PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 21464033-0 2011 Induction of retinoid X receptor activity and consequent upregulation of p21WAF1/CIP1 by indenoisoquinolines in MCF7 cells. indenoisoquinolines 89-108 retinoid X receptor alpha Homo sapiens 13-32 31283877-6 2019 Here, we report that anticancer indenoisoquinolines strongly bind and stabilize MycG4 and lower MYC expression levels in cancer cells, using various biochemical, biophysical, computer modeling, and cell-based methods. indenoisoquinolines 32-51 MYC proto-oncogene, bHLH transcription factor Homo sapiens 96-99 31283877-7 2019 Significantly, a large number of active indenoisoquinolines cause strong MYC downregulation in cancer cells. indenoisoquinolines 40-59 MYC proto-oncogene, bHLH transcription factor Homo sapiens 73-76 31283877-10 2019 Therefore, this study uncovers a novel mechanism of action of indenoisoquinolines as a new family of drugs targeting the MYC promoter G-quadruplex for MYC suppression. indenoisoquinolines 62-81 MYC proto-oncogene, bHLH transcription factor Homo sapiens 121-124 31283877-10 2019 Therefore, this study uncovers a novel mechanism of action of indenoisoquinolines as a new family of drugs targeting the MYC promoter G-quadruplex for MYC suppression. indenoisoquinolines 62-81 MYC proto-oncogene, bHLH transcription factor Homo sapiens 151-154 24800942-3 2014 This study describes the successful design and synthesis of 2-position-modified indenoisoquinolines as dual Top1-TDP1 inhibitors using a structure-based drug design approach. indenoisoquinolines 80-99 tyrosyl-DNA phosphodiesterase 1 Homo sapiens 113-117 24800942-4 2014 Enzyme inhibition studies indicate that indenoisoquinolines modified at the 2-position with three-carbon side chains ending with amino substituents show both promising Top1 and TDP1 inhibitory activity. indenoisoquinolines 40-59 tyrosyl-DNA phosphodiesterase 1 Homo sapiens 177-181 23472886-4 2013 This communication presents the design, synthesis, and biological evaluation of both acidic and nonacidic indenoisoquinolines as new RXR ligands. indenoisoquinolines 106-125 retinoid X receptor alpha Homo sapiens 133-136 23259865-0 2013 Synthesis and biological evaluation of indenoisoquinolines that inhibit both tyrosyl-DNA phosphodiesterase I (Tdp1) and topoisomerase I (Top1). indenoisoquinolines 39-58 tyrosyl-DNA phosphodiesterase 1 Homo sapiens 110-114 23259865-2 2013 This report documents the design, synthesis, and evaluation of new indenoisoquinolines that are dual inhibitors of both Tdp1 and Top1. indenoisoquinolines 67-86 tyrosyl-DNA phosphodiesterase 1 Homo sapiens 120-124 23259865-4 2013 The potencies of the indenoisoquinolines against Tdp1 ranged from 5 muM to 111 muM, which places the more active compounds among the most potent known inhibitors of this target. indenoisoquinolines 21-40 tyrosyl-DNA phosphodiesterase 1 Homo sapiens 49-53 23259865-4 2013 The potencies of the indenoisoquinolines against Tdp1 ranged from 5 muM to 111 muM, which places the more active compounds among the most potent known inhibitors of this target. indenoisoquinolines 21-40 latexin Homo sapiens 68-71 23259865-4 2013 The potencies of the indenoisoquinolines against Tdp1 ranged from 5 muM to 111 muM, which places the more active compounds among the most potent known inhibitors of this target. indenoisoquinolines 21-40 latexin Homo sapiens 79-82 21843105-5 2011 Tdp1 inhibitors should synergize not only with Top1-targeting drugs (camptothecins, indenoisoquinolines), but also with bleomycin, topoisomerase II (Top2) inhibitors (etoposide, doxorubicin) and DNA alkylating agents. indenoisoquinolines 84-103 tyrosyl-DNA phosphodiesterase 1 Homo sapiens 0-4 31409613-10 2019 RESULTS: CellMinerCDB reveals that SLFN11, which kills cells undergoing replicative stress, is a dominant drug determinant to the clinical indenoisoquinolines. indenoisoquinolines 139-158 schlafen family member 11 Homo sapiens 35-41 31409613-11 2019 In addition, BRCA1-, BRCA2-, and PALB2-deficient cells were hypersensitive to the indenoisoquinolines. indenoisoquinolines 82-101 BRCA1 DNA repair associated Homo sapiens 13-18 31409613-11 2019 In addition, BRCA1-, BRCA2-, and PALB2-deficient cells were hypersensitive to the indenoisoquinolines. indenoisoquinolines 82-101 BRCA2 DNA repair associated Homo sapiens 21-26 31409613-11 2019 In addition, BRCA1-, BRCA2-, and PALB2-deficient cells were hypersensitive to the indenoisoquinolines. indenoisoquinolines 82-101 partner and localizer of BRCA2 Homo sapiens 33-38 31409613-14 2019 CONCLUSIONS: Our results provide a rationale for molecularly designed clinical trials with the indenoisoquinolines as single agents and in combination with PARP inhibitors in HRD cancers expressing SLFN11. indenoisoquinolines 95-114 schlafen family member 11 Homo sapiens 198-204 21464033-0 2011 Induction of retinoid X receptor activity and consequent upregulation of p21WAF1/CIP1 by indenoisoquinolines in MCF7 cells. indenoisoquinolines 89-108 cyclin dependent kinase inhibitor 1A Homo sapiens 81-85 20534341-2 2010 Camptothecins and novel noncamptothecins in clinical development (indenoisoquinolines and ARC-111) target eukaryotic type IB topoisomerases (Top1), whereas human type IIA topoisomerases (Top2alpha and Top2beta) are the targets of the widely used anticancer agents etoposide, anthracyclines (doxorubicin, daunorubicin), and mitoxantrone. indenoisoquinolines 66-85 DNA topoisomerase II beta Homo sapiens 201-209 20924131-9 2010 CONCLUSIONS: Our gammaH2AX assay is sufficiently accurate and sensitive to quantify gammaH2AX in tumor samples and will be used in correlative studies of two indenoisoquinolines in a phase I clinical trial at the National Cancer Institute. indenoisoquinolines 158-177 H2A.X variant histone Mus musculus 17-26 20630766-3 2010 The SAR of these compounds overlaps with indenoisoquinolines, suggesting that they may intercalate into the Top1-DNA complex similarly. indenoisoquinolines 41-60 sarcosine dehydrogenase Homo sapiens 4-7 24900212-4 2010 Indenoisoquinolines demonstrated potent inhibition of cell growth in the GIST882 patient-derived gastrointestinal stromal tumor cell line, accompanied by inhibition of both c-Kit transcription and KIT oncoprotein levels. indenoisoquinolines 0-19 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 173-178 24900212-4 2010 Indenoisoquinolines demonstrated potent inhibition of cell growth in the GIST882 patient-derived gastrointestinal stromal tumor cell line, accompanied by inhibition of both c-Kit transcription and KIT oncoprotein levels. indenoisoquinolines 0-19 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 197-200 19383846-9 2009 The trapping of Top1 cleavage complexes by indenoisoquinolines in cells results in the rapid and sustained phosphorylation of histone H2AX (gamma-H2AX). indenoisoquinolines 43-62 H2A.X variant histone Homo sapiens 126-138