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2016 Fiscal Year Final Research Report

Polypharmacology based on dynamism of the target protein

Research Project

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Project/Area Number 26293025
Research Category

Grant-in-Aid for Scientific Research (B)

Allocation TypePartial Multi-year Fund
Section一般
Research Field Drug development chemistry
Research InstitutionThe University of Tokyo

Principal Investigator

Hashimoto Yuichi  東京大学, 分子細胞生物学研究所, 教授 (90164798)

Co-Investigator(Renkei-kenkyūsha) ISHIKAWA Minoru  東京大学, 分子細胞生物学研究所, 准教授 (70526839)
Research Collaborator FUJII Shinya  東京大学, 分子細胞生物学研究所, 講師 (60389179)
YACHIDE Tomomi  東京大学, 分子細胞生物学研究所, 助教 (20401284)
Project Period (FY) 2014-04-01 – 2017-03-31
Keywords多重薬理 / 核内受容体リガンド / 構造展開 / 阻害剤 / プロテインノックダウン / ハンチンチン / ブロモドメイン / ケイ素
Outline of Final Research Achievements

One of novel strategy in the drug development would be "polypharmacology" (or "shot-gun approach"). It focuses on the robust biological functions and captures the actions of drug from wide and various aspects. Therefore, it stands in contrast to the conventional one-drug-one-target approach. Polypharmacology drug candidates involve bio-active compounds with multiple targets, i.e., multiple pathological/pathophysiological proteins and/or genes, in drug design. The limited success of one-molecular targeted drug discovery nowadays and clarification of robustness of biological system prompt us to develop polypharmacological strategy-based new drugs. Also, functional multiplicity in addition to the multiplicity of the target proteins, i.e., protein-knockdown activity and/or pharmacological chaperon activity, were also pursued in this study.

Free Research Field

生物有機化学 医薬化学

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Published: 2018-03-22  

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