MTOR inhibitors
MTOR inhibitors are a class of drugs that inhibit the mechanistic target of rapamycin (mTOR), which is a serine/threonine-specific protein kinase that belongs to the family of phosphatidylinositol-3 kinase (PI3K) related kinases (PIKKs). MTOR regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, autophagy, and transcription.
Mechanism of Action
MTOR inhibitors work by binding to the FKBP12 protein to inhibit the mTORC1 pathway. This results in a decrease in protein synthesis and cell cycle arrest, which can lead to decreased tumor growth and proliferation. Some mTOR inhibitors also inhibit the mTORC2 pathway, which can lead to further decreases in cell proliferation and survival.
Uses
MTOR inhibitors are used in the treatment of various types of cancer, including kidney cancer, breast cancer, neuroendocrine tumors, and certain types of lung cancer. They are also used in organ transplantation to prevent rejection, and in the treatment of certain rare diseases, such as tuberous sclerosis complex and lymphangioleiomyomatosis.
Side Effects
Common side effects of MTOR inhibitors include mouth sores, rash, diarrhea, fatigue, and high blood sugar levels. More serious side effects can include lung or breathing problems, infections, kidney problems, and high cholesterol levels.
Examples
Examples of MTOR inhibitors include sirolimus (Rapamune), everolimus (Afinitor), and temsirolimus (Torisel).
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