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
收藏
页码:2690 / 2697
页数:8
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