Development of a stimulus-responsive amino acid that enables functional control of peptides and proteins

2017 Fiscal Year Final Research Report

• Project/Area Number: 15K07858
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Chemical pharmacy
• Research Institution: The University of Tokushima
• Principal Investigator: SHIGENAGA Akira 徳島大学, 大学院医歯薬学研究部(薬学域), 講師 (10423394)
• Co-Investigator(Renkei-kenkyūsha): OTAKA Akira 徳島大学, 大学院医歯薬学研究部(薬学域), 教授 (20201973) ; INOKUMA Tsubasa 徳島大学, 大学院医歯薬学研究部(薬学域), 助教 (40541272)
• Project Period (FY): 2015-04-01 – 2018-03-31
• Keywords: トリメチルロック / 機能制御 / ペプチド / タンパク質 / 刺激応答 / ラクトン化 / アミド結合切断 / ペプチド結合切断

Outline of Final Research Achievements

A stimulus-responsive amino acid, which induces stimulus-triggered amide/peptide bond cleavage, enables functional control of peptides and proteins. In this project, we challenged to accelerate the amide bond cleavage of the stimulus-responsive unit that should be the bases for practical stimulus-responsive amino acids. We first established a fluorescence-based system to easily monitor the amide bond cleavage. Then, several new stimulus-responsive units were synthesized and their kinetics of the amide bond cleavage was evaluated based on the fluorescence monitoring. Finally, we successfully found out a new stimulus-responsive unit, its amide bond cleavage is significantly accelerated under acid conditions.

Free Research Field

有機合成化学