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Updated: Sep 14, 2025

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

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Innovative dual-target AKT inhibitors unveiling novel mechanisms and translational potential

Shuang Yan1, Lin Wang2, Dan Liu3

  • 1Sichuan University of Arts and Science, DaZhou 635000, China; Key Laboratory of Exploitation and Study of Distinctive Plants in Education Department of Sichuan Province, DaZhou 635000, China; Key Laboratory of Green Chemistry of Sichuan Institutes of Higher Education, ZiGong 643002, China; Key Laboratory of Low-cost Rural Environmental Treatment Technology at Sichuan University of Arts and Science, Education Department of Sichuan Province, DaZhou 635000, China.

Bioorganic Chemistry
|July 22, 2025
PubMed

Insights

Dual-target AKT inhibitors offer enhanced cancer therapy by simultaneously targeting multiple pathways, overcoming resistance and improving efficacy compared to traditional single-target drugs. Future research focuses on novel strategies like nano-delivery and combination therapies.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • The serine/threonine kinase AKT is a critical regulator of cell proliferation, survival, and metabolism, making it a key target in cancer therapy.
  • Traditional AKT inhibitors like capivasertib show promise but face challenges such as drug resistance and limited efficacy.
  • Dual-target inhibitors, which inhibit AKT alongside other signaling pathways (e.g., PI3K/AKT/mTOR, AKT/EGFR), present a strategy to overcome these limitations.

Purpose of the Study:

  • To review recent advancements in the development of dual-target AKT inhibitors for cancer treatment.
  • To examine both established and novel therapeutic targets for dual inhibition strategies.
  • To discuss innovative approaches like nano-drug delivery and combination therapies to enhance the clinical application of AKT inhibitors.

Main Methods:

  • Literature review of recent scientific publications on dual-target AKT inhibitors.
  • Analysis of classical and emerging therapeutic targets for dual inhibition.
  • Exploration of advanced strategies including nano-drug delivery systems and combination therapies.

Main Results:

  • Dual-target AKT inhibitors demonstrate enhanced therapeutic potential by addressing resistance and efficacy issues seen with single-target agents.
  • Various dual-target strategies are being explored, including combinations with PI3K, mTOR, and EGFR inhibitors.
  • Innovative delivery systems and combination therapies are emerging as promising avenues to improve treatment outcomes.

Conclusions:

  • Dual-target AKT inhibitors represent a significant advancement in cancer therapy, offering improved efficacy and overcoming resistance.
  • Further research into novel targets, nano-delivery systems, and combination therapies is crucial for optimizing clinical applications.
  • These strategies hold promise for developing more effective treatments for various cancers.
Keywords:
AKT signalingClinicalDual-target inhibitorNanodrug delivery systemPI3K/AKT/mTOR signaling pathway

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