Covalent Inhibition of HIV-1 Integrase by N-Succinimidyl Peptides

Koushik Chandra, Priyadip Das, Samarasimhareddy Mamidi, Mattan Hurevich, Anat Iosub-Amir, Norman Metanis, Meital Reches, Assaf Friedler

Research output: Contribution to journalArticlepeer-review

Abstract

We present a new approach for the covalent inhibition of HIV-1 integrase (IN) by an LEDGF/p75-derived peptide modified with an N-terminal succinimide group. The covalent inhibition is mediated by direct binding of the succinimide to the amine group of a lysine residue in IN. The peptide serves as a specific recognition sequence for the target protein, while the succinimide serves as the binding moiety. The combination of a readily synthesizable peptide precursor with easy and efficient binding to the target protein makes this approach a promising new strategy for designing lead compounds.

Original languageAmerican English
Pages (from-to)1987-1994
Number of pages8
JournalChemMedChem
DOIs
StatePublished - 2016

Keywords

  • HIV-1 integrase
  • covalent inhibitors
  • peptides
  • succinimide

All Science Journal Classification (ASJC) codes

  • Drug Discovery
  • General Pharmacology, Toxicology and Pharmaceutics
  • Molecular Medicine
  • Biochemistry
  • Pharmacology
  • Organic Chemistry

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