title: Chemical biology of lipidated proteins.
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.
authors.affiliation: Abteilung Chemische Biologie, Max-Planck-Institut für molekulare Physiologie, Dortmund, Germany. gemma.triola@mpi-dortmund.mpg.de
authors.forename: Gemma
authors.initials: G
authors.lastname: Triola
authors.forename: Herbert
authors.initials: H
authors.lastname: Waldmann
authors.forename: Christian
authors.initials: C
authors.lastname: Hedberg
mesh_terms: D000215:Acylation; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D050356:Lipid Metabolism; D008074:Lipoproteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D054878:Lipoylation; D008958:Models, Molecular; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology; D054876:Prenylation; D011499:Protein Processing, Post-Translational; D015398:Signal Transduction; D014166:Transferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D018631:ras Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D008074:Lipoproteins; D014166:Transferases; D018631:ras Proteins