Synthesis and evaluation of acyl protein thioesterase 1 (APT1) inhibitors

Chemistry : a European Journal
Markus BielHerbert Waldmann

Abstract

Lipid-modified proteins play decisive roles in important biological processes such as signal transduction, organisation of the cytoskeleton and vesicular transport. Lipidation of these proteins is essential for correct biological function. Among the modifications with lipids, prenylation and myristoylation are well understood. However, the machinery of palmitoylation is still under investigation. Recently, an enzyme, acyl protein thioesterase 1 (APT1), that may play a regulatory role in the palmitoylation cycle of H-Ras and G-protein alpha subunits, was purified. Motivated by this work, several inhibitors of APT1 were designed, synthesized and biologically evaluated leading to highly active compounds.

References

Aug 21, 1992·Journal of Medicinal Chemistry·J H Van MaarseveenC G Kruse
Jan 20, 1995·The Journal of Biological Chemistry·L J RobinsonT Michel
Mar 29, 1994·Proceedings of the National Academy of Sciences of the United States of America·S M MumbyA G Gilman
Mar 29, 1996·The Journal of Biological Chemistry·H SugimotoS Yamashita
Mar 22, 1996·The Journal of Biological Chemistry·J T DunphyM E Linder
Sep 20, 1996·The Journal of Biological Chemistry·J A Duncan, A G Gilman
Jun 23, 1998·The Journal of Biological Chemistry·J A Duncan, A G Gilman
Dec 5, 1998·Biochimica Et Biophysica Acta·J T Dunphy, M E Linder
Aug 24, 2002·The Journal of Biological Chemistry·Sandra LoboRobert J Deschenes
Oct 31, 2002·Chembiochem : a European Journal of Chemical Biology·Elisabeth AddicksAthanassios Giannis
Dec 14, 2002·Trends in Cell Biology·Marie-José Bijlmakers, Mark Marsh
Apr 16, 2003·Biochemistry·Maurine E Linder, Robert J Deschenes
Nov 3, 2004·EMBO Reports·Lars E P Dietrich, Christian Ungermann
Jul 9, 2005·Angewandte Chemie·Patrick DeckHerbert Waldmann

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Citations

Dec 21, 2010·Chemical Reviews·Dyeison Antonow, David E Thurston
Sep 17, 2011·Chemical Reviews·Howard C Hang, Maurine E Linder
Jun 14, 2012·Journal of the American Chemical Society·Alexander AdibekianBenjamin F Cravatt
Dec 22, 2006·Nature Reviews. Molecular Cell Biology·Maurine E Linder, Robert J Deschenes
May 15, 2009·Biochimica Et Biophysica Acta·Tohko HiranoTakashi Izumi
Jul 19, 2011·Peptides·Motoyasu SatouHiroyuki Sugimoto
Jun 30, 2015·Chemistry & Biology·Armand B CognettaBenjamin F Cravatt
Apr 27, 2010·Nature Chemical Biology·Frank J DekkerHerbert Waldmann
Dec 31, 2008·Molecular Membrane Biology·Ruth ZeidmanAnthony I Magee
Jul 4, 2012·Acta Crystallographica. Section F, Structural Biology and Crystallization Communications·Ye YuanYongxiang Gao
Sep 20, 2012·Angewandte Chemie·Imants KreitussJeffrey W Bode
Apr 2, 2008·The Journal of Organic Chemistry·Gemma TriolaHerbert Waldmann
Oct 29, 2019·The Journal of Organic Chemistry·Sarah Jane Mear, Timothy F Jamison
Jul 21, 2011·The Journal of Organic Chemistry·Suneel P SinghAdrian L Schwan

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