High-affinity A/T-rich DNA binding with a dimeric bisbenzamidine
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ISSN: 2976-856X
E-ISSN: 2976-856X
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Oxford Academic
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Abstract
A bisbenzamidine DNA binding agent can be easily dimerized by alkylation of its terminal amidine groups to afford an extended minor groove binder with over 20-fold enhanced DNA affinity toward extended A/T-rich sites. Nuclear magnetic resonance experiments in combination with molecular dynamics simulation studies provide structural insight into the insertion of this compound in the DNA minor groove, and antimicrobial assays demonstrate that the increased affinity translates into higher antileishmanial activity.
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Bouzada, D., Paul, A., Sánchez, M. I., Domínguez-Asenjo, B., Lence, E., Melle-Franco, M., Ardá, A., Barreiro-Piñeiro, N., Penas, C., Gómez-González, J., Jiménez-Barbero, J., Moreno, J., González-Bello, C., Wilson, W. D., Mascareñas, J. L., & Vázquez, M. E. (2024). High-affinity A/T-rich DNA binding with a dimeric bisbenzamidine. NAR Molecular Medicine, 1(4), Article ugae022 . https://doi.org/10.1093/narmme/ugae022
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https://doi.org/10.1093/narmme/ugae022Sponsors
Agencia Estatal de Investigación [RTI2018-099877-B-I00, PID2022-136963OB-I00, PID2021-127702NB-I00]; Xunta de Galicia [ED431C 2021/29, ED431G 2023/03]; European Regional Development Fund; CICECO [IF/00894/2015, UIDB/50011/2020, UIDP/50011/2020, LA/P/0006/2020]; EDCTP [RIA2020S-3301]; ISCIII [PI21CIII/00005]; CIBERINFEC [CB21/13/00018].
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Attribution-NonCommercial 4.0 International