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Related Concept Videos

mTOR Signaling and Cancer Progression03:03

mTOR Signaling and Cancer Progression

The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
mTOR Signaling and Cancer Progression03:03

mTOR Signaling and Cancer Progression

The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
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PI3K/mTOR/AKT Signaling Pathway

The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a rapamycin-insensitive companion...
Drug Discovery: Overview01:26

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Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
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Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...

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Updated: Jun 3, 2026

A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction
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A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction

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Blocking the mTOR pathway: a drug discovery perspective.

Carlos Garcia-Echeverria1

  • 1Oncology Drug Discovery and Preclinical Research, Sanofi-Aventis, Vitry-sur-Seine, France.

Biochemical Society Transactions
|March 25, 2011
PubMed
Summary
This summary is machine-generated.

Researchers are developing mammalian target of rapamycin (mTOR) kinase inhibitors for cancer therapy. These mTOR modulators offer new insights into cancer biology and show promise for clinical benefit in patients.

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Last Updated: Jun 3, 2026

A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction
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Isolation of Primary Mouse Hepatocytes for Nascent Protein Synthesis Analysis by Non-radioactive L-azidohomoalanine Labeling Method
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Published on: October 23, 2018

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Significant research has focused on discovering and developing modulators of the mammalian target of rapamycin (mTOR) kinase.
  • Numerous mTOR inhibitors with varying mechanisms and kinase selectivity profiles have emerged.
  • These inhibitors are crucial tools for understanding the role of the phosphoinositide 3-kinase/mTOR pathway in cancer.

Purpose of the Study:

  • To review the current landscape of mTOR kinase modulators.
  • To elucidate the role of mTOR and related pathway components in human cancer.
  • To highlight the clinical potential of these compounds in cancer treatment.

Main Methods:

  • Review of existing scientific literature on mTOR inhibitors.
  • Analysis of the mechanisms of action and selectivity profiles of various compounds.
  • Examination of preclinical and clinical data regarding mTOR pathway modulation in cancer.

Main Results:

  • A variety of mTOR inhibitors with diverse properties have been developed.
  • These inhibitors have enhanced understanding of mTOR pathway involvement in cancer.
  • Several mTOR inhibitors have demonstrated positive clinical outcomes in cancer patients.

Conclusions:

  • mTOR kinase modulators represent a significant advancement in cancer drug discovery.
  • Targeting the phosphoinositide 3-kinase/mTOR pathway offers therapeutic opportunities in oncology.
  • Ongoing development of mTOR inhibitors holds promise for improved cancer patient care.