Construction of molecular switching system based on dipeptide framework

基于二肽骨架的分子开关系统构建

• 批准号: 16550095
• 负责人: KAWAI Masao
• 金额: $ 2.37万
• 依托单位: Nagoya Institute of Technology
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 2004
• 资助国家: 日本
• 起止时间: 2004 至 2005
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/en/grant/KAKENHI-PROJECT-16550095/
• 关键词: α,α-dialkylated amino acid; 4-aminoproline; conformationally restricted; control of stereostructure dipeptide; control of function; host-guest interaction; dinuclear zinc complex; phosphodiester bond cleavage; ジアルキルアミノ酸; ピリジルメチル誘導体; RNAモデル基質加水分解

The dipeptide sequence α-aminoisobutyryl-L-proline (Aib-L-Pro) adopts only two conformations, i.e., a folded (β-turn) conformation and an unfolded rather extended conformation. Based on this unique nature, it was attempted to utilize the Aib-L-Pro-based dipeptide for the construction of molecular switching system. The protected dipeptides possessing protected amino group in each side chain was designed, to which functional groups could be introduced for enabling their cooperative functioning. By the coupling of protected L/D-α,γ-diamino-α-methylbutyric acid (L/D-MeDab) derivative and protected L-4α/β-aminoproline [L-Pro(4β-NH_2] derivative, Boc-DL-DabMe(4-Cbz-NH)-L-Pro(4β-CbzNH)-OEt was synthesized. As for the function which could be manifested and controlled, we have chosen cooperative functioning of two Zn(II)-complexed bispicolylamino groups to cleave phosphodiester linkage of ribonucleotide model substrate. The activity could be controlled by conformational control of the dipeptide using interterminal host-guest inclusion.

二肽序列α-氨基异丁酰二酰丙烯酰基-L-丙烯（AIB-L-PRO）仅采用两个构象，即折叠（β-转移）构象和展开的相当扩展的构象。基于这种独特的性质，它试图利用基于AIB-L-Pro的二肽来构建分子开关系统。设计了每个侧链中具有受保护氨基的保护二肽，可以引入官能团以实现其合作功能。通过受保护的L/D-α，γ-二氨基-α-甲基丁基酸（L/D-Medab）衍生物的偶联和受保护的L-4α/β-氨基氨基氨基氨酸[L-PRO（4β-NH_2]衍生物，BOC-DL-DL-DABME（BOC-DL-DABME）（4-CBZ-NH）-L-LISH-lip-pro（4-CBZ-NH）-L-PRO（4β-cybe）均可依次（4β-cybe） - 均可能是合成的。表现出来的和受控的，我们选择了两个锌（II）的双链氨基氨基氨基含量的合作功能，以清除核糖核苷酸模型底物的磷酸二酯连接。

项目成果

α-Aminoisobutyryl-L-Prolyl Sequence as Framework for Molecular Switching System.

α-氨基异丁酰-L-脯氨酰序列作为分子开关系统的框架。

• 发表时间: 2006
• 期刊: Peptide Science 2005
• 作者: F.Mori;H.Yamamura;Y.Inai;H.Yasuda;K.Kishikawa;H.Koike;R.Nakazawa;M.Kawai
• 通讯作者: M.Kawai

4α/β-(Dipicolylamino) Prolyl Residue-Containing Dipeptide Sequences as Ligands for Dinuclear Zinc(II) Complexes

含有 4α/β-(二吡啶氨基)脯氨酰残基的二肽序列作为双核锌 (II) 配合物的配体

• 发表时间: 2006
• 期刊: Peptide Science 2005
• 作者: S.Miyata;H.Yamamura;Y.Inai;R.Tanaka;M.Yamakoshi;M.Kawai
• 通讯作者: M.Kawai

Dinuclear Zinc(II) Complex of a Dipeptide Possessing Host and Guest Moieties Promoted Phosphpdiester Bond Cleavage.

拥有主体和客体部分的二肽的双核锌 (II) 复合物促进磷酸二酯键断裂。

• 发表时间: 2006
• 期刊: Peptide Science 2005
• 作者: I.Goshima;N.Sakai;N.Izuhara;H.Yamamura;M.Kawai
• 通讯作者: M.Kawai