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• Toward synthesis of thioglycosyl-phosphonate analogues of lipid ll

  Viktor Kelemen

  Milán Csiszár

  Anikó Borbás

  Views:

  161

  Although a multitude of epidemics have already been eradicated with the use of modern antibiotics, in the 20th century, a new and increasingly serious phenomenon has arisen - the resistance against antibiotic therapies, necessiting the need for the development of novel antibiotic compounds. Transglycosylases are key enzymes in the biosynthesis of the bacterial cell wall, and currently there is no approved drug in human use against them, so they are an excellent target for further antibiotic development. During our research, the main goal was to synthesize compounds that are structurally similar to lipid ll, the substrate of bacterial transglycosylases, however, with significant modifications, such as the incorporation of an α-thioglycosidic unit instead of the α-O-glycosidic bond and an alkylphosphonate unit instead of the pyrophosphate part, making the molecules suitable to act as enzyme inhibitors. The key step of our work is the stereoselective construction of the 1,2-cis-α-thioglycosidic bond by photoinitiated thiol ene coupling reaction. ln this paper, the novel synthesis route is described which can be applied to furnish different lipid ll analogues, on example synthesis of a D-glucose derivative.

• Medicines for influencing the posttranslational modifications of histones – a tutorial review

  14

  Miklós Bege

  Anikó Borbás

  Views:

  166

  Epigenetic therapy is a relatively novel, but undoubtedly a promising area of pharmacology. Most epigenetic drugs act by affecting enzymes and play a role in post-translational modifications of histones. The molecular targets of these medicines include histone methyltransferases, histone demethylases, isocitrate dehydrogenases, histone acetyltransferases and histone deacetylases. Since histone modifications are important regulatory signals, abnormalities in this process often lead to tumorigenesis, therefore these medicines constitute an important class of antitumor therapy. In this tutorial review, we would like to briefly overview the medicines that affect histone modifications, focusing on the currently approved ones, and briefly mention other interesting examples.

• New anticancer medicines approved by the EMA in 2024

  Miklós Bege

  Anikó Borbás

  Views:

  109

  Tumorous diseases are among the leading causes of death in the developed world, therefore there is a constant need for new antineoplastic medicines. In 2024, the EMA approved 28 anticancer drugs, of which 13 contains new active substances. In this review, we briefly summarize the mechanism of action and use of the new drugs approved by the EMA.

• Avacincaptad pegol, the second approved aptamer medicine – A mini review

  Miklós Bege

  Rasha Ghanem Kattoub

  Anikó Borbás

  Views:

  158

  Therapeutic oligonucleotides are employed in the treatment of a variety of diseases, primarily functioning through mechanisms associated with gene silencing technologies. In contrast, aptamers exhibit mechanisms of action that are more akin to those of protein-based monoclonal antibodies. However, owing to their oligonucleotide structure, aptamers possess several advantages over antibodies. Despite these benefits, the adoption of aptamers in clinical medicine has not reached the levels observed with monoclonal antibodies or gene-silencing oligonucleotides. Almost two decades after the approval of pegaptanib, the first approved aptameric therapeutic for the treatment of neovascular AMD (age-related macular degeneration), a second aptamer has recently received approval to treat geographic atrophy, an advanced form of AMD. In this review, we aim to provide an overview of the pharmacology and chemistry of avacincaptad pegol, the second approved aptameric drug.