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Overview of Research into mTOR Inhibitors

Beibei Mao1, Qi Zhang1, Li Ma2

  • 1College of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan 250355, China.

Molecules (Basel, Switzerland)
|August 26, 2022
PubMed

Insights

Mammalian target of rapamycin (mTOR) inhibitors offer therapeutic potential for various diseases. This review details mTOR structure, pathways, and inhibitors, highlighting new directions for targeted therapies and overcoming resistance.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • The mammalian target of rapamycin (mTOR) is a key kinase in the phosphoinositide 3-kinase (PI3K)-related kinase (PIKK) family, regulating cell growth, proliferation, metabolism, and survival.
  • Dysregulated mTOR kinase activity is implicated in numerous human diseases, including cancer, inflammation, and neurological disorders.
  • mTOR inhibitors have demonstrated antiviral, anti-inflammatory, and antiproliferative effects, making them valuable research tools and therapeutic agents.

Purpose of the Study:

  • To review the structure of mTOR protein and its associated signaling pathways.
  • To analyze the structure and characteristics of various existing mTOR inhibitors.
  • To explore the therapeutic potential and future directions for mTOR-targeted therapies.

Main Methods:

  • Comprehensive literature review of mTOR structure, signaling, and inhibitor mechanisms.
  • Classification of mTOR inhibitors based on their binding sites (allosteric, ATP-competitive, dual-binding).
  • Analysis of dual-target inhibitors that engage mTOR alongside other kinases (PI3K, HDAC, ATR).

Main Results:

  • Existing mTOR inhibitors are categorized into allosteric, ATP-competitive, and dual-binding site types.
  • Dual-target inhibitors offer strategies to overcome resistance by inhibiting multiple pathways.
  • Non-rapalog allosteric inhibitors represent a promising avenue for developing novel mTORC1-specific therapeutics.

Conclusions:

  • Non-rapalog allosteric inhibitors offer new therapeutic strategies targeting mTORC1.
  • ATP-competitive inhibitors show promise for expanded indications in CNS diseases, viral infections, and inflammation.
  • Dual-binding site and dual-target inhibitors are crucial for overcoming resistance to mTOR-based therapies.
Keywords:
dual inhibitorshuman diseasesmTORmTOR inhibitors

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