The 20th Anniversary of Pharmaceuticals: Advances in Peptide Drug Design and Development: From Sequences to Drug Candidates

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Biopharmaceuticals".

Deadline for manuscript submissions: 30 June 2024 | Viewed by 742

Special Issue Editors

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Guest Editor
Institut National de la Recherche Scientifique, Centre Armand-Frappier Santé Biotechnologie, Groupe de Recherche en Ingénierie des Peptides et en Pharmacothérapie (GRIPP), Université du Québec, Laval, QC H7V 5B7, Canada
Interests: medicinal chemistry; drug discovery and development; G protein-coupled receptors; drug optimization; GPCR signaling; biased signaling; allosteric modulators

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Guest Editor
Institut National de la Rechercher Scientifique—Centre Armand-Frappier Santé Biotechnologie, 531 Boulevard des Prairies, Laval, QC H7V 1B7, Canada
Interests: peptide-based drugs; peptide chemistry; G protein-coupled receptors; pharmacology; cardiovascular pharmacology; allosteric modulators; biased agonists

Special Issue Information

Dear Colleagues, 

The upcoming Special Issue "Advances in Peptide Drug Design and Development: from Sequences to Drug Candidates" will explore the research landscape of peptide-based bioactive molecules. Peptides have emerged as versatile motifs to be explored in the drug discovery and development research field, offering unique advantages such as target specificity and low toxicity compared to small molecule counterparts. This Special Issue aims to showcase recent advances in peptide engineering, highlighting strategies such as identifying promising peptide sequences as well as translating them into viable drug candidates. 

We invite researchers in the drug development research field, medicinal chemistry, pharmacology, physiology, molecular biology, and clinicians to contribute their original research findings as well as insights and perspectives on the current trends and challenges in designing peptide-based drug candidates.

The key areas to be addressed include: 

  1. Peptide Sequencing and Screening: Identification of biologically active peptide sequences and essential pharmacophore motifs.
  2. Peptide Modifications and Engineering: Cutting-edge strategies for optimizing sequences to enhance the stability, bioavailability, pharmacokinetics, and pharmacological properties of peptides.
  3. Structural Insights: Exploring the impact of tridimensional structures on peptide activity, employing NMR spectroscopy data, and computational models.
  4. Peptide Synthesis: Advances in synthesis techniques, including solid-phase and microwave-assisted methods, orthogonal chemistry, and late-stage modifications.
  5. Bioconjugation and Drug Delivery: Development of peptide–drug conjugates and strategies for targeted delivery and controlled release.
  6. Peptide-Based Therapeutics: Case studies characterizing the pharmacological properties of peptide-based therapeutics, from in vitro to clinical settings.
  7. Toxicology and Safety Assessment: Methodologies for and challenges in evaluating safety, toxicity, and the immunogenicity of peptide-based drug candidates.
  8. Emerging Technologies: Exploration of innovative technologies, such as mRNA-encoding peptides, CRISPR-mediated therapies, and AI-driven drug design.
  9. Future Perspectives: Insights into the evolving landscape of peptide drug development, including personalized medicine, combination therapies, and addressing unmet medical needs.

Dr. Juliana C. C. Dallagnol
Prof. Dr. David Chatenet
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at 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. Pharmaceuticals is an international peer-reviewed open access monthly 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 2900 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.


  • peptide-based drugs
  • drug design
  • therapeutic peptides
  • peptide synthesis
  • structure–activity relationship
  • peptide drug delivery
  • bioavailability
  • formulation strategies
  • peptide therapeutics

Published Papers (1 paper)

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13 pages, 3336 KiB  
Biological Activities of Deer Antler-Derived Peptides on Human Chondrocyte and Bone Metabolism
by Tsung-Jung Ho, Wan-Ting Tsai, Jia-Ru Wu and Hao-Ping Chen
Pharmaceuticals 2024, 17(4), 434; - 28 Mar 2024
Viewed by 437
Orally administered “tortoiseshell and deer antler gelatin” is a common traditional medicine for patients with osteoporosis or osteoarthritis. From the pepsin-digested gelatin, we previously isolated and identified the osteoblast-stimulating pentapeptide, TSKYR. Its trypsin digestion products include the dipeptide YR, enhancing calcium ion uptake, [...] Read more.
Orally administered “tortoiseshell and deer antler gelatin” is a common traditional medicine for patients with osteoporosis or osteoarthritis. From the pepsin-digested gelatin, we previously isolated and identified the osteoblast-stimulating pentapeptide, TSKYR. Its trypsin digestion products include the dipeptide YR, enhancing calcium ion uptake, and tripeptide TSK, resulting in remarkable 30- and 50-fold increases in mineralized nodule area and density in human osteoblast cells. These peptides were chemically synthesized in this study. The composition of deer antler preparations comprises not only proteins and peptides but also a significant quantity of metal ion salts. By analyzing osteoblast growth in the presence of peptide YR and various metal ions, we observed a synergistic effect of calcium and strontium on the effects of YR. Those peptides could also stimulate the growth of C2C12 skeletal muscle cells and human chondrocytes, increasing collagen and glycosaminoglycan content in a three-dimensional environment. The maintenance of bone homeostasis relies on a balance between osteoclasts and osteoblasts. Deer antler peptides were observed to inhibit osteoclast differentiation, as evidenced by ROS generation, tartrate-resistant acid phosphatase (TRACP) activity assays, and gene expression in RAW264.7 cells. In summary, our findings provide a deep understanding of the efficacy of this folk medicine. Full article
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