LY2584702 is an orally active, ATP-competitive, potent and selective ribosomal protein S6 kinase (p70 S6 kinase, p70S6K, S6K1) inhibitor (IC50 = 4 nM; selective over 83 other kinases and 45 cell surface markers). LY2584702 inhibits HCT116 cellular S6 phosphorylation (IC50 0.1-0.24 μM) and shows anti-tumor efficacy in U87MG glioblastoma and HCT116 colon carcinoma xenograft models in vivo (2.5 mg/kg bid. po.).
Orally active, ATP-competitive, potent and selective ribosomal protein S6 kinase (p70 S6 kinase, p70S6K, S6K1) inhibitor with in vivo anti-tumor efficacy.
BRAF and MEK inhibitors have shown remarkable clinical efficacy in BRAF-mutant melanoma; however, most patients develop resistance, which limits the clinical benefit of these agents. In this study, we found that the human melanoma cell clones, A375-DR and A375-TR, with
The mechanisms that govern organelle adaptation and remodelling remain poorly defined. The endo-lysosomal system degrades cargo from various routes, including endocytosis, phagocytosis, and autophagy. For phagocytes, endosomes and lysosomes (endo-lysosomes) are kingpin organelles because they are essential to kill pathogens
Plasmodium parasites are highly selective when infecting hepatocytes and induce many changes within the host cell upon infection. While several host cell factors have been identified that are important for liver infection, our understanding of what facilitates the maintenance of
Journal of immunology (Baltimore, Md. : 1950), 203(1), 137-147 (2019-05-17)
PI3K is one of the most frequently mutated genes in cancers and has been the target of numerous anticancer therapies. With the additional development of therapeutics that mobilize the immune system, such as Abs with effector functions, bispecific Abs, and
LTB4 is an inflammatory lipid mediator mainly biosynthesized by leukocytes. Since its implication in inflammatory diseases is well recognized, many tools to regulate its biosynthesis have been developed and showed promising results in vitro and in vivo, but mixed results
