Design of peptide ligands based on protein-protein interaction and their application to protein knockdown technology

2017 Fiscal Year Final Research Report

• Project/Area Number: 16K15121
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Biological pharmacy
• Research Institution: National Institute of Health Sciences
• Principal Investigator: Naito Mikihiko 国立医薬品食品衛生研究所, 遺伝子医薬部, 部長 (00198011)
• Co-Investigator(Kenkyū-buntansha): 大岡 伸通 国立医薬品食品衛生研究所, 遺伝子医薬部, 室長 (80568519)
• Co-Investigator(Renkei-kenkyūsha): DEMIZU Yosuke 国立医薬品食品衛生研究所, 有機化学部, 部長 (90389180)
• Project Period (FY): 2016-04-01 – 2018-03-31
• Keywords: プロテインノックダウン / SNIPER / ヘリカルペプチド / エストロゲン受容体 / Notch

Outline of Final Research Achievements

We developed novel SNIPER compounds against estrogen receptor and Notch1 proteins by incorporating helical peptides, PERM3 and SAHM1, respectively, to SNIPERs as target ligands. These SNIPER compounds induced proteasomal degradation of the target proteins, and a SNIPER(Notch) suppressed the expression of c-myc, a downstream gene regulated by Notch signaling. These results indicate that functional SNIPER compounds can be developed by incorporating helical peptides as a target ligand.

Free Research Field

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