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Molecules
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Peptide Conjugate as Therapeutic, Diagnostic and Theranostic Agents
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Peptide Conjugate as Therapeutic, Diagnostic and Theranostic Agents

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

Deadline for manuscript submissions: closed (31 March 2023) | Viewed by 3669

Special Issue Editor

Prof. Dr. Andreas Tzakos

E-Mail Website
Guest Editor
Lab of Organic Chemistry and Biochemistry, Chemistry Department, University of Ioannina, Ioannina, Greece
Interests: bioactive compounds; phytochemicals; plant extracts; metabolomics; anticancer compounds
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

There is currently a very active revival of interest in the exploitation of peptides as core tools to develop novel drugs, diagnostics, and theranostics for new high value-added products to address unmet medical needs. This emanates from their biocompatibility, enhanced biochemical characteristics with respect to targeted delivery, and ease in rational design and production. In particular, Peptide–Drug Conjugates (PDCs) are arguably an inextricable accessory in our armamentarium against cancer and are continuously gaining attention as a viable approach to selectively target malignant cells. Besides, conjugation of a bioimaging agent, a drug, or of both modalities to a peptide that targets a specific biomarker expressed in a diseased location in a tissue can result in a potent diagnostic, therapeutic, or theranostic agent. This Special Issue will collect recent advances and developments in the field of peptide conjugation to drugs (PDCs), imaging (diagnostic), or dual modalities (theranostics) against cancer and other diseases, including the rational design and novel methodologies for the synthesis (e.g., rapid click chemistry reactions) of novel peptide conjugates. The contributions will also be focused on the impact of the linker in the overall pharmaceutical profile of peptide conjugates, the interactions with the targeted biomarker, the discovery of novel targets, and the possible side-product formation that may occur during such conjugations.

PDCs consist of three building blocks: the tumor-targeting peptide, the cytotoxic drug, and the biodegradable tether (linker). This Special Issue will collect recent advances in the field of peptide–drug conjugation against cancer, mainly including the rational design of novel peptide–drug conjugates and novel methodologies for their synthesis (e.g., the development of rapid click reactions). The contributions will also be focused on the impact of the linker in the overall pharmaceutical profile of PDCs, the receptor binding interactions, the discovery of novel molecular targets, and the possible side-product formation that may occur during such conjugations.

Dr. Andreas Tzakos
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

  • peptide–drug conjugates
  • peptide-based diagnostics
  • peptide-based theranostics
  • rational design
  • cancer research

Published Papers (2 papers)

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Research

14 pages, 2432 KiB  
Article
A Straightforward Method for the Development of Positively Charged Gold Nanoparticle-Based Vectors for Effective siRNA Delivery
by Tatiana N. Elizarova, Maxim L. Antopolsky, Denis O. Novichikhin, Artemiy M. Skirda, Alexey V. Orlov, Vera A. Bragina and Petr I. Nikitin
Molecules 2023, 28(8), 3318; https://doi.org/10.3390/molecules28083318 - 08 Apr 2023
Cited by 2 | Viewed by 1871
Abstract
The therapeutic potential of short interfering RNA (siRNA) to treat many diseases that are incurable with traditional preparations is limited by the extensive metabolism of serum nucleases, low permeability through biological membrane barriers because of a negative charge, and endosomal trapping. Effective delivery [...] Read more.
The therapeutic potential of short interfering RNA (siRNA) to treat many diseases that are incurable with traditional preparations is limited by the extensive metabolism of serum nucleases, low permeability through biological membrane barriers because of a negative charge, and endosomal trapping. Effective delivery vectors are required to overcome these challenges without causing unwanted side effects. Here, we present a relatively simple synthetic protocol to obtain positively charged gold nanoparticles (AuNPs) with narrow size distribution and the surface modified with Tat-related cell-penetrating peptide. The AuNPs were characterized using TEM and the localized surface plasmon resonance technique. The synthesized AuNPs showed low toxicity in experiments in vitro and were able to effectively form complexes with double-stranded siRNA. The obtained delivery vehicles were used for intracellular delivery of siRNA in an ARPE-19 cell line transfected with secreted embryonic alkaline phosphatase (SEAP). The delivered oligonucleotide remained intact and caused a significant knockdown effect on SEAP cell production. The developed material could be useful for delivery of negatively charged macromolecules, such as antisense oligonucleotides and various RNAs, particularly for retinal pigment epithelial cell drug delivery. Full article
(This article belongs to the Special Issue Peptide Conjugate as Therapeutic, Diagnostic and Theranostic Agents)
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14 pages, 2850 KiB  
Article
The Molecular Basis of Heat-Stable Enterotoxin for Vaccine Development and Cancer Cell Detection
by Masaya Goto, Shinya Yoshino, Kyona Hiroshima, Toru Kawakami, Kaeko Murota, Shigeru Shimamoto and Yuji Hidaka
Molecules 2023, 28(3), 1128; https://doi.org/10.3390/molecules28031128 - 23 Jan 2023
Cited by 2 | Viewed by 1512
Abstract
Heat-stable enterotoxin (STa) produced by Enterotoxigenic E. coli is responsible for causing acute diarrhea in infants in developing countries. However, the chemical synthesis of STa peptides with the native conformation and the correct intra-molecular disulfide bonds is a major hurdle [...] Read more.
Heat-stable enterotoxin (STa) produced by Enterotoxigenic E. coli is responsible for causing acute diarrhea in infants in developing countries. However, the chemical synthesis of STa peptides with the native conformation and the correct intra-molecular disulfide bonds is a major hurdle for vaccine development. To address this issue, we herein report on the design and preparation of STa analogs and a convenient chemical method for obtaining STa molecules with the correct conformation. To develop an STa vaccine, we focused on a structure in a type II β-turn in the STa molecule and introduced a D-Lys residue as a conjugation site for carrier proteins. In addition, the -Glu-Leu- sequence in the STa molecule was replaced with a -Asp-Val- sequence to decrease the toxic activity of the peptide to make it more amenable for use in vaccinations. To solve several issues associated with the synthesis of STa, such as the formation of non-native disulfide isomers, the native disulfide pairings were regioselectively formed in a stepwise manner. A native form or topological isomer of the designed STa peptide, which possesses a right-handed or a left-handed spiral structure, respectively, were synthesized in high synthetic yields. The conformation of the synthetic STa peptide was also confirmed by CD and NMR spectroscopy. To further utilize the designed STa peptide, it was labeled with fluorescein for fluorescent detection, since recent studies have also focused on the use of STa for detecting cancer cells, such as Caco-2 and T84. The labeled STa peptide was able to specifically and efficiently detect 293T cells expressing the recombinant STa receptor (GC-C) protein and Caco-2 cells. The findings reported here provide an outline of the molecular basis for using STa for vaccine development and in the detection of cancer cells. Full article
(This article belongs to the Special Issue Peptide Conjugate as Therapeutic, Diagnostic and Theranostic Agents)
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