2026-04-13T05:53:25Zhttps://recercat.cat/oai/request
oai:recercat.cat:2445/1784942025-12-04T19:36:57Zcom_2072_1057col_2072_478813col_2072_478917
RECERCAT author Dallavalle, Sabrina author Mattio, Luce M. author Artali, Roberto author Musso, Loana author Aviñó Andrés, Anna author Fàbrega i Claveria, Ma. Carme author Eritja i Casadellà, Ramon author Gargallo Gómez, Raimundo author Mazzini, Stefania 2021-06-17T08:25:08Z2021-06-17T08:25:08Z2021-06-172021-06-17T08:25:08Z Curaxins and especially the second-generation derivative curaxin CBL0137 have important antitumor activities in multiple cancers such as glioblastoma, melanoma and others. Although most of the authors suggest that their mechanism of action comes from the activation of p53 and inactivation of NF-kB by targeting FACT, there is evidence supporting the involvement of DNA binding in their antitumor activity. In this work, the DNA binding properties of curaxin CBL0137 with model quadruplex DNA oligomers were studied by 1H NMR, CD, fluorescence and molecular modeling. We provided molecular details of the interaction of curaxin with two G-quadruplex structures, the single repeat of human telomere d(TTAGGGT)4 and the c-myc promoter Pu22 sequence. We also performed 1H and 31P NMR experiments were also performed in order to investigate the interaction with duplex DNA models. Our data support the hypothesis that the interaction of curaxin with G-quadruplex may provide a novel insight into the DNA-binding properties of CBL0137, and it will be helpful for the design of novel selective DNA-targeting curaxin analogues. cc-by (c) Dallavalle, Sabrina et al., 2021 https://creativecommons.org/licenses/by/4.0/ info:eu-repo/semantics/openAccess G-estructures Espectroscòpia de ressonància magnètica nuclear Oligòmers G-structures Nuclear magnetic resonance spectroscopy Oligomers Exploring the interaction of Curaxin CBL0137 with G-Quadruplex DNA oligomers info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion