850209-99-3Relevant articles and documents
A General Approach to the Asymmetric Synthesis of Unsaturated Lipidic α-Amino Acids. the First Synthesis of α-Aminoarachidonic Acid
Kokotos, George,Padron, Jose M.,Martin, Tomas,Gibbons, William A.,Martin, Victor S.
, p. 3741 - 3744 (1998)
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Mechanism-Based Inhibitors of the Human Sirtuin 5 Deacylase: Structure–Activity Relationship, Biostructural, and Kinetic Insight
Rajabi, Nima,Auth, Marina,Troelsen, Kathrin R.,Pannek, Martin,Bhatt, Dhaval P.,Fontenas, Martin,Hirschey, Matthew D.,Steegborn, Clemens,Madsen, Andreas S.,Olsen, Christian A.
, p. 14836 - 14841 (2017/11/10)
The sirtuin enzymes are important regulatory deacylases in a variety of biochemical contexts and may therefore be potential therapeutic targets through either activation or inhibition by small molecules. Here, we describe the discovery of the most potent inhibitor of sirtuin 5 (SIRT5) reported to date. We provide rationalization of the mode of binding by solving co-crystal structures of selected inhibitors in complex with both human and zebrafish SIRT5, which provide insight for future optimization of inhibitors with more “drug-like” properties. Importantly, enzyme kinetic evaluation revealed a slow, tight-binding mechanism of inhibition, which is unprecedented for SIRT5. This is important information when applying inhibitors to probe mechanisms in biology.
Aldehyde acetal based processes for the manufacture of macrocyclic depsipeptides and new intermediates
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, (2015/03/28)
The invention relates to a method or process for the chemical manufacture of depsipeptides of the formula I employing an aldehyde acetal intermediate, wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments.
