Exploring Modifications of an HIV-1 Capsid Inhibitor: Design, Synthesis, and Mechanism of Action.

Published on Jan 1, 2018
Jimmy P. Xu2
Estimated H-index: 2
Ashwanth Francis1
Estimated H-index: 1
+ 5 AuthorsSimon Cocklin19
Estimated H-index: 19
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Cited By2
#1Lin Sun (SDU: Shandong University)H-Index: 4
#2Tianguang Huang (SDU: Shandong University)H-Index: 1
Last. Lee Kuo-Hsiung (UNC: University of North Carolina at Chapel Hill)H-Index: 71
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Abstract HIV-1 CA is involved in different stages of the viral replication cycle, performing essential roles in both early (uncoating, reverse transcription, nuclear import, integration) and late events (assembly). Recent efforts have demonstrated HIV-1 CA protein as a prospective therapeutic target for the development of new antivirals. The most extensively studied CA inhibitor, PF-3450074 (PF-74, discovered by Pfizer), that targets an inter-protomer pocket within the CA hexamer. Herein we repo...
2 CitationsSource
#1Sara E. Jones-Burrage (IU: Indiana University)H-Index: 1
#2Zhenning Tan (IU: Indiana University Bloomington)H-Index: 8
Last. Suchetana Mukhopadhyay (IU: Indiana University Bloomington)H-Index: 19
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The alphavirus Chikungunya virus is transmitted to humans via infected mosquitos. Most infected humans experience symptoms which can range from short-term fatigue and fever to debilitating arthritis that can last for months or years. Some patients relapse and experience symptoms months or years after the initial bout of disease. The capsid protein of Chikungunya virus forms a shell around the viral RNA genome; this structure is called the nucleocapsid core. The core protects the genome during vi...
#1Gaochan Wu (SDU: Shandong University)H-Index: 6
#2Waleed A. Zalloum (American University of Madaba)H-Index: 6
Last. Peng Zhan (SDU: Shandong University)H-Index: 29
view all 12 authors...
Abstract The HIV-1 capsid (CA) protein plays essential roles in both early and late stages of HIV-1 replication and is considered an important, clinically unexploited therapeutic target. As such, small drug-like molecules that inhibit this critical HIV-1 protein have become a priority for several groups. Therefore, in this study we explore small molecule targeting of the CA protein, and in particular a very attractive inter-protomer pocket. We report the design, parallel synthesis, and anti-HIV-...
6 CitationsSource