Discovery of a small-molecule antiviral targeting the HIV-1 matrix protein

被引：23

作者：

Zentner, Isaac ^{[1
]}

Sierra, Luz-Jeannette ^{[2
]}

Maciunas, Lina ^{[1
]}

Vinnik, Andrei ^{[3
]}

Fedichev, Peter ^{[3
]}

Mankowski, Marie K. ^{[4
]}

Ptak, Roger G. ^{[4
]}

Martin-Garcia, Julio ^{[2
]}

Cocklin, Simon ^{[1
]}

机构：

[1] Drexel Univ Coll Med, Dept Biochem & Mol Biol, Philadelphia, PA 19102 USA

[2] Drexel Univ Coll Med, Dept Microbiol & Immunol, Philadelphia, PA 19102 USA

[3] Quantum Pharmaceut, QuantumLead, Moscow, Russia

[4] So Res Inst, Dept Infect Dis Res, Frederick, MD 21701 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 04期

关键词：

Virtual screening; HIV-1 matrix protein; Surface plasmon resonance; Antiviral; IMMUNODEFICIENCY-VIRUS TYPE-1; MEMBRANE-BINDING; PLASMA-MEMBRANE; MYRISTYL SWITCH; GAG-PROTEIN; TERMINAL REGION; MUTATIONS; PRECURSOR; DOMAIN; PHOSPHATIDYLINOSITOL-(4,5)-BISPHOSPHATE;

D O I：

10.1016/j.bmcl.2012.11.041

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Due to the emergence of drug-resistant strains and the cumulative toxicities associated with current therapies, demand remains for new inhibitors of HIV-1 replication. The HIV-1 matrix (MA) protein is an essential viral component with established roles in the assembly of the virus. Using virtual and surface plasmon resonance (SPR)-based screening, we describe the identification of the first small molecule to bind to the HIV-1 MA protein and to possess broad range anti-HIV properties. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：1132 / 1135

页数：4

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