Journal of Peptide Science最新文献

Modulation of Antimicrobial Activities of Aib-Based Artificial Amphipathic α-Helical Peptides by Incorporating Histidine Residues 组氨酸残基对aib型人工两性α-螺旋肽抗菌活性的调节作用

IF 1.8 4区生物学

Journal of Peptide Science Pub Date : 2025-07-29 DOI: 10.1002/psc.70046

Ami Koga, Manami Fuchinoue, Kiyohiko Seki, Kaoru Araki, Tomoichirou Kusumoto, Junichi Taira, Hiroaki Kodama, Satoshi Osada

{"title":"Modulation of Antimicrobial Activities of Aib-Based Artificial Amphipathic α-Helical Peptides by Incorporating Histidine Residues","authors":"Ami Koga, Manami Fuchinoue, Kiyohiko Seki, Kaoru Araki, Tomoichirou Kusumoto, Junichi Taira, Hiroaki Kodama, Satoshi Osada","doi":"10.1002/psc.70046","DOIUrl":"https://doi.org/10.1002/psc.70046","url":null,"abstract":"<div>\u0000 \u0000 Cationic antimicrobial peptides (CAMPs) exhibit potent antibacterial activity by disrupting bacterial membranes. We investigated the effect of histidine incorporation on BKBA-20, a designed amphiphilic helical peptide composed of alternating 2-aminoisobutyric acid (Aib) and lysine. Substitution at lysine sites (1a–1e series) reduced net charge and antimicrobial activity, though certain analogues (1c, 1d) demonstrated minimal antibacterial activity against Escherichia coli. In contrast, substitution at Aib sites (2a–2c series) preserved some extent of helical structure and improved activity under acidic conditions. Notably, substitutions at the terminal of the peptide were more effective at acidic pH, while the slightly medial side of the peptide favored activity at neutral pH. Hemolysis assays confirmed low cytotoxicity of the modified peptides. These results suggest histidine incorporation as a promising strategy to broaden the spectrum of CAMPs, particularly against Gram-negative bacteria, without increasing toxicity.\u0000 </div>","PeriodicalId":16946,"journal":{"name":"Journal of Peptide Science","volume":"31 9","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144725748","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Controversial Nomenclature in Peptide Synthesis: A Call for Clarity 肽合成中有争议的命名法：呼吁澄清

IF 1.8 4区生物学

Journal of Peptide Science Pub Date : 2025-07-27 DOI: 10.1002/psc.70044

Anamika Sharma, Ashish Kumar, Beatriz G. de la Torre, Fernando Albericio

引用次数: 0

Peptide Synthesis Nomenclature 肽合成术语

IF 1.8 4区生物学

Journal of Peptide Science Pub Date : 2025-07-27 DOI: 10.1002/psc.70043

Christian F. W. Becker, Florine Cavelier, Yosuke Demizu, Xuechen Li, William Lubell, John Wade, Paolo Rovero

引用次数: 0

Therapeutic Potential of Stylissatin A and Related Cyclic Peptides From Marine Sponges 海海绵中Stylissatin A及相关环肽的治疗潜力

IF 1.8 4区生物学

Journal of Peptide Science Pub Date : 2025-07-24 DOI: 10.1002/psc.70045

Aaqib Ullah, Farzana Shaheen, Uzma Salar, Andreas G. Tzakos, Ioannis P. Gerothanassis

{"title":"Therapeutic Potential of Stylissatin A and Related Cyclic Peptides From Marine Sponges","authors":"Aaqib Ullah, Farzana Shaheen, Uzma Salar, Andreas G. Tzakos, Ioannis P. Gerothanassis","doi":"10.1002/psc.70045","DOIUrl":"https://doi.org/10.1002/psc.70045","url":null,"abstract":"Marine sponges are sessile invertebrates found in moderate, arctic, and tropical regions, serving as a valuable reservoir of bioactive compounds, particularly Pro-rich peptides. Among these, cyclic peptides have attracted significant interest due to their diverse therapeutic properties. One notable example is Stylissatin A (SA), a Pro-rich cyclic peptide reported from the marine sponge Stylissa massa. SA and its analogues have shown promising biological activities, including anti-inflammatory, anticancer, and anti-obesity effects. Despite the vast potential of marine-derived peptides, only a small number have progressed to the pharmaceutical market. Cyclic peptides like SA offer unique opportunities for molecular modifications and total synthesis, enabling the enhancement of potency, improvement of physicochemical properties, and optimization of synthetic yields. This review highlights the synthetic strategies developed for the total synthesis of SA, explores its structural features and related analogues, and discusses their therapeutic potential, underscoring the promise of SA-based scaffolds as novel peptide-based drug candidates.","PeriodicalId":16946,"journal":{"name":"Journal of Peptide Science","volume":"31 9","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/psc.70045","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144687876","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Chemical Synthesis of Medin via a Removable Aggregation-Suppressing Linker 用可移动抑制聚集连接剂化学合成麦丁

IF 1.8 4区生物学

Journal of Peptide Science Pub Date : 2025-07-13 DOI: 10.1002/psc.70041

Matthias De Vleeschouwer, Brajabandhu Pradhan, Frederic Rousseau, Joost Schymkowitz

{"title":"Chemical Synthesis of Medin via a Removable Aggregation-Suppressing Linker","authors":"Matthias De Vleeschouwer, Brajabandhu Pradhan, Frederic Rousseau, Joost Schymkowitz","doi":"10.1002/psc.70041","DOIUrl":"https://doi.org/10.1002/psc.70041","url":null,"abstract":"<div>\u0000 \u0000 Medin, a 50-amino acid fragment derived from the protein MFG-E8 (lactadherin), is the most prevalent amyloid found in humans, present in the vasculature of nearly all individuals over the age of 50. Its biological relevance is highlighted by its co-localization with amyloid-β (Aβ) deposits in both Alzheimer's disease patients and transgenic mice models. Notably, Medin promotes amyloid-β aggregation, forming mixed fibrils with Aβ and enhancing its deposition in blood vessels. Here we report a new and efficient strategy to chemically access this compound. Our approach employs a solubilizing linker that not only ensures high solubility but also suppresses aggregation, allowing efficient purification of the product. The linker can be removed without a trace, after which the product behaves identically to wild-type Medin and forms amyloid fibrils. The synthesis route allows opening up a new chemical space, including nonnatural modifications like biotinylation. Together with the control over the aggregation properties, this is a powerful tool for amyloid protein studies.\u0000 </div>","PeriodicalId":16946,"journal":{"name":"Journal of Peptide Science","volume":"31 8","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-07-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144615394","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Peptide-Drug Conjugates: A New Hope for Cancer 肽-药物偶联物：癌症的新希望

IF 1.8 4区生物学

Journal of Peptide Science Pub Date : 2025-07-11 DOI: 10.1002/psc.70040

Amy Armstrong, Fleur Coburn, Yanyamba Nsereko, Othman Al Musaimi

{"title":"Peptide-Drug Conjugates: A New Hope for Cancer","authors":"Amy Armstrong, Fleur Coburn, Yanyamba Nsereko, Othman Al Musaimi","doi":"10.1002/psc.70040","DOIUrl":"https://doi.org/10.1002/psc.70040","url":null,"abstract":"Peptide-drug conjugates (PDCs) are advancing as targeted cancer therapies, leveraging lessons from antibody-drug conjugates (ADCs) to improve tumour specificity. These molecules combine a homing peptide with a cytotoxic payload via a linker, enabling precise drug delivery while sparing healthy tissue. Despite their potential, PDCs face challenges including metabolic instability, premature payload release and rapid clearance, limiting clinical success. Only Lutathera remains FDA-approved after Pepaxto's withdrawal, though Pepaxto retains EMA and MHRA approval—highlighting regulatory and technical complexities. Most PDCs target overexpressed receptors (e.g., somatostatin and GnRH), though novel designs like CBX-12 employ alternative strategies. Currently, six PDCs are in Phase III trials, with ~96 in development, signalling growing interest. This review explores how ADC research has guided PDC optimisation, particularly in linker chemistry and payload selection. We analyse key structural features governing PDC efficacy, including peptide-receptor binding and intracellular trafficking. Innovations in stable linkers and tumour-selective activation mechanisms are critical to overcoming pharmacokinetic hurdles. Promising candidates in late-stage trials are highlighted, emphasising their potential to address unmet needs in oncology. By refining targeting precision and payload delivery, next-generation PDCs may expand treatment options for resistant cancers, bridging the gap between biologics and small-molecule therapies.","PeriodicalId":16946,"journal":{"name":"Journal of Peptide Science","volume":"31 8","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-07-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/psc.70040","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144606656","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Chemical Synthesis of Crustacean Insulin-Like Peptide Using a Novel Method to Prevent Methionine Oxidation During Solid Phase Peptide Synthesis 一种防止甲硫氨酸在固相合成过程中氧化的新方法合成甲壳类胰岛素样肽

IF 1.8 4区生物学

Journal of Peptide Science Pub Date : 2025-07-11 DOI: 10.1002/psc.70042

Hidekazu Katayama, Naoaki Tsutsui

{"title":"Chemical Synthesis of Crustacean Insulin-Like Peptide Using a Novel Method to Prevent Methionine Oxidation During Solid Phase Peptide Synthesis","authors":"Hidekazu Katayama, Naoaki Tsutsui","doi":"10.1002/psc.70042","DOIUrl":"https://doi.org/10.1002/psc.70042","url":null,"abstract":"The oxidation of Met residue(s) in peptides and proteins is sometimes found in solid phase peptide synthesis (SPPS). In this study, in order to develop a method to prevent the oxidation of Met during SPPS, various sulfide compounds were added to the solvent and the oxidation rate was measured. As a result, it was found that tetrahydrothiophene (THT) was most efficient for reducing the extent of Met oxidation. THT tended to prevent the oxidation of Met in a concentration-dependent manner, although the oxidation of Met could not be completely prevented even at a concentration of 20% (v/v). On the other hand, when the SPPS in the presence of THT and then reduction of Met(O) to Met with NH4I were performed, the yield was much improved. These results indicate that the combination of preventing oxidation with THT and reducing Met with NH4I is effective for the synthesis of peptides containing Met residue(s). Using the method established here, we could synthesize an insulin-like peptide from the kuruma shrimp. This method is likely to be applicable to the synthesis of various Met-containing peptides.","PeriodicalId":16946,"journal":{"name":"Journal of Peptide Science","volume":"31 8","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-07-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/psc.70042","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144606732","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Influence of Buffering Capacity, pH, and Temperature on the Stability of Semaglutide: A Preformulation Study 缓冲容量、pH和温度对西马鲁肽稳定性影响的预制剂研究

IF 1.8 4区生物学

Journal of Peptide Science Pub Date : 2025-07-09 DOI: 10.1002/psc.70039

Adarsh Malgave, Sideequl Akbar, Ayushi Tiwari, Shamal Hande, Anumol Joseph, Rajkumar Malayandi

{"title":"Influence of Buffering Capacity, pH, and Temperature on the Stability of Semaglutide: A Preformulation Study","authors":"Adarsh Malgave, Sideequl Akbar, Ayushi Tiwari, Shamal Hande, Anumol Joseph, Rajkumar Malayandi","doi":"10.1002/psc.70039","DOIUrl":"https://doi.org/10.1002/psc.70039","url":null,"abstract":"<div>\u0000 \u0000 Therapeutic peptides' physical and chemical stability is of significant interest to the pharmaceutical industry. This study examines the effects of pH, temperature, and buffer strength on semaglutide (SEMA) stability using two orthogonal stability-indicating reverse-phase high-performance liquid chromatography (RP-HPLC) methods. The findings aid in designing novel oral and long-acting injectable (LAI) SEMA formulations. Two RP-HPLC methods were developed and validated to separate SEMA and its degradants. Stability studies were conducted at 25°C, 40°C, and 55°C for 24 h in water, with extended studies at 5°C, 25°C, 40°C, 60°C, and 80°C. pH and buffer strength effects were assessed at 25°C and 40°C. SEMA remained stable for 3 h at 80°C. The results obtained from pH-dependent stability studies indicated that SEMA was relatively stable at pH 1.2 at 25°C and 40°C for a day. A higher extent of degradation was observed between the pH of 4.5–5.5; this is due to the isoelectric point of SEMA (pH 5.4), and hence, the finished product pH should be > 7.0. These findings highlight the critical influence of buffer, temperature, and pH on SEMA stability. The results obtained by this study would help develop both oral and LAI SEMA formulations.\u0000 </div>","PeriodicalId":16946,"journal":{"name":"Journal of Peptide Science","volume":"31 8","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-07-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144589626","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Photocatalytic Diselenide Contraction as a Tool for Site-Selective Isosteric Ubiquitylation 光催化二烯醛收缩作为位点选择性等构泛素化的工具

IF 1.8 4区生物学

Journal of Peptide Science Pub Date : 2025-07-03 DOI: 10.1002/psc.70037

Herwig Weissinger, Moritz Urschbach, Luca Ferrari, Sascha Martens, Christian F. W. Becker

{"title":"Photocatalytic Diselenide Contraction as a Tool for Site-Selective Isosteric Ubiquitylation","authors":"Herwig Weissinger, Moritz Urschbach, Luca Ferrari, Sascha Martens, Christian F. W. Becker","doi":"10.1002/psc.70037","DOIUrl":"https://doi.org/10.1002/psc.70037","url":null,"abstract":"Ubiquitylation is a highly conserved post-translational modification (PTM) in eukaryotes, which serves as a critical regulatory mechanism for protein homeostasis, cellular transport, signal transduction pathways, and numerous other functions. The biological function of ubiquitylation is dictated predominantly by the topology of its linkage. Deciphering ubiquitin's complex biochemistry necessitates novel synthetic methods that deliver well-defined, biosimilar ubiquitylation. To this end, a semisynthetic strategy relying on the recombinant expression of ubiquitin combined with chemoselective photocatalytic diselenide contraction (PDC) was established to enable site-selective biomimetic selenalysine-linked ubiquitylation. The modification of ubiquitin with a C-terminal selenol was fine-tuned to avoid hydrolysis. The conditions of the PDC reaction, such as solvent composition, phosphine concentration, and irradiation, were optimized for efficient ubiquitylation of a Tau F derived peptide. Furthermore, it was demonstrated that the selenalysine linkage undergoes efficient cleavage by deubiquitylating enzymes, comparable to the native isopeptide linkage. The presented method expands the toolbox of site-selective ubiquitylation techniques. It is tolerant to many functional groups and will help to further elucidate the complexities of ubiquitylation.","PeriodicalId":16946,"journal":{"name":"Journal of Peptide Science","volume":"31 8","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/psc.70037","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144551152","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Toward a Green SPPS: The Use of an Innovative Mesoporous pDVB Support for Environmentally Friendly Solvents 迈向绿色SPPS：使用创新的介孔pDVB支持环保溶剂

IF 1.8 4区生物学

Journal of Peptide Science Pub Date : 2025-06-30 DOI: 10.1002/psc.70038

Luana Lastella, Marco Zecca, Paolo Centomo, Karel Jeřábek, Fernando Formaggio, Ivan Guryanov, Antonio Ricci, Barbara Biondi

{"title":"Toward a Green SPPS: The Use of an Innovative Mesoporous pDVB Support for Environmentally Friendly Solvents","authors":"Luana Lastella, Marco Zecca, Paolo Centomo, Karel Jeřábek, Fernando Formaggio, Ivan Guryanov, Antonio Ricci, Barbara Biondi","doi":"10.1002/psc.70038","DOIUrl":"https://doi.org/10.1002/psc.70038","url":null,"abstract":"This study explores the use of a novel polymeric mesoporous support (pDVB) for solid-phase peptide synthesis (SPPS), with the aim of improving the efficiency and sustainability of the process. The pDVB support, functionalized with the Fmoc-Rink amide linker, offers advantages over conventional supports based on gel-type, lightly crosslinked polymer skeletons, particularly with regard to reduced reliance on swelling capacity, which allows the use of a wider range of solvents. The work focuses on greener and eco-friendly solvents such as TEP, ACN, IPA, and their mixtures with DMSO to replace toxic solvents such as DMF. The synthesis of two model peptide sequences, Fmoc-LLVF-NH2 and ACP(65–74), showed that pDVB-Rink performs better than a conventional-type Rink Amide MBHA support, especially when using environmentally friendly solvents. These results suggest that mesoporous pDVB-Rink is a promising solid support for SPPS to reduce the use of toxic solvents and to improve sustainability.","PeriodicalId":16946,"journal":{"name":"Journal of Peptide Science","volume":"31 8","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/psc.70038","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144520229","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0