Antimicrobial peptides have received increasing attention as potential antitumor drugs due to their new mode of action. However, the systemic toxicity at high concentration always hampers their successful utilization for tumor therapy. Here, we designed a new type of acid-activated antimicrobial peptide AMitP by conjugating antimicrobial peptide MitP to its anionic binding partner MitPE via a disulfide linker. Compared with MitP, AMitP displayed significant antitumor activity at acidic pH and low cytotoxicity at normal pH. The results of MD simulations demonstrate that the changes of structure and membrane binding tendency of AMitP at different pH values played an important role in its pH-dependent antitumor activity. In addition, AMitP showed significant enzymatic stability compared with MitP, suggesting a potential for in vivo application. In short, our work opens a new avenue to develop antimicrobial peptides as potential antitumor drugs with high selectivity.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/mp400052s | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Bottom-up reconstitution design of a biomimetic atelocollagen microfibril for enhancing hemostatic, antibacterial, and biodegradable benefits.
J Mater Chem B
January 2025
Key Laboratory of Leather Chemistry and Engineering (Ministry of Education), Sichuan University, Chengdu 610065, P. R. China.
Powdered collagen is emerging as a promising topical hemostat owing to its adaptability to various wounds, active hemostatic abilities, and biosafety. The reproduction of a bionic structure similar to natural collagen is crucial for effective hemostasis and bioactivity. Additional factors relevant to clinical application include antimicrobial properties, minimal immune response, and straightforward preparation.
View Article and Find Full Text PDFAAV-based gene delivery of antimicrobial peptides to combat drug-resistant pathogens.
Appl Environ Microbiol
January 2025
Animal Sciences Research Center, Division of Animal Sciences, University of Missouri, Columbia, Missouri, USA.
Antimicrobial peptides (AMPs) have emerged as potential alternatives to conventional antibiotics due to their novelty and multiple mechanisms of action. Because they are peptides, AMPs are amenable to bioengineering and suitable for cloning and expression at large production scales. However, the efficient delivery of AMPs is an unaddressed issue, particularly due to their large size, possible toxicities, and the development of adverse immune responses.
View Article and Find Full Text PDFImmunomodulatory peptides: new therapeutic horizons for emerging and re-emerging infectious diseases.
Front Microbiol
December 2024
School of Biosciences and Technology, Vellore Institute of Technology SBST, Vellore, Tamil Nadu, India.
The emergence and re-emergence of multi-drug-resistant (MDR) infectious diseases have once again posed a significant global health challenge, largely attributed to the development of bacterial resistance to conventional anti-microbial treatments. To mitigate the risk of drug resistance globally, both antibiotics and immunotherapy are essential. Antimicrobial peptides (AMPs), also referred to as host defense peptides (HDPs), present a promising therapeutic alternative for treating drug-resistant infections due to their various mechanisms of action, which encompass antimicrobial and immunomodulatory effects.
View Article and Find Full Text PDFOrganocatalysed synthesis of -(4-oxo-2-phenyl-1,2-dihydroquinazolin-3(4)-yl)isonicotinamide: computational, electrochemical, drug-likeness and antimicrobial studies.
3 Biotech
January 2025
Peptide and Medicinal Chemistry Research Laboratory, Department of Chemistry, Rani Channamma University, P-B, NH-4, Belagavi, 591 156 India.
Unlabelled: We have developed novel and sustainable homogeneous catalysts employing Glutamic acid (Glu) as a biodegradable and eco-friendly organocatalyst for the synthesis of -(4-oxo-2-phenyl-1,2-dihydroquinazolin-3(4)-yl)isonicotinamide derivatives (-) via multicomponent reactions (MCRs) of isatoic anhydride, isoniazid and heteroaromatic/aromatic aldehyde in ethanol on oil bath stirring at 60 °C. Selected final product homogeneity was examined by various spectroscopic techniques such as C-, H- NMR, FT-IR and LC-MS. For the first time, herein investigated electrochemical behavior of selected derivatives (-) using cyclic voltammetry method.
View Article and Find Full Text PDFRoles of NET Peptides With Known Antimicrobial Activity and Toxicity in Immune Response.
J Immunol Res
December 2024
Department of Medical Microbiology, School of Medicine, Acibadem Mehmet Ali Aydinlar University, Istanbul, Türkiye.
Antimicrobial peptides (AMPs) are crucial components of the innate immune system in all living organisms, playing a vital role in the body's defense against diseases and infections. The immune system's primary functions include preventing disease-causing agents from entering the body and eliminating them without causing harm. These peptides exhibit broad-spectrum activity against bacteria, viruses, fungi, parasites, and cancer cells.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!