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2016 Fiscal Year Final Research Report

Building and establishing platform technologies for Structure Based Drug Design targeting AdipoR

Research Project

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Project/Area Number 26293216
Research Category

Grant-in-Aid for Scientific Research (B)

Allocation TypePartial Multi-year Fund
Section一般
Research Field Metabolomics
Research InstitutionThe University of Tokyo

Principal Investigator

Iwabu Miki  東京大学, 医学部附属病院, 特任講師 (70392529)

Co-Investigator(Renkei-kenkyūsha) IWABU Masato  東京大学, 医学部附属病院, 特任准教授 (30557236)
YAMAUCHI Toshimasa  東京大学, 医学部附属病院, 准教授 (40372370)
KADOWAKI Takashi  東京大学, 医学部附属病院, 教授 (30185889)
TOKOYAMA Shigeyuki  独立行政法人理化学研究所, 横山構造生物学研究室, 上席研究員 (00159229)
Project Period (FY) 2014-04-01 – 2017-03-31
Keywords糖尿病 / 薬理学 / トランスレーショナルリサーチ
Outline of Final Research Achievements

We have so far clarified that adiponectin, an adipocyte-secreted physiologically active substance, is decreased with the onset of obesity and that lifestyle-related diseases are primarily accounted for by the systemically decreased action of adiponectin/adiponectin receptors (AdipoRs). We were the first in the world to succeed in identifying small-molecule compounds that serve as seed compounds for candidate AdipoR-activating drugs. In the process, we have also reported the crystal structures of AdipoRs, which allowed the seed compounds to be structurally developed, examined for their anti-diabetic properties at the cellular and organism levels, and optimized as candidate compounds for clinical development, with their activity, specificity and safety highly enhanced over those of existing small-molecule AdipoR-activating compounds. It is hoped that these milestones will lead to the development of novel anti-diabetic drugs.

Free Research Field

生化学

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Published: 2018-03-22  

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