Abstract
Bacterial resistance to conventional antibiotics poses a challenge medicine to search for alternatives. Cationic antimicrobial peptides (AMPs) are promising for the development of a new class of antibiotics. This review focuses on the use of technetium-99m labeled synthetic AMPs, derived from human natural cationic AMPs, for target-delivery to and in vivo detection of infection sites caused by (drug-resistant) micro-organisms. The scintigraphic approach has proven to be a reliable method for evaluating AMPs in pharmacological studies and for optimizing target-delivery of radiolabeled AMPs to pathological sites in animals and humans. In addition, the effect of alterations in amphipathicity, amino acid substitution, and dimerization on the biological performance of AMPs is reported. Radiolabeled AMPs offer good perspectives for diagnosis of infections, for monitoring therapy, and, most importantly, for the ability to discriminate between infections and sterile inflammatory processes.
Keywords: Antimicrobial peptides, technetium-99m labeling, target-delivery, pharmacology, molecular imaging, infection detection, treatment monitoring
Mini-Reviews in Medicinal Chemistry
Title: The Use of Technetium-99m Radiolabeled Human Antimicrobial Peptides for Infection Specific Imaging
Volume: 8 Issue: 10
Author(s): C. P.J.M. Brouwer, L. Sarda-Mantel, A. Meulemans, D. Le Guludec and M. M. Welling
Affiliation:
Keywords: Antimicrobial peptides, technetium-99m labeling, target-delivery, pharmacology, molecular imaging, infection detection, treatment monitoring
Abstract: Bacterial resistance to conventional antibiotics poses a challenge medicine to search for alternatives. Cationic antimicrobial peptides (AMPs) are promising for the development of a new class of antibiotics. This review focuses on the use of technetium-99m labeled synthetic AMPs, derived from human natural cationic AMPs, for target-delivery to and in vivo detection of infection sites caused by (drug-resistant) micro-organisms. The scintigraphic approach has proven to be a reliable method for evaluating AMPs in pharmacological studies and for optimizing target-delivery of radiolabeled AMPs to pathological sites in animals and humans. In addition, the effect of alterations in amphipathicity, amino acid substitution, and dimerization on the biological performance of AMPs is reported. Radiolabeled AMPs offer good perspectives for diagnosis of infections, for monitoring therapy, and, most importantly, for the ability to discriminate between infections and sterile inflammatory processes.
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Cite this article as:
Brouwer P.J.M. C., Sarda-Mantel L., Meulemans A., Guludec Le D. and Welling M. M., The Use of Technetium-99m Radiolabeled Human Antimicrobial Peptides for Infection Specific Imaging, Mini-Reviews in Medicinal Chemistry 2008; 8 (10) . https://dx.doi.org/10.2174/138955708785740670
DOI https://dx.doi.org/10.2174/138955708785740670 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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