pathway necessary for bone resorption
36. Expression of Src family kinases and their putative substrates in the human preosteoclastic cell line FLG 29.1
37. Pyk2 in osteoclasts is an adhesion kinase, localized in the sealing zone, activated by ligation of αvβ3 integrin and phosphorylated by Src kinase
38. Impaired osteoclast function in Pyk2 knockout mice and cumulative effects in Pyk2/Src double knockout
39. Decreased tumorigenicity of a human colon adenocarcinoma cell line by an antisense expression vector specific for c-Src
40. Downregulation of vascular endothelial growth factor in a human colon carcinoma cell line transfected with an antisense expression vector specific for c-Src
41. Activating SRC mutation in a subset of advanced human colon cancers
42. Loss of p120ctn in human colorectal cancer predicts metastasis and poor survival
43. Abnormal expression of p120 correlates with poor survival in patients with bladder cancer
44. Herbimycin A, a pp60c-Src tyrosine kinase inhibitor, inhibits osteoclastic bone resorption in vitro and hypercalcemia in vivo
45. A dual inhibitor of platelet-derived growth factor β-receptor and Src kinase activity potently interferes with motogenic and mitogenic responses to PDGF in vascular smooth muscle cells. A novel candidate for prevention of vascular remodeling
46. Active recombinant human tyrosine kinase c-Yes: Expression in baculovirus system, purification, comparison to c-Src, and inhibition by a c-Src inhibitor