title: Stapled peptides: providing the best of both worlds in drug development.
abstract: Peptide-based drug discovery has experienced a remarkable resurgence within the past decade due to the emerging class of inhibitors known as stapled peptides. Stapled peptides are therapeutic protein mimetics that have been locked within a specific conformational structure by hydrocarbon stapling. These peptides are highly important in selectively impairing disease-relevant protein-protein interactions and exhibit significant pharmacokinetic advantages over other forms of therapeutics in terms of affinity, specificity, size, synthetic accessibility and resistance to proteolytic degradation. A series of stapled peptides are currently in development, and the potential successes of these peptides, either as single-agent treatments or as combinational treatments with other therapeutic modalities, could potentially change the landscape of protein therapeutic development. Here, we provide examples of successful discovery efforts to illustrate the research strategies of stapled peptides in drug design and development.
authors.affiliation: Department of Pediatrics, Emory Children's Center, Emory University, Atlanta, GA 30322, USA.
authors.forename: Xiayang
authors.initials: X
authors.lastname: Xie
authors.affiliation: Department of Oral Biology, Dental College of Georgia, Augusta University, Augusta, GA 30912, USA.
authors.forename: Lixia
authors.initials: L
authors.lastname: Gao
authors.affiliation: Department of Biology, Presbyterian College, Clinton, SC 29325, USA.
authors.forename: Austin Y
authors.initials: AY
authors.lastname: Shull
authors.affiliation: Department of Oral Biology, Dental College of Georgia, Augusta University, Augusta, GA 30912, USA.|Georgia Cancer Center, Medical College of Georgia, Augusta University, Augusta, GA 30912, USA.|Department of Biochemistry & Molecular Biology, Medical College of Georgia, Augusta University, Augusta, GA 30912, USA.
authors.forename: Yong
authors.initials: Y
authors.lastname: Teng
keywords: drug development; protein–protein interactions; stapled peptides