@article { WOS:000383693800004, title = {Covalent Inhibition of HIV-1 Integrase by N-Succinimidyl Peptides}, journal = {CHEMMEDCHEM}, volume = {11}, year = {2016}, note = {[[{"fid":"263824","view_mode":"default","type":"media","attributes":{"style":"width: 400px; height: 91px;","alt":"cmd","class":"img-responsive media-element file-default "}}]] }, month = {SEP}, pages = {1987-1994}, 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.


}, issn = {1860-7179}, doi = {10.1002/cmdc.201600190}, author = {Koushik Chandra and Priyadip Das and Samarasimhareddy Mamidi and Mattan Hurevich and Iosub-Amir, Anat and Norman Metanis and Meital Reches and Assaf Friedler} }