HIV-1 Integrase

MSH derivatives may serve as leads for antiviral therapeutics

Published in AIDS Weekly, February 17th, 2003

According to recent research from the United States, "Human immunodeficiency virus type 1 integrase (HIV-1 IN) is an essential enzyme for effective viral replication. Therefore, IN inhibitors are being sought for chemotherapy against AIDS.

"Herein, we report the design, synthesis, and antiviral activity of three novel mercaptosalicylhydrazide (MSH) derivatives. MSHs were effective against the IN catalytic core domain and inhibited IN binding to HIV LTR DNA. They also inhibited catalytic activities of IN in IN-DNA preassembled complexes. Site-directed mutagenesis and molecular modeling studies suggest that MSHs bind to cysteine 65 and chelate Mg²⁺ at the...

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Source: AIDS Weekly (2003-02-17)

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