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Updated: Aug 29, 2026

A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction
Published on: August 27, 2019
Mammalian target of rapamycin (mTOR) Inhibitors
1Our Lady of Mercy Cancer Center, New York Medical College, 600 East 233rd Street, Bronx, NY 10466, USA. jpd4401@aol.com
Abstract:
Current efforts in anticancer drug development are targeting key factors in cell-cycle regulation. Mammalian target of rapamycin (mTOR) is one such protein kinase that facilitates cell growth by stimulating the cell to traverse the G1 to S phase of the cell cycle. Rapamycin is the first defined inhibitor of mTOR, and the demonstration of its antitumor activity has led to great interest in this pathway as an antitumor mechanism. Analogues with better pharmacologic properties have been developed and have entered clinical trials. Human cell lines of renal cell cancer, among several other tumors, are sensitive to growth inhibition via this pathway. Ongoing clinical trials are evaluating renal cell cancer and other malignancies using therapy with mTOR inhibitors. These agents are more likely to induce growth inhibition rather than tumor regression.
Insights
New anticancer drugs target cell-cycle regulation, focusing on the mammalian target of rapamycin (mTOR) pathway. Inhibitors show promise for treating renal cell cancer by slowing tumor growth.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Anticancer drug development focuses on cell-cycle regulation.
- Mammalian target of rapamycin (mTOR) is crucial for cell growth and proliferation.
- Rapamycin, an mTOR inhibitor, has demonstrated antitumor activity.
Purpose of the Study:
- To investigate the role of mTOR pathway inhibitors in cancer treatment.
- To evaluate the efficacy of mTOR inhibitors in renal cell cancer and other malignancies.
Main Methods:
- Utilizing rapamycin and its analogues as mTOR inhibitors.
- Conducting preclinical studies on human cancer cell lines.
- Initiating clinical trials for various malignancies, including renal cell cancer.
Main Results:
- Human cell lines, including renal cell cancer, exhibit sensitivity to mTOR inhibition.
- Ongoing clinical trials are assessing mTOR inhibitors for multiple cancer types.
- These agents primarily induce growth inhibition rather than tumor regression.
Conclusions:
- The mTOR pathway is a viable target for anticancer therapies.
- mTOR inhibitors represent a promising class of drugs for managing renal cell cancer and other tumors.
- Current mTOR inhibitors are more effective at controlling tumor growth than causing regression.
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