| Project/Area Number |
23658100
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Bioproduction chemistry/Bioorganic chemistry
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| Research Institution | Kyoto University |
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Principal Investigator |
IRIE Kazuhiro 京都大学, 大学院・農学研究科, 教授 (00168535)
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| Co-Investigator(Kenkyū-buntansha) |
YANAGITA Ryo 香川大学, 農学部, 助教 (10598121)
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| Project Period (FY) |
2011 – 2012
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| Project Status |
Completed (Fiscal Year 2012)
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| Budget Amount *help |
¥3,770,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥870,000)
Fiscal Year 2012: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2011: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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| Keywords | 海洋天然物 / ブリオスタチン / プロテインキナーゼC / がん / アルツハイマー病 / プロテインキナーゼＣ / ホルボールエステル / 海綿 / 珪藻 / 発がん促進物質 / フサコケムシ / ラン藻 / Epstein-Barrウィルス |
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| Research Abstract |
Protein kinase C (PKC) involved in cellular signal transduction is one of the target enzymes fortherapeutics of cancer and Alzheimer’s disease. To explore PKC ligands with novel skeleton, we employed our screening system utilizing synthetic peptides of PKC C1 domains, to succeed to identify several bryostatins, anti-neoplastic marine macrolides, from Japanese bryozoan Bugula neritina. Structure-activity studies of bryostatins 4, 10 and 14 suggested that the ester group at position C20 was not necessary for binding to and activating PKC. Moreover, we screened novel PKC ligands from marine sponges, and found that a marine sponge Theonellasp. contains PKC ligands with high binding affinitycomparable to bryostatins.
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