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BAY 43-9006 Exhibits Broad Spectrum Oral Antitumor Activity and Targets the RAF/MEK/ERK Pathway and Receptor Tyrosine Kinases Involved in Tumor Progression and Angiogenesis
Data demonstrate that BAY 43-9006 is a novel dual action RAF kinase and VEGFR inhibitor that targets tumor cell proliferation and tumor angiogenesis. Expand
Syk tyrosine kinase required for mouse viability and B-cell development
Analysis of syk−/− lymphoid cells showed that the syk mutation impaired the differentiation of B-lineage cells, apparently by disrupting signalling from the pre-BCR complex and thereby preventing the clonal expansion, and further maturation, of pre-B cells. Expand
BAY 80-6946 Is a Highly Selective Intravenous PI3K Inhibitor with Potent p110α and p110δ Activities in Tumor Cell Lines and Xenograft Models
BAY 80-6946 is a promising agent with differential pharmacologic and pharmacokinetic properties for the treatment of PI3K-dependent human tumors and induced 100% complete tumor regression when dosed as a single agent every second day in rats bearing HER2-amplified and PIK3CA-mutated KPL4 breast tumors. Expand
Tumor development by transgenic expression of a constitutively active insulin-like growth factor I receptor.
A novel animal model that involves transgenic expression of a fusion receptor that is constitutively activated by homodimerization is described that should provide new opportunities for further understanding how aberrant IGF-IR signaling leads to tumorigenesis and for optimizing novel antagonists of the receptor kinase. Expand
A novel assay for discovery and characterization of pro-apoptotic drugs and for monitoring apoptosis in patient sera
It is proposed that compounds that induce rapid CK18 cleavage have mechanisms of actions distinct from conventional genotoxic and microtubuli-targeting agents, and one example of an agent that induces almost immediate mitochondrial depolarization and cytochrome c release is presented. Expand
Disruption of epithelial gamma delta T cell repertoires by mutation of the Syk tyrosine kinase.
Chimeric mice in which lymphocytes are deficient in the Syk tyrosine kinase have been created, and subsets of intraepithelial gamma delta T cells are similar to B cells, but distinct from splenic gammaDelta T cells that develop and expand in Syk-deficient mice. Expand
Homoisocitric dehydrogenase from yeast.
  • B. Rowley, A. Tucci
  • Chemistry, Medicine
  • Archives of biochemistry and biophysics
  • 1 December 1970
Purified homoisocitric dehydrogenase did not catalyze the oxidation of ethanol, isocitrate, malate, or glutamate in the presence of the appropriate cofactors. Expand
Abstract C18: Assessment of Gli1 expression during skin regeneration in mouse models and normal healthy volunteers
Gli1 protein level at 24h post‐skin wounding assessed by immunohistochemistry is currently being used as a surrogate tissue pharmacodynamic measurement in a first‐in‐human multiple ascending dose trial in subjects with advanced or metastatic solid tumors. Expand
Constitutively active receptor tyrosine kinases as oncogenes in preclinical models for cancer therapeutics
This approach provides excellent cell and tumor models for the characterization of signaling properties of diverse RTKs and for the evaluation of rationally designed antagonists targeting these kinases. Expand
Constitutively Active Insulin-Like Growth Factor I Receptor Tumor Development by Transgenic Expression of a
The insulin-like growth factor I receptor (IGF-IR) is a transmembrane tyrosine kinase that is essential to growth and development and also thought to provide a survival signal for the maintenance ofExpand