Related Experiment Video

Updated: May 8, 2026

Identification of Kinase-substrate Pairs Using High Throughput Screening
11:13

Identification of Kinase-substrate Pairs Using High Throughput Screening

Published on: August 29, 2015

Identification of two novel inhibitors of mTOR signaling pathway based on high content screening

Juming Yan1, Hongyu Zhou, Lingmei Kong

  • 1State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, 650201, China.

Cancer Chemotherapy and Pharmacology
|August 13, 2013
PubMed
Abstract

Insights

Two natural compounds, IM-1 and IM-2, were found to inhibit the mTOR signaling pathway, demonstrating significant anticancer activity by inducing cancer cell death and apoptosis. These novel inhibitors warrant further investigation as potential cancer therapeutics.

Area of Science:

  • Biochemistry and Molecular Biology
  • Oncology
  • Pharmacology

Background:

  • The mammalian target of rapamycin (mTOR) signaling pathway is crucial for cell growth, proliferation, and survival.
  • Dysregulation of mTOR signaling is implicated in cancer development and resistance to chemotherapy.
  • mTOR inhibitors are promising therapeutic agents for cancer treatment.

Purpose of the Study:

  • To identify novel inhibitors of the mTOR signaling pathway from a natural compound library.
  • To evaluate the potential of these compounds as anticancer therapeutics.

Main Methods:

  • High content screening assay based on eukaryotic initiation factor 4E (eIF4E) nuclear translocation in mouse embryonic fibroblast cells.
  • Assessment of candidate compounds in cancer cells, including Western blot analysis for phosphorylation levels, MTS assay for cytotoxicity, and flow cytometry for apoptosis.

Main Results:

  • Two compounds, 1,4-O-diferuloylsecoisolariciresinol (IM-1) and Pierreione B (IM-2), were identified.
  • Both IM-1 and IM-2 induced eIF4E nuclear translocation in cancer cells.
  • Compounds decreased phosphorylation of p70 ribosomal protein S6 kinase (S6K) and 4E-binding protein 1 (4E-BP1), leading to cytotoxicity and apoptosis.

Conclusions:

  • IM-1 and IM-2 are novel inhibitors of mTOR signaling with potent anticancer activity.
  • These compounds represent potential candidates for anticancer drug development targeting the mTOR pathway.
  • Further research into IM-1 and IM-2 is warranted for their therapeutic potential.

More Related Videos

A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction05:28

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

Published on: August 27, 2019

System for Efficacy and Cytotoxicity Screening of Inhibitors Targeting Intracellular Mycobacterium tuberculosis09:57

System for Efficacy and Cytotoxicity Screening of Inhibitors Targeting Intracellular Mycobacterium tuberculosis

Published on: April 5, 2017

Related Concept Videos

PI3K/mTOR/AKT Signaling Pathway01:22

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...
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...