mTOR inhibitors in renal cell carcinoma.
نویسندگان
چکیده
The mammalian target of rapamycin (mTOR) is a downstream effector of the PI3-K/Akt/mTOR pathway. Allosteric inhibitors of mTOR, everolimus and temsirolimus, have shown promising clinical activity in advanced renal cell carcinoma but their effect is far from durable and only a subset of patients experience substantial benefit from these agents. The PI3-K/Akt/mTOR pathway represents an intricate network of fine regulation and feedback loops, and resistance to allosteric mTOR inhibitors may be embedded within this complexity. In this article we highlight the molecular elements of the PI3-K/Akt/mTOR pathway, the clinical experience with everolimus and temsirolimus in advanced renal cell carcinoma, and the future directions in terms of sequential therapy, combinational therapy and development of novel therapeutic agents.
منابع مشابه
PI3K/Akt/mTOR and CDK4 combined inhibition enhanced apoptosis of thyroid cancer cell lines
Introduction Thyroid cancer is a malignant disease with poor prognosis. The PI3K/Akt/mTOR and Cyclin-Dependent Kinase 4 (CDK4) pathways are vital regulators of tumor cell proliferation and survival. Therefore the present study was designed to use dual inhibition of such pathways to kill thyroid cancer cells. Methods and materials The effects of each inhibitors on human ATC and...
متن کاملPI3K/Akt/mTOR and CDK4 combined inhibition enhanced apoptosis of thyroid cancer cell lines
Introduction Thyroid cancer is a malignant disease with poor prognosis. The PI3K/Akt/mTOR and Cyclin-Dependent Kinase 4 (CDK4) pathways are vital regulators of tumor cell proliferation and survival. Therefore the present study was designed to use dual inhibition of such pathways to kill thyroid cancer cells. Methods and materials The effects of each inhibitors on human ATC and...
متن کاملATP-competitive inhibitors of mTOR: new perspectives in the treatment of renal cell carcinoma.
Targeting mTOR (mammalian target of rapamycin) is an effective approach in the treatment of advanced RCC (renal cell carcinoma). Rapamycin-like drugs (rapalogues) have shown clinical activities and have been approved for the treatment of RCC. Recently, with the development of ATP-competitive inhibitors of mTOR, therapies targeting mTOR have entered a new era. Here, we discuss the biological rel...
متن کاملTreatment Options in Metastatic Renal Cell Carcinoma: Focus on mTOR Inhibitors
THE AGENTS CURRENTLY APPROVED FOR USE IN METASTATIC RENAL CELL CARCINOMA (MRCC) CAN BE DIVIDED BROADLY INTO TWO CATEGORIES: (1) vascular endothelial growth factor receptor (VEGFR)-directed therapies or (2) inhibitors of the mammalian target of rapamycin (mTOR). The latter category includes everolimus and temsirolimus, both approved for distinct indications in mRCC. Everolimus gained its approva...
متن کاملPreclinical Development Modulation of Akt/mTOR Signaling Overcomes Sunitinib Resistance in Renal and Prostate Cancer Cells
Tyrosine kinase inhibitors exhibit impressive activity against advanced renal cell carcinoma. However, recent clinical studies have shown an equivocal response to sunitinib in patients with castration-resistant prostate cancer. The tumor suppressor PTEN acts as a gatekeeper of the phosphoinositide 3-kinase (PI3K)/ Akt/mTOR cell–survival pathway. Our experiments showed that PTEN expression inver...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Therapy
دوره 8 4 شماره
صفحات -
تاریخ انتشار 2011