peptide-serum-or-niacinamide-first The solid-phase peptide synthesis (SPPS) of lacticin 3147, a two-component lantibiotic, represents a significant achievement in the chemical synthesis of complex antimicrobial peptides. This method allows for the construction of both constituent peptides, Ltnα and Ltnβ, which are essential for lacticin 3147's dual-acting bacteriocin activity. SPPS offers a versatile platform for generating not only the native peptides but also valuable analogues, enabling detailed studies into their structure-activity relationships and potential therapeutic applications. The development of robust SPPS strategies for lacticin 3147 facilitates the exploration of modified backbones, altered ring structures, and the incorporation of unnatural amino acids, pushing the boundaries of peptide synthesisLanthipeptides: chemical synthesis versus in vivo biosynthesis ....
Early research focused on the successful construction of both peptides comprising lacticin 3147 through solid-phase peptide synthesis. This marked a crucial step in enabling researchers to obtain sufficient quantities of these peptides for detailed biological and structural characterization. The ability to perform these syntheses on-resin proved to be a general and effective approach, paving the way for further modifications and analogue development. Subsequent work has explored various SPPS techniques, including those combined with ring-closing metathesis, to efficiently synthesize the olefin-containing lacticin 3147 A2.Standard practices for Fmoc-based solid-phase peptide ...
Beyond the native sequence, SPPS has been instrumental in creating analogues of lacticin 3147. These modifications often target specific regions, such as the N-terminus A-ring fragment, or involve replacing key amino acids to investigate their impact on activity. For instance, the synthesis of lacticin 3147 analogues with modifications at position 5, including Dha replacements with glycine or alanine, has been achievedThe role of chemical synthesis in developing RiPP antibiotics. Furthermore, SPPS techniques have been employed in the synthesis of non-lanthionine-containing carbocyclic analogues of the lacticin 3147 β-peptide, expanding the scope of structural explorationThe role of chemical synthesis in developing RiPP antibiotics.
Lacticin 3147 is characterized by its unique two-peptide structure, consisting of Ltnα and Ltnβ. These peptides work synergistically to exert their antimicrobial effect, primarily against Gram-positive bacteria, including pathogenic species like *Listeria monocytogenes*.作者：VR Pattabiraman·2008—Vederas and co-workers describe the firstsolid-supported synthesis of lacticin 3147, the bis(desmethyl) analogue of lacticin A2. This compound ... The dual-acting nature means that the peptides sequentially target the bacterial cell wall, ultimately leading to cell deathSPPS is a synthetic method that allows for the efficient and rapid production ofpeptidesusingsolid-phasesupports. This technique involves stepwise addition .... This complex mode of action makes lacticin 3147 an attractive candidate for antimicrobial research and potential biotechnological applications.
Solid-phase peptide synthesis (SPPS) provides a powerful and widely adopted method for the efficient and rapid production of peptides. Its core principle involves the stepwise addition of amino acids to a growing peptide chain anchored to an insoluble solid support. This approach simplifies purification, as excess reagents and byproducts can be easily washed away after each coupling step作者：A Kuipers·2008·被引用次数：46—The lantibiotics nisin andlacticin 3147are produced by some distinct Lactococcus lactis strains and inhibit a broad range of gram-positive bacterial species.. The development of protocols, such as those based on Fmoc chemistry, has further enhanced the efficiency and reliability of SPPS for synthesizing complex peptides, including those with challenging sequences and post-translational modifications characteristic of lantibiotics like lacticin 3147.
SPPS techniques are not limited to linear peptide synthesis; they also extend to the creation of cyclic peptides作者：SM Rowe·2021·被引用次数：38—The chemical synthesis of cyclotides typically involvessolid-phase peptide synthesis... lacticin 3147 A1 peptide, but loses its inherent .... For complex structures like lacticin 3147, which contains thioether bridges and potentially other cyclic elements, SPPS combined with cyclization strategies (like ring-closing metathesis or on-resin cyclizations) is essentialSynthesis Notes. The ability to synthesize analogues with unnatural amino acids or modified backbones using SPPS opens up avenues for improving stability, potency, or delivery characteristics of bacteriocins.
The chemical synthesis of lacticin 3147 and its analogues through solid-phase peptide synthesis is crucial for understanding its fundamental biological functions and exploring its potential applications. Research into its biosynthesis, molecular mechanisms, and immunity systems continues, often supported by synthetically produced peptides. The ability to generate lacticin 3147 and related compounds via SPPS could lead to their use in various fields, from food preservation, as part of multi-bacteriocin starter cultures, to therapeutic interventions against resistant bacterial strains. The ongoing refinement of SPPS methodologies promises to make the synthesis of such complex peptides more accessible and efficient, driving further innovation in the field of antimicrobial peptides作者：PJ Knerr·2012·被引用次数：92—The successful construction of lactocin S and both peptides of lacticin 3147 bysolid-phase peptide synthesis(SPPS) highlight the ....
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