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Miscellaneous

Dipyrimidine-based inhibitors of HIV-1 integrase

Pages 289-292 | Published online: 02 Mar 2005

Bibliography

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  • ••An important paper validating HIV-1integrase as a target of a series of diketo acid-containing compounds.
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  • ••The first review of the entire patentliterature covering the small-molecule inhibitors of HIV-1 integrase for the years 1992-2002.
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  • •This paper describes that a selected diketo acid-containing inhibitor competes with target DNA and provides evidence that a conformation of integrase that is only adopted after assembly is important for drug binding.
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  • ••This paper describes a series of sulfonesand a mercaptobenzene sulfone as inhibitors of HIV-1 integrase.
  • NEAMATI N, MAZUMDER A, SUNDERS etal.: 2-Mercaptobenzenesulfonamides as novel class of human immunodeficiency Type 1 (HIV-1) integrase and HIV-1 replication. Antimicrob. Agents Chemother. (1997) 8:485–495.
  • ••The first report of mercaptobenzenecontaining inhibitors of HIV-1 integrase.
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  • •An important paper describing the role ofdivalent metals and cysteine 65 for binding of the mercaptosalicylhydrazides on the active site of HIV-1 integrase.

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