Targeting protein prenylation for cancer therapy
Copyright policy )Targeting protein prenylation for cancer therapy
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.
- Florida Southern College United States
- University of Oxford United Kingdom
- University of South Florida United States
- Moffitt Cancer Center United States
Alkyl and Aryl Transferases, Cell Survival, Cell Cycle, Neuropeptides, Protein Prenylation, Antineoplastic Agents, Neoplasms, Animals, Farnesyltranstransferase, Humans, Ras Homolog Enriched in Brain Protein, Molecular Targeted Therapy, Enzyme Inhibitors, Cell Proliferation, Monomeric GTP-Binding Proteins, Randomized Controlled Trials as Topic, Signal Transduction
Alkyl and Aryl Transferases, Cell Survival, Cell Cycle, Neuropeptides, Protein Prenylation, Antineoplastic Agents, Neoplasms, Animals, Farnesyltranstransferase, Humans, Ras Homolog Enriched in Brain Protein, Molecular Targeted Therapy, Enzyme Inhibitors, Cell Proliferation, Monomeric GTP-Binding Proteins, Randomized Controlled Trials as Topic, Signal Transduction
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