| Project/Area Number |
17209004
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| Research Category |
Grant-in-Aid for Scientific Research (A)
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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 | Kyoto University |
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Principal Investigator |
FUJII Nobutaka Kyoto University, Graduate School of Pharmaceutical Sciences, Professor (60109014)
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| Co-Investigator(Kenkyū-buntansha) |
OISHI Shinya Kyoto University, Graduate School of Pharmaceutical Sciences, Assistant Professor (80381739)
渡部 毅 京都大学, 薬学研究科, 研究員 (00397788)
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| Project Period (FY) |
2005 – 2007
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| Project Status |
Completed (Fiscal Year 2007)
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| Budget Amount *help |
¥52,130,000 (Direct Cost: ¥40,100,000、Indirect Cost: ¥12,030,000)
Fiscal Year 2007: ¥7,020,000 (Direct Cost: ¥5,400,000、Indirect Cost: ¥1,620,000)
Fiscal Year 2006: ¥7,540,000 (Direct Cost: ¥5,800,000、Indirect Cost: ¥1,740,000)
Fiscal Year 2005: ¥37,570,000 (Direct Cost: ¥28,900,000、Indirect Cost: ¥8,670,000)
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| Keywords | Seven transmembrane protein / chemical proteomics / CXCR4 / T140 / G-protein coupled receptor / 7TMGPCR / Cysteine-ligation / 光感受性保護基 / GPR-54 / 非ペプチド化 / Bioluminescece Resonance Energy Transfer / Intein-splicing system |
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| Research Abstract |
In recent drug discovery researches, rational drug design is one of principal approaches to develop pharmaceutical agents. Recent progressive structural analyses of enzyme-substrate or receptor-ligand complex by X-ray crystallography have practically contributed to the inhibitor or antagonist designs. With increase in numbers of disclosed natural and unnatural peptide ligands from genome/proteome researches, this technique is increasingly expected to be an attractive methodology to find out lead compounds rationally, as well as random screening. Meanwhile, in the case of membrane protein ligands, it is much more difficult to assume what functional groups could be the pharmacophore, because exact structure analyses of these complexes are not available. In this program, we have engaged in evolutional development of technology for G-protein-coupled receptors, which are one of the major targets for recent drug discovery, including (1) establishment of chemical synthetic methodology for membrane proteins; (2) development of specific GPR54 ligands and the rational down-sizing; (3) development of efficient strategy for the preparation of non-peptide ligands.
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