2012 Fiscal Year Final Research Report
Development of Receptor Regulators Utilizing Novel HydrophobicStructure and Its Application for Medicinal Drug Design
| Project/Area Number |
20390035
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Tohoku Pharmaceutical University |
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Principal Investigator |
ENDO Yasuyuki 東北薬科大学, 薬学部, 教授 (80126002)
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| Co-Investigator(Kenkyū-buntansha) |
INOMATA Kohei 東北薬科大学, 薬学部, 准教授 (60221785)
OHTA Kiminori 東北薬科大学, 薬学部, 講師 (90347906)
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| Co-Investigator(Renkei-kenkyūsha) |
KAGECHIKA Hiroyuki 東京医科歯科大学, 疾患生命科学研究部, 教授 (20177348)
FUJII Shinya 東京医科歯科大学, 疾患生命科学研究部, 助教 (60389179)
FABIO Pichierri 東北大学, 工学研究科, COEフェロー (40374920)
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| Project Period (FY) |
2008 – 2012
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| Keywords | 医薬品化学 |
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| Research Abstract |
Estrogen receptor and androgen receptor participate sexual function as well as bone maintenance and nervous system. Creation of tissue selective ligands, which separate these functions, requires drug design in consideration of conformational change of receptor-ligand complex. In this project, we focused designand synthesis of new estrogen receptor ligands and androgen receptor ligands utilizing a new hydrophobic structure for the design. We have developed lead compounds for anti-osteoporosis agent and anti-prostate cancer agent which anti-androgen withdrawal syndrome.
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[Journal Article] Boron Cluster-based DevNon-Secosteroidal Vitamin D Receptor Ligands: Direct Observation of Hydrophobic Interaction between Protein Surface and Carborane2011
Author(s)
Shinya Fujii, Hiroyuki Masuno, Yoshiyuki Taoda, Atsushi Kano, Angsuma Wongmayura, Makoto Nakabayashi, Nobutoshi Ito, Masato Shimizu, Emiko Kawachi, Tomoya Hirano, YasuyukiEndo, Aya Tanatani, Hiroyuki Kagechika
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Journal Title
J. Am. Chem. Soc
Volume: 133
Pages: 20933-20941
DOI
Peer Reviewed
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