The Sound of Evolution
Sirolimus/Rapamycin
Mechanism of action:
Sirolimus is an mTOR inhibitor (mammalian target of rapamycin inhibitor) and belongs to the class of macrolide immunosuppressants (macrolide immunosuppressant). After entering T cells or B cells, sirolimus first binds to intracellular FKBP12 (FK506-binding protein 12), forming a sirolimus-FKBP12 complex. This complex selectively inhibits mTORC1 (mTOR complex 1). Under normal conditions, when the IL-2 receptor (interleukin-2 receptor) on T cells and B cells binds IL-2, the mTORC1 pathway drives these cells into S phase (S phase). After sirolimus inhibits mTORC1, T cells and B cells are unable to proliferate.
Reference(s):
1. Sun SY et al. (2005). Activation of Akt and eIF4E survival pathways by rapamycin-mediated mammalian target of rapamycin inhibition. Cancer Res.
2. Chan S et al. (2004). Targeting the mammalian target of rapamycin (mTOR): a new approach to treating cancer. Br J Cancer.
3. Sehgal SN et al. (2003). Sirolimus: its discovery, biological properties, and mechanism of action. Transplant Proc.