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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:23

Article

Zentner, Isaac¹  Sierra, Luz-Jeannette²  Maciunas, Lina¹  Vinnik, Andrei³  Fedichev, Peter³  Mankowski, Marie K.⁴  Ptak, Roger G.⁴  Martin-Garcia, Julio²  Cocklin, Simon¹ 

[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

关键词: Virtual screening;    HIV-1 matrix protein;    Surface plasmon resonance;    Antiviral;   

DOI  :  10.1016/j.bmcl.2012.11.041

来源: Elsevier

【 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.

【 授权许可】

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