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N. Boggetto, M. Reboud-Ravaux

Dimerization Inhibitors of HIV-1 Protease

By targeting the highly conserved antiparallel ?sheet formed by the interdigitation of the N and Cterminal strands of each monomer, dimerization inhibitors of HIV-1 protease may be useful to overcome the drug resistance observed with current activesite directed antiproteases. Sequestration of the monomer by the inhibitor (or disruption of the dimer interface) prevents the correct assembly of the inactive monomers to active enzyme. Strategies for the design of drugs targeting the dimer interface are described. Various dimerization inhibitors are reported including N and Cterminal mimetics, lipopeptides and crosslinked interface peptides.

Biological Chemistry, Walter de Gruyter

Print ISSN: 1431-6730
Volume: 383, 09/2002
Pages: 1321 - 1324

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