Structural modification of Fas C-terminal tripeptide and its effects on the inhibitory activity of Fas/FAP-1 binding

E Sawa, M Takahashi, M Kamishohara…

Index: Sawa, Eiji; Takahashi, Motoo; Kamishohara, Masaru; Tazunoki, Tetsushi; Kimura, Kaname; Arai, Midori; Miyazaki, Tetsuko; Kataoka, Shiro; Nishitoba, Tsuyoshi Journal of Medicinal Chemistry, 1999 , vol. 42, # 17 p. 3289 - 3299

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Citation Number: 9

Abstract

We report the structural requirements of the C-terminal tripeptide derivative of Fas (Ac-Ser- Leu-Val-OH, 1) for the inhibitory activity of Fas/FAP-1 binding. The presence of a carboxyl group and a l-Val residue at the C-terminus is essential for the inhibitory activity, and the hydroxyl group of Ser plays an important role as the donor of a hydrogen bond. The introduction of hydrophobic groups to the N-terminal region of 1, especially the ...