Concept
Hydrolase des amides d'acides gras
Publications associées (9)
The Molecular Basis for Dual Fatty Acid Amide Hydrolase (FAAH)/Cyclooxygenase (COX) Inhibition
The design of multitarget-directed ligands is a promising strategy for discovering innovative drugs. Here, we report a mechanistic study that clarifies key aspects of the dual inhibition of the fatty acid amide hydrolase (FAAH) and the cyclooxygenase (COX) ...
Wiley-V C H Verlag Gmbh2016Computational insights into function and inhibition of fatty acid amide hydrolase
Ursula Röthlisberger, Andrea Cavalli, Giulia Palermo
The Fatty Acid Amide Hydrolase (FAAH) enzyme is a membrane-bound serine hydrolase responsible for the deactivating hydrolysis of a family of naturally occurring fatty acid amides. FAAH is a critical enzyme of the endocannabinoid system, being mainly respon ...
Elsevier2015Anandamide Hydrolysis in FAAH Reveals a Dual Strategy for Efficient Enzyme-Assisted Amide Bond Cleavage via Nitrogen Inversion
Ursula Röthlisberger, Andrea Cavalli, Pablo Campomanes Ramos, Giulia Palermo
Herein, we combined classical molecular dynamics (MD) and quantum mechanical/molecular mechanics (QM/MM) simulations to unravel the whole catalytic cycle of fatty acid amide hydrolase (FAAH) in complex with anandamide, the main neurotransmitters involved i ...
2015Keys to Lipid Selection in Fatty Acid Amide Hydrolase Catalysis: Structural Flexibility, Gating Residues and Multiple Binding Pockets
Ursula Röthlisberger, Andrea Cavalli, Pablo Campomanes Ramos, Giulia Palermo
The fatty acid amide hydrolase (FAAH) regulates the endocannabinoid system cleaving primarily the lipid messenger anandamide. FAAH has been well characterized over the years and, importantly, it represents a promising drug target to treat several diseases, ...
2015Protein residue linking in a single spectrum for magic-angle spinning NMR assignment
David Lyndon Emsley, Andrea Bertarello
Here we introduce a new pulse sequence for resonance assignment that halves the number of data sets required for sequential linking by directly correlating sequential amide resonances in a single diagonal-free spectrum. The method is demonstrated with both ...
Springer Verlag2015Wagging the Tail: Essential Role of Substrate Flexibility in FAAH Catalysis
Ursula Röthlisberger, Andrea Cavalli, Pablo Campomanes Ramos, Giulia Palermo, Marilisa Neri
The serine hydrolase, fatty acid amide hydrolase (FAAH), is responsible for the intracellular degradation of anandamide and other bioactive fatty acid ethanolamides involved in the regulation of pain, inflammation, and other pathophysiological processes. T ...
Amer Chemical Soc2013Bis(trifluoromethylsulfonyl)amide based "polymeric ionic liquids": Synthesis, purification and peculiarities of structure-properties relationships
A series of bis(trifluoromethylsulfonyl)amide based "polymeric ionic liquids" (PILs) as high molecular mass analogues of the corresponding imidazolium, ammonium and pyrrolidinium ionic liquids (ILs) was synthesized with high purity and fully characterized ...
Elsevier2011Switch-peptides as folding precursors in amyloid fibrillogenesis
Richard Alan Mimna, Sonia Dos Santos, Karine Murat, Lydiane Jeanine Saucède, Marie-Stéphanie Camus, Jérémy Bérard
Intramol. O,N-acyl migration reactions were used as structural switch (S-elements) from a depsipeptide bond contg., unfolded state (Soff) to an all-amide, native states (Son). Chem. or enzymically triggered acyl migrations allowed for the controlled induct ...
2006Comparative characterization of a wild type and transmembrane domain-deleted fatty acid amide hydrolase: identification of the transmembrane domain as a site for oligomerization
Fatty acid amide hydrolase (FAAH) is an integral membrane protein responsible for the hydrolysis of a number of primary and secondary fatty acid amides, including the neuromodulatory compounds anandamide and oleamide. Analysis of FAAH's primary sequence re ...
American Chemical Society1998