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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)
Author(s) -
Pellicciari Roberto,
Rizzo Rosa C.,
Costantino Gabriele,
Marinozzi Maura,
Amori Laura,
Guidetti Paolo,
Wu HuiQiu,
Schwarcz Robert
Publication year - 2006
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200690014
Subject(s) - kynurenine , kynurenine pathway , kynurenic acid , chemistry , metabolite , nicotinic agonist , pharmacology , nmda receptor , metabolism , tryptophan , receptor , biochemistry , biology , amino acid
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.)