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Peptide Therapeutics 2.0
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Peptide Therapeutics 2.0

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 May 2022) | Viewed by 24409

Special Issue Editor

Prof. Dr. Beatriz G. De la Torre

E-Mail Website
Guest Editor
School of Laboratory Medicine and Medical Sciences, University of KwaZulu-Natal, Durban 4001, South Africa
Interests: peptides; solid-phase synthesis; cell penetrating peptides; antimicrobial peptides; oligonucleotides; peptide nucleic acids; drug discovery; peptide–drug conjugates
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Interest in peptide drug discovery is continuously growing in the pharmaceutical industry; thus, the number of therapeutic peptides evaluated in clinical trials is increasing. As a result, year on year, the Food and Drug Administration (FDA) and the European Medicines Agency (EMA) have approved several of these chemical entities as new drugs.

As well as being present in new drugs as active pharmaceutical ingredients (APIs), peptides are also used as shuttles to address other drugs to a specific cell or as linkers, for instance, in antibody–drug conjugates (ADCs).

This Special Issue of Molecules, Peptide Therapeutics 2.0, aims to highlight the newest discoveries related to peptides as therapeutic agents.

Prof. Dr. Beatriz G. De la Torre
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. Molecules is an international peer-reviewed open access semimonthly 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 2700 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

  • therapeutic peptides
  • solid-phase peptide synthesis
  • antimicrobial peptides
  • peptides and Alzheimer’s disease
  • peptides and metabolic syndrome
  • peptides and cancer
  • peptides as shuttles
  • peptide-based drug delivery
  • peptide-based vaccines
  • peptide–drug conjugates

Published Papers (5 papers)

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Editorial

Jump to: Research, Review

3 pages, 168 KiB  
Editorial
Peptide Therapeutics 2.0
by Beatriz G. de la Torre and Fernando Albericio
Molecules 2020, 25(10), 2293; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules25102293 - 13 May 2020
Cited by 92 | Viewed by 6480
Abstract
In recent years, the peptide drug discovery field has shown a high level of dynamism, with hundreds of academic groups working on this topic, the creation of new peptide-focused companies, and the consolidation of peptide business by so-called big pharma [...] Full article
(This article belongs to the Special Issue Peptide Therapeutics 2.0)

Research

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19 pages, 2791 KiB  
Article
Tea Bags for Fmoc Solid-Phase Peptide Synthesis: An Example of Circular Economy
by Fanny Guzmán, Adriana Gauna, Tanya Roman, Omar Luna, Claudio Álvarez, Claudia Pareja-Barrueto, Luis Mercado, Fernando Albericio and Constanza Cárdenas
Molecules 2021, 26(16), 5035; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26165035 - 19 Aug 2021
Cited by 18 | Viewed by 4406
Abstract
Peptide synthesis is an area with a wide field of application, from biomedicine to nanotechnology, that offers the option of simultaneously synthesizing a large number of sequences for the purpose of preliminary screening, which is a powerful tool. Nevertheless, standard protocols generate large [...] Read more.
Peptide synthesis is an area with a wide field of application, from biomedicine to nanotechnology, that offers the option of simultaneously synthesizing a large number of sequences for the purpose of preliminary screening, which is a powerful tool. Nevertheless, standard protocols generate large volumes of solvent waste. Here, we present a protocol for the multiple Fmoc solid-phase peptide synthesis in tea bags, where reagent recycling steps are included. Fifty-two peptides with wide amino acid composition and seven to twenty amino acid residues in length were synthesized in less than three weeks. A clustering analysis was performed, grouping the peptides by physicochemical features. Although a relationship between the overall yield and the physicochemical features of the sequences was not established, the process showed good performance despite sequence diversity. The recycling system allowed to reduce N, N-dimethylformamide usage by 25–30% and reduce the deprotection reagent usage by 50%. This protocol has been optimized for the simultaneous synthesis of a large number of peptide sequences. Additionally, a reagent recycling system was included in the procedure, which turns the process into a framework of circular economy, without affecting the quality of the products obtained. Full article
(This article belongs to the Special Issue Peptide Therapeutics 2.0)
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15 pages, 5637 KiB  
Article
The Bioactive Peptide SL-13R Expands Human Umbilical Cord Blood Hematopoietic Stem and Progenitor Cells In Vitro
by Takenobu Nii, Katsuhiro Konno, Masaki Matsumoto, Kanit Bhukhai, Suparerk Borwornpinyo, Kazuhiro Sakai, Suradej Hongeng and Daisuke Sugiyama
Molecules 2021, 26(7), 1995; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26071995 - 01 Apr 2021
Cited by 2 | Viewed by 2778
Abstract
Hematopoietic stem and progenitor cell (HSPC) transplantation is a curative treatment of hematological disorders that has been utilized for several decades. Although umbilical cord blood (UCB) is a promising source of HSPCs, the low dose of HSPCs in these preparations limits their use, [...] Read more.
Hematopoietic stem and progenitor cell (HSPC) transplantation is a curative treatment of hematological disorders that has been utilized for several decades. Although umbilical cord blood (UCB) is a promising source of HSPCs, the low dose of HSPCs in these preparations limits their use, prompting need for ex vivo HSPC expansion. To establish a more efficient method to expand UCB HSPCs, we developed the bioactive peptide named SL-13R and cultured UCB HSPCs (CD34+ cells) with SL-13R in animal component-free medium containing a cytokine cocktail. Following 9 days of culture with SL-13R, the numbers of total cells, CD34+, CD38− cells, and hematopoietic stem cell (HSC)-enriched cells were significantly increased relative to control. Transplantation of cells cultured with SL-13R into immunodeficient NOD/Shi-scid/IL-2Rγ knockout mice confirmed that they possess long-term reconstitution and self-renewal ability. AHNAK, ANXA2, and PLEC all interact with SL-13R. Knockdown of these genes in UCB CD34+ cells resulted in reduced numbers of hematopoietic colonies relative to SL-13R-treated and non-knockdown controls. In summary, we have identified a novel bioactive peptide SL-13R promoting expansion of UCB CD34+ cells with long-term reconstitution and self-renewal ability, suggesting its clinical use in the future. Full article
(This article belongs to the Special Issue Peptide Therapeutics 2.0)
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Review

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16 pages, 1359 KiB  
Review
EDR Peptide: Possible Mechanism of Gene Expression and Protein Synthesis Regulation Involved in the Pathogenesis of Alzheimer’s Disease
by Vladimir Khavinson, Natalia Linkova, Ekaterina Kozhevnikova and Svetlana Trofimova
Molecules 2021, 26(1), 159; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26010159 - 31 Dec 2020
Cited by 6 | Viewed by 3781
Abstract
The EDR peptide (Glu-Asp-Arg) has been previously established to possess neuroprotective properties. It activates gene expression and synthesis of proteins, involved in maintaining the neuronal functional activity, and reduces the intensity of their apoptosis in in vitro and in vivo studies. The EDR [...] Read more.
The EDR peptide (Glu-Asp-Arg) has been previously established to possess neuroprotective properties. It activates gene expression and synthesis of proteins, involved in maintaining the neuronal functional activity, and reduces the intensity of their apoptosis in in vitro and in vivo studies. The EDR peptide interferes with the elimination of dendritic spines in neuronal cultures obtained from mice with Alzheimer’s (AD) and Huntington’s diseases. The tripeptide promotes the activation of the antioxidant enzyme synthesis in the culture of cerebellum neurons in rats. The EDR peptide normalizes behavioral responses in animal studies and improves memory issues in elderly patients. The purpose of this review is to analyze the molecular and genetics aspects of the EDR peptide effect on gene expression and synthesis of proteins involved in the pathogenesis of AD. The EDR peptide is assumed to enter cells and bind to histone proteins and/or ribonucleic acids. Thus, the EDR peptide can change the activity of the MAPK/ERK signaling pathway, the synthesis of proapoptotic proteins (caspase-3, p53), proteins of the antioxidant system (SOD2, GPX1), transcription factors PPARA, PPARG, serotonin, calmodulin. The abovementioned signaling pathway and proteins are the components of pathogenesis in AD. The EDR peptide can be AD. Full article
(This article belongs to the Special Issue Peptide Therapeutics 2.0)
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21 pages, 3974 KiB  
Review
Peptides: Prospects for Use in the Treatment of COVID-19
by Vladimir Khavinson, Natalia Linkova, Anastasiia Dyatlova, Boris Kuznik and Roman Umnov
Molecules 2020, 25(19), 4389; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules25194389 - 24 Sep 2020
Cited by 31 | Viewed by 5680
Abstract
There is a vast practice of using antimalarial drugs, RAS inhibitors, serine protease inhibitors, inhibitors of the RNA-dependent RNA polymerase of the virus and immunosuppressants for the treatment of the severe form of COVID-19, which often occurs in patients with chronic diseases and [...] Read more.
There is a vast practice of using antimalarial drugs, RAS inhibitors, serine protease inhibitors, inhibitors of the RNA-dependent RNA polymerase of the virus and immunosuppressants for the treatment of the severe form of COVID-19, which often occurs in patients with chronic diseases and older persons. Currently, the clinical efficacy of these drugs for COVID-19 has not been proven yet. Side effects of antimalarial drugs can worsen the condition of patients and increase the likelihood of death. Peptides, given their physiological mechanism of action, have virtually no side effects. Many of them are geroprotectors and can be used in patients with chronic diseases. Peptides may be able to prevent the development of the pathological process during COVID-19 by inhibiting SARS-CoV-2 virus proteins, thereby having immuno- and bronchoprotective effects on lung cells, and normalizing the state of the hemostasis system. Immunomodulators (RKDVY, EW, KE, AEDG), possessing a physiological mechanism of action at low concentrations, appear to be the most promising group among the peptides. They normalize the cytokines’ synthesis and have an anti-inflammatory effect, thereby preventing the development of disseminated intravascular coagulation, acute respiratory distress syndrome and multiple organ failure. Full article
(This article belongs to the Special Issue Peptide Therapeutics 2.0)
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