The development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity.

No abstract is available for this paper.

• Publication year

  2009

• Venue

  Cancer Research

• Publication date

  2009-08-01

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1158/0008-5472.CAN-09-0301PMID 19638587PMCID PMC2875168
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Transcriptional inhibitors, p53 and apoptoss.

  2008cited by this paper
• A unique quinolineboronic acid-based supramolecular structure that relies on double intermolecular B-N bonds for self-assembly in solid state and in solution.

  2007cited by this paper
• Gene-specific requirement for P-TEFb activity and RNA polymerase II phosphorylation within the p53 transcriptional program.

  2006cited by this paper
• ZNF366 is an estrogen receptor corepressor that acts through CtBP and histone deacetylases

  2006cited by this paper
• A phase I trial of the selective oral cyclin-dependent kinase inhibitor seliciclib (CYC202; R-Roscovitine), administered twice daily for 7 days every 21 days

  2006cited by this paper
• Extra precision glide: docking and scoring incorporating a model of hydrophobic enclosure for protein-ligand complexes.

  2006cited by this paper
• Cyclin-dependent kinase pathways as targets for cancer treatment.

  2006influential reference
• Selectivity and potency of cyclin-dependent kinase inhibitors

  2006influential reference
• CAK—Cyclin-Dependent Activating Kinase: A Key Kinase in Cell Cycle Control and a Target for Drugs?

  2005cited by this paper
• In vitro and In vivo Pharmacokinetic-Pharmacodynamic Relationships for the Trisubstituted Aminopurine Cyclin-Dependent Kinase Inhibitors Olomoucine, Bohemine and CYC202

  2005cited by this paper
• Flavopiridol: an antitumor drug with potential application in the treatment of neurodegenerative diseases.

  2005cited by this paper
• Transcription inhibition by flavopiridol: mechanism of chronic lymphocytic leukemia cell death.

  2005cited by this paper
• Secrets of a double agent: CDK7 in cell-cycle control and transcription

  2005cited by this paper
• Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.

  2005cited by this paper
• Mammalian cyclin-dependent kinases.

  2005cited by this paper
• Glide: a new approach for rapid, accurate docking and scoring. 1. Method and assessment of docking accuracy.

  2004cited by this paper
• The Use of CDK Inhibitors in Oncology: A Pharmaceutical Perspective

  2004cited by this paper
• Minireview: Cyclin D1: normal and abnormal functions.

  2004cited by this paper
• Living with or without cyclins and cyclin-dependent kinases.

  2004cited by this paper
• Transcriptional signature of flavopiridol-induced tumor cell death.

  2004influential reference
• Small-molecule cyclin-dependent kinase modulators

  2003cited by this paper
• Pharmacological inhibitors of cyclin-dependent kinases.

  2002cited by this paper
• In vitro and in vivo antitumor properties of the cyclin dependent kinase inhibitor CYC202 (R‐roscovitine)

  2002cited by this paper
• Targeted inactivation of p53 in human cells does not result in aneuploidy.

  2002cited by this paper
• Genomic-scale measurement of mRNA turnover and the mechanisms of action of the anti-cancer drug flavopiridol

  2001cited by this paper
• Inability to enter S phase and defective RNA polymerase II CTD phosphorylation in mice lacking Mat1

  2001cited by this paper
• To cycle or not to cycle: a critical decision in cancer

  2001cited by this paper
• Session 4: Molecular Oncology

  2000cited by this paper
• Activation of estrogen receptor alpha by S118 phosphorylation involves a ligand-dependent interaction with TFIIH and participation of CDK7.

  2000cited by this paper
• The role of Cdk7 in CAK function, a retro-retrospective.

  1998cited by this paper
• Cyclin-dependent kinases: engines, clocks, and microprocessors.

  1997cited by this paper
• Palladium catalyzed amination of 2-chloro-1,3-azole derivatives: Mild entry to potent H1- antihistaminic norastemizole

  1997cited by this paper
• Stimulation of RARα Activation Function AF-1 through Binding to the General Transcription Factor TFIIH and Phosphorylation by CDK7

  1997cited by this paper
• Cancer Cell Cycles

  1996cited by this paper
• Association of Cdk-activating kinase subunits with transcription factor TFIIH

  1995cited by this paper
• Potent inhibition of CDC2 kinase activity by the flavonoid L86-8275.

  1994cited by this paper
• The MO15 cell cycle kinase is associated with the TFIIH transcription-DNA repair factor.

  1994cited by this paper
• New colorimetric cytotoxicity assay for anticancer-drug screening.

  1990cited by this paper

• Transcriptome-conditioned molecule generation via gene interaction-aware fragment modeling with a GPT-based architecture

  2025cites this paper
• Structural basis of T-loop-independent recognition and activation of CDKs by the CDK-activating kinase

  2025cites this paper
• Recent advances in development of CDK7 inhibitors and their clinical trials: a narrative review

  2025cites this paper
• Resistance to CDK7 inhibitors directed by acquired mutation of a conserved residue in cancer cells

  2025cites this paper
• SAGE: A Segment-Anchor-Guided Exploration Framework for the Optimization of CDK7 Inhibitors as Promising Cancer Therapy.

  2025cites this paper
• Synthesis, Spectroscopic, Electronic and Molecular Docking Studies of Pyrazole Based Chalcones as Potential Anticancer Agents

  2025cites this paper
• Cyclin-dependent kinases as mediators of aberrant transcription in prostate cancer

  2025cites this paper
• Drug design for cyclin-dependent kinase 9 (CDK9) inhibitors in silico

  2025cites this paper
• Solid-phase synthesis and cytotoxic evaluation of novel pyridinium bromides

  2025cites this paper
• An in silico and in vitro approach for understanding CDK2 expression pattern and prognostic implications in breast cancer

  2025cites this paper
• PRR11 Promotes Bladder Cancer Growth and Metastasis by Facilitating G1/S Progression and Epithelial‐Mesenchymal Transition

  2025cites this paper
• Targeted Colon Cancer and Chemotherapeutic Through Metal Glycoconjugates: Design, Synthesis, Molecular Docking, and DFT Investigations

  2025cites this paper
• Synthesis, docking, MD simulation, ADMET, drug likeness, and DFT studies of novel furo[2,3-b]indol-3a-ol as promising Cyclin-dependent kinase 2 inhibitors

  2024cites this paper
• Ibulocydine Inhibits Migration and Invasion of TNBC Cells via MMP-9 Regulation

  2024cites this paper
• CDK2-based CDK7 mimic as a tool for structural analysis: Biochemical validation and crystal structure with SY5609.

  2024cites this paper
• Using bioinformatics and artificial intelligence to map the cyclin-dependent kinase 4/6 inhibitor biomarker landscape in breast cancer

  2024cites this paper
• Emerging roles of cyclin-dependent kinase 7 in health and diseases.

  2024cites this paper
• Cimicifugin, a broad-spectrum inhibitor of Theileria annulata and Plasmodium falciparum CDK7

  2024cites this paper
• Discovery of bivalent small molecule degraders of cyclin-dependent kinase 7 (CDK7).

  2024cites this paper
• Cell cycle machinery in oncology: A comprehensive review of therapeutic targets

  2024cites this paper
• CDK7 in breast cancer: mechanisms of action and therapeutic potential

  2024cites this paper
• Design and Synthesis of Novel Macrocyclic Derivatives as Potent and Selective Cyclin-Dependent Kinase 7 Inhibitors.

  2024cites this paper
• High-resolution cryo-EM of the human CDK-activating kinase for structure-based drug design

  2024influential citation
• Cyclin-dependent kinase 7 (CDK7) inhibitors as a novel therapeutic strategy for different molecular types of breast cancer

  2024cites this paper
• Discovery and optimization of thieno[3,2-d]pyrimidine derivatives as highly selective inhibitors of cyclin-dependent kinase 7.

  2023cites this paper
• Targeting cyclin-dependent kinases in rheumatoid arthritis and psoriasis – a review of current evidence

  2023cites this paper
• Design and synthesis of certain 7-Aryl-2-Methyl-3-Substituted Pyrazolo{1,5-a}Pyrimidines as multikinase inhibitors.

  2023cites this paper
• Enhancer in cancer pathogenesis and treatment

  2023cites this paper
• High-throughput screening identifies cell cycle-associated signaling cascades that regulate a multienzyme glucosome assembly in human cells

  2023cites this paper
• Dose escalation and expansion cohorts in patients with advanced breast cancer in a Phase I study of the CDK7-inhibitor samuraciclib

  2023cites this paper
• Transcriptional pausing induced by ionizing radiation enables the acquisition of radioresistance in nasopharyngeal carcinoma

  2023cites this paper
• Tyrosine kinase inhibitors as an alternative treatment in canine mast cell tumor

  2023cites this paper
• Anti-cancer drug molecules targeting cancer cell cycle and proliferation.

  2023cites this paper
• High-resolution cryo-electron microscopy of the human CDK-activating kinase for structure-based drug design

  2023cites this paper
• A patent review of cyclin-dependent kinase 7 (CDK7) inhibitors (2018-2022)

  2023cites this paper
• Characterization of new highly selective pyrazolo[4,3-d]pyrimidine inhibitor of CDK7

  2023cites this paper
• Inhibition of CDK7-dependent transcriptional addiction is a potential therapeutic target in synovial sarcoma.

  2022cites this paper
• Type B and type A influenza polymerases have evolved distinct binding interfaces to recruit the RNA polymerase II CTD

  2022cites this paper
• CDK7-dependent transcriptional addiction in bone and soft tissue sarcomas: Present and future.

  2022cites this paper
• Study of potent CDK7 inhibitor secondary metabolites from Tecomella undulata

  2022cites this paper
• Discovery of Potent Inhibitors of Cyclin‐Dependent Kinases 7 and 9: Design, Synthesis, Structure‐Activity Relationship Analysis and Biological Evaluation

  2022cites this paper
• Design, Synthesis, Anticancer Activity and Docking Studies of Thiazole Linked Phenylsulfone Moiety as Cyclin-Dependent Kinase 2 (CDK2) Inhibitors

  2022cites this paper
• FMR1NB Involved in Glioma Tumorigenesis Is a Promising Target for Prognosis and Therapy

  2022cites this paper
• High-content quantitative high-throughput screening identifies a cell cycle-associated signaling cascade that regulates a multienzyme metabolic assembly for glucose metabolism

  2022cites this paper
• Targeting CDK7 in oncology: The avenue forward.

  2022cites this paper
• Transcription associated cyclin-dependent kinases as therapeutic targets for prostate cancer

  2022cites this paper
• Identification of 3-(piperazinylmethyl)benzofuran derivatives as novel type II CDK2 inhibitors: design, synthesis, biological evaluation, and in silico insights

  2022cites this paper
• Three targets in one complex: A molecular perspective of TFIIH in cancer therapy.

  2021cites this paper
• CDK inhibitors in cancer therapy, an overview of recent development.

  2021cites this paper
• Targeting the transcription cycle and RNA processing in cancer treatment.

  2021cites this paper
• Efficient microwave-assisted Suzuki–Miyaura cross-coupling reaction of 3-bromo pyrazolo[1,5-a]pyrimidin-5(4H)-one: towards a new access to 3,5-diarylated 7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine derivatives

  2021cites this paper
• Cyclin-dependent kinase 7 (CDK7) is an emerging prognostic biomarker and therapeutic target in osteosarcoma

  2021cites this paper
• Enhancer rewiring in tumors: an opportunity for therapeutic intervention

  2021cites this paper
• Targeting cell-cycle machinery in cancer.

  2021cites this paper
• Inhibitors of Cyclin-Dependent Kinases: Types and Their Mechanism of Action

  2021cites this paper
• Identifying Novel Drug Targets by iDTPnd: A Case Study of Kinase Inhibitors

  2021cites this paper
• Transcriptional cyclin-dependent kinases: Potential drug targets in cancer therapy.

  2021cites this paper
• Tetracaine hydrochloride induces cell cycle arrest in melanoma by downregulating hnRNPA1.

  2021cites this paper
• Elevated pausing of RNA Polymerase II underlies acquired resistance to ionizing radiation

  2021cites this paper
• Elevated transcriptional pausing of RNA polymerase II underlies acquired resistance to radiotherapy

  2021influential citation
• Analyzing the scaffold diversity of cyclin‐dependent kinase inhibitors and revisiting the clinical and preclinical pipeline

  2021influential citation
• Identification of CDK7 Inhibitors from Natural Sources Using Pharmacoinformatics and Molecular Dynamics Simulations

  2021cites this paper
• Discovery of Potent and Selective CDK9 Degraders for Targeting Transcription Regulation in Triple-Negative Breast Cancer.

  2021cites this paper
• Development of Pyrazolopyrimidine Anti-Wolbachia Agents for the Treatment of Filariasis

  2021cites this paper
• p53–GSDME Elevation: A Path for CDK7 Inhibition to Suppress Breast Cancer Cell Survival

  2021cites this paper
• Structure-based design of highly selective 2,4,5-trisubstituted pyrimidine CDK9 inhibitors as anti-cancer agents.

  2021cites this paper
• Cyclin-dependent kinase 7 inhibitors in cancer therapy.

  2020cites this paper
• A kinase of many talents: non-neuronal functions of CDK5 in development and disease

  2020cites this paper
• CDK9 Blockade Exploits Context-dependent Transcriptional Changes to Improve Activity and Limit Toxicity of Mithramycin for Ewing Sarcoma

  2020cites this paper
• CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success?

  2020cites this paper
• Urban Health Risk and Resilience in Asian Cities

  2020cites this paper
• Tradition Meets Innovation: Herbal Medicine as a Sustainable Source of Anticancer Agents

  2020cites this paper
• Efficient Access to 3,5-Disubstituted 7-(Trifluoromethyl)pyrazolo[1,5-a]pyrimidines Involving SNAr and Suzuki Cross-Coupling Reactions

  2020cites this paper
• CDK7 inhibitors as anticancer drugs

  2020cites this paper
• P38-β/SAPK-inhibiting and apoptosis-inducing activities of (E)-4-chloro-2-((3-ethoxy-2-hydroxybenzylidene) amino)phenol

  2020cites this paper
• Therapeutic Targeting of the General RNA Polymerase II Transcription Machinery

  2020cites this paper
• Screening and analysis of bioactive food compounds for modulating the CDK2 protein for cell cycle arrest: Multi-cheminformatics approaches for anticancer therapeutics

  2020cites this paper
• Novel Oral Derivative UD-017, a Highly Selective CDK7 Inhibitor, Exhibits Anticancer Activity by Inducing Cell-Cycle Arrest and Apoptosis in Human Colorectal Cancer

  2020cites this paper
• Quantifying CDK inhibitor selectivity in live cells

  2020cites this paper
• Systematic Characterization of Recurrent Genomic Alterations in Cyclin-Dependent Kinases Reveals Potential Therapeutic Strategies for Cancer Treatment.

  2020cites this paper
• A review on kinases phosphorylating the carboxyl-terminal domain of RNA polymerase II-Biological functions and inhibitors.

  2020cites this paper
• Recent progress in development of cyclin-dependent kinase 7 inhibitors for cancer therapy

  2020cites this paper
• Novel oxindole/benzofuran hybrids as potential dual CDK2/GSK-3β inhibitors targeting breast cancer: design, synthesis, biological evaluation, and in silico studies

  2020cites this paper
• G1 Cell Cycle Arrest and Extrinsic Apoptotic Mechanisms Underlying the Anti-Leukemic Activity of CDK7 Inhibitor BS-181

  2020cites this paper
• Palladium‐Catalyzed Selective Synthesis of Dibenzo[ c , e ]azepin‐5‐ols and Benzo[ c ]pyrido[2,3‐ e ]azepin‐5‐ols

  2019cites this paper
• Recent advances in the development of cyclin-dependent kinase 7 inhibitors.

  2019cites this paper
• Ex vivo screen identifies CDK12 as a metastatic vulnerability in osteosarcoma.

  2019influential citation
• University of Dundee CDK 7 is a component of the integrated stress response regulating SNAT 2 ( SLC 38 A 2 ) / System A adaptation in response to cellular amino acid deprivation

  2019cites this paper
• Inhibition of cyclin‐dependent kinase 7 down‐regulates yes‐associated protein expression in mesothelioma cells

  2019cites this paper
• CDK9 modulates circadian clock by attenuating REV-ERBα activity.

  2019cites this paper
• Identifying Novel Targets by using Drug-binding Site Signature: A Case Study of Kinase Inhibitors

  2019cites this paper
• Comprehensive Survey of CDK Inhibitor Selectivity in Live Cells with Energy Transfer Probes

  2019cites this paper
• CDK7 is a component of the integrated stress response regulating SNAT2 (SLC38A2)/System A adaptation in response to cellular amino acid deprivation

  2019cites this paper
• Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype.

  2019cites this paper
• ABC-transporter upregulation mediates resistance to the CDK7 inhibitors THZ1 and ICEC0942

  2019cites this paper
• Evaluation of drug candidature: In silico ADMET, binding interactions with CDK7 and normal cell line studies of potentially anti-breast cancer enamidines

  2019cites this paper
• Development of a Selective CDK 7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype Graphical

  2019cites this paper
• Mechanisms of the CDK4/6 inhibitor palbociclib (PD 0332991) and its future application in cancer treatment (Review).

  2018cites this paper
• Recent advances in CDK inhibitors for cancer therapy.

  2018cites this paper
• RNA cytosine methylation and methyltransferases mediate chromatin organization and 5-azacytidine response and resistance in leukaemia

  2018cites this paper