Search for Inhibitors of Ras-Driven Cancers

摘要: Cancer is a leading cause of death in the developed world, resulting 500,000 deaths per year United States alone. Ras genes are mutated approximately one-third cancers that result constitutive activation signaling, which critically important oncogenic protein drives malignant transformation. Current molecular targeted therapeutics, and several development, inhibit various proteins canonical mitogen-activated kinase phosphoinositide 3-kinase/mechanistic target rapamycin effector pathways. In addition, compounds directly catalytic activity, by Son Sevenless (SOS), inactivation P120-Ras GTPase activating protein, interaction with Raf early stages development. Furthermore, process maturation localization to plasma membrane an active area drug discovery, despite setbacks from previous failed attempts suppress inhibiting farnesyl transferase. Additional selective inhibitors targets have been identified through phenotypic approaches used for including mitotic oxidative stress, apoptosis-related proteins, Ras-specific metabolic dependencies, epithelial–mesenchymal transition, other signal transduction The search Ras-selective drugs continues along many fronts.