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

作者: Xiayang Xie , Lixia Gao , Austin Y Shull , Yong Teng

DOI: 10.4155/FMC-2016-0102

关键词: Therapeutic modalitiesTherapeutic proteinDrugDrug discoveryDrug developmentPeptidePharmacologyProtein–protein interactionChemistryComputational biologyResearch strategies

摘要: Peptide-based drug discovery has experienced a remarkable resurgence within the past decade due to emerging class of inhibitors known as stapled peptides. Stapled peptides are therapeutic protein mimetics that have been locked specific conformational structure by hydrocarbon stapling. These highly important in selectively impairing disease-relevant protein–protein interactions and exhibit significant pharmacokinetic advantages over other forms therapeutics terms affinity, specificity, size, synthetic accessibility resistance proteolytic degradation. A series currently development, potential successes these peptides, either single-agent treatments or combinational with modalities, could potentially change landscape development. Here, we provide examples successful efforts illustrate research strategies design develo...

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