Citation:
Chandra, K. ; Das, P. ; Mamidi, S. ; Hurevich, M. ; Iosub-Amir, A. ; Metanis, N. ; Reches, M. ; Friedler, A. . Covalent Inhibition Of Hiv-1 Integrase By N-Succinimidyl Peptides. CHEMMEDCHEM 2016, 11, 1987-1994.
Date Published:
SEPAbstract:
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.
Notes:
