ArticleCancer cell2014
Targeting transcriptional addictions in small cell lung cancer with a covalent CDK7 inhibitor.
Erratum issuedOpen access · bronzeAbstract read
In one paragraph
Article in Cancer cell, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 283 papers, 1 of them a synthesis that pooled it.
0numbers the graph read from it
0cells of the map it votes in
283citing papers in PubMed, 1 pooled it
13.0field-weighted citation impact, top 1% of its field
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Who cites it
283 citing papers in PubMed, 1 synthesis or guideline pooled it, 451 citations in OpenAlex.
- Efficacy and toxicity of lurbinectedin in subsequent systemic therapy of extensive-stage small cell lung cancer: a meta-analysis.BMC cancer · 2024Pooled it
- ATLANTIS: a Phase III study of lurbinectedin/doxorubicin versus topotecan or cyclophosphamide/doxorubicin/vincristine in patients with small-cell lung cancer who have failed one prior platinum-containing line.Future oncology (London, England) · 2019Trial
- Cyclins and Cyclin-Dependent Kinases: Structure, Biological Functions, and Innovative Targeting Strategies in Cancer.MedComm · 2026Review
- Targeting CDKs in the RNAPII transcription cycle.Nature reviews. Drug discovery · 2026Review
- Inhibition of RNA polymerase II-activating CDK9 and CDK12/13, but not of cell cycle relevant CDKs, induces apoptosis by downregulating the short-lived Bcl-2 proteins Mcl1 and Bfl1/A1.Cell death & disease · 2026Article
- ZNF274 constrains lineage plasticity and drives intrinsic resistance to CDK7 inhibitors in pancreatic cancer.Nature communications · 2026Article
- Cdk7 promotes neuritogenesis in cortical neurons and contributes to social behavior in mice.Cellular and molecular life sciences : CMLS · 2026Article
- Genome-Wide CRISPR/Cas9 Screening Identifies Modulators of THZ1 Response in Acute Myeloid Leukemia.Biomedicines · 2026Article
- CDK12/CDK13 inhibition disrupts transcriptional elongation and replication fork progression in glioblastoma.EMBO molecular medicine · 2026Article
- Super-enhancer-driven recruitment of C/EBPβ by SULT1B1 is implicated in metabolic dysfunction-associated steatotic liver disease progression.Clinical epigenetics · 2026Article
- Emerging Strategies to Inhibit the G1/S Transition for Cancer Therapy.Cancer research · 2026Review
- The Emerging Role of Transcription-Associated Cyclin-Dependent Kinases in Gastrointestinal Tumors.Cancers · 2026Review
- The research landscape and future of targeting super-enhancers for cancer therapy: a bibliometric analysis.Discover oncology · 2026Article
- Targeting super-enhancer-driven SKIL transcription by CDK7 inhibitor THZ1 to suppress gastric cancer progression.Journal of translational medicine · 2026Article
- Disrupting CDK9 activity suppresses triple-negative breast cancer and is enhanced by EGFR Inhibition.Cellular oncology (Dordrecht, Netherlands) · 2026Article
- CDK3 induces neuronal death and brain atrophy in Alzheimer's disease.Nature aging · 2026Article
- Unmasking biomarkers in small cell lung cancer: implication for precision oncology.Frontiers in oncology · 2026Review
- Article
- Recent advances in development of CDK7 inhibitors and their clinical trials: a narrative review.Translational cancer research · 2025Review
- Exploiting targeted degradation of cyclins and cyclin-dependent kinases for cancer therapeutics: a review.Journal of Zhejiang University. Science. B · 2025Review
223 more citing papers are in PubMed but not listed here.
Corrections and comments
- Commented on by
- Erratum issued
Authors and funding
26 authors at 8 institutions in 3 countries.
Camilla L ChristensenDepartment of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA.
Nicholas KwiatkowskiWhitehead Institute for Biomedical Research, Massachusetts Institute of Technology, Cambridge, MA 02142, USA.
Brian J AbrahamWhitehead Institute for Biomedical Research, Massachusetts Institute of Technology, Cambridge, MA 02142, USA.
Julian CarreteroDepartament de Fisiologia, Facultat de Farmacia, Universitat de Valencia, Valencia 46010, Spain.
Fatima Al-ShahrourTranslational Bioinformatics Unit, Clinical Research Programme, Spanish National Cancer Research Centre, 28029 Madrid, Spain.
Tinghu ZhangDepartment of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA.
Edmond ChipumuroDepartment of Pediatric Hematology/Oncology, Dana-Farber Cancer Institute and Children's Hospital, Boston, MA 02115, USA.
Grit S Herter-SprieDepartment of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA.
Esra A AkbayDepartment of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA.
Abigail AltabefDepartment of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA.
Jianming ZhangDepartment of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA.
Takeshi ShimamuraDepartment of Molecular Pharmacology and Therapeutics, Oncology Research Institute, Loyola University Chicago, Stritch School of Medicine, Maywood, IL 60153, USA.
Marzia CapellettiDepartment of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA.
Jakob B ReibelDepartment of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA.
Jillian D CavanaughDepartment of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA.
Peng GaoDepartment of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA.
Yan LiuDepartment of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA.
Signe R MichaelsenDepartment of Radiation Biology, The Finsen Center, Copenhagen University Hospital, 2100 Copenhagen, Denmark.
Hans S PoulsenDepartment of Radiation Biology, The Finsen Center, Copenhagen University Hospital, 2100 Copenhagen, Denmark.
Amir R ArefDepartment of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA.
David A BarbieDepartment of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA.
James E BradnerDepartment of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA.
Rani E GeorgeDepartment of Pediatric Hematology/Oncology, Dana-Farber Cancer Institute and Children's Hospital, Boston, MA 02115, USA.
Nathanael S GrayDepartment of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA.
Richard A YoungWhitehead Institute for Biomedical Research, Massachusetts Institute of Technology, Cambridge, MA 02142, USA; Department of Biology, Massachusetts Institute of Technology, Cambridge, MA 02139, USA. Electronic address: young@wi.mit.edu.
Kwok-Kin WongDepartment of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA; Belfer Institute for Applied Cancer Science, Dana-Farber Cancer Institute, Boston, MA 02115, USA. Electronic address: kwong1@partners.org.
Dana-Farber Cancer Institute · USHarvard University · USCopenhagen University Hospital · DKMassachusetts Institute of Technology · USLoyola University Chicago · USSpanish National Cancer Research Centre · ESUniversitat de València · ESWhitehead Institute for Biomedical Research · US
Funding
VIRUS PRODUCTION COREP30CA014051 · NCI · MASSACHUSETTS INSTITUTE OF TECHNOLOGY · PI MATTHEW G. VANDER HEIDEN · 1985 to 2026
$93.9MTuberous Sclerosis-Pathway and PathogenesisP01CA120964 · NCI · BRIGHAM AND WOMEN'S HOSPITAL · PI David J. Kwiatkowski · 2007 to 2026
$35.9MStructureP01CA154303 · NCI · DANA-FARBER CANCER INST · PI JANNE, PASI A · 2012 to 2021
$17.8MMUC1-C Oncoprotein Evades Immune Destruction in Non-small Cell Lung CancerR01CA166480 · NCI · DANA-FARBER CANCER INST · PI KUFE, DONALD W., WONG, KWOK KIN · 2012 to 2021
$6.3MTherapeutic strategies for specific subsets of KRAS mutant lung cancersR01CA140594 · NCI · NEW YORK UNIVERSITY SCHOOL OF MEDICINE · PI WONG, KWOK KIN · 2009 to 2017
$4.5MIn vivo analysis of EGFR mutant driven lung cancers responses to radiation therapR01CA122794 · NCI · DANA-FARBER CANCER INST · PI WONG, KWOK KIN · 2006 to 2015
$2.8MIn vivo murine models of metastasis for therapeutic testingR01CA163896 · NCI · UNIV OF NORTH CAROLINA CHAPEL HILL · PI SHARPLESS, NORMAN E, WONG, KWOK KIN · 2012 to 2016
$2.0MDevelopment and Application of Selective Covalent Cdk7 InhibitorsR01CA179483 · NCI · DANA-FARBER CANCER INST · PI GRAY, NATHANAEL SCHIANDER, MITSIADES, CONSTANTINE S. · 2014 to 2016
$1.5MNCI NIH HHS CA120964NCI NIH HHS CA122794NCI NIH HHS CA140594NCI NIH HHS CA154303NCI NIH HHS CA163896NCI NIH HHS CA166480NCI NIH HHS P01 CA120964NCI NIH HHS P01 CA154303NCI NIH HHS P30 CA014051NCI NIH HHS R01 CA122794NCI NIH HHS R01 CA140594NCI NIH HHS R01 CA163896NCI NIH HHS R01 CA166480NCI NIH HHS R01 CA179483NCI NIH HHS R01 CA179483-01A1
Abstract
Small cell lung cancer (SCLC) is an aggressive disease with high mortality, and the identification of effective pharmacological strategies to target SCLC biology represents an urgent need. Using a high-throughput cellular screen of a diverse chemical library, we observe that SCLC is sensitive to transcription-targeting drugs, in particular to THZ1, a recently identified covalent inhibitor of cyclin-dependent kinase 7. We find that expression of super-enhancer-associated transcription factor genes, including MYC family proto-oncogenes and neuroendocrine lineage-specific factors, is highly vulnerability to THZ1 treatment. We propose that downregulation of these transcription factors contributes, in part, to SCLC sensitivity to transcriptional inhibitors and that THZ1 represents a prototype drug for tailored SCLC therapy.
Indexed as
AnimalsAntineoplastic AgentsCell Line, TumorCyclin-Dependent KinasesEnzyme InhibitorsGene Expression Regulation, NeoplasticHigh-Throughput Screening AssaysHumansLung NeoplasmsMiceMolecular Sequence DataNeoplasms, ExperimentalSequence Analysis, DNASmall Cell Lung CarcinomaTranscription FactorsTranscription, GeneticAntineoplastic AgentsCyclin-Dependent KinasesEnzyme InhibitorsTranscription Factors
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.