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      Targeting protein prenylation for cancer therapy.

      Nature reviews. Cancer

      Alkyl and Aryl Transferases, antagonists & inhibitors, Animals, Antineoplastic Agents, therapeutic use, Cell Cycle, drug effects, Cell Proliferation, Cell Survival, Enzyme Inhibitors, pharmacology, Farnesyltranstransferase, Humans, Molecular Targeted Therapy, Monomeric GTP-Binding Proteins, metabolism, Neoplasms, drug therapy, Neuropeptides, Protein Prenylation, Randomized Controlled Trials as Topic, Signal Transduction

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          Abstract

          Protein farnesylation and geranylgeranylation, together referred to as prenylation, are lipid post-translational modifications that are required for the transforming activity of many oncogenic proteins, including some RAS family members. This observation prompted the development of inhibitors of farnesyltransferase (FT) and geranylgeranyl-transferase 1 (GGT1) as potential anticancer drugs. In this Review, we discuss the mechanisms by which FT and GGT1 inhibitors (FTIs and GGTIs, respectively) affect signal transduction pathways, cell cycle progression, proliferation and cell survival. In contrast to their preclinical efficacy, only a small subset of patients responds to FTIs. Identifying tumours that depend on farnesylation for survival remains a challenge, and strategies to overcome this are discussed. One GGTI has recently entered the clinic, and the safety and efficacy of GGTIs await results from clinical trials.

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          Journal
          22020205
          4037130
          10.1038/nrc3151

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