2005 Fiscal Year Final Research Report Summary
A novel strategy for the elucidation of interaction between biologically active amino acids and/or peptides and their receptor proteins.
| Project/Area Number |
16550151
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Chemistry related to living body
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| Research Institution | Kinki University |
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Principal Investigator |
WAKAMIYA Tateaki Kinki University, Faculty of Science and Engineering, Professor, 理工学部, 教授 (10028243)
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| Project Period (FY) |
2004 – 2005
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| Keywords | spider toxin / fluorescent label / phytosiderofore / receptor protein / mechanism of neurotransmission / mugineic acid / deoxymugineic acid / Fe(III) transporting protein |
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| Research Abstract |
In the present project, we studied to develop a novel strategy for the elucidation of interaction between biologically active amino acids and/or peptides and their receptor proteins.
(1)Elucidation of a blocking mechanism of neurotransmission by spider toxins - Synthesis of fluorescent labeled analogs of a spider toxin
1)The NPTX-594 analog, in which the α- or ε-amino group of the Lys residue at right terminus in NPTX-594 was substituted with 4-nitrobenzo-2-oxa-1,3-diazole (NBD) as the fluorescent labeling group, was synthesized. Furthermore, the analog, in which the 2,4-dihydroxyphenyl acetic acid (Dhpa) residue at left terminus in NPTX-594 was substituted with NBD, was also synthesized. However, these analogs did not show the paralytic activity against cricket.
2)We next synthesized the analog in which the Dhpa residue was substituted with the 7-hydroxycoumarin-3-carbonyl (HCC) group. This analog shows the activity of 1/10 potent compared with NPTX-594, and seems to be quite promising compound for the elucidation of a blocking mechanism of neurotransmission by spider toxins.
(2)Elucidation of the Fe(III) ion transporting mechanism into plant body by mugineic acid.
1) Fe(III) transporting activity of five deoxymugineic acid (DMA) analogs was examined by the use of an iron uptake-defective yeast mutant in which Fe(III) complex transporter ZmYS1 fond in maize was expressed. As a result of this study, we suggest that the stereochemistry at 3"-carbon atom in the MA molecule may be important to form the active structure for the Fe(III) complexes of MA and DMA analogs.
2) We synthesized two DMA analogs labeled with NBD and/or HCC as the fluorescent group, respectively. However, the activities of these analogs were not clear, since they may be not able to form Fe(III) complex due to their poor solubility in water. We are currently synthesizing novel fluorescent labeled analogs being soluble in water.
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