Coibamide A, an Cytotoxic Depsipeptide, Induces Autophagosome Accumulation
Autophagy is the key structure of macroautophagy. Macroautophagy is an intracellular degradation system of cytoplasmic contents. Meanwhile, autophagy is a new double-membrane vesicle formed during autophagy, which can phagocytose a variety of intracellular substances. It transports this autophagic material to the lysosome for subsequent degradation. The lysosomal hydrolase degrades...
Vistusertib (AZD2014) is an ATP Competitive mTOR Inhibitor
mTOR is an atypical serine threonine kinase involved in regulating major cellular functions, such as nutrients sensing, growth, and proliferation. mTOR is part of the multiprotein complexes mTORC1 and mTORC2. mTORC1 and mTORC2 have been shown to play critical yet functionally distinct roles in the regulation of cellular processes....
Sapanisertib is an Orally Active and ATP-Dependent mTOR Inhibitor
Acute myelogenous leukemia (AML) is a heterogeneous disease. It often relapses after standard chemotherapy or proves refractory to available treatments. Therefore, It needs novel therapies for AML. In AML, many signaling pathways are abnormally activated and lead to uncontrolled proliferation/survival of immature myeloid progenitors. The 50% to 80% of...
Everolimus (RAD001), a Rapamycin Derivative, is a Selective and Orally Active mTOR1 Inhibitor
mTOR is a member of the phosphatidylinositol 3-kinase related kinase family of protein kinases. Meanwhile, mTOR is linked to other proteins and serves as the core component of two different protein complexes, mTOR complex 1 and mTOR complex 2. They regulate different cellular processes. Nonetheless, mTOR C1 phosphorylates p70...
Rapamycin is a Specific mTOR Inhibitor
mTOR (mammalian target of Rapamycin) is a protein that in humans is encoded by the mTOR gene. mTOR is a serine/threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, and transcription. In addition, mTOR links with other proteins and serves as a core...
PF-06843195 is a Selective PI3Kα Inhibitor
Phosphoinositide 3-kinases (PI3Ks) can catalyze the synthesis of the phosphatidylinositol (PI) second messengers, including PI(3)P (PIP), PI(3,4)P2 (PIP2), and PI(3,4,5)P3 (PIP3). The PI3K lipid kinase family contains three classes based on sequence homology. Class, I PI3Ks are further divided into class IA (PI3Kα, PI3Kβ, and PI3Kδ) and class IB...
RapaLink-1, a Third-Generation Bivalent mTOR Inhibitor, Combines Rapamycin with MLN0128
Glioblastoma (GBM), the most common primary brain tumor, represents one of the most aggressive cancers. The signaling from PI3K and AKT to mTOR is commonly dysregulated in GBM. But, blockade of these upstream targets minimally affects mTOR activity in glioma. Allosteric mTOR inhibitors, such as rapamycin, incompletely block mTORC1...