Antimicrobial peptides (AMPs) are considered a promising therapeutic approach against multi-drug resistant microorganisms. Besides their advantages, there are limitations to be overcome so that these molecules can become market competitive. One of the biggest limitations is proteolytic susceptibility, which could be overcome by structural modifications such as cyclization, especially for helix-constraining strategies. Over the years, many helix stabilization techniques have arisen, such as lactam-bridging, triazole-based, N-alkylation and all-hydrocarbon stapling. All-hydrocarbon stapling takes advantage of modified amino acid residues and olefinic cross-linking to constrain peptide helices. Despite being a well-established strategy and presenting efficient stability results, there are different limitations especially related to toxicity. In this review, recent studies on stapled AMPs for antimicrobial usage are explored with the aim of understanding the future of these molecules as putative antimicrobial agents.
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http://dx.doi.org/10.3390/antibiotics12091400 | DOI Listing |
Viruses
January 2025
Key Laboratory of Tropical Marine Bio-resources and Ecology, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 511458, China.
is a common opportunistic pathogen associated with nosocomial infections. The primary treatment for infections typically involves antibiotics, which can lead to the emergence of multidrug-resistant strains. Therefore, there is a pressing need for safe and effective alternative methods.
View Article and Find Full Text PDFPharmaceuticals (Basel)
January 2025
MML Medical Centre, Bagno 2, 00-112 Warsaw, Poland.
Inappropriate and excessive use of antibiotics is responsible for the rapid development of antimicrobial resistance, which is associated with increased patient morbidity and mortality. There is an urgent need to explore new antibiotics or alternative antimicrobial agents. a commensal microorganism but is also responsible for numerous infections.
View Article and Find Full Text PDFJ Clin Med
January 2025
Department of Anatomy, Jagiellonian University Medical College, 33-332 Cracow, Poland.
: Excessive body fatness is the basis of many diseases, especially civilization-related ones. The aim of this study is to analyze the body composition and serum levels of selected antimicrobial peptides (AMPs) in patients with basal cell carcinoma (BCC), in comparison to healthy controls (HCs), and investigate whether any specific parameter significantly increases the risk of BCC development. : The body composition and measurements of serum levels of cathelicidin and human-beta-defensin-2 were analyzed in a group of 100 subjects (50 patients with BCC and 50 HCs).
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January 2025
College of Life Science, Liaoning Normal University, Dalian 116081, China.
Liver-expressed antimicrobial peptide 2 (LEAP-2) was originally discovered as an antimicrobial peptide that plays a vital role in the host innate immune system of various vertebrates. Recent research discovered LEAP-2 as an endogenous antagonist and inverse agonist of the GHSR1a receptor. By acting as a competitive antagonist to ghrelin, LEAP-2 influences energy balance and metabolic processes via the ghrelin-GHSR1a signaling pathway.
View Article and Find Full Text PDFMolecules
January 2025
Department of Biochemistry and Organic Chemistry, Institute of Chemistry, São Paulo State University (UNESP), Araraquara 14800-060, SP, Brazil.
Leishmaniasis is a neglected tropical disease caused by a protozoan of the genus Leishmania, which has visceral and cutaneous forms. The symptoms of leishmaniasis include high fever and weakness, and the cutaneous infection also causes lesions under the skin. The drugs used to treat leishmaniasis have become less effective due to the resistance mechanisms of the protozoa.
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