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Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers.
Pharmacologic Characterization of the Cloned Human Trace Amine-Associated Receptor1 (TAAR1) and Evidence for Species Differences with the Rat TAAR1
- D. Wainscott, S. Little, D. Nelson
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 January 2007
The TAAR1 receptor exhibits a pharmacologic profile uniquely different from those of classic monoaminergic receptors, consistent with the structural information that places them in a distinct family of receptors, and suggests the potential for development of TAAR-selective agonists and antagonists to study their physiologic roles.
Tissue-specific Pattern of Stress Kinase Activation in Ischemic/Reperfused Heart and Kidney*
A significant increase in DNA laddering was evident in both heart and kidney following ischemia/reperfusion and correlated with the pattern of kinase activation, supporting a link between stress kinaseactivation and apoptotic cell death in these tissues.
Transcription Factor Nuclear Factor-Kappa B is Activated in Neurons after Focal Cerebral Ischemia
It is demonstrated that transient focal cerebral ischemia results in activation ofNF-kB in neurons and supports previous observations that neuroprotective antioxidants may inhibit neuronal death by preventing the activation of NF-kB.
Critical Cytoplasmic Domains of Human Interleukin-9 Receptor α Chain in Interleukin-9-mediated Cell Proliferation and Signal Transduction*
Results suggest that cooperation or cross-talk of signaling molecules associated with different domains of IL-9Rα other than STAT3 is essential for IL- 9-mediated cell growth.
Oncogenic BRAF Deletions That Function as Homodimers and Are Sensitive to Inhibition by RAF Dimer Inhibitor LY3009120.
Oncogenic BRAF deletions with a distinct activation mechanism dependent on the BRAF dimer formation in tumor cells are discovered and LY3009120 is active against these cells and represents a potential treatment option for patients with cancer, or other atypical BRAF mutations where BRAF functions as a dimer.
Molecular cloning and pharmacological characterization of the guinea pig 5-HT1E receptor.
Cdk1 Activity Is Required for Mitotic Activation of Aurora A during G2/M Transition of Human Cells
The data suggest that Cdk1, Aurora A, and Plk1 mitotic kinases participate in a feedback activation loop and that activation of Cdk 1 initiates the feedback loop activity, leading to rapid and timely entry into mitosis in human cells.
Specificity of Interleukin-2 Receptor γ Chain Superfamily Cytokines Is Mediated by Insulin Receptor Substrate-dependent Pathway*
The role of IRS proteins in determining cytokine specificity was corroborated by their ability to interact with different downstream signaling molecules, which suggest that IRS-dependent signaling pathways work by recruiting different signaling molecules to determine specificity of IL-2Rγ superfamily cytokines.
A Novel CDK9 Inhibitor Shows Potent Antitumor Efficacy in Preclinical Hematologic Tumor Models
A potent CDK9 inhibitor is described that significantly reduces RNAP II CTD phosphorylation and dramatically decreases MCL1 protein levels to result in apoptosis in a variety of leukemia and solid tumor cell lines.