Knowra Sirolimus Sirolimus Sirolimus is an immunosuppressant that binds FKBP12 and inhibits mechanistic target of rapamycin complex 1 (mTORC1). It is used to prevent organ-transplant rejection and treat selected cancers and rare diseases.
FKBP12 : FKBP12 is a cellular protein that binds sirolimus and forms a complex that inhibits mTORC1. Sirolimus must bind FKBP12 to create the complex that blocks its main target.
Organ transplantation : Organ transplantation is the transfer of an organ from a donor to a recipient to replace failing function. Sirolimus helps prevent immune rejection of transplanted organs.
Tacrolimus : Tacrolimus is an immunosuppressant that binds FKBP12 and inhibits calcineurin. Both drugs bind FKBP12, but tacrolimus inhibits calcineurin rather than mTORC1.
Immunosuppression : Immunosuppression is the reduction of immune-system activity, whether caused by disease, treatment, or other factors. Sirolimus lowers immune defenses, increasing susceptibility to infections and some complications.
mTORC1 : mTORC1 is a protein complex that regulates cell growth, metabolism, and protein synthesis in response to nutrients and signals. The FKBP12–sirolimus complex directly inhibits this target complex.
Kidney transplantation : Kidney transplantation is the surgical placement of a donor kidney in a person with kidney failure. Sirolimus is used in some kidney-transplant regimens, often alongside other immunosuppressants.
Cyclosporine : Cyclosporine is an immunosuppressant that binds cyclophilin and inhibits calcineurin. It suppresses T-cell activation through a different binding protein and target enzyme.
Stomatitis : Stomatitis is inflammation of the mucous lining of the mouth. Mouth ulcers and inflammation are common adverse effects of sirolimus.
mTOR signaling pathway : The mTOR signaling pathway is a network that regulates cell growth, metabolism, and survival. mTORC1 inhibition places sirolimus within this broader cellular signaling network.
Drug-eluting stent : A drug-eluting stent is an implanted vascular scaffold that releases medication to limit tissue growth inside an artery. Sirolimus-coated stents use its growth-inhibiting action to reduce restenosis.
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