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- Title
Inhibitory profile of a LEDGF/p75 peptide against HIV-1 integrase: Insight into integrase–DNA complex formation and catalysis
- Authors
Al-Mawsawi, Laith Q.; Christ, Frauke; Dayam, Raveendra; Debyser, Zeger; Neamati, Nouri
- Abstract
Abstract: A lens epithelium-derived growth factor (LEDGF)/p75 peptide was evaluated for human immunodeficiency virus type 1 integrase (IN) inhibitory activity. The LEDGF/p75 peptide modestly inhibited IN catalysis and was dependent on IN–DNA assembly. The peptide was also effective at disrupting LEDGF/p75–IN complex formation. We next investigated the activity of the LEDGF/p75 peptide on IN mutant proteins that are unable to catalyze the DNA strand transfer reaction. The LEDGF/p75 peptide displayed an increased potency on these IN proteins, from 5-fold to greater than 10-fold, indicating the IN multimeric state greatly influences the peptide inhibitory effects. These results shed light on IN–DNA multimeric formation, and how this process influences the LEDGF/p75–IN interaction.
- Subjects
HIV; GROWTH factors; PEPTIDES; CATALYSIS
- Publication
FEBS Letters, 2008, Vol 582, Issue 10, p1425
- ISSN
0014-5793
- Publication type
Article
- DOI
10.1016/j.febslet.2008.02.076