NEW FLUOROGENIC SYNTHETIC SUBSTRATES AND INHIBITORS FOR MICROSOMAL METALLOENDOPEPTIDASE

微粒体金属内肽酶的新型荧光合成底物和抑制剂

• 批准号: 04558025
• 负责人: KAWABATA Shun-ichiro
• 金额: $ 3.46万
• 依托单位: KYUSHU UNIVERSITY
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Developmental Scientific Research (B)
• 财政年份: 1992
• 资助国家: 日本
• 起止时间: 1992 至 1993
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-04558025/
• 关键词: Processing protease; Metalloendopeptidase; Synthetic substrate; Fluorogenic substrate; Metalloprotease; プロペプチド酵素; プロセシング; メタルプロテアーゼ; 蛍光性ペプチド基質; 合成阻害剤

Ten fluorogenic synthetic substrates of Abz (2-aminobenzoyl)-peptide-Dna(2,4-dinitro-anilinoethylamide) were newly synthesized and tested to find specific substrates for rabbit liver microsomal metalloendopeptidase (MEP) as shown in Table. Among these substrates, Abz-ARVRRANS-Dna or Abz-ARVTRANS-Dna was found to be the most sensitive substrates for MEP.The assay method using these peptide substrates enabled us to detect MEP activity in an aliquot (20-50 mul) of the crude extract.

新合成并测试了 Abz（2-氨基苯甲酰基）-肽-Dna（2,4-二硝基苯胺基乙酰胺）的 10 种荧光合成底物，以找到兔肝微粒体金属内肽酶（MEP）的特异性底物，如表所示。在这些底物中，Abz-ARVRRANS-Dna 或 Abz-ARVTRANS-Dna 被发现是 MEP 最敏感的底物。使用这些肽底物的测定方法使我们能够检测等分试样（20-50 μl）的 MEP 活性。粗提物。

项目成果

Miura, Y., Kawabata, S., and Iwanaga, S.: "A Limulus Intracelluar Coagulation Inhibitor with Characteristics of the Serpin Superfamily, Purification, Characterization, and cDNA Cloning." J.Biol.Chem.269. 542-547 (1994)

Miura, Y.、Kawabata, S. 和 Iwanaga, S.：“具有丝氨酸蛋白酶抑制剂超家族特征的鲎细胞内凝血抑制剂、纯化、表征和 cDNA 克隆。”

Ikura, T., Go, N., Kohda, D., Inagaki, F., Yanagawa, H., Kawabata, M., Kawabata, S., Iwanaga, S., Noguti, T., and Go. M.: "Secondary Structural Features of Modules M2 and M3 of Barnase in Solution by NMR Experiment and Distance Geometry Calculation" Prote

Ikura, T.、Go, N.、Kohda, D.、Inagaki, F.、Yanakawa, H.、Kawabata, M.、Kawabata, S.、Iwanaga, S.、Noguti, T. 和 Go。

Ikura,T.: "Secondary Structural Features of Modules M2 and M3 of Barnase in Solution by NMR Experiment and Distance Geometry Calculation." Proteins. 16. 341-356 (1993)

Ikura,T.：“通过 NMR 实验和距离几何计算研究溶液中 Barnase 模块 M2 和 M3 的二级结构特征。”

Sakumi,K.: "Cloning and Expression of cDNA for a Human Enzyme That Hydrolyzes 8-Oxo-dGTP,a Mutagenic Substrate for DNA Synthesis." The Journal of Biological Chemistry. 268. 23524-23530 (1993)

Sakumi,K.：“水解 8-Oxo-dGTP（一种用于 DNA 合成的诱变底物）的人类酶 cDNA 的克隆和表达。”

Sumihiro Hase: "The structure(Xylose)2glucose-o-serine 53 found in the first epidermal growth factor-like domain of bovine blood clotting factor IX." Journal of Biological Chemistry. 265. 1858-1861 (1990)

Sumihiro Hase：“在牛凝血因子 IX 的第一个表皮生长因子样结构域中发现了结构（木糖）2 葡萄糖-o-丝氨酸 53。”