dc.contributor.advisor | Raghavan, Sathees C | |
dc.contributor.author | Ray, Ujjayinee | |
dc.date.accessioned | 2021-07-12T04:04:06Z | |
dc.date.available | 2021-07-12T04:04:06Z | |
dc.date.submitted | 2020 | |
dc.identifier.uri | https://etd.iisc.ac.in/handle/2005/5193 | |
dc.description.abstract | To summarize, in the present study, we have synthesized and characterized three novel NHEJ inhibitors targeting DNA Ligase IV, with several fold better efficacy compared to SCR7 and thus potential to be developed as cancer therapeutic agents. While SCR130 showed up to 22-fold better efficacy, compounds A and B exhibited
>100 fold better cytotoxicity in cancer cell lines. First level preclinical studies reveal that novel inhibitors, A and B are interesting molecules and could be used in clinical trials for targeted therapy, particularly by a combinatorial mode. Considering that there is no drug currently used in clinic that target DNA double-strand break repair, these NHEJ inhibitors could be developed as cancer therapeutics against cancers with higher expression of Ligase IV, as well as against radio- and chemoresistant cancers | en_US |
dc.language.iso | en_US | en_US |
dc.rights | I grant Indian Institute of Science the right to archive and to make available my thesis or dissertation in whole or in part in all forms of media, now hereafter known. I retain all proprietary rights, such as patent rights. I also retain the right to use in future works (such as articles or books) all or part
of this thesis or dissertation | en_US |
dc.subject | Nonhomologous End Joining | en_US |
dc.subject | DNA double-strand break | en_US |
dc.subject | thioxo triazospiro derivatives | en_US |
dc.subject.classification | Research Subject Categories::NATURAL SCIENCES::Chemistry::Biochemistry | en_US |
dc.title | Identification and Biochemical Characterization of Novel Inhibitors of Nonhomologous End Joining: Implications in DNA Double-Strand Break Repair and Cancer Therapy | en_US |
dc.type | Thesis | en_US |
dc.degree.name | PhD | en_US |
dc.degree.level | Doctoral | en_US |
dc.degree.grantor | Indian Institute of Science | en_US |
dc.degree.discipline | Faculty of Science | en_US |