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Binding thermodynamics of paromomycin, neomycin, neomycin‐dinucleotide and ‐diPNA conjugates to bacterial and human rRNA
Author(s) -
Alguacil Javier,
Robles Jordi,
Ràfols Clara,
Bosch Elisabeth
Publication year - 2016
Publication title -
journal of molecular recognition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.401
H-Index - 79
eISSN - 1099-1352
pISSN - 0952-3499
DOI - 10.1002/jmr.2513
Subject(s) - neomycin , paromomycin , isothermal titration calorimetry , chemistry , context (archaeology) , antimicrobial , aminoglycoside , biochemistry , antibiotics , biology , organic chemistry , paleontology
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. Copyright © 2015 John Wiley & Sons, Ltd.