Small-molecule inhibition of APT1 affects Ras localization and signaling

Reversible palmitoylation controls the localization and signaling of Ras. Development of a potent and specific small molecule inhibitor of the thioesterase APT1 reveals that this enzyme depalmitoylates Ras in cells. Inhibition of APT1 led to redistribution and altered activity of HRas, NRas and an o...

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Bibliographic Details
Published in:	Nature chemical biology Vol. 6; no. 6; pp. 449 - 456
Main Authors:	Dekker, Frank J, Rocks, Oliver, Vartak, Nachiket, Menninger, Sascha, Hedberg, Christian, Balamurugan, Rengarajan, Wetzel, Stefan, Renner, Steffen, Gerauer, Marc, Schölermann, Beate, Rusch, Marion, Kramer, John W, Rauh, Daniel, Coates, Geoffrey W, Brunsveld, Luc, Bastiaens, Philippe I H, Waldmann, Herbert
Format:	Journal Article
Language:	English
Published:	New York Nature Publishing Group US 01.06.2010 Nature Publishing Group
Subjects:	631/80/2023 631/80/86 631/92/613 Animals Biochemical Engineering Biochemistry Bioorganic Chemistry Cell Biology Cell division Cell Line Chemistry Chemistry and Materials Science Chemistry/Food Science Dogs Down-Regulation Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Genes Humans Inhibitor drugs Kidney - drug effects Kidney - physiology Ligands Lipase - chemistry Lipase - metabolism Lipoylation - drug effects Models, Molecular Molecules Propiolactone - analogs & derivatives Propiolactone - chemical synthesis Propiolactone - chemistry Propiolactone - pharmacology Protein Conformation Proteins ras Proteins - drug effects ras Proteins - metabolism ras Proteins - physiology Signal Transduction Stomach - enzymology Thiolester Hydrolases - antagonists & inhibitors Thiolester Hydrolases - chemistry Thiolester Hydrolases - genetics
ISSN:	1552-4450, 1552-4469, 1552-4469
Online Access:	Get full text
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