Development of a fluorogenic small substrate for dipeptidyl peptidase-4

被引：4

作者：

Ogawa, Futa ^{[1
]}

Takeda, Masanori ^{[1
]}

Miyanaga, Kanae ^{[2
]}

Tani, Keita ^{[2
]}

Yamazawa, Ryuji ^{[1
]}

Ito, Kiyoshi ^{[1
]}

Tarui, Atsushi ^{[1
]}

Sato, Kazuyuki ^{[1
]}

Omote, Masaaki ^{[1
]}

机构：

[1] Setsunan Univ, Fac Pharmaceut Sci, 45-1 Nagaotoge Cho, Hirakata, Osaka 5730101, Japan

[2] Osaka Kyoiku Univ, Div Nat Sci, Osaka 5828582, Japan

来源：

BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY | 2017年 / 13卷

关键词：

dipeptidyl peptidase-4; fluorogenic substrate; fluorometry; small fluorescent molecule; SOLID-STATE; FLUORESCENT-PROBE; IN-VIVO; CELLS; DESIGN; VIOLET; TUMOR; IV;

D O I：

10.3762/bjoc.13.267

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A series of aniline and m-phenylenediamine derivatives with electron-withdrawing 3,3,3-trifluoropropenyl substituents were synthesized as small and chemically stable fluorescent organic compounds. Their fluorescence performances were evaluated by converting 2,4-disubstituted aniline 1 to the non-fluorescent dipeptide analogue H-Gly-Pro-1 for the use as a fluorogenic substrate for dipeptidyl peptidase-4 (DPP-4). The progress of the enzymatic hydrolysis of H-Gly-Pro-1 with DPP-4 was monitored by fluorometric determination of 1 released into the reaction medium. The results suggest that 1 could be used as fluorophore in OFF-ON-type fluorogenic probes.

引用

页码：2690 / 2697

页数：8

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