Stapled peptides: Providing the best of both worlds in drug development

Xiayang Xie, Lixia Gao, Austin Y. Shull, Yong Teng

Research output: Contribution to journalReview articlepeer-review

13 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)1969-1980
Number of pages12
JournalFuture Medicinal Chemistry
Issue number16
StatePublished - Oct 2016


  • drug development
  • protein-protein interactions
  • stapled peptides

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Drug Discovery


Dive into the research topics of 'Stapled peptides: Providing the best of both worlds in drug development'. Together they form a unique fingerprint.

Cite this