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Mechanistic target of rapamycin (mTOR) inhibitors act on a kinase that links nutrient signals to cell growth. In 1994 mTOR was identified as the mammalian protein targeted by rapamycin bound to its receptor. The kinase forms a nutrient-sensitive complex with raptor, known as mTOR complex 1 (mTORC1), and a second complex, mTOR complex 2 (mTORC2). Sirolimus and its derivative everolimus act through FK506-binding protein 12 (FKBP12) and mainly inhibit mTORC1. Catalytic-site inhibitors such as Torin 1 and AZD8055 block both complexes. With Torin 1, rapamycin-resistant functions of mTORC1 were revealed in 2009. Dual phosphoinositide 3-kinase (PI3K)/mTOR inhibitors such as dactolisib are also listed here.
PI3K/mTOR ligand-1 is a ligand targeting the PI3K/mTOR pathway, crucial for cell growth and metabolism regulation. It functions as a building block for the synthesis of PROTACs aimed at modulating PI3K/mTOR signaling. This compound is valuable in cancer research and drug discovery efforts focusing on targeted protein degradation and pathway inhibition.
