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

Bioorg Med Chem Lett.. 2013-02; 23(4):1132-5

Zentner I, Sierra LJ, Maciunas L, Vinnik A, Fedichev P, Mankowski MK, Ptak RG, MartÍn-GarcÍa J, Cocklin S. a Department of Biochemistry & Molecular Biology, Drexel University College of Medicine, 245 N. 15th Street, Philadelphia, PA 19102, USAb Department of Microbiology & Immunology, Drexel University College of Medicine, 245 N. 15th Street, Philadelphia, PA 19102, USAc QuantumLead, Quantum Pharmaceuticals, Moscow, Russiad Department of Infectious Disease Research, Southern Research Institute, 431 Aviation Way, Frederick, MD 21701, USA

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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.