Cover Picture: Modulators of the Kynurenine Pathway of Tryptophan Metabolism: Synthesis and Preliminary Biological Evaluation of (S)-4-(Ethylsulfonyl)benzoylalanine, a Potent and Selective Kynurenine Aminotransferase II (KAT II) Inhibitor (ChemMedChem 5/2006)

✍ Scribed by Roberto Pellicciari; Rosa C. Rizzo; Gabriele Costantino; Maura Marinozzi; Laura Amori; Paolo Guidetti; Hui-Qiu Wu; Robert Schwarcz

• Publisher: John Wiley and Sons
• Year: 2006
• Tongue: English
• Weight: 58 KB
• Volume: 1
• Category: Article
• ISSN: 1860-7179
• DOI: 10.1002/cmdc.200690014

✦ Synopsis

The cover picture shows one branch of the kynurenine pathway of tryptophan metabolism, which is mainly localized in astrocytes. One key metabolite, kynurenic acid (KYNA), is transported in the extracellular space, where it modulates synaptically localized α7 nicotinic acetylcholine receptors and NMDA receptors. The inset shows the active site of kynurenine aminotransferase II (KAT II), the enzyme that synthesizes KYNA in the CNS, and the structure of (S)‐4‐(ethylsulfonyl)benzoylalanine, a potent and selective KAT II inhibitor. Selective inhibition of KAT II may have a fundamental role in the understanding of CNS processes related to cognitive function. For more details, see the Communication by R. Pellicciari et al. on p. 528 ff. (Daniele Bellocchi is acknowledged for the cover image.)