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Template-constrained cyclic sulfopeptide HIV-1 entry inhibitors.


ABSTRACT: Template-constrained cyclic sulfopeptides that inhibit HIV-1 entry were rationally designed based on a loop from monoclonal antibody (mAb) 412d. A focused set of sulfopeptides was synthesized using Fmoc-Tyr(SO3DCV)-OH (DCV = 2,2-dichlorovinyl). Three cyclic sulfopeptides that inhibit entry of HIV-1 and complement the activity of known CCR5 antagonists were identified.

SUBMITTER: Rudick JG 

PROVIDER: S-EPMC3889485 | biostudies-literature | 2013 Nov

REPOSITORIES: biostudies-literature

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Template-constrained cyclic sulfopeptide HIV-1 entry inhibitors.

Rudick Jonathan G JG   Laakso Meg M MM   Schloss Ashley C AC   DeGrado William F WF  

Organic & biomolecular chemistry 20131101 41


Template-constrained cyclic sulfopeptides that inhibit HIV-1 entry were rationally designed based on a loop from monoclonal antibody (mAb) 412d. A focused set of sulfopeptides was synthesized using Fmoc-Tyr(SO3DCV)-OH (DCV = 2,2-dichlorovinyl). Three cyclic sulfopeptides that inhibit entry of HIV-1 and complement the activity of known CCR5 antagonists were identified. ...[more]

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