Issue 3, 2013
From the journal:

MedChemComm

Prenyltransferase inhibitors: treating human ailments from cancer to parasitic infections

Joshua D. Ochockia  and  Mark D. Distefano*a  

* Corresponding authors

a Department of Chemistry, University of Minnesota, Minneapolis, MN 55455, USA
E-mail: diste001@umn.edu

Abstract

The posttranslational modification of protein prenylation is a covalent lipid modification on the C-terminus of substrate proteins that serves to enhance membrane affinity. Oncogenic proteins such as Ras have this modification and significant effort has been placed into developing inhibitors of the prenyltransferase enzymes for clinical therapy. In addition to cancer therapy, prenyltransferase inhibitors have begun to find important therapeutic uses in other diseases, including progeria, hepatitis C and D, parasitic infections, and other maladies. This review will trace the evolution of prenyltransferase inhibitors from their initial use as cancer therapeutics to their expanded applications for other diseases.

Graphical abstract: Prenyltransferase inhibitors: treating human ailments from cancer to parasitic infections

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Article information

DOI
https://doi.org/10.1039/C2MD20299A
Article type
Review Article
Submitted
04 Oct 2012
Accepted
24 Nov 2012
First published
27 Nov 2012

Med. Chem. Commun., 2013,4, 476-492

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Prenyltransferase inhibitors: treating human ailments from cancer to parasitic infections

J. D. Ochocki and M. D. Distefano, Med. Chem. Commun., 2013, 4, 476 DOI: 10.1039/C2MD20299A

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