2013 Fiscal Year Final Research Report
Structural studies on antibiotic-resistance mechanisms and their application to drug design
| Project/Area Number |
23790054
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Physical pharmacy
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| Research Institution | Sophia University |
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Principal Investigator |
KONDO Jiro 上智大学, 理工学部, 助教 (10546576)
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| Research Collaborator |
HANESSIAN Stephen モントリオール大学, 教授
BAASOV Timor テクニオン工科大学, 教授
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| Project Period (FY) |
2011 – 2013
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| Keywords | 薬剤耐性菌 / 抗生物質 / リボソーム / Ｘ線結晶解析 / ドラッグデザイン |
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| Research Abstract |
Aminoglycosides are broad spectrum antibiotics acting against a variety of Gram-negative and certain Gram-positive bacteria. Aminoglycosides specifically bind to one of the active sites of the bacterial ribosome called the A site, and disturb the fidelity of the decoding process in protein synthesis. Bacteria acquire high-level resistance against aminoglycosides by mutating the position 1408 of the ribosomal RNA A site, from A to G or 1-methyl-A. In the present study, we have performed X-ray analyses of the ribosomal RNA A sites with these antibiotic-resistant mutations and revealed structural bases for the antibiotic resistance conferred by the point mutatations. In addition, we have successfully designed and synthesized a new compound with high activity against antibiotic-resistant bacteria and parasitic protozoa.
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Research Products
(22 results)
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[Remarks] Biotechdaily - Online bioresearch news - 2013年8月20日 Light shed on differential effectiveness of aminoglycosides against parasitic protozoa
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[Remarks] 化学工業日報 2011年12月12日 「上智大 細菌の抗生物質耐性獲得メカニズム解明 新薬の設計・開発に応用も」
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