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Binding thermodynamics of paromomycin, neomycin, neomycin-dinucleotide and -diPNA conjugates to bacterial and human rRNA

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Isothermal titration calorimetry (ITC) is a powerful technique able to evaluate the energetics of target-drug binding within the context of drug discovery. In this work, the interactions of RNAs reproducing bacterial and human ribosomal A-site, with two well-known antibiotic aminoglycosides, Paromomycin and Neomycin, as well as several Neomycin-dinucleotide and -diPNA conjugates, have been evaluated by ITC and the corresponding thermodynamic quantities determined. The comparison of the thermodynamic data of aminoglycosides and their chemical analogues allowed to select Neomycin-diPNA conjugates as the best candidates for antimicrobial activity.

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ALGUACIL, Javier, ROBLES I BRAU, Jordi, RÀFOLS LLACH, Clara, BOSCH, Elisabeth. Binding thermodynamics of paromomycin, neomycin, neomycin-dinucleotide and -diPNA conjugates to bacterial and human rRNA. _Journal of Molecular Recognition_. 2016. Vol. 29, núm. 4, pàgs. 142-150. [consulta: 25 de febrer de 2026]. ISSN: 0952-3499. [Disponible a: https://hdl.handle.net/2445/152818]

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