Identification of small peptides inhibiting the integrase-LEDGF/p75 interaction through targeting the cellular co-factor (pages 651–658)
Claudia Cavalluzzo, Frauke Christ, Arnout Voet, Ajendra Sharma, Brajendra Kumar Singh, Kam Y.J. Zhang, Eveline Lescrinier, Marc De Maeyer, Zeger Debyser and Erik Van der Eycken
Article first published online: 27 AUG 2013 | DOI: 10.1002/psc.2543
In this work, we present the design, synthesis, and evaluation of LP21, a short peptide that is able to inhibit the LEDGF/p75-IN interaction at low μM concentration through its binding to the IN binding site of LEDGF/p75. Our discovery could lead to the synthesis of a peptidomimetic with high anti-HIV activity targeting the cellular co-factor LEDGF/p75 and not the viral protein IN.