The Ras proteins are well-known drivers of many cancers and thus represent attractive targets for the development of anticancer therapeutics. Inhibitors that disrupt the association of the Ras proteins with membranes by blocking the addition of the farnesyl lipid moiety to the Ras C-terminus failed in clinical trials. Here, we explore the possibility of targeting a second lipid modification, S-acylation, commonly referred to as palmitoylation, as a strategy to disrupt the membrane interaction of specific Ras isoforms. We review the enzymes involved in adding and removing palmitate from Ras and discuss their potential roles in regulating Ras tumorigenesis. In addition, we examine other proteins that affect Ras protein localization and may serve as future drug targets.
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August 2017
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Activating and inhibitory long non-coding RNAs of the NF-κβ canonical pathway. In this issue, Magagula et al. explore the lncRNAs that are directly involved in regulating innate immunity at various branches of the NF-κβ pathway, and also consider their potential diagnostic and therapeutic significance. For further details, see pages 953–962
Review Article|
June 16 2017
Targeting the Ras palmitoylation/depalmitoylation cycle in cancer
David Tse Shen Lin;
David Tse Shen Lin
1Centre for Molecular Medicine and Therapeutics, Department of Medical Genetics, University of British Columbia, Vancouver, British Columbia, Canada V5Z 4H4
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Nicholas G. Davis;
Nicholas G. Davis
2Department of Pharmacology, Wayne State University, Detroit, MI 48201, U.S.A.
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Elizabeth Conibear
1Centre for Molecular Medicine and Therapeutics, Department of Medical Genetics, University of British Columbia, Vancouver, British Columbia, Canada V5Z 4H4
Correspondence: Elizabeth Conibear (conibear@cmmt.ubc.ca)
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Publisher: Portland Press Ltd
Accepted:
April 07 2014
Received:
March 08 2017
Revision Received:
April 05 2017
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© 2017 The Author(s); published by Portland Press Limited on behalf of the Biochemical Society
2017
Biochem Soc Trans (2017) 45 (4): 913–921.
Article history
Accepted:
April 07 2014
Received:
March 08 2017
Revision Received:
April 05 2017
Citation
David Tse Shen Lin, Nicholas G. Davis, Elizabeth Conibear; Targeting the Ras palmitoylation/depalmitoylation cycle in cancer. Biochem Soc Trans 15 August 2017; 45 (4): 913–921. doi: https://doi.org/10.1042/BST20160303
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