西罗莫司

Sirolimus (INN/USAN), also known as rapamycin, is an immunosuppressant drug used to prevent rejection in organ transplantation;西罗莫司（INN / USAN），也被称为雷帕霉素，是一种免疫抑制剂，用于预防器官移植中的排斥反应。 it is especially useful in kidney transplants.它在肾脏移植中特别有用。 A macrolide, sirolimus was first discovered as a product of the bacterium Streptomyces hygroscopicus in a soil sample from Easter Island - an island also known as "Rapa Nui", hence the name.大环内酯类西罗莫司是作为吸水链霉菌的产物在复活节岛的一个土壤样品中发现的，该岛也被称为“ Rapa Nui”，因此得名。 It is marketed under the trade name Rapamune by Wyeth.它由惠氏以商品名Rapamune销售。
Sirolimus was originally developed as an antifungal agent.西罗莫司最初是作为抗真菌剂开发的。 However, this was abandoned when it was discovered that it had potent immunosuppressive and antiproliferative properties.然而，当发现它具有有效的免疫抑制和抗增殖特性时，它被放弃了。
The anti-proliferative effects of sirolimus may have a role in treating cancer.西罗莫司的抗增殖作用可能在治疗癌症中起作用。 Recently, it was shown that sirolimus inhibited the progression of dermal Kaposi's sarcoma in patients with renal transplants.最近，显示西罗莫司抑制肾移植患者皮肤卡波西氏肉瘤的进展。 Other mTOR inhibitors such as temsirolimus (CCI-779) or everolimus (RAD001) are being tested for use in cancers such as glioblastoma multiforme and mantle cell lymphoma.正在测试其他mTOR抑制剂，例如替西罗莫司（CCI-XNUMX）或依维莫司（RADXNUMX）在多形性胶质母细胞瘤和套细胞淋巴瘤等癌症中的使用。
Akt信号传导可促进Akt阳性淋巴瘤中的细胞存活，并起到防止化学药物如阿霉素或环磷酰胺的细胞毒性作用的作用。 Bcl-2阳性淋巴瘤对治疗完全耐药； nor are eIF4E expressing lymphomas sensitive to sirolimus.表达eIFXNUMXE的淋巴瘤对西罗莫司也不敏感。 Rapamycin showed no effect on its own.雷帕霉素本身没有作用。