The study for elucidating the mechanisms of HIV-1's EFdA resistance.

该研究旨在阐明HIV-1的EFdA耐药机制。

• 批准号: 17K15710
• 负责人: Hayashi Hironori
• 金额: $ 2.66万
• 依托单位: Tohoku University (2018)National Center for Global Health and Medicine (2017)
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Young Scientists (B)
• 财政年份: 2017
• 资助国家: 日本
• 起止时间: 2017-04-01 至 2019-03-31
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/en/grant/KAKENHI-PROJECT-17K15710/
• 关键词: HIV; 逆転写酵素; EFdA; 薬剤耐性化; HIV-1; ＨＩＶ－１; 結晶構造解析; 創薬

项目成果

Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.

• DOI: 10.1021/acs.jmedchem.7b00172
• 发表时间: 2017-05-25
• 期刊: Journal of medicinal chemistry
• 影响因子: 7.3
• 作者: Ghosh AK;Rao KV;Nyalapatla PR;Osswald HL;Martyr CD;Aoki M;Hayashi H;Agniswamy J;Wang YF;Bulut H;Das D;Weber IT;Mitsuya H
• 通讯作者: Mitsuya H

The High Genetic Barrier of EFdA/MK-8591 Stems from Strong Interactions with the Active Site of Drug-Resistant HIV-1 Reverse Transcriptase.

• DOI: 10.1016/j.chembiol.2018.07.014
• 发表时间: 2018-10-18
• 期刊: Cell chemical biology
• 影响因子: 8.6
• 作者: Takamatsu Y;Das D;Kohgo S;Hayashi H;Delino NS;Sarafianos SG;Mitsuya H;Maeda K
• 通讯作者: Maeda K

HIV-1 with HBV-associated Q151M substitution in RT becomes highly susceptible to entecavir: structural insights into HBV-RT inhibition by entecavir.

• DOI: 10.1038/s41598-018-19602-9
• 发表时间: 2018-01-26
• 期刊: Scientific reports
• 影响因子: 4.6
• 作者: Yasutake Y;Hattori SI;Hayashi H;Matsuda K;Tamura N;Kohgo S;Maeda K;Mitsuya H
• 通讯作者: Mitsuya H

GRL-079, a Novel HIV-1 Protease Inhibitor, Is Extremely Potent against Multidrug-Resistant HIV-1 Variants and Has a High Genetic Barrier against the Emergence of Resistant Variants.

GRL-079 是一种新型 HIV-1 蛋白酶抑制剂，对多重耐药 HIV-1 变异体非常有效，并且对耐药变异体的出现具有很高的遗传屏障。

• DOI: 10.1128/aac.02060-17
• 发表时间: 2018
• 期刊: Antimicrobial agents and chemotherapy
• 影响因子: 4.9
• 作者: Delino,NicoleS;Aoki,Manabu;Hayashi,Hironori;Hattori,Shin-Ichiro;Chang,SimonB;Takamatsu,Yuki;Martyr,CuthbertD;Das,Debananda;Ghosh,ArunK;Mitsuya,Hiroaki
• 通讯作者: Mitsuya,Hiroaki

Mechanism of Darunavir (DRV)'s High Genetic Barrier to HIV-1 Resistance: A Key V32I Substitution in Protease Rarely Occurs, but Once It Occurs, It Predisposes HIV-1 To Develop DRV Resistance.

• DOI: 10.1128/mbio.02425-17
• 发表时间: 2018-03-06
• 期刊: mBio
• 影响因子: 6.4
• 作者: Aoki M;Das D;Hayashi H;Aoki-Ogata H;Takamatsu Y;Ghosh AK;Mitsuya H
• 通讯作者: Mitsuya H