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

Autor:	Tsutomu Ando, Yoshihisa Toda, Takuya Fukunaga, Chu Yiwen, Takeshi Aoki, Osamu Nozawa, Li Jun-ying, Akira Kawashima, Yuichi Terui
Rok vydání:	2008
Předmět:	Glycine transporter chemistry.chemical_classification Tetrapeptide Stereochemistry Chemistry Organic Chemistry Drug Discovery Inhibitory postsynaptic potential Biochemistry Combinatorial chemistry IC50 Amino acid
Zdroj:	Tetrahedron Letters. 49:3067-3070
ISSN:	0040-4039
Popis:	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′-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 IC50 of 20 nM.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::1a62405526f9f0016e77f97b0cadb08b https://doi.org/10.1016/j.tetlet.2008.03.054 Zobrazit plný text záznamu Full Text from ScienceDirect