Topoisomerases inhibition and DNA binding mode of daunomycin-oligoarginine conjugate
| Autor: | Ildikò Szabò, Zoltán Bánóczi, Giuseppe Perugino, Valeria Visone, Ferenc Hudecz, Anna Valenti |
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| Přispěvatelé: | Visone, Valeria, Szabó, Ildikó, Perugino, Giuseppe, Hudecz, Ferenc, Bánóczi, Zoltán, Valenti, Anna |
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
Spectrometry
Mass Electrospray Ionization medicine.drug_class topoisomerase inhibitor Antineoplastic Agents RM1-950 [object Object] 01 natural sciences Antineoplastic Agent Biological pathway chemistry.chemical_compound Drug Discovery medicine Topoisomerase II Inhibitors Protein–DNA interaction DNA topoisomerase Chromatography High Pressure Liquid Pharmacology chemistry.chemical_classification Oligopeptide biology topoisomerase inhibitors 010405 organic chemistry Brief Report Circular Dichroism Topoisomerase Daunorubicin DNA General Medicine 0104 chemical sciences 010404 medicinal & biomolecular chemistry Spectrometry Fluorescence Enzyme chemistry Biochemistry Peptide biology.protein Therapeutics. Pharmacology DNA–protein interaction Peptides Topoisomerase inhibitor daunomycin Conjugate |
| Zdroj: | Journal of enzyme inhibition and medicinal chemistry (Online) 35 (2020): 1363–1371. doi:10.1080/14756366.2020.1780226 info:cnr-pdr/source/autori:Visone V.; Szabo I.; Perugino G.; Hudecz F.; Banoczi Z.; Valenti A./titolo:Topoisomerases inhibition and DNA binding mode of daunomycin-oligoarginine conjugate/doi:10.1080%2F14756366.2020.1780226/rivista:Journal of enzyme inhibition and medicinal chemistry (Online)/anno:2020/pagina_da:1363/pagina_a:1371/intervallo_pagine:1363–1371/volume:35 Journal of Enzyme Inhibition and Medicinal Chemistry article-version (VoR) Version of Record Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 35, Iss 1, Pp 1363-1371 (2020) |
| DOI: | 10.1080/14756366.2020.1780226 |
| Popis: | Cancer is a major health issue adsorbing the attention of a biomedical research. To fight this disease, new drugs are developed, specifically tailored to target biological pathways or peculiar components of the tumour cells. Particularly interesting is the use of intercalating agents as drugs capable to bind DNA and inhibit enzymes involved in DNA metabolism. Anthracyclines are the most commonly used anticancer drugs. In particular, daunomycin is used to cancer treatment by exploiting its ability to intercalate DNA and inhibit the activity of DNA topoisomerases implicated in the replication processes. Unfortunately, clinical application of anthracyclines is limited by their side effects. The conjugation with specific carriers could affect the selectivity and reduce side effect by improving stability and/or cellular uptake properties. We here report the biochemical characterisation of a daunomycin oligopeptide conjugate containing six residues of arginine, by the analysis of its fluorescence properties, DNA interaction and topoisomerases inhibitory effects. |
| Databáze: | OpenAIRE |
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