Special Issue "New Applications and Developments in Synthetic Peptide Chemistry"

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Biopharmaceuticals".

Deadline for manuscript submissions: 15 July 2022 | Viewed by 3900

Special Issue Editors

Dr. Giovanni N. Roviello
E-Mail Website
Guest Editor
Istituto di Biostrutture e Bioimmagini, Naples, Italy
Interests: peptide chemistry; solid phase synthesis; solution synthesis; nucleopeptides; PNA; nucleic acid chemistry; spectroscopic studies; SARS-CoV-2 and MERS-CoV coronaviruses; computational studies
Special Issues, Collections and Topics in MDPI journals
Dr. Rosanna Palumbo
E-Mail Website
Guest Editor
Istituto di Biostrutture e Bioimmagini, Naples, Italy
Interests: qualitative determination of peptides; toxicity screening; antioxidant properties; bioactive peptides; cell culture

Special Issue Information

Dear Colleagues,

Peptide-based therapeutics are of great relevance in biomedicine for the treatment of pathologies of enormous social impact, including cancer, neurodegeneration, and viral diseases, like the current COVID-19 pandemic. In this context, peptide inhibitors of SARS-CoV-2 enzymes are under investigation in the fight against the novel coronavirus. Peptides are able to interact with biomacromolecules involved in crucial biological pathways such as proteins and nucleic acids. Moreover, after functionalization by DNA nucleobases, they become powerful tools in DNA and RNA targeting, as testified by the scientific literature on peptide nucleic acids (PNAs) and nucleopeptides, with known diagnostic and therapeutic potential. Nonetheless, peptide analogues of a different nature are endowed with self-assembly properties at the origin of supramolecular assemblies and nanomaterials, which are attracting increasing attention in nanomedicine and biotechnology. In this Special Issue, we wish to focus on the novel experimental and theoretical approaches for peptide design and development, with particular attention being paid to the solid phase synthesis of natural peptides, PNA, nucleopeptides, peptoids and more general peptide analogs. However, contributions to the solution synthesis of amino acid monomers as building blocks for peptide chain elongation, as well as peptide-nucleic acid and peptide–protein interaction, peptide aggregation, nucleoamino acid and nucleopeptide chemistry, peptide–metal complexes and antimicrobial poly-amino acids are also welcome, as they could improve overall knowledge with regard to the amino acid-based chemistry at the interface between peptide design and pharmaceutical applications. Other themes of interest are inherent to the computational chemistry applied to peptide science.

This Special Issue is open to the submission of both original articles and reviews that describe research and ideas on themes treated in this issue for new applications and developments in synthetic peptide chemistry.

Dr. Giovanni N. Roviello
Dr. Rosanna Palumbo
Guest Editors

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. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2000 CHF (Swiss Francs). 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
  • Amyloid
  • Alzheimer’s disease
  • Parkinson’s disease
  • Neuropeptides
  • Peptide inhibitors
  • Antiviral peptides
  • Anti-COVID-19 peptides
  • Peptide aggregation
  • Polyamino acids
  • Synthetic antivirals
  • Anticancer peptides
  • Peptide synthesis
  • Peptoids
  • PNA
  • Nucleopeptides
  • Nucleoamino acids
  • Peptide supramolecular materials
  • Peptide–-metal complexes
  • Peptide characterization
  • Solid phase peptide synthesis

Published Papers (3 papers)

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Research

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Article
C16 Peptide and Ang-1 Improve Functional Disability and Pathological Changes in an Alzheimer’s Disease Model Associated with Vascular Dysfunction
Pharmaceuticals 2022, 15(4), 471; https://doi.org/10.3390/ph15040471 - 13 Apr 2022
Viewed by 528
Abstract
Alzheimer’s disease (AD) is a neurological disorder characterized by neuronal cell death, tau pathology, and excessive inflammatory responses. Several vascular risk factors contribute to damage of the blood–brain barrier (BBB), secondary leak-out of blood vessels, and infiltration of inflammatory cells, which aggravate the [...] Read more.
Alzheimer’s disease (AD) is a neurological disorder characterized by neuronal cell death, tau pathology, and excessive inflammatory responses. Several vascular risk factors contribute to damage of the blood–brain barrier (BBB), secondary leak-out of blood vessels, and infiltration of inflammatory cells, which aggravate the functional disability and pathological changes in AD. Growth factor angiopoietin-1 (Ang-1) can stabilize the endothelium and reduce endothelial permeability by binding to receptor tyrosine kinase 2 (Tie2). C16 peptide (KAFDITYVRLKF) selectively binds to integrin ανβ3 and competitively inhibits leukocyte transmigration into the central nervous system by interfering with leukocyte ligands. In the present study, 45 male Sprague-Dawley (SD) rats were randomly divided into three groups: vehicle group, C16 peptide + Ang1 (C + A) group, and sham control group. The vehicle and C + A groups were subjected to two-vessel occlusion (2-VO) with artery ligation followed by Aβ1-42 injection into the hippocampus. The sham control group underwent sham surgery and injection with an equal amount of phosphate-buffered saline (PBS) instead of Aβ1-42. The C + A group was administered 1 mL of drug containing 2 mg of C16 and 400 µg of Ang-1 daily for 2 weeks. The sham control and vehicle groups were administered 1 mL of PBS for 2 weeks. Our results showed that treatment with Ang-1 plus C16 improved functional disability and reduced neuronal death by inhibiting inflammatory cell infiltration, protecting vascular endothelial cells, and maintaining BBB permeability. The results suggest that these compounds may be potential therapeutic agents for AD and warrant further investigation. Full article
(This article belongs to the Special Issue New Applications and Developments in Synthetic Peptide Chemistry)
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Article
Structure-Activity Relationship Investigations of Novel Constrained Chimeric Peptidomimetics of SOCS3 Protein Targeting JAK2
Pharmaceuticals 2022, 15(4), 458; https://doi.org/10.3390/ph15040458 - 09 Apr 2022
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Abstract
SOCS3 (suppressor of cytokine signaling 3) protein suppresses cytokine-induced inflammation and its deletion in neurons or immune cells increases the pathological growth of blood vessels. Recently, we designed several SOCS3 peptidomimetics by assuming as template structures the interfacing regions of the ternary complex [...] Read more.
SOCS3 (suppressor of cytokine signaling 3) protein suppresses cytokine-induced inflammation and its deletion in neurons or immune cells increases the pathological growth of blood vessels. Recently, we designed several SOCS3 peptidomimetics by assuming as template structures the interfacing regions of the ternary complex constituted by SOCS3, JAK2 (Janus Kinase 2) and gp130 (glycoprotein 130) proteins. A chimeric peptide named KIRCONG chim, including non-contiguous regions demonstrated able to bind to JAK2 and anti-inflammatory and antioxidant properties in VSMCs (vascular smooth muscle cells). With the aim to improve drug-like features of KIRCONG, herein we reported novel cyclic analogues bearing different linkages. In detail, in two of them hydrocarbon cycles of different lengths were inserted at positions i/i+5 and i/i+7 to improve helical conformations of mimetics. Structural features of cyclic compounds were investigated by CD (Circular Dichroism) and NMR (Nuclear Magnetic Resonance) spectroscopies while their ability to bind to catalytic domain of JAK2 was assessed through MST (MicroScale Thermophoresis) assay as well as their stability in biological serum. Overall data indicate a crucial role exerted by the length and the position of the cycle within the chimeric structure and could pave the way to the miniaturization of SOCS3 protein for therapeutic aims. Full article
(This article belongs to the Special Issue New Applications and Developments in Synthetic Peptide Chemistry)
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Review

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Review
Usage of Synthetic Peptides in Cosmetics for Sensitive Skin
Pharmaceuticals 2021, 14(8), 702; https://doi.org/10.3390/ph14080702 - 21 Jul 2021
Cited by 2 | Viewed by 2060
Abstract
Sensitive skin is characterized by symptoms of discomfort when exposed to environmental factors. Peptides are used in cosmetics for sensitive skin and stand out as active ingredients for their ability to interact with skin cells by multiple mechanisms, high potency at low dosage [...] Read more.
Sensitive skin is characterized by symptoms of discomfort when exposed to environmental factors. Peptides are used in cosmetics for sensitive skin and stand out as active ingredients for their ability to interact with skin cells by multiple mechanisms, high potency at low dosage and the ability to penetrate the stratum corneum. This study aimed to analyze the composition of 88 facial cosmetics for sensitive skin from multinational brands regarding usage of peptides, reviewing their synthetic pathways and the scientific evidence that supports their efficacy. Peptides were found in 17% of the products analyzed, namely: acetyl dipeptide-1 cetyl ester, palmitoyl tripeptide-8, acetyl tetrapeptide-15, palmitoyl tripeptide-5, acetyl hexapeptide-49, palmitoyl tetrapeptide-7 and palmitoyl oligopeptide. Three out of seven peptides have a neurotransmitter-inhibiting mechanism of action, while another three are signal peptides. Only five peptides present evidence supporting their use in sensitive skin, with only one clinical study including volunteers having this condition. Noteworthy, the available data is mostly found in patents and supplier brochures, and not in randomized placebo-controlled studies. Peptides are useful active ingredients in cosmetics for sensitive skin. Knowing their efficacy and synthetic pathways provides meaningful insight for the development of new and more effective ingredients. Full article
(This article belongs to the Special Issue New Applications and Developments in Synthetic Peptide Chemistry)
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