Mechanism of spontaneous degradation observed in the insertioncontaining HIV-1 Capsid proteins
| Project/Area Number |
23791140
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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 |
Infectious disease medicine
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| Research Institution | Kumamoto University |
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Principal Investigator |
AMANO Masayuki 熊本大学, エイズ学研究センター・gCOEリサーチ, アソシエイト (30575080)
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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 |
¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2012: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2011: ¥2,730,000 (Direct Cost: ¥2,100,000、Indirect Cost: ¥630,000)
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| Keywords | HIV-1 / Gag 蛋白 / アミノ酸挿入変異 / Gag 自壊 / Capsid自壊 / HIV-1 Gag蛋白 / Capsid阻害剤 / Gag蛋白 / Gag蛋白自壊 |
|---|
| Research Abstract |
We previously reported that amino acid (AA) insertions at certainpositions of Gag Capsid proteins (CA) caused significant CA degradation, and such AAinsert-containing HIV-1 variants had significantly compromised infectivity andreplication capacity. We attempted to identify small compounds capable of binding to CAbased on our previous data. We calculated binding scores of more than 8 million compoundswith the putative target cavity on CA using virtual docking simulation and evaluatingtheir anti-HIV-1 activity using the cell-based assay. We could find 29 compounds whichcan inhibit replication of HIV-1 by these methods.
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Report
(3 results)
Research Products
(21 results)
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[Journal Article] GRL-0519, a Novel Oxatricyclic Ligand-Containing Nonpeptidic HIV-1 Protease Inhibitor (PI), Potently Suppresses Replication of a Wide Spectrum of Multi-PI-Resistant HIV-1 Variants In Vitro, Antimicrob2013
Author(s)
Amano M, Tojo Y, Gomez PMS, Campbell JR, Das D, Aoki M, Xu CX, Rao KV, Ghosh AK, and Mitsuya H
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Journal Title
Agents Chemother
Volume: 57
Issue: 5
Pages: 2036-2046
DOI
Related Report
Peer Reviewed
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[Journal Article] Design of HIV-1 Protease Inhibitors with C3-Substituted Hexahydrocyclopentafuranyl Urethane as P2-Ligands: Synthesis, Biological Evaluations, and Protein-Ligand X-ray Crystal Structure.2011
Author(s)
Arun K. Ghosh, Bruno D. Chapsal, Garth L. Parham, Melinda Steffey, Johnson Agniswamy, Yuan-Fang Wang, Masayuki Amano, Irene T. Weber, Hiroaki Mitsuya.
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Journal Title
Journal of Medicinal Chemistry.
Volume: 54
Pages: 5890-5901
Related Report
Peer Reviewed
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[Journal Article] Novel HIV-1 protease inhibitors (PIs) containing a bicyclic P2 functional moiety, tetrahydropyrano-tetrahydrofuran, that are potent against multi-PI-resistant HIV-1 variants.2011
Author(s)
Kazuhiko Ide, Manabu Aoki, Masayuki Amano, Yasuhiro Koh, Ravikiran S. Yedidi, Debananda Das, Sofiya Leschenko, Bruno Chapsal, Arun K. Ghosh, Hiroaki Mitsuya.
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Journal Title
Antimicrobial Agents and Chemotherapy.
Volume: 55
Pages: 1717-1727
Related Report
Peer Reviewed
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