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

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Chandra K, Das P, Mamidi S, Hurevich M, Iosub-Amir A, Metanis N, Reches M, Friedler A,


Chandra K, Das P, Mamidi S, Hurevich M, Iosub-Amir A, Metanis N, Reches M, Friedler A, (click to view)

Chandra K, Das P, Mamidi S, Hurevich M, Iosub-Amir A, Metanis N, Reches M, Friedler A,

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ChemMedChem 2016 6 22() doi 10.1002/cmdc.201600190

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.

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