Lessons from Nature: Sources and Strategies for Developing AMPK Activators for Cancer Chemotherapeutics

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Lessons from Nature: Sources and Strategies for Developing AMPK Activators for Cancer Chemotherapeutics

Anti-Cancer Agents in Medicinal Chemistry, 15(5): 657-671.

Author(s): Richard T. Arkwright, Rahul Deshmukh, Nikhil Adapa, Ryan Stevens, Emily Zonder, Zhongyu Zhang, Pershang Farshi, Reda Saber Ibrahim Ahmed, Hossny Awad El-Banna, Tak-Hang Chan and Q Ping Dou.

Affiliation: Barbara Ann Karmanos Cancer Institute and Department of Oncology, School of Medicine, Wayne State University, 540.1 HWCRC, 4100 John R Road, Detroit, MI 48201- 2013.


Adenosine Monophosphate-Activated Protein Kinase or AMPK is a highly-conserved master-regulator of numerous cellular processes, including: Maintaining cellular-energy homeostasis, modulation of cytoskeletaldynamics, directing cell growth-rates and influencing cell-death pathways. AMPK has recently emerged as a promising molecular target in cancer therapy. In fact, AMPK deficiencies have been shown to enhance cell growth and proliferation, which is consistent with enhancement of tumorigenesis by AMPK-loss. Conversely, activation of AMPK is associated with tumor growth suppression via inhibition of the Mammalian Target of Rapamycin Complex-1 (mTORC1) or the mTOR signal pathway. The scientific communities’ recognition that AMPK-activating compounds possess an anti-neoplastic effect has contributed to a rush of discoveries and developments in AMPK-activating compounds as potential anticancer-drugs. One such example is the class of compounds known as Biguanides, which include Metformin and Phenformin. The current review will showcase natural compounds and their derivatives that activate the AMPK-complex and signaling pathway. In addition, the biology and history of AMPK-signaling and AMPK-activating compounds will be overviewed, their anticancer-roles and mechanisms-of-actions will be discussed, and potential strategies for the development of novel, selective AMPK-activators with enhanced efficacy and reduced toxicity will be proposed.


AMPK, AMPK-activators, AMPK-signaling pathway, aspirin, BCA2, cancer, chemotherapy, drug discovery, metformin, natural compounds, salicylate.

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Article Details

Volume: 15
Issue Number: 5
First Page: 657
Last Page: 671
Page Count: 15
DOI: 10.2174/1871520615666141216145417
Price: $58

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