期刊
ACS CHEMICAL BIOLOGY
卷 7, 期 1, 页码 87-99出版社
AMER CHEMICAL SOC
DOI: 10.1021/cb200460u
关键词
Farnesyl Transferase (FTase) and Geranylgeranyl Transferase (GGTase); Rab geranylgeranyl transferase (GGTase); TAG tunnel (Tunnel adjacent to the GGPP); Lipid binding site (LBS); Palmitoyl acyl transferases (PAT); Palmitoyl protein thioesterase (PPT); Acyl protein thioesterase (APT)
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.
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