Statins and Protein Prenylation in Cancer Cell Biology and Therapy

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

Volume 16, 12 Issues, 2016

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex

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Statins and Protein Prenylation in Cancer Cell Biology and Therapy

Anti-Cancer Agents in Medicinal Chemistry, 12(4): 303-315.

Author(s): Carmen Garcia-Ruiz, Albert Morales and Jose C Fernandez-Checa.

Affiliation: Centro Esther Koplowitz, C/ Rossello 151, 08036-Barcelona, Spain.


The use of statins has scaled up to become one of the most prescribed medicines in the world and have been very useful in the manegement of cardiovascular diseases and related mortality. The disclosure of their chemical structure similar to that of hydroxy methyl glutaryl-CoA (HMG-CoA) revealed their ability to compete with and inhibit the rate-limiting enzyme HMG-CoA reductase that catalyzes the synthesis of mevalonate, which then serves as the precursor for isoprenoids and cholesterol in the mevalonate pathway. While most of the effects of statins are associated with the lowering of cellular cholesterol levels, it is clear that they also blunt the non-sterol branch of the mevalonate pathway, decreasing formation of isoprenoids and altering protein-prenylation, a critical event in the posttranslational modulation of proteins involved in the regulation of cell cycle progression, proliferation and signaling pathways. Randomized controlled trials for the prevention of cardiovascular diseases indicated that statins elicited provocative and unexpected benefits for reducing a number of different types of cancers, including colorectal carcinoma, melanoma, prostate and hepatocellular carcinoma, although in other cancer types the preclinical expectations of statins were dissapointing. In this review, we will describe the evidence and mechanisms underlying the potential beneficial use of statins and the role of protein prenylation in cancer prevention. Of relevance, the combination of statins with other anti cancer drugs may be a significant asset in malignancies resistant to current therapy.


Cholesterol, Isoprenoids, Protein modification, Chemotherapy, Hedgehog pathway, proliferation, hepatocellular carcinoma, geranylgeranyl pyrophosphate, carboxyesterases, cell adhesion .

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Article Details

Volume: 12
Issue Number: 4
First Page: 303
Last Page: 315
Page Count: 13
DOI: 10.2174/187152012800228715
Price: $58

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