Biomedicines

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Dear Colleagues,

Peptides and amino acids are ubiquitously found as important building blocks and gaining interest in pharmaceutical research and drug development. Peptide chemistry is extensively utilized for the preparation of therapeutic peptides, signaling peptides, penetrating peptides, peptide–drug conjugates, cyclic peptides, and peptidomimetics. Over 150 peptide-based drug candidates are in clinical trials. In recent years, a paradigm shift in the Pharmaceutical Industry for peptide and amino acid-based drugs because of high selectivity for the targets, improved bioavailability, and reduced toxicity. Peptides and amino acids have the potential to offer the versatility needed for a successful drug discovery approach. Peptide–drug conjugates (PDCs) are an emerging targeted therapeutic that is composed of a drug candidate, peptide, and a linker. Alternatively, to enhance the penetration and selectivity peptides and amino acids are also used as linkers in molecular hybridized compounds.

Dr. Siva Panda
Guest Editor

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Keywords

peptide chemistry
amino acids
drug conjugates
drug development
drug delivery
coupling reagents
peptidomimetics
cyclic peptides
peptide ligation

Published Papers (2 papers)

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Research

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17 pages, 3496 KiB

Open AccessArticle

Synthesis, Hydrolytic Stability and In Vivo Biological Study of Bioconjugates of the Tetrapeptides FELL Containing Pyrrole Moiety

by Boryana Borisova, Stanislava Vladimirova, Hristina Nocheva, Marie Laronze-Cochard, Stéphane Gérard, Stoyko Petrin and Dancho Danalev

Biomedicines 2023, 11(12), 3265; https://doi.org/10.3390/biomedicines11123265 - 9 Dec 2023

Viewed by 821

Abstract

Background: Bioconjugates are promising alternatives for the multiple targeting of any disease. Pyrrole heterocycle is well known with many activities and is a building block of a lot of medical drugs. On the other hand, peptides are short molecules with many advantages such as small size, ability to penetrate the cell membrane and bond-specific receptors, vectorizing potential, etc. Thus, hybrid molecules between peptide and pyrrole moiety could be a promising alternative as an anti-pain tool. Methods: New bioconjugates with a general formula Pyrrole (α-/β-acid)-FELL-OH (NH₂) were synthesized using Fmoc/OtBu peptide synthesis on solid support. HPLC was used to monitor the purity of newly synthesized bioconjugates. Their structures were proven by electrospray ionization mass spectrometry. The Paw Pressure test (Randall–Selitto test) was used to examinate the analgesic activity. Hydrolytic stability of targeted structures was monitored in three model systems with pH 2.0, 7.4 and 9.0, including specific enzymes by means of the HPLC-UV method. Results: The obtained results reveal that all newly synthesized bioconjugates have analgesic activity according to the used test but free pyrrole acids have the best analgesic activity. Conclusions: Although free pyrrole acids showed the best analgesic activity, they are the most unstable for hydrolysis. Combination with peptide structure leads to the hydrolytic stabilization of the bioconjugates, albeit with slightly reduced activity. Full article

(This article belongs to the Special Issue Peptides and Amino Acids in Drug Development: Here and Now)

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Review

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19 pages, 2972 KiB

Open AccessReview

Role of Functionalized Peptides in Nanomedicine for Effective Cancer Therapy

by Kibeom Kim and Myoung-Hwan Park

Biomedicines 2024, 12(1), 202; https://doi.org/10.3390/biomedicines12010202 - 16 Jan 2024

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Abstract

Peptide-functionalized nanomedicine, which addresses the challenges of specificity and efficacy in drug delivery, is emerging as a pivotal approach for cancer therapy. Globally, cancer remains a leading cause of mortality, and conventional treatments, such as chemotherapy, often lack precision and cause adverse effects. The integration of peptides into nanomedicine offers a promising solution for enhancing the targeting and delivery of therapeutic agents. This review focuses on the three primary applications of peptides: cancer cell-targeting ligands, building blocks for self-assembling nanostructures, and elements of stimuli-responsive systems. Nanoparticles modified with peptides improved targeting of cancer cells, minimized damage to healthy tissues, and optimized drug delivery. The versatility of self-assembled peptide structures makes them an innovative vehicle for drug delivery by leveraging their biocompatibility and diverse nanoarchitectures. In particular, the mechanism of cell death induced by self-assembled structures offers a novel approach to cancer therapy. In addition, peptides in stimuli-responsive systems enable precise drug release in response to specific conditions in the tumor microenvironment. The use of peptides in nanomedicine not only augments the efficacy and safety of cancer treatments but also suggests new research directions. In this review, we introduce systems and functionalization methods using peptides or peptide-modified nanoparticles to overcome challenges in the treatment of specific cancers, including breast cancer, lung cancer, colon cancer, prostate cancer, pancreatic cancer, liver cancer, skin cancer, glioma, osteosarcoma, and cervical cancer. Full article

(This article belongs to the Special Issue Peptides and Amino Acids in Drug Development: Here and Now)

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