Strategies employed in the design of antimicrobial peptides with enhanced proteolytic stability

Biotechnology Advances, Год журнала: 2022, Номер 59, С. 107962 - 107962

Опубликована: Апрель 19, 2022

Язык: Английский

---

Cyclic Peptides in Pipeline: What Future for These Great Molecules?

Pharmaceuticals, Год журнала: 2023, Номер 16(7), С. 996 - 996

Опубликована: Июль 12, 2023

Cyclic peptides are molecules that already used as drugs in therapies approved for various pharmacological activities, example, antibiotics, antifungals, anticancer, and immunosuppressants. Interest these has been growing due to the improved pharmacokinetic pharmacodynamic properties of cyclic structure over linear by evolution chemical synthesis, computational, vitro methods. To date, 53 have different regulatory authorities, many others clinical trials a wide diversity conditions. In this review, potential is presented, general aspects their synthesis development discussed. Furthermore, an overview also given, summarized.

Язык: Английский

---

Enhancing Antimicrobial Peptide Activity through Modifications of Charge, Hydrophobicity, and Structure

International Journal of Molecular Sciences, Год журнала: 2024, Номер 25(19), С. 10821 - 10821

Опубликована: Окт. 9, 2024

Antimicrobial peptides (AMPs) are emerging as a promising alternative to traditional antibiotics due their ability disturb bacterial membranes and/or intracellular processes, offering potential solution the growing problem of antimicrobial resistance. AMP effectiveness is governed by factors such net charge, hydrophobicity, and form amphipathic secondary structures. When properly balanced, these characteristics enable AMPs selectively target while sparing eukaryotic cells. This review focuses on roles positive structure in influencing activity toxicity, explores strategies optimize them for enhanced therapeutic potential. We highlight delicate balance between properties how various modifications, including amino acid substitutions, peptide tagging, or lipid conjugation, can either enhance impair performance. Notably, an increase parameters does not always yield best results; sometimes, slight reduction structural stability improves overall Understanding complex interactions key developing with greater reduced making viable candidates fight against antibiotic-resistant bacteria.

Язык: Английский

---

Advance in peptide-based drug development: delivery platforms, therapeutics and vaccines

Signal Transduction and Targeted Therapy, Год журнала: 2025, Номер 10(1)

Опубликована: Март 5, 2025

The successful approval of peptide-based drugs can be attributed to a collaborative effort across multiple disciplines. integration novel drug design and synthesis techniques, display library technology, delivery systems, bioengineering advancements, artificial intelligence have significantly expedited the development groundbreaking drugs, effectively addressing obstacles associated with their character, such as rapid clearance degradation, necessitating subcutaneous injection leading increasing patient discomfort, ultimately advancing translational research efforts. Peptides are presently employed in management diagnosis diverse array medical conditions, diabetes mellitus, weight loss, oncology, rare diseases, additionally garnering interest facilitating targeted platforms advancement vaccines. This paper provides an overview present market clinical trial progress therapeutics, platforms, It examines key areas through literature analysis emphasizes structural modification principles well recent advancements screening, design, technologies. accelerated including peptide-drug complexes, new vaccines, innovative diagnostic reagents, has potential promote era precise customization disease therapeutic schedule.

Язык: Английский

---

Targeting Peptides: The New Generation of Targeted Drug Delivery Systems

Pharmaceutics, Год журнала: 2023, Номер 15(6), С. 1648 - 1648

Опубликована: Июнь 3, 2023

Peptides can act as targeting molecules, analogously to oligonucleotide aptamers and antibodies. They are particularly efficient in terms of production stability physiological environments; recent years, they have been increasingly studied agents for several diseases, from tumors central nervous system disorders, also thanks the ability some them cross blood–brain barrier. In this review, we will describe techniques employed their experimental silico design, well possible applications. We discuss advancements formulation chemical modifications that make even more stable effective. Finally, how use could effectively help overcome various problems improve existing treatments.

Язык: Английский

---

Non‐canonical amino acid bioincorporation into antimicrobial peptides and its challenges

Journal of Peptide Science, Год журнала: 2024, Номер 30(6)

Опубликована: Янв. 23, 2024

The rise of antimicrobial resistance and multi‐drug resistant pathogens has necessitated explorations for novel antibiotic agents as the discovery conventional antibiotics is becoming economically less viable technically more challenging biopharma. Antimicrobial peptides (AMPs) have emerged a promising alternative because their particular mode action, broad spectrum difficulty that microbes in to them. AMPs bacitracin, gramicidin, polymyxins daptomycin are currently used clinically. However, susceptibility proteolytic degradation, toxicity profile, complexities large‐scale manufacture hindered development. To improve stability, methods such integrating non‐canonical amino acids (ncAAs) into peptide sequence been adopted, which also improves potency action. benefits ncAA incorporation made possible by solid‐phase synthesis. this method not always suitable commercial production poor yield, scale‐up difficulties, its non‐‘green’ nature. Bioincorporation integration an emerging field geared towards tackling challenges synthesis green, cheaper, scalable commercialisation AMPs. This review focusses on bioincorporation ncAAs; some associated with outlined, notes given how overcome these challenges. particularly addressing two key challenges: AMP cytotoxicity microbial cell factories uptake ncAAs unfavourable Overcoming will draw us closer greater yield environmentally friendly sustainable approach make druggable.

Язык: Английский

---

Site-selective cleavage of peptides and proteins targeting aromatic amino acid residues

RSC Advances, Год журнала: 2025, Номер 15(12), С. 9159 - 9179

Опубликована: Янв. 1, 2025

This review provides an account of the site-selective cleavage peptides and proteins at aromatic amino acid residues, developed over last seven decades (1958–2024).

Язык: Английский

---

Ex Situ Synthesis of N-Capped Peptides in the Solution Phase via Palladium-Catalyzed Aminocarbonylation Utilizing Chloroform-COware

The Journal of Organic Chemistry, Год журнала: 2025, Номер unknown

Опубликована: Янв. 28, 2025

We report the synthesis of N-capped peptides under mild conditions using oxidative aminocarbonylation aryl iodides and peptide esters as nucleophiles in solution phase. Ex situ chloroform chamber A generates CO, which diffuses to B, contains other reactants. This method offers at 80 °C for 12 h. synthesized 36 this method, including an anticancer drug bortezomib analogue, with isolated yield ranging from 52 91%. The present gives easy access previously inaccessible N-capping groups, heteroaromatic ring-capped enable robust analogue designs peptide-based discovery.

Язык: Английский

---

Potentials of Neuropeptides as Therapeutic Agents for Neurological Diseases

Biomedicines, Год журнала: 2022, Номер 10(2), С. 343 - 343

Опубликована: Фев. 1, 2022

Despite recent leaps in modern medicine, progress the treatment of neurological diseases remains slow. The near impermeable blood-brain barrier (BBB) that prevents entry therapeutics into brain, and complexity processes, limits specificity potential therapeutics. Moreover, a lack etiological understanding irreversible nature conditions have resulted low tolerability high failure rates towards existing small molecule-based treatments. Neuropeptides, which are proteinaceous molecules produced by body, either nervous system or peripheral organs, modulate function. Although peptide-based originated from metabolic 1920s, adoption development peptide drugs for relatively recent. In this review, we examine natural roles neuropeptides modulation function disorders. Furthermore, highlight these filling gaps current

Язык: Английский

---

USFDA-approved parenteral peptide formulations and excipients: Industrial perspective

Journal of Drug Delivery Science and Technology, Год журнала: 2024, Номер 95, С. 105589 - 105589

Опубликована: Март 15, 2024

Язык: Английский

---