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Template-constrained cyclic sulfopeptide HIV-1 entry inhibitors†
Jonathan G. Rudick,Meg M. Laakso,Ashley C. Schloss,William F. DeGrado
Organic & Biomolecular Chemistry Pub Date : 09/17/2013 00:00:00 , DOI:10.1039/C3OB41395K
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.

Graphical abstract: Template-constrained cyclic sulfopeptide HIV-1 entry inhibitors
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