منابع مشابه
Hydrocarbon Stapled Antimicrobial Peptides
Antimicrobial peptides are promising candidates for anti-infective pharmaceuticals. Unfortunately, because of their low proteolytic and chemical stability, their usage is generally narrowed down to topical formulations. Until now, numerous approaches to increase peptide stability have been proposed. One of them, peptide hydrocarbon stapling, a modification based on stabilizing peptide secondary...
متن کاملHydrocarbon-Stapled Peptides: Principles, Practice, and Progress
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 r...
متن کاملDiaminodiacid-based solid-phase synthesis of all-hydrocarbon stapled α-helical peptides.
An alternative stapling strategy is described herein using Fmoc-solid phase peptide synthesis (SPPS) that employed pre-prepared diaminodiacid building blocks to introduce all-hydrocarbon staples into peptides by on-resin cyclization. Compared to unstapled native peptides, diaminodiacid-based stapled peptides exhibited an increased α-helicity ratio and stability toward protease. Moreover, the li...
متن کاملCorrection to Isoform-Selective Disruption of AKAP-Localized PKA Using Hydrocarbon Stapled Peptides
This correction is in regard to Figure 3a. Compound 2K-3 contains a typo in its sequence at position 13 (S instead of K). The sequence should read KKLAKFLVS*ALK*ALK. Its scramble control, 2K-3-scramble, is listed correctly. Compound analysis and all experiments were performed using the compound with the correct sequence. This typo does not change any of the analysis or conclusions in this paper...
متن کاملIsoform-Selective Disruption of AKAP-Localized PKA Using Hydrocarbon Stapled Peptides
A-kinase anchoring proteins (AKAPs) play an important role in the spatial and temporal regulation of protein kinase A (PKA) by scaffolding critical intracellular signaling complexes. Here we report the design of conformationally constrained peptides that disrupt interactions between PKA and AKAPs in an isoform-selective manner. Peptides derived from the A Kinase Binding (AKB) domain of several ...
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ژورنال
عنوان ژورنال: The Protein Journal
سال: 2018
ISSN: 1572-3887,1573-4943
DOI: 10.1007/s10930-018-9755-0