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PI3K/Akt/mTOR and Ras/Raf/MEK/ERK signaling pathways inhibitors as anticancer agents: Structural and pharmacological

Vivek Asati1, Debarshi Kar Mahapatra1, Sanjay Kumar Bharti1

  • 1Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur 495009, Chhattisgarh, India.

European Journal of Medicinal Chemistry
|January 26, 2016
PubMed

Insights

This review highlights the Ras/Raf/MEK/ERK and PI3K/Akt/mTOR pathways as key targets in cancer therapy. It discusses specific and dual inhibitors, structure-activity relationships, and clinical trial progress for novel anticancer agents.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Protein kinases regulate vital cellular functions via phosphorylation.
  • Dysregulated signaling pathways, particularly PI3K, are implicated in oncogenesis.
  • The PI3K/Akt/mTOR and Ras/Raf/MEK/ERK pathways are frequently altered in cancers, promoting tumor growth and survival.

Purpose of the Study:

  • To review the Ras/Raf/MEK/ERK and PI3K/Akt/mTOR signaling pathways as therapeutic targets in cancer.
  • To explore specific and dual inhibitors targeting these pathways.
  • To discuss structure-activity relationships and inhibitors currently in clinical trials.

Main Methods:

  • Literature review of scientific publications and clinical trial data.
  • Analysis of signaling pathway dysregulation in various cancers.
  • Examination of inhibitor design, specificity, and pharmacokinetic properties.

Main Results:

  • The PI3K/Akt/mTOR and Ras/Raf/MEK/ERK pathways are crucial for cancer cell proliferation, survival, and metabolism.
  • Targeted kinase inhibitors show promise for cancer treatment.
  • Development of specific and dual inhibitors with improved properties is ongoing.

Conclusions:

  • Targeting the Ras/Raf/MEK/ERK and PI3K/Akt/mTOR pathways represents a significant therapeutic strategy in oncology.
  • Further research into kinase inhibitors, SARs, and clinical evaluation is essential for advancing cancer therapy.
Keywords:
CancerInhibitorsPI3KRasSARSignaling pathways

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