Identification of Acyl Protein Thioesterases 1 and 2 as the Cellular Targets of the Ras-Signaling Modulators Palmostatin B and M

Finding the target: Activity‐based proteomic profiling probes based on the depalmitoylation inhibitors palmostatin B and M (see picture) have been synthesized and were found to target acyl protein thioesterase 1 (APT1) and 2 (APT2) in cells.

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Bibliographische Detailangaben
Veröffentlicht in:	Angewandte Chemie International Edition 2011-10, Vol.50 (42), p.9838-9842
Hauptverfasser:	Rusch, Marion, Zimmermann, Tobias J., Bürger, Marco, Dekker, Frank J., Görmer, Kristina, Triola, Gemma, Brockmeyer, Andreas, Janning, Petra, Böttcher, Thomas, Sieber, Stephan A., Vetter, Ingrid R., Hedberg, Christian, Waldmann, Herbert
Format:	Artikel
Sprache:	eng
Schlagworte:	acyl protein thioesterase Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Fatty Acid Synthases - antagonists & inhibitors HeLa Cells Humans inhibition Molecular Structure Palmitoyl-CoA Hydrolase - antagonists & inhibitors Propiolactone - analogs & derivatives Propiolactone - chemistry Propiolactone - pharmacology Proteome proteomics Ras proteins ras Proteins - metabolism signal transduction Signal Transduction - drug effects Structure-Activity Relationship Sulfones - chemistry Sulfones - pharmacology Thiolester Hydrolases - antagonists & inhibitors
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Beschreibung
Zusammenfassung:	Finding the target: Activity‐based proteomic profiling probes based on the depalmitoylation inhibitors palmostatin B and M (see picture) have been synthesized and were found to target acyl protein thioesterase 1 (APT1) and 2 (APT2) in cells.
ISSN:	1433-7851 1521-3773
DOI:	10.1002/anie.201102967