reviewJournal of Medicinal ChemistryFeb 19, 2014HYBRID OA

Hydrocarbon-Stapled Peptides: Principles, Practice, and Progress

Boston Children's Hospital · Harvard University · +1 more institution

PubMed
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Abstract

Protein structure underlies essential biological processes and provides a blueprint for molecular mimicry that drives drug discovery. Although small molecules represent the lion's share of agents that target proteins for therapeutic benefit, there remains no substitute for the natural properties of proteins and their peptide subunits in the majority of biological contexts. The peptide α-helix represents a common structural motif that mediates communication between signaling proteins. Because peptides can lose their shape when taken out of context, developing chemical interventions to stabilize their bioactive structure remains an active area of research. The all-hydrocarbon staple has emerged as one such…

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