Lurbinectedin Specifically Triggers the Degradation of Phosphorylated RNA Polymerase II and the Formation of DNA Breaks in Cancer Cells

Hoadley, 2014, Multiplatform analysis of 12 cancer types reveals molecular classification within and across tissues of origin, Cell, 158, 929, 10.1016/j.cell.2014.06.049

Dooley, 2011, Nuclear factor I/B is an oncogene in small cell lung cancer, Genes Dev, 25, 1470, 10.1101/gad.2046711

Jiang, 2009, Achaete-scute complex homologue 1 regulates tumor-initiating capacity in human small cell lung cancer, Cancer Res, 69, 845, 10.1158/0008-5472.CAN-08-2762

Osborne, 2013, NeuroD1 regulates survival and migration of neuroendocrine lung carcinomas via signaling molecules TrkB and NCAM, Proc Natl Acad Sci U S A, 110, 6524, 10.1073/pnas.1303932110

Pedersen, 2003, Transcriptional gene expression profiling of small cell lung cancer cells, Cancer Res, 63, 1943

Rudin, 2012, Comprehensive genomic analysis identifies SOX2 as a frequently amplified gene in small-cell lung cancer, Nat Genet, 44, 1111, 10.1038/ng.2405

Voortman, 2010, Array comparative genomic hybridization-based characterization of genetic alterations in pulmonary neuroendocrine tumors, Proc Natl Acad Sci U S A, 107, 13040, 10.1073/pnas.1008132107

Wang, 2015, CDK7-dependent transcriptional addiction in triple-negative breast cancer, Cell, 163, 174, 10.1016/j.cell.2015.08.063

Franco, 2015, No Driver behind the Wheel? Targeting transcription in cancer, Cell, 163, 28, 10.1016/j.cell.2015.09.013

Damsma, 2007, Mechanism of transcriptional stalling at cisplatin-damaged DNA, Nat Struct Mol Biol, 14, 1127, 10.1038/nsmb1314

Kwiatkowski, 2014, Targeting transcription regulation in cancer with a covalent CDK7 inhibitor, Nature, 511, 616, 10.1038/nature13393

Coin, 2015, Revisiting the function of CDK7 in transcription by virtue of a recently described TFIIH kinase inhibitor, Mol Cell, 59, 513, 10.1016/j.molcel.2015.08.006

Pommier, 2013, Drugging topoisomerases: Lessons and challenges, ACS Chem Biol, 8, 82, 10.1021/cb300648v

Falkenberg, 2014, Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders, Nat Rev Drug Discov, 13, 673, 10.1038/nrd4360

Navada, 2014, Clinical development of demethylating agents in hematology, J Clin Invest, 124, 40, 10.1172/JCI69739

Bueren-Calabuig, 2011, Temperature-induced melting of double-stranded DNA in the absence and presence of covalently bonded antitumour drugs: Insight from molecular dynamics simulations, Nucleic Acids Res, 39, 8248, 10.1093/nar/gkr512

Romano, 2013, Comparison of in vitro and in vivo biological effects of trabectedin, lurbinectedin (PM01183) and Zalypsis(R) (PM00104), Int J Cancer, 133, 2024, 10.1002/ijc.28213

Soares, 2011, Trabectedin and its C subunit modified analogue PM01183 attenuate nucleotide excision repair and show activity toward platinum-resistant cells, Mol Cancer Ther, 10, 1481, 10.1158/1535-7163.MCT-11-0252

Allavena, 2016, Lurbinectedin reduces tumor-associated macrophages and the production of inflammatory cytokines, chemokines, and angiogenic factors in preclinical models, AACR Annual Meeting 2016, A1284

Vidal, 2012, Lurbinectedin (PM01183), a new DNA minor groove binder, inhibits growth of orthotopic primary graft of cisplatin-resistant epithelial ovarian cancer, Clin Cancer Res, 18, 5399, 10.1158/1078-0432.CCR-12-1513

Feuerhahn, 2011, XPF-dependent DNA breaks and RNA polymerase II arrest induced by antitumor DNA interstrand crosslinking-mimetic alkaloids, Chem Biol, 18, 988, 10.1016/j.chembiol.2011.06.007

Coin, 2008, Nucleotide excision repair driven by the dissociation of CAK from TFIIH, Mol Cell, 31, 9, 10.1016/j.molcel.2008.04.024

Singh, 2015, TFIIH subunit alterations causing xeroderma pigmentosum and trichothiodystrophy specifically disturb several steps during transcription, Am J Hum Genet, 96, 194, 10.1016/j.ajhg.2014.12.012

Dubaele, 2003, Basal transcription defect discriminates between xeroderma pigmentosum and trichothiodystrophy in XPD patients, Mol Cell, 11, 1635, 10.1016/S1097-2765(03)00182-5

Ostling, 1984, Microelectrophoretic study of radiation-induced DNA damages in individual mammalian cells, Biochem Biophys Res Commun, 123, 291, 10.1016/0006-291X(84)90411-X

Zhang, 2008, Model-based analysis of ChIP-Seq (MACS), Genome Biol, 9, R137, 10.1186/gb-2008-9-9-r137

Heinz, 2010, Simple combinations of lineage-determining transcription factors prime cis-regulatory elements required for macrophage and B cell identities, Mol Cell, 38, 576, 10.1016/j.molcel.2010.05.004

Erba, 2000, Isolation and characterization of an IGROV-1 human ovarian cancer cell line made resistant to Ecteinascidin-743 (ET-743), Br J Cancer, 82, 1732

Marco, 2006, Further insight into the DNA recognition mechanism of trabectedin from the differential affinity of its demethylated analogue ecteinascidin ET729 for the triplet DNA binding site CGA, J Med Chem, 49, 6925, 10.1021/jm060640y

Yang, 2007, Inhibitors of ubiquitin-activating enzyme (E1), a new class of potential cancer therapeutics, Cancer Res, 67, 9472, 10.1158/0008-5472.CAN-07-0568

Sanso, 2013, Pause, play, repeat: CDKs push RNAP II's buttons, Transcription, 4, 146, 10.4161/trns.25146

Ju, 2006, A topoisomerase IIbeta-mediated dsDNA break required for regulated transcription, Science, 312, 1798, 10.1126/science.1127196

Dynan, 1983, The promoter-specific transcription factor Sp1 binds to upstream sequences in the SV40 early promoter, Cell, 35, 79, 10.1016/0092-8674(83)90210-6

Peltonen, 2014, A targeting modality for destruction of RNA polymerase I that possesses anticancer activity, Cancer Cell, 25, 77, 10.1016/j.ccr.2013.12.009

Compe, 2012, TFIIH: When transcription met DNA repair, Nat Rev Mol Cell Biol, 13, 343, 10.1038/nrm3350

Le May, 2012, XPG and XPF endonucleases trigger chromatin looping and DNA demethylation for accurate expression of activated genes, Mol Cell, 47, 622, 10.1016/j.molcel.2012.05.050

Hanawalt, 2008, Transcription-coupled DNA repair: Two decades of progress and surprises, Nat Rev Mol Cell Biol, 9, 958, 10.1038/nrm2549

Laine, 2006, When transcription and repair meet: A complex system, Trends Genet, 22, 430, 10.1016/j.tig.2006.06.006

McNeil, 2012, DNA repair endonuclease ERCC1-XPF as a novel therapeutic target to overcome chemoresistance in cancer therapy, Nucleic Acids Res, 40, 9990, 10.1093/nar/gks818

Haffner, 2010, Androgen-induced TOP2B-mediated double-strand breaks and prostate cancer gene rearrangements, Nat Genet, 42, 668, 10.1038/ng.613

Beaudenon, 1999, Rsp5 ubiquitin-protein ligase mediates DNA damage-induced degradation of the large subunit of RNA polymerase II in Saccharomyces cerevisiae, Mol Cell Biol, 19, 6972, 10.1128/MCB.19.10.6972

Wilson, 2013, Ubiquitylation and degradation of elongating RNA polymerase II: The last resort, Biochim Biophys Acta, 1829, 151, 10.1016/j.bbagrm.2012.08.002

Forster, 2015, Lurbinectedin (PM01183) with doxorubicin (DOX), an active treatment as second-line therapy in small cell lung cancer (SCLC), J Clin Oncol, 33, 10.1200/jco.2015.33.15_suppl.7509

Christensen, 2014, Targeting transcriptional addictions in small cell lung cancer with a covalent CDK7 inhibitor, Cancer Cell, 26, 909, 10.1016/j.ccell.2014.10.019

Osada, 2005, ASH1 gene is a specific therapeutic target for lung cancers with neuroendocrine features, Cancer Res, 65, 10680, 10.1158/0008-5472.CAN-05-1404

Poveda, 2014, Lurbinectedin (PM01183), an active compound in platinum-resistant/refractory ovarian cancer (PRROC) patients: results of a two -stage, controlled phase II study, J Clin Oncol, 32, abstr 5505, 10.1200/jco.2014.32.15_suppl.5505

Flemming, 2015, Anticancer drugs: Finding the perfect combination, Nat Rev Drug Discov, 14, 13, 10.1038/nrd4524

Koti, 2015, A distinct pre-existing inflammatory tumour microenvironment is associated with chemotherapy resistance in high-grade serous epithelial ovarian cancer, Br J Cancer, 112, 1215, 10.1038/bjc.2015.81

Mozzetti, 2012, Gli family transcription factors are drivers of patupilone resistance in ovarian cancer, Biochem Pharmacol, 84, 1409, 10.1016/j.bcp.2012.08.019

Sandberg, 2004, Updates on the cytogenetics and molecular genetics of bone and soft tissue tumors: Lipoma, Cancer Genet Cytogenet, 150, 93, 10.1016/j.cancergencyto.2003.12.018

Tomlins, 2009, ETS gene fusions in prostate cancer: from discovery to daily clinical practice, Eur Urol, 56, 275, 10.1016/j.eururo.2009.04.036