doi: 10.1016/j.bmc.2008.02.060.
Epub 2008 Mar 11.
Sidechain-linked inhibitors of HIV-1 protease dimerization
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- PMID: 18337105
- DOI: 10.1016/j.bmc.2008.02.060
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Sidechain-linked inhibitors of HIV-1 protease dimerization
Bioorg Med Chem.
.
Abstract
There is a great need for alternative modes of inhibition for the design of anti-HIV therapies, due to the increased resistance of HIV to currently approved drugs. A novel strategy for generating potent dimerization inhibitors of HIV-1 protease is described based on sidechain-linked interfacial peptides. In a number of cases the activity of these agents against HIV-1 protease was found to be among the most potent reported, with inhibitory constants in the low nM range.
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