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Peptides and Their Synthetic Analogs in Medicine and Biotechnology

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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: closed (1 October 2022) | Viewed by 16940

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Dr. Volker Knecht

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Institute of Physics, Universität Freiburg im Breisgau, Freiburg im Breisgau, Germany
Interests: biomolecular simulation; protein function; biomembranes; neurodegenerative diseases; viral diseases; antimicrobial peptides; molecular recognition; surface adsorption; thermodynamics
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Dear Colleagues,

Peptides and short proteins provide a promising new generation of biologically active tools with a wide range of novel applications in medicine and biotechnology. Structural modification of peptides leads to the class of peptidomimetics whose value is considerably enhanced compared to their native predecessors. Peptides are employed to fight microbes or cancer, as neuromodulators or hormones or as a basis of vaccines and drug delivery systems. Self-assembling peptides may serve as biomaterials in tissue engineering for creating blood vessels or as substrates for neurite outgrowth and synapse formation. Finally, peptides may be applied in bionanotechnology to create microchips, sensors, electronic devices, as well as nanosized rods or tubes.

For this Special Issue, we invite submissions of both topical reviews and original research articles focused on the synthesis as well as structural and functional studies of peptides and peptidomimetics to be applied in medicine or biotechnology.

Dr. Volker Knecht
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

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.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

peptides
short proteins
peptidomimetics
antimicrobial peptides
anticancer peptides
peptide neuromodulation
peptide hormones
peptide-based vaccines
peptide-based drug delivery systems
peptide-based biomaterials
peptide-based substrates
self-assembling peptides
peptide nanotechnology
peptide chips
peptide microarrays
peptide-based biosensors
peptide-based bioelectronics
peptide-based nanorods
peptide-based nanotubes
radio-labeled peptides
peptide–metal wires

Published Papers (6 papers)

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Research

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14 pages, 3127 KiB

Open AccessArticle

Tailoring the Structure of Cell Penetrating DNA and RNA Binding Nucleopeptides

by Stefano Tomassi, Caterina Ieranò, Alessandra Del Bene, Antonia D’Aniello, Maria Napolitano, Giuseppina Rea, Federica Auletta, Luigi Portella, Anna Capiluongo, Vincenzo Mazzarella, Rosita Russo, Angela Chambery, Stefania Scala, Salvatore Di Maro and Anna Messere

Int. J. Mol. Sci. 2022, 23(15), 8504; https://doi.org/10.3390/ijms23158504 - 31 Jul 2022

Cited by 3 | Viewed by 1591

Abstract

Synthetic nucleic acid interactors represent an exciting research field due to their biotechnological and potential therapeutic applications. The translation of these molecules into drugs is a long and difficult process that justifies the continuous research of new chemotypes endowed with favorable binding, pharmacokinetic and pharmacodynamic properties. In this scenario, we describe the synthesis of two sets of homo-thymine nucleopeptides, in which nucleobases are inserted in a peptide structure, to investigate the role of the underivatized amino acid residue and the distance of the nucleobase from the peptide backbone on the nucleic acid recognition process. It is worth noting that the CD spectroscopy investigation showed that two of the reported nucleopeptides, consisting of alternation of thymine functionalized L-Orn and L-Dab and L-Arg as underivatized amino acids, were able to efficiently bind DNA and RNA targets and cross both cell and nuclear membranes. Full article

(This article belongs to the Special Issue Peptides and Their Synthetic Analogs in Medicine and Biotechnology)

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14 pages, 2310 KiB

Open AccessArticle

Improving the Therapeutic Index of Smp24, a Venom-Derived Antimicrobial Peptide: Increased Activity against Gram-Negative Bacteria

by Kirstie M. Rawson, Melissa M. Lacey, Peter N. Strong and Keith Miller

Int. J. Mol. Sci. 2022, 23(14), 7979; https://doi.org/10.3390/ijms23147979 - 20 Jul 2022

Cited by 4 | Viewed by 2665

Abstract

Antimicrobial peptides (AMPs) are naturally occurring compounds which possess a rapid killing mechanism and low resistance potential. Consequently, they are being viewed as potential alternatives to traditional antibiotics. One of the major factors limiting further development of AMPs is off-target toxicity. Enhancements to antimicrobial peptides which can maximise antimicrobial activity whilst reducing mammalian cytotoxicity would make these peptides more attractive as future pharmaceuticals. We have previously characterised Smp24, an AMP derived from the venom of the scorpion Scorpio maurus palmatus. This study sought to better understand the relationship between the structure, function and bacterial selectivity of this peptide by performing single amino acid substitutions. The antimicrobial, haemolytic and cytotoxic activity of modified Smp24 peptides was determined. The results of these investigations were compared with the activity of native Smp24 to determine which modifications produced enhanced therapeutic indices. The structure–function relationship of Smp24 was investigated by performing N-terminal, mid-chain and C-terminal amino acid substitutions and determining the effect that they had on the antimicrobial and cytotoxic activity of the peptide. Increased charge at the N-, mid- and C-termini of the peptide resulted in increased antimicrobial activity. Increased hydrophobicity at the N-terminus resulted in reduced haemolysis and cytotoxicity. Reduced antimicrobial, haemolytic and cytotoxic activity was observed by increased hydrophobicity at the mid-chain. Functional improvements have been made to modified peptides when compared with native Smp24, which has produced peptides with enhanced therapeutic indices. Full article

(This article belongs to the Special Issue Peptides and Their Synthetic Analogs in Medicine and Biotechnology)

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19 pages, 13099 KiB

Open AccessArticle

Pep19 Has a Positive Effect on Insulin Sensitivity and Ameliorates Both Hepatic and Adipose Tissue Phenotype of Diet-Induced Obese Mice

by Renata Silvério, Robson Barth, Andrea S. Heimann, Patrícia Reckziegel, Gustavo J. dos Santos, Silvana Y. Romero-Zerbo, Francisco J. Bermúdez-Silva, Alex Rafacho and Emer S. Ferro

Int. J. Mol. Sci. 2022, 23(8), 4082; https://doi.org/10.3390/ijms23084082 - 7 Apr 2022

Cited by 1 | Viewed by 3907

Abstract

Peptide DIIADDEPLT (Pep19) has been previously suggested to improve metabolic parameters, without adverse central nervous system effects, in a murine model of diet-induced obesity. Here, we aimed to further evaluate whether Pep19 oral administration has anti-obesogenic effects, in a well-established high-fat diet-induced obesity model. Male Swiss mice, fed either a standard diet (SD) or high-fat diet (HFD), were orally administrated for 30 consecutive days, once a day, with saline vehicle or Pep19 (1 mg/kg). Next, several metabolic, morphological, and behavioral parameters were evaluated. Oral administration of Pep19 attenuated HFD body-weight gain, reduced in approximately 40% the absolute mass of the endocrine pancreas, and improved the relationship between circulating insulin and peripheral insulin sensitivity. Pep19 treatment of HFD-fed mice attenuated liver inflammation, hepatic fat distribution and accumulation, and lowered plasma alanine aminotransferase activity. The inguinal fat depot from the SD group treated with Pep19 showed multilocular brown-fat-like cells and increased mRNA expression of uncoupling protein 1 (UCP1), suggesting browning on inguinal white adipose cells. Morphological analysis of brown adipose tissue (BAT) from HFD mice showed the presence of larger white-like unilocular cells, compared to BAT from SD, Pep19-treated SD or HFD mice. Pep19 treatment produced no alterations in mice behavior. Oral administration of Pep19 ameliorates some metabolic traits altered by diet-induced obesity in a Swiss mice model. Full article

(This article belongs to the Special Issue Peptides and Their Synthetic Analogs in Medicine and Biotechnology)

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13 pages, 1939 KiB

Open AccessArticle

Synthetic Collagen-like Polymer That Undergoes a Sol–Gel Transition Triggered by O–N Acyl Migration at Physiological pH

by Shinichiro F. Ichise and Takaki Koide

Int. J. Mol. Sci. 2022, 23(3), 1584; https://doi.org/10.3390/ijms23031584 - 29 Jan 2022

Viewed by 2966

Abstract

We previously reported an artificial collagen gel that can be used as a cell-culture substrate by end-to-end cross-linking of collagen-like triple-helical peptides via disulfide bonds. However, the gel had to be formed a priori by polymerizing the peptide in an acidic solution containing dimethyl sulfoxide for several days, which prevented its use as an injectable gel or three-dimensional (3D) scaffold for cell culture. In this study, we developed a collagen-like peptide polymer by incorporating an O–N acyl migration-triggered triple helix formation mechanism into a collagen-like peptide, which formed a gel within 10 min. We demonstrated that the collagen-like peptide polymer can be used as a 3D cell scaffold and that the 3D structure formation of cells can be controlled by collagen-derived bioactive sequences introduced into the peptide sequence. Full article

(This article belongs to the Special Issue Peptides and Their Synthetic Analogs in Medicine and Biotechnology)

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Review

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27 pages, 2420 KiB

Open AccessReview

Antiviral Peptides as Anti-Influenza Agents

by Mariangela Agamennone, Marialuigia Fantacuzzi, Giovanni Vivenzio, Maria Carmina Scala, Pietro Campiglia, Fabiana Superti and Marina Sala

Int. J. Mol. Sci. 2022, 23(19), 11433; https://doi.org/10.3390/ijms231911433 - 28 Sep 2022

Cited by 8 | Viewed by 2607

Abstract

Influenza viruses represent a leading cause of high morbidity and mortality worldwide. Approaches for fighting flu are seasonal vaccines and some antiviral drugs. The development of the seasonal flu vaccine requires a great deal of effort, as careful studies are needed to select the strains to be included in each year’s vaccine. Antiviral drugs available against Influenza virus infections have certain limitations due to the increased resistance rate and negative side effects. The highly mutative nature of these viruses leads to the emergence of new antigenic variants, against which the urgent development of new approaches for antiviral therapy is needed. Among these approaches, one of the emerging new fields of “peptide-based therapies” against Influenza viruses is being explored and looks promising. This review describes the recent findings on the antiviral activity, mechanism of action and therapeutic capability of antiviral peptides that bind HA, NA, PB1, and M2 as a means of countering Influenza virus infection. Full article

(This article belongs to the Special Issue Peptides and Their Synthetic Analogs in Medicine and Biotechnology)

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17 pages, 670 KiB

Open AccessReview

Roles of Antimicrobial Peptides in Gynecological Cancers

by Chongyi Zhao, Shuo Yan, Yuzhu Song and Xueshan Xia

Int. J. Mol. Sci. 2022, 23(17), 10104; https://doi.org/10.3390/ijms231710104 - 3 Sep 2022

Cited by 5 | Viewed by 2412

Abstract

Antimicrobial peptides (AMPs) are essential components of the mucosal barrier of the female reproductive tract (FRT) and are involved in many important physiological processes, including shaping the microbiota and maintaining normal reproduction and pregnancy. Gynecological cancers seriously threaten women’s health and bring a heavy burden to society so that new strategies are needed to deal with these diseases. Recent studies have suggested that AMPs also have a complex yet intriguing relationship with gynecological cancers. The expression level of AMPs changes during tumor progression and they may act as promising biomarkers in cancer detection and prognosis prediction. Although AMPs have long been considered as host protective, they actually play a “double-edged sword” role in gynecological cancers, either tumorigenic or antitumor, depending on factors such as AMP and cancer types, as well as AMP concentrations. Moreover, AMPs are associated with chemoresistance and regulation of AMPs’ expression may alter sensitivity of cancer cells to chemotherapy. However, more work is needed, especially on the identification of molecular mechanisms of AMPs in the FRT, as well as the clinical application of these AMPs in detection, diagnosis and treatment of gynecological malignancies. Full article

(This article belongs to the Special Issue Peptides and Their Synthetic Analogs in Medicine and Biotechnology)

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