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Structural Basis for the Autoinhibition of c-Abl Tyrosine Kinase
TLDR
Crystal structures of c-Abl show that the N-terminal myristoyl modification of c -Abl 1b binds to the kinase domain and induces conformational changes that allow the SH2 and SH3 domains to dock onto it. Expand
Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571).
The inadvertent fusion of the bcr gene with the abl gene results in a constitutively active tyrosine kinase (Bcr-Abl) that transforms cells and causes chronic myelogenous leukemia. Small moleculeExpand
Mutations in the EGFR kinase domain mediate STAT3 activation via IL-6 production in human lung adenocarcinomas.
Persistently activated or tyrosine-phosphorylated STAT3 (pSTAT3) is found in 50% of lung adenocarcinomas. pSTAT3 is found in primary adenocarcinomas and cell lines harboring somatic-activatingExpand
Disabling poxvirus pathogenesis by inhibition of Abl-family tyrosine kinases
TLDR
It is shown that cell-associated enveloped virions (CEV) use Abl- and Src-family tyrosine kinases for actin motility, and that these kinases act in a redundant fashion, perhaps permitting motility in a greater range of cell types. Expand
L576P KIT mutation in anal melanomas correlates with KIT protein expression and is sensitive to specific kinase inhibition
TLDR
Results suggest that a subset of anal melanomas show activating KIT mutations, which are susceptible for therapy with specific kinase inhibitors, which is intriguing since KIT expression is downregulated in most melanomas progressing to more aggressive lesions. Expand
Gleevec inhibits β-amyloid production but not Notch cleavage
TLDR
It is demonstrated that γ-secretase generation of Aβ in an N2a cell-free system is ATP dependent, and the efficacy of STI571 in reducing Aβ without affecting Notch-1 cleavage may prove useful as a basis for developing novel therapies for Alzheimer's disease. Expand
Caenorhabditis elegans ABL-1 antagonizes p53-mediated germline apoptosis after ionizing irradiation
TLDR
It is shown that worms carrying an abl-1 deletion allele, abl- 1(ok171), are specifically hypersensitive to radiation-induced apoptosis in the Caenorhabditis elegans germ line and that C. elegans might provide tissue models for development of anticancer drugs. Expand
Gleevec inhibits beta-amyloid production but not Notch cleavage.
TLDR
It is demonstrated that gamma-secretase generation of Abeta in an N2a cell-free system is ATP dependent, and the efficacy of STI571 in reducing Abeta without affecting Notch-1 cleavage may prove useful as a basis for developing novel therapies for Alzheimer's disease. Expand
Enteropathogenic Escherichia coli use redundant tyrosine kinases to form actin pedestals.
TLDR
It is shown that Abl and Arg are sufficient for pedestal formation in the absence of other tyrosine kinase activity, but they are not necessary, and the results suggest that additional kinases that are sensitive to inhibition by PD also can suffice. Expand
Characterization of potent inhibitors of the Bcr-Abl and the c-kit receptor tyrosine kinases.
TLDR
Compared with other pyrido[2,3-d]pyrimidine analogues studied, PD166326 was the most potent inhibitor of Bcr-Abl-dependent cell growth and PD173955 inhibited kit ligand-dependent c-kit autophosphorylation and had a lesser effect on interleukin 3-dependent or granulocyte macrophage colony-stimulating factor-induced cell growth. Expand
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