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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| Project Status |
Completed (Fiscal Year 2013)
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| Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2013: ¥650,000 (Direct Cost: ¥500,000、Indirect Cost: ¥150,000)
Fiscal Year 2012: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2011: ¥2,730,000 (Direct Cost: ¥2,100,000、Indirect Cost: ¥630,000)
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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 / X線結晶解析 |
|---|
| 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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Report
(4 results)
Research Products
(40 results)
