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Novel Strategies in the Development of Peptide-Based Therapeutics
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Novel Strategies in the Development of Peptide-Based Therapeutics

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

Deadline for manuscript submissions: closed (31 January 2024) | Viewed by 3133

Special Issue Editor

Prof. Dr. Ruhong Zhou

E-Mail Website
Guest Editor
Institute of Quantitative Biology, Zhejiang University, Hangzhou 310027, China
Interests: molecular dynamics; protein folding; protein-protein interaction; machine learning
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In this Special Issue, we will focus on the latest development of peptide-based therapies and novel strategies to design therapeutic peptides. In recent years, peptides have become a unique class of therapeutic agents, due to their distinct biochemical characteristics and pharmacological profiles. Therapeutic peptides bind to cell surface receptors and trigger intracellular effects with high affinity and selectivity. The combined use of chemical and biological synthetic approaches enables efficient and reliable large-scale production of synthetic peptides. In turn, the integration of conventional high-throughput discovery methods with novel technologies, such as rational design and artificial intelligence, provides an effective method of generating lead peptides. These peptides can be further modified in a site-specific manner to enhance stability and physiological activities.

In light of the above, this Special Issue aims to bring together wet- and dry-lab researchers with common interests in peptide design and to provide a forum for sharing relevant research efforts. We welcome various types of submissions, including research articles, communications, and reviews, that focus on peptide-based therapeutics; peptide–target interactions; modes of action of therapeutical peptides and peptide vaccines; and the design of multifunctional peptides, cell penetrating peptides and peptide drug conjugates. 

Prof. Dr. Ruhong Zhou
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
  • peptide based therapy
  • rational design
  • artificial intelligence
  • molecular modeling
  • peptide vaccines

Published Papers (2 papers)

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Research

10 pages, 2062 KiB  
Article
Development of Hydrophobic Cell-Penetrating Stapled Peptides as Drug Carriers
by Keisuke Tsuchiya, Kanako Horikoshi, Minami Fujita, Motoharu Hirano, Maho Miyamoto, Hidetomo Yokoo and Yosuke Demizu
Int. J. Mol. Sci. 2023, 24(14), 11768; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms241411768 - 21 Jul 2023
Cited by 1 | Viewed by 1339
Abstract
Cell-penetrating peptides (CPPs) are widely used for the intracellular delivery of a variety of cargo molecules, including small molecules, peptides, nucleic acids, and proteins. Many cationic and amphiphilic CPPs have been developed; however, there have been few reports regarding hydrophobic CPPs. Herein, we [...] Read more.
Cell-penetrating peptides (CPPs) are widely used for the intracellular delivery of a variety of cargo molecules, including small molecules, peptides, nucleic acids, and proteins. Many cationic and amphiphilic CPPs have been developed; however, there have been few reports regarding hydrophobic CPPs. Herein, we have developed stapled hydrophobic CPPs based on the hydrophobic CPP, TP10, by introducing an aliphatic carbon side chain on the hydrophobic face of TP10. This side chain maintained the hydrophobicity of TP10 and enhanced the helicity and cell penetrating efficiency. We evaluated the preferred secondary structures, and the ability to deliver 5(6)-carboxyfluorescein (CF) as a model small molecule and plasmid DNA (pDNA) as a model nucleotide. The stapled peptide F-3 with CF, in which the stapling structure was introduced at Gly residues, formed a stable α-helical structure and the highest cell-membrane permeability via an endocytosis process. Meanwhile, peptide F-4 demonstrated remarkable stability when forming a complex with pDNA, making it the optimal choice for the efficient intracellular delivery of pDNA. The results showed that stapled hydrophobic CPPs were able to deliver small molecules and pDNA into cells, and that different stapling positions in hydrophobic CPPs can control the efficiency of the cargo delivery. Full article
(This article belongs to the Special Issue Novel Strategies in the Development of Peptide-Based Therapeutics)
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12 pages, 3153 KiB  
Article
Lung Surfactant Protein B Peptide Mimics Interact with the Human ACE2 Receptor
by Alan J. Waring, Grace C.-L. Jung, Shantanu K. Sharma and Frans J. Walther
Int. J. Mol. Sci. 2023, 24(13), 10837; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms241310837 - 29 Jun 2023
Cited by 1 | Viewed by 1244
Abstract
Lung surfactant is a complex mixture of phospholipids and surfactant proteins that is produced in alveolar type 2 cells. It prevents lung collapse by reducing surface tension and is involved in innate immunity. Exogenous animal-derived and, more recently, synthetic lung surfactant has shown [...] Read more.
Lung surfactant is a complex mixture of phospholipids and surfactant proteins that is produced in alveolar type 2 cells. It prevents lung collapse by reducing surface tension and is involved in innate immunity. Exogenous animal-derived and, more recently, synthetic lung surfactant has shown clinical efficacy in surfactant-deficient premature infants and in critically ill patients with acute respiratory distress syndrome (ARDS), such as those with severe COVID-19 disease. COVID-19 pneumonia is initiated by the binding of the viral receptor-binding domain (RBD) of SARS-CoV-2 to the cellular receptor angiotensin-converting enzyme 2 (ACE2). Inflammation and tissue damage then lead to loss and dysfunction of surface activity that can be relieved by treatment with an exogenous lung surfactant. Surfactant protein B (SP-B) is pivotal for surfactant activity and has anti-inflammatory effects. Here, we study the binding of two synthetic SP-B peptide mimics, Super Mini-B (SMB) and B-YL, to a recombinant human ACE2 receptor protein construct using molecular docking and surface plasmon resonance (SPR) to evaluate their potential as antiviral drugs. The SPR measurements confirmed that both the SMB and B-YL peptides bind to the rhACE2 receptor with affinities like that of the viral RBD–ACE2 complex. These findings suggest that synthetic lung surfactant peptide mimics can act as competitive inhibitors of the binding of viral RBD to the ACE2 receptor. Full article
(This article belongs to the Special Issue Novel Strategies in the Development of Peptide-Based Therapeutics)
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