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Small Molecule Modulators of AMP-Activated Protein Kinase (AMPK) Activity and Their Potential in Cancer Therapy

Juliet E Strang1, Daniel D Astridge1, Vu T Nguyen1

  • 1Department of Pharmaceutical Sciences, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of Colorado Anschutz Medical Campus, 12850 East Montview Boulevard, Aurora, Colorado 80045, United States.

Journal of Medicinal Chemistry
|January 29, 2025
PubMed

Insights

AMP-activated protein kinase (AMPK) regulates cellular metabolism and ATP production. Targeting AMPK shows promise in treating metabolic diseases and cancer, influencing tumor growth and drug resistance.

Area of Science:

  • Biochemistry
  • Cellular Metabolism
  • Oncology

Background:

  • AMP-activated protein kinase (AMPK) is a key regulator of cellular energy homeostasis, activated by low ATP levels.
  • AMPK influences both anabolic and catabolic pathways to restore cellular energy balance.
  • AMPK plays a dual role in cancer, acting as a tumor suppressor or promoting cancer cell survival.

Purpose of the Study:

  • To review the multifaceted role of AMPK in cancer development and drug resistance.
  • To discuss the impact of the tumor microenvironment on AMPK signaling.
  • To summarize current strategies for developing AMPK activators and inhibitors for cancer therapy.

Main Methods:

  • Literature review and synthesis of existing research on AMPK in cancer.
  • Analysis of preclinical data on small molecule AMPK modulators.
  • Discussion of emerging concepts in AMPK isoform-selective targeting.

Main Results:

  • Small molecule AMPK activators and inhibitors have shown efficacy in preclinical cancer models.
  • The tumor microenvironment significantly influences AMPK activity in cancer cells.
  • Isoform-selective targeting of AMPK presents a promising therapeutic avenue.

Conclusions:

  • AMPK is a critical therapeutic target in oncology with potential for both tumor suppression and modulation of cancer cell survival.
  • Understanding AMPK's role in the tumor microenvironment is crucial for effective therapeutic development.
  • Targeted approaches, including isoform selectivity, are key to optimizing AMPK-based cancer treatments.

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