molecules-logo

Journal Browser

Journal Browser

Special Issue "Peptide-Based Drug and Drug Delivery Systems"

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

Deadline for manuscript submissions: 28 February 2022.

Special Issue Editor

Dr. Kathrin Bellmann-Sickert
E-Mail Website
Guest Editor
Universität Leipzig, Faculty of Life Sciences, Institute of Biochemistry, Brüderstrasse 34, 04103 Leipzig, Germany
Interests: peptide synthesis; peptide stabilization; immobilization of biologically functional peptides and proteins on solid supports; biased peptide ligands in GPCRs

Special Issue Information

Dear Colleagues,

Peptides are gaining increasing interest as potential therapeutics, especially in clinical fields where classical small molecules have, to date, not been successful. Although they face challenges such as short half and shelf lives due to proteolytic cleavage and fast kidney clearance, they bear advantages over small molecule drugs as they are potentially less toxic and more selective. Additionally, due to their selective binding, peptides can be used as shuttle systems to target drugs to certain diseased sites, thereby reducing systemic side effects. This Special Issue aims at compiling new and exciting insights into the prosperous field of peptide-based drug and delivery systems, including synthesis and biomedical evaluation of both peptidic drugs and peptide–drug conjugates for targeted delivery. Researchers are welcome to contribute any work dedicated to the synthesis as well as biological and therapeutic evaluation of peptides and peptide–drug conjugates. The following topics and key words may serve as orientation:

  • Therapeutic applications of peptides (antimicrobial peptides, cancer treatment, vaccination, but also new applications);
  • Enhancing peptide–drug bioavailability (stabilization against renal clearance and proteolytic degradation);
  • Dual-functional peptides;
  • Peptide diagnostics and theranostics (e.g., PET tracers, radionuclide therapy) and peptide-based reporters;
  • Drug shuttle systems crossing membrane barriers;
  • Self-assembling peptides;
  • Nanoparticles, liposomes, peptide dendrimers, peptide hydrogels;
  • Cell- and nucleus-targeting peptides;
  • Chemical synthesis and conjugation techniques (biorthogonal coupling techniques);
  • Drug release strategies (cleavable linkers, masking, etc.);
  • Endosomal release strategies. 

Dr. Kathrin Bellmann-Sickert
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 papers will be 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 2300 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 drugs
  • Peptide diagnostics
  • Peptide theranostics
  • Peptide bioavailability
  • Drug shuttling
  • Peptide nanoparticles
  • Dual-active peptides
  • Self-assembling peptides
  • Peptide drug release

Published Papers (2 papers)

Order results
Result details
Select all
Export citation of selected articles as:

Research

Jump to: Review

Article
Synthesis and Biological Studies on (KLAKLAK)2-NH2 Analog Containing Unnatural Amino Acid β-Ala and Conjugates with Second Pharmacophore
Molecules 2021, 26(23), 7321; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26237321 - 02 Dec 2021
Viewed by 438
Abstract
(1) Background: Peptides are good candidates for anticancer drugs due to their natural existence in the body and lack of secondary effects. (KLAKLAK)2 is an antimicrobial peptide that also shows good anticancer properties. (2) Methods: The Solid Phase Peptide Synthesis (Fmoc-strategy) was [...] Read more.
(1) Background: Peptides are good candidates for anticancer drugs due to their natural existence in the body and lack of secondary effects. (KLAKLAK)2 is an antimicrobial peptide that also shows good anticancer properties. (2) Methods: The Solid Phase Peptide Synthesis (Fmoc-strategy) was used for the synthesis of target molecules, analogs of (KLAKLAK)2-NH2. The purity of all compounds was monitored by HPLC, and their structures were proven using mass spectrometry. Cytotoxicity and antiproliferative effects were studied using 3T3 NRU and MTT tests, respectively. For determination of antimicrobial activity, the disc-diffusion method was used. Hydrolytic stability at three pH values, which mimic the physiological pH in the body, was investigated by means of the HPLC technique. (3) Results: A good selective index against MCF-7 tumor cell lines, combined with good cytotoxicity and antiproliferative properties, was revealed for conjugates NphtG-(KLAKLAK)2-NH2 and Caf-(KLAKLAK)2-NH2. The same compounds showed very good antifungal properties and complete hydrolytic stability for 72 h. The compound Caf-(KLβ-AKLβ-AK)2-NH2 containing β-Ala in its structures exhibited good antimicrobial activity against Escherichia coli K12 407 and Bacillus subtilis 3562, in combination with very good antiproliferative and cytotoxic properties, as well as hydrolytic stability. (4) Conclusions: The obtained results reveal that all synthesized conjugates could be useful for medical practice as anticancer or antimicrobial agents. Full article
(This article belongs to the Special Issue Peptide-Based Drug and Drug Delivery Systems)
Show Figures

Figure 1

Review

Jump to: Research

Review
Progress and Future Directions with Peptide-Drug Conjugates for Targeted Cancer Therapy
Molecules 2021, 26(19), 6042; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26196042 - 05 Oct 2021
Viewed by 1031
Abstract
We review drug conjugates combining a tumor-selective moiety with a cytotoxic agent as cancer treatments. Currently, antibody-drug conjugates (ADCs) are the most common drug conjugates used clinically as cancer treatments. While providing both efficacy and favorable tolerability, ADCs have limitations due to their [...] Read more.
We review drug conjugates combining a tumor-selective moiety with a cytotoxic agent as cancer treatments. Currently, antibody-drug conjugates (ADCs) are the most common drug conjugates used clinically as cancer treatments. While providing both efficacy and favorable tolerability, ADCs have limitations due to their size and complexity. Peptides as tumor-targeting carriers in peptide-drug conjugates (PDCs) offer a number of benefits. Melphalan flufenamide (melflufen) is a highly lipophilic PDC that takes a novel approach by utilizing increased aminopeptidase activity to selectively increase the release and concentration of cytotoxic alkylating agents inside tumor cells. The only other PDC approved currently for clinical use is 177Lu-dotatate, a targeted form of radiotherapy combining a somatostatin analog with a radionuclide. It is approved as a treatment for gastroenteropancreatic neuroendocrine tumors. Results with other PDCs combining synthetic analogs of natural peptide ligands with cytotoxic agents have been mixed. The field of drug conjugates as drug delivery systems for the treatment of cancer continues to advance with the application of new technologies. Melflufen provides a paradigm for rational PDC design, with a targeted mechanism of action and the potential for deepening responses to treatment, maintaining remissions, and eradicating therapy-resistant stem cells. Full article
(This article belongs to the Special Issue Peptide-Based Drug and Drug Delivery Systems)
Show Figures

Figure 1

Back to TopTop