Abstract
Many signaling proteins such as the members of the Ras superfamily of GTPases are posttranslationally modified by covalent attachment of lipid groups, which is crucial for the correct localization and function of these proteins. Numerous lipidated proteins are oncogens often found mutated in several human cancers. Therefore, several therapeutic strategies have been developed based on the inhibition of the enzymes involved in these lipidation steps. Here, we will summarize the results on protein lipidation inhibition, mainly focusing on the small molecules targeting the isoprenylation and acylation of proteins.
MeSH terms
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Acylation
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology
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Humans
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Inhibitory Concentration 50
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Lipid Metabolism
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Lipoproteins / antagonists & inhibitors*
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Lipoproteins / metabolism
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Lipoylation
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Models, Molecular
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Neoplasms / drug therapy
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Neoplasms / enzymology
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Prenylation
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Protein Processing, Post-Translational*
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Signal Transduction
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Transferases / antagonists & inhibitors*
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Transferases / metabolism
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ras Proteins / antagonists & inhibitors*
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ras Proteins / metabolism
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Lipoproteins
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Transferases
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ras Proteins