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Bioactive Peptides: Synthesis, Functions, and Medicinal Chemistry Applications
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Bioactive Peptides: Synthesis, Functions, and Medicinal Chemistry Applications

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

Deadline for manuscript submissions: 20 May 2025 | Viewed by 1875

Special Issue Editor

Prof. Dr. Giovanni Grazioso

E-Mail Website
Guest Editor
Department of Pharmaceutical Science, University of Milano, Via L. Mangiagalli 25, Milano, Italy
Interests: drug design; peptides; peptidomimetics; molecular dynamics simulations; MM-GBSA; binding free energy
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Peptides have emerged as promising therapeutic tools, with molecular weights and pharmacological properties that sit between traditional small molecule drugs and therapeutic proteins, such as monoclonal antibodies. Numerous peptides are clinically available for the treatment of various diseases, such as infections, cancer, osteoporosis, chronic pain, hormonal therapy, and skin aging. Additionally, peptides show significant potential for drug delivery applications and for disrupting protein–protein interactions (PPIs), displaying capabilities to be utilized in every biochemical pathway.

In recent years, we have seen substantial progress in the discovery and development of bioactive peptides, as testified by the increasing number of deposited patents. Advances that have been made include the following: genome mining, the development of new chemical methods for peptide cyclization, efficient synthesis of long peptides through peptide ligation, the creation of peptide libraries for high-throughput screening, and an enhancement of our understanding of peptide intracellular delivery and metabolic protection.

Lead by Prof. Dr. Giovanni Grazioso and assisted by our Topical Advisory Panel Member Dr. Enrico M. A. Fassi (University of Milan), this Special Issue focuses on recent studies contributing to our understanding of peptides on their discovery, bio- and organic synthesis, delivery, improvement of their pharmacokinetic properties, conjugation, and any other medicinal chemistry aspect.

We welcome the submissions of original research articles and reviews on these and related topics to this Special Issue.

Prof. Dr. Giovanni Grazioso
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
  • protein–protein interactions (PPIs)
  • peptide intracellular delivery

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Published Papers (3 papers)

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15 pages, 1143 KiB  
Article
Drug Administration Before or After Exposure to Low Temperatures—Does It Matter for the Therapeutic Effect?
by Kadir Bezirci, Boryana Borisova, Konstantinos Papadakis, Dancho Danalev and Hristina Nocheva
Int. J. Mol. Sci. 2025, 26(8), 3883; https://doi.org/10.3390/ijms26083883 - 19 Apr 2025
Viewed by 164
Abstract
The adaptation of the body when exposed to a lower-than-usual temperature is a challenge that involves neuro-endocrine–immune mechanisms and affects the pharmacokinetics and/or pharmacodynamics of drugs taken before or after cold exposure. The experiments presented in this study clearly show differences in the [...] Read more.
The adaptation of the body when exposed to a lower-than-usual temperature is a challenge that involves neuro-endocrine–immune mechanisms and affects the pharmacokinetics and/or pharmacodynamics of drugs taken before or after cold exposure. The experiments presented in this study clearly show differences in the analgesic effect of an exogenously introduced model substance (C-terminal fragment of calcium-binding protein, spermatid-specific 1) before and after cold exposure compared to its effect at an ambient temperature. The model substance used for the experiments is an octapeptide, TDIFELLK, which was synthesized via standard solid-phase peptide synthesis. Preliminary studies proved TDIFELLK’s analgesic activity. The ANOVA analysis performed showed statistically significant differences in the pain thresholds, measured by a paw pressure test, in 109 rats distributed among 14 groups and subjected to cold exposure according to different set-ups. Cold exposure immediately after TDIFELLK administration appears to enhance its analgesic effect, while cold exposure before administration reduces the effect. In some of the set-ups, antagonists of the most significant for analgesia receptors, i.e., opioid, cannabinoid, and serotonergic, were also introduced. The results showed that cold exposure had a modulating influence on the effect of the exogenously administered substances. The modulating effect was manifested differently depending on whether the intake occurred before or after cold exposure. The results also showed that the interaction with individual mediator systems was also subjected to differences depending on intake occurring before and after cold exposure. Full article
(This article belongs to the Special Issue Bioactive Peptides: Synthesis, Functions, and Medicinal Chemistry Applications)
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21 pages, 4051 KiB  
Article
TRPA1-Activated Peptides from Saiga Antelope Horn: Screening, Interaction Mechanism, and Bioactivity
by Chengwei Wang, Chunjie Wu and Linjiang Song
Int. J. Mol. Sci. 2025, 26(5), 2119; https://doi.org/10.3390/ijms26052119 - 27 Feb 2025
Viewed by 543
Abstract
Saiga antelope horn (SAH), a rare traditional Chinese medicine, exhibits activities of anti-feverish convulsions and anti-inflammation, whereas its underlying mechanism and specific pharmacological components are still unclear. In the present study, transient receptor potential ankyrin 1 (TRPA1), a major transient receptor potential cation [...] Read more.
Saiga antelope horn (SAH), a rare traditional Chinese medicine, exhibits activities of anti-feverish convulsions and anti-inflammation, whereas its underlying mechanism and specific pharmacological components are still unclear. In the present study, transient receptor potential ankyrin 1 (TRPA1), a major transient receptor potential cation channel was used as a target protein to identified TRPA1 high-affinity peptides (THPs) from SAH digests. Firstly, the SAH was digested under in vitro gastrointestinal conditions. With the method of affinity ultrafiltration and liquid chromatography–mass spectrometry (AUF-LC/MS), about 200 peptides that have a high-affinity interaction with the TRPA1 protein were screened from SAH digests. Subsequently, bioactivity databases and molecular docking were further exploited to identified three THPs, including RCWPDCR, FGFDGDF, and WFCEGSF. Furthermore, RIN-14B cells, characterized by the high expression of TRPA1 on cell surfaces, were used as the cell model to investigate the biological effect of THPs. Immunofluorescence and ELISA were conducted and showed that THPs can increase the intracellular Ca2+ concentration and serotonin (5-HT) secretion in RIN-14B cells by activating TRPA1, which is evidenced by impaired upregulation of intracellular Ca2+ levels and 5-HT secretion after pretreatment with the TRPA1 inhibitor (HC-030031). Moreover, an analysis of Western blots displayed that THPs up-regulated the expression levels of the 5-HT synthesis rate-limiting enzyme (TPH1) and 5-hydroxytryptophan decarboxylase (Ddc), while serotonin reuptake transporter (SERT) levels were down-regulated, suggesting that THPs enhance 5-HT secretion by regulating the 5-HT synthesis pathway. In summary, our findings demonstrate that THPs, which were identified from SAH digest via TRPA1-targeted affinity panning, exhibited the activation of the TRPA1 channel and enhanced 5-HT release in RIN-14B cells. Full article
(This article belongs to the Special Issue Bioactive Peptides: Synthesis, Functions, and Medicinal Chemistry Applications)
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16 pages, 1605 KiB  
Article
Novel Peptidomimetic Cyclo-{E(I)-E(W)}Na (CP-88) with Hematopoietic Activity Sustained in Invasive and Oral Administration: Experimental and Preclinical Evaluation
by Vladislav Deigin, Yulia Vinogradova, Dmitriy Vinogradov, Natalia Linkova, Anastasiia Dyatlova, Dmitrii Medvedev, Alexander Krasichkov and Victoria Polyakova
Int. J. Mol. Sci. 2024, 25(24), 13385; https://doi.org/10.3390/ijms252413385 - 13 Dec 2024
Viewed by 809
Abstract
Over the last decades, significant progress has been made in studying agonistic and antagonistic hematopoietic peptides. The main disadvantage of this class of peptides is their low stability with noninvasive administration methods, which limits the widespread use of hematopoiesis-regulated peptide drugs in medical [...] Read more.
Over the last decades, significant progress has been made in studying agonistic and antagonistic hematopoietic peptides. The main disadvantage of this class of peptides is their low stability with noninvasive administration methods, which limits the widespread use of hematopoiesis-regulated peptide drugs in medical practice. The aim of this work is to study novel peptidomimetics with hematopoietic activity sustained in invasive and oral administration. The activity of the leading compound cyclopeptide Cyclo—[Glu(Ile)-Glu(Trp)] (CP-88) was compared to that of the pharmaceutical preparation Stemokin in stimulating the population of committed colony-forming cells in intact and irradiated mice. CP-88 peptide increases the relative number of CD34+ cells in the blood and bone marrow, leading to expanded hematopoietic stem cells. CP-88 peptide, applied 48 h before bone marrow extraction, stimulates the population of committed colony-forming cells in the normal bone marrow by 33–37% above the normal level. In recipient mice injected with irradiated bone marrow, this peptide was restored practically to normal levels of colony-forming cells in a wide range of doses at intraperitoneal and oral administration. The toxicological results conclude that in humans, considering interspecies extrapolation, the CP-88 peptide can be practically safe with a single and course administration in doses of up to 100 μg/kg. The results of this investigation underscore the significant potential of CP-88 peptide as a hematopoiesis-regulated drug and instill optimism for its future application in medical practice. Full article
(This article belongs to the Special Issue Bioactive Peptides: Synthesis, Functions, and Medicinal Chemistry Applications)
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