WSS2220, a novel cyclic tetrapeptide with a new sulfonoamino acid, exhibits potent and selective inhibitory activity against GlyT1

✍ Scribed by Yuichi Terui; Chu Yi-wen; Li Jun-ying; Osamu Nozawa; Tsutomu Ando; Takuya Fukunaga; Takeshi Aoki; Yoshihisa Toda; Akira Kawashima

• Book ID: 104095216
• Publisher: Elsevier Science
• Year: 2008
• Tongue: French
• Weight: 170 KB
• Volume: 49
• Category: Article
• ISSN: 0040-4039
• DOI: 10.1016/j.tetlet.2008.03.054

✦ Synopsis

In the course of our screening program for novel glycine transporter inhibitors, we obtained a novel cyclic tetrapeptide (WSS2220) from the culture broth of Nonomuraea sp. The structure of WSS2220 was elucidated based on physicochemical data. WSS2220 contained a novel amino acid (4-oxo-3 0 -sulfoisoleucine), the absolute stereochemistry of which was determined by chemical modifications and the modified Mosher's method. WSS2220 selectively inhibited glycine transporter type1 with an IC 50 of 20 nM.