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Synthesis and Functions of Peptides and Peptidomimetics

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A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Macromolecules".

Deadline for manuscript submissions: 20 September 2024 | Viewed by 4471

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Special Issue Editor

Prof. Dr. Gábor Mező

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Guest Editor

Department of Organic Chemistry, ELTE Eötvös Loránd University, Pázmány Péter sétány 1/A, H-1117 Budapest, Hungary
Interests: targeted tumor therapy; peptide synthesis; peptide–drug conjugates; GnRH derivatives; combination of drug delivery systems
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Dear Colleagues,

In recent decades, peptides have received increasing interest in many areas of research; this is due to their high selectivity caused by specific interactions with their targets. There is a broad spectrum in the possible applications of peptides from therapies of illnesses, a part of diagnostic tools, targeting moieties for drug delivery, and the development of hydrogels or other nanoparticles, up to being ingredients in cosmetics. The number of approved peptide-based drugs is continuously increasing, and on average ca. 20 new compounds reach clinical-phase studies, showing the importance of peptides in drug development. Next to the advantages like high specificity and low immunogenicity as well as toxicity, there are some weaknesses of peptides, including a short half-life and fast degradation in human plasma, low oral bioavailability, and, in the case of many short peptides, high conformational flexibility, and therefore low binding affinity. Thus, the main efforts for the development of peptide-based drugs focus on suitable modifications with which to overcome these drawbacks. Substitution with non-native amino acids, cyclization, and using retro-inverso peptides till the development of peptidomimetics all may help to prepare potential drug candidates with not only high efficacy but also higher bioavailability and slower decomposition as well as clearance.

Now we start a new Special Issue in the open access MDPI journal International Journal of Molecular Science, with the title “Synthesis and Functions of Peptides and Peptidomimetics”. We eagerly await review or full papers on the topics mentioned above.

Prof. Dr. Gábor Mező
Guest Editor

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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

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Keywords

peptides
peptidomimetics
peptide-based drugs
structure optimization
synthesis

Published Papers (4 papers)

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Research

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17 pages, 1293 KiB

Open AccessArticle

Antibacterial and Hemolytic Activity of Antimicrobial Hydrogels Utilizing Immobilized Antimicrobial Peptides

by Edvin Blomstrand, Elin Posch, Annija Stepulane, Anand K. Rajasekharan and Martin Andersson

Int. J. Mol. Sci. 2024, 25(8), 4200; https://doi.org/10.3390/ijms25084200 - 10 Apr 2024

Viewed by 584

Abstract

Antimicrobial peptides (AMPs) are viewed as potential compounds for the treatment of bacterial infections. Nevertheless, the successful translation of AMPs into clinical applications has been impeded primarily due to their low stability in biological environments and potential toxicological concerns at higher concentrations. The covalent attachment of AMPs to a material’s surface has been sought to improve their stability. However, it is still an open question what is required to best perform such an attachment and the role of the support. In this work, six different AMPs were covalently attached to a long-ranged ordered amphiphilic hydrogel, with their antibacterial efficacy evaluated and compared to their performance when free in solution. Among the tested AMPs were four different versions of synthetic end-tagged AMPs where the sequence was altered to change the cationic residue as well as to vary the degree of hydrophobicity. Two previously well-studied AMPs, Piscidin 1 and Omiganan, were also included as comparisons. The antibacterial efficacy against Staphylococcus aureus remained largely consistent between free AMPs and those attached to surfaces. However, the activity pattern against Pseudomonas aeruginosa on hydrogel surfaces displayed a marked contrast to that observed in the solution. Additionally, all the AMPs showed varying degrees of hemolytic activity when in solution. This activity was entirely diminished, and all the AMPs were non-hemolytic when attached to the hydrogels. Full article

(This article belongs to the Special Issue Synthesis and Functions of Peptides and Peptidomimetics)

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13 pages, 3064 KiB

Open AccessArticle

Unveiling the Oxazolidine Character of Pseudoproline Derivatives by Automated Flow Peptide Chemistry

by Szebasztián Szaniszló, Antal Csámpai, Dániel Horváth, Richárd Tomecz, Viktor Farkas and András Perczel

Int. J. Mol. Sci. 2024, 25(8), 4150; https://doi.org/10.3390/ijms25084150 - 9 Apr 2024

Viewed by 578

Abstract

Pseudoproline derivatives such as Thr(ΨPro)-OH are commonly used in peptide synthesis to reduce the likelihood of peptide aggregation and to prevent aspartimide (Asi) formation during the synthesis process. In this study, we investigate notable by-products such as aspartimide formation and an imine derivative of the Thr(ΨPro) moiety observed in flow peptide chemistry synthesis. To gain insight into the formation of these unexpected by-products, we design a series of experiments. Furthermore, we demonstrate the oxazolidine character of the pseudoproline moiety and provide plausible mechanisms for the two-way ring opening of oxazolidine leading to these by-products. In addition, we present evidence that Asi formation appears to be catalyzed by the presence of the pseudoproline moiety. These observed side reactions are attributed to elevated temperature and pressure; therefore, caution is advised when using ΨPro derivatives under such harsh conditions. In addition, we propose a solution whereby thermodynamically controlled Asi formation can be kinetically prevented. Full article

(This article belongs to the Special Issue Synthesis and Functions of Peptides and Peptidomimetics)

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21 pages, 2878 KiB

Open AccessArticle

Targeting the Melanocortin 1 Receptor in Melanoma: Biological Activity of α-MSH–Peptide Conjugates

by Ildikó Szabó, Beáta Biri-Kovács, Balázs Vári, Ivan Ranđelović, Diána Vári-Mező, Éva Juhász, Gábor Halmos, Szilvia Bősze, József Tóvári and Gábor Mező

Int. J. Mol. Sci. 2024, 25(2), 1095; https://doi.org/10.3390/ijms25021095 - 16 Jan 2024

Cited by 1 | Viewed by 939

Abstract

Malignant melanoma is one of the most aggressive and resistant tumor types, with high metastatic properties. Because of the lack of suitable chemotherapeutic agents for treatment, the 5-year survival rate of melanoma patients with regional and distant metastases is lower than 10%. Targeted tumor therapy that provides several promising results might be a good option for the treatment of malignant melanomas. Our goal was to develop novel melanoma-specific peptide–drug conjugates for targeted tumor therapy. Melanocortin-1-receptor (MC1R) is a cell surface receptor responsible for melanogenesis and it is overexpressed on the surface of melanoma cells, providing a good target. Its native ligand, α-MSH (α-melanocyte-stimulating hormone) peptide, or its derivatives, might be potential homing devices for this purpose. Therefore, we prepared three α-MSH derivative–daunomycin (Dau) conjugates and their in vitro and in vivo antitumor activities were compared. Dau has an autofluorescence property; therefore, it is suitable for preparing conjugates for in vitro (e.g., cellular uptake) and in vivo experiments. Dau was attached to the peptides via a non-cleavable oxime linkage that was applied efficiently in our previous experiments, resulting in conjugates with high tumor growth inhibition activity. The results indicated that the most promising conjugate was the compound in which Dau was connected to the side chain of Lys (Ac-SYSNleEHFRWGK(Dau=Aoa)PV-NH₂). The highest cellular uptake by melanoma cells was demonstrated using the compound, with the highest tumor growth inhibition detected both on mouse (38.6% on B16) and human uveal melanoma (55% on OMC-1) cells. The effect of the compound was more pronounced than that of the free drug. Full article

(This article belongs to the Special Issue Synthesis and Functions of Peptides and Peptidomimetics)

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Review

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35 pages, 2084 KiB

Open AccessReview

Exploring the Potential of Bioactive Peptides: From Natural Sources to Therapeutics

by Kruttika Purohit, Narsimha Reddy and Anwar Sunna

Int. J. Mol. Sci. 2024, 25(3), 1391; https://doi.org/10.3390/ijms25031391 - 23 Jan 2024

Cited by 2 | Viewed by 1962

Abstract

Bioactive peptides, specific protein fragments with positive health effects, are gaining traction in drug development for advantages like enhanced penetration, low toxicity, and rapid clearance. This comprehensive review navigates the intricate landscape of peptide science, covering discovery to functional characterization. Beginning with a peptidomic exploration of natural sources, the review emphasizes the search for novel peptides. Extraction approaches, including enzymatic hydrolysis, microbial fermentation, and specialized methods for disulfide-linked peptides, are extensively covered. Mass spectrometric analysis techniques for data acquisition and identification, such as liquid chromatography, capillary electrophoresis, untargeted peptide analysis, and bioinformatics, are thoroughly outlined. The exploration of peptide bioactivity incorporates various methodologies, from in vitro assays to in silico techniques, including advanced approaches like phage display and cell-based assays. The review also discusses the structure–activity relationship in the context of antimicrobial peptides (AMPs), ACE-inhibitory peptides (ACEs), and antioxidative peptides (AOPs). Concluding with key findings and future research directions, this interdisciplinary review serves as a comprehensive reference, offering a holistic understanding of peptides and their potential therapeutic applications. Full article

(This article belongs to the Special Issue Synthesis and Functions of Peptides and Peptidomimetics)

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