Transcription inhibition by flavopiridol: mechanism of chronic lymphocytic leukemia cell death.

No abstract is available for this paper.

• Publication year

  2005

• Venue

  Blood

• Publication date

  2005-10-01

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.1182/BLOOD-2005-04-1678PMID 15972445PMCID PMC1895272
• 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.

• New Directions in the Diagnosis and Treatment of Chronic Lymphocytic Leukaemia

  2012cited by this paper
• Chronic lymphocytic leukemia.

  2010cited by this paper
• Flavopiridol administered using a pharmacologically derived schedule is associated with marked clinical efficacy in refractory, genetically high-risk chronic lymphocytic leukemia.

  2007cited by this paper
• In vivo measurements document the dynamic cellular kinetics of chronic lymphocytic leukemia B cells.

  2005cited by this paper
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• Cell death of bioenergetically compromised and transcriptionally challenged CLL lymphocytes by chlorinated ATP.

  2005cited by this paper
• A novel CDK inhibitor, CYC202 (R-roscovitine), overcomes the defect in p53-dependent apoptosis in B-CLL by down-regulation of genes involved in transcription regulation and survival.

  2005influential reference
• Cyclin-dependent kinase inhibitor Roscovitine induces apoptosis in chronic lymphocytic leukemia cells

  2004cited by this paper
• Characterisation of TP53 abnormalities in chronic lymphocytic leukaemia.

  2004cited by this paper
• Gene profiling and the cyclin-dependent kinase inhibitor flavopiridol: what's in a name?

  2004cited by this paper
• Small-molecule antagonists of apoptosis suppressor XIAP exhibit broad antitumor activity.

  2004cited by this paper
• Alemtuzumab is an effective therapy for chronic lymphocytic leukemia with p53 mutations and deletions.

  2004cited by this paper
• Downregulation of Bcl-2, FLIP or IAPs (XIAP and survivin) by siRNAs sensitizes resistant melanoma cells to Apo2L/TRAIL-induced apoptosis

  2004cited by this paper
• Mcl-1 is required for Akata6 B-lymphoma cell survival and is converted to a cell death molecule by efficient caspase-mediated cleavage

  2004cited by this paper
• Flavopiridol Administered as a Pharmacologically-Derived Schedule Demonstrates Marked Clinical Activity in Refractory, Genetically High Risk, Chronic Lymphocytic Leukemia (CLL).

  2004cited by this paper
• Preclinical and Clinical Development of the Cyclin-Dependent Kinase Inhibitor Flavopiridol

  2004cited by this paper
• Cleavage of Mcl-1 by caspases impaired its ability to counteract Bim-induced apoptosis

  2004cited by this paper
• Potent antileukemic interactions between flavopiridol and TRAIL/Apo2L involve flavopiridol-mediated XIAP downregulation

  2004cited by this paper
• Elongation by RNA polymerase II: the short and long of it.

  2004cited by this paper
• The crystal structure of human CDK7 and its protein recognition properties.

  2004cited by this paper
• RNA-directed actions of 8-chloro-adenosine in multiple myeloma cells.

  2003cited by this paper
• Regulation and targeting of antiapoptotic XIAP in acute myeloid leukemia

  2003cited by this paper
• Investigating RNA polymerase II carboxyl-terminal domain (CTD) phosphorylation.

  2003influential reference
• Clinical Pharmacology of Flavopiridol following a 72-Hour Continuous Infusion

  2003cited by this paper
• Addiction to Oncogenes--the Achilles Heal of Cancer

  2002cited by this paper
• Role of cyclinT/Cdk9 complex in basal and regulated transcription (review).

  2002cited by this paper
• The cyclin-dependent kinase inhibitor flavopiridol induces apoptosis in multiple myeloma cells through transcriptional repression and down-regulation of Mcl-1.

  2002cited by this paper
• Phase I clinical and pharmacokinetic trial of the cyclin-dependent kinase inhibitor flavopiridol

  2002cited by this paper
• Cancer genome targets: RAF-ing up tumor cells to overcome oncogene addiction

  2002cited by this paper
• Phase I clinical and pharmacokinetic study of flavopiridol administered as a daily 1-hour infusion in patients with advanced neoplasms.

  2002cited by this paper
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  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
• Flavopiridol Inactivates P-TEFb and Blocks Most RNA Polymerase II Transcription in Vivo *

  2001cited by this paper
• Mechanisms of action of flavopiridol.

  2001cited by this paper
• Flavopiridol circumvents Bcl‐2 family mediated inhibition of apoptosis and drug resistance in B‐cell chronic lymphocytic leukaemia

  2001cited by this paper
• Protein kinase inhibitors flavopiridol and 7-hydroxy-staurosporine down-regulate antiapoptosis proteins in B-cell chronic lymphocytic leukemia.

  2000cited by this paper
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  2000cited by this paper
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  2000cited by this paper
• Inhibition of RNA transcription: a biochemical mechanism of action against chronic lymphocytic leukemia cells by fludarabine

  2000cited by this paper
• A conserved AU‐rich element in the 3’ untranslated region of bcl‐2 mRNA is endowed with a destabilizing function that is involved in bcl‐2 down‐regulation during apoptosis

  2000cited by this paper
• Antisense‐mediated suppression of Bcl‐2 highlights its pivotal role in failed apoptosis in B‐cell chronic lymphocytic leukaemia

  1999cited by this paper
• Expression of apoptosis-regulating proteins in chronic lymphocytic leukemia: correlations with In vitro and In vivo chemoresponses.

  1998cited by this paper
• Phase I trial of continuous infusion flavopiridol, a novel cyclin-dependent kinase inhibitor, in patients with refractory neoplasms.

  1998cited by this paper
• An update on European randomized studies in non-small cell lung cancer.

  1998cited by this paper
• Flavopiridol induces apoptosis in chronic lymphocytic leukemia cells via activation of caspase-3 without evidence of bcl-2 modulation or dependence on functional p53.

  1998cited by this paper
• Molecular biology of chronic lymphocytic leukemia.

  1998cited by this paper
• Control of RNA Polymerase II Elongation Potential by a Novel Carboxyl-terminal Domain Kinase*

  1996cited by this paper
• PEST sequences and regulation by proteolysis.

  1996cited by this paper
• bcl-2 protein downregulation is not required for differentiation of multidrug resistant HL60 leukemia cells.

  1996cited by this paper
• AU-rich elements: characterization and importance in mRNA degradation.

  1995cited by this paper
• The intracellular distribution and pattern of expression of Mcl-1 overlap with, but are not identical to, those of Bcl-2

  1995cited by this paper
• mRNA decay mediated by two distinct AU-rich elements from c-fos and granulocyte-macrophage colony-stimulating factor transcripts: different deadenylation kinetics and uncoupling from translation

  1995cited by this paper
• A novel cyclin associates with M015/CDK7 to form the CDK-activating kinase

  1994cited by this paper
• Developmental regulation of the Bcl‐2 protein and susceptibility to cell death in B lymphocytes.

  1994cited by this paper
• Regulation of bcl-2 proto-oncogene expression during normal human lymphocyte proliferation.

  1987cited by this paper
• Amino acid sequences common to rapidly degraded proteins: the PEST hypothesis.

  1986cited by this paper

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  2026cites this paper
• Flavopiridol induces cell cycle arrest and apoptosis by interfering with CDK1 signaling pathway in human ovarian granulosa cells

  2024cites this paper
• Flavopiridol inhibits oocyte maturation, reduces oocyte quality and blocks cumulus cell function.

  2024cites this paper
• Flavopiridol: a promising cyclin-dependent kinase inhibitor in cancer treatment

  2024influential citation
• Potent inhibitors targeting cyclin-dependent kinase 9 discovered via virtual high-throughput screening and absolute binding free energy calculations.

  2024cites this paper
• Spectroscopic, molecular structure electronic topology surface and pharmaceutical investigation of 1-[(4-Chlorophenyl) methyl]-1H-indole-3-carboxaldehyde by quantum computation- Prediction of antitumor activity

  2024cites this paper
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  2024cites this paper
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  2023cites this paper
• Cyclin-dependent kinase-9 in B-cell malignancies: pathogenic role and therapeutic implications

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• Targeting CDK9 with selective inhibitors or degraders in tumor therapy: an overview of recent developments

  2023cites this paper
• Single cell transcriptomic analysis of the immune cell compartment in the human small intestine and in Celiac disease

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• CDK9 inhibitors in cancer research.

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  2022cites this paper
• Molecular insights on selective and specific inhibitors of Cyclin Dependent Kinase 9 enzyme (CDK9) for the purpose of cancer therapy.

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• Nuclear oligo hashing improves differential analysis of single-cell RNA-seq

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

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• Cyclin-dependent kinase inhibitor fadraciclib (CYC065) depletes anti-apoptotic protein and synergizes with venetoclax in primary chronic lymphocytic leukemia cells

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  2022cites this paper
• Mechanisms of Resistance to BCL2 Inhibitor Therapy in Chronic Lymphocytic Leukaemia and Potential Future Therapeutic Directions.

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• CDK9 inhibitors in multiple myeloma: a review of progress and perspectives

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• Vir2Drug: a drug repurposing framework based on protein similarities between pathogens

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• Targeting Mcl-1 by AMG-176 During Ibrutinib and Venetoclax Therapy in Chronic Lymphocytic Leukemia

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

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• The multi-kinase inhibitor TG02 induces apoptosis and blocks B-cell receptor signaling in chronic lymphocytic leukemia through dual mechanisms of action

  2021cites this paper
• Development and characterization of a novel flavopiridol formulation for treatment of acute myeloid leukemia.

  2021cites this paper
• CDK9 keeps RNA polymerase II on track

  2021cites this paper
• New Targetable Pathways in Chronic Lymphocytic Leukemia (CLL)

  2021cites this paper
• Targeting the p53 Pathway in CLL: State of the Art and Future Perspectives

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• Inhibitors, PROTACs and Molecular Glues as Diverse Therapeutic Modalities to Target Cyclin-Dependent Kinase

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• CDK9: A Comprehensive Review of Its Biology, and Its Role as a Potential Target for Anti-Cancer Agents

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• Selective CDK9 degradation using a proteolysis-targeting chimera (PROTAC) strategy.

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• Balancing Properties with Carboxylates: A Lead Optimization Campaign for Selective and Orally Active CDK9 Inhibitors.

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• Small-molecule inhibitors of breast cancer-related targets: Potential therapeutic agents for breast cancer.

  2020cites this paper
• MCL-1 inhibitors, fast-lane development of a new class of anti-cancer agents

  2020cites this paper
• Enhancing venetoclax activity in hematological malignancies

  2020cites this paper
• Discovery of coumarin derivatives as potent and selective cyclin-dependent kinase 9 (CDK9) inhibitors with high antitumour activity.

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  2020cites this paper
• Targeting MCL-1 in hematologic malignancies: Rationale and progress.

  2020cites this paper
• Cell Death Pathways in Lymphoid Malignancies

  2020cites this paper
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  2020cites this paper
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• Design and pharmaceutical applications of proteolysis-targeting chimeric molecules.

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  2020cites this paper
• AMG-176, an Mcl-1 Antagonist, Shows Preclinical Efficacy in Chronic Lymphocytic Leukemia

  2020cites this paper
• CDK7 inhibitors as anticancer drugs

  2020cites this paper
• Myeloid cell leukemia-1 dependence in acute myeloid leukemia: a novel approach to patient therapy

  2019cites this paper
• Creating novel translation inhibitors to target pro-survival proteins in chronic lymphocytic leukemia

  2019cites this paper
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  2019cites this paper
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  2019cites this paper
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  2019cites this paper
• Cyclin-Dependent Kinase-9 Is a Therapeutic Target in MYC-Expressing Diffuse Large B-Cell Lymphoma

  2019cites this paper
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  2019cites this paper
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  2019cites this paper
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  2018cites this paper
• Targeting oncogenic Myc as a strategy for cancer treatment

  2018cites this paper
• Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor.

  2018cites this paper
• Cytotoxicity and Apoptosis Induction by Coumarins in CLL

  2018cites this paper
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  2018influential citation
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  2018cites this paper
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  2018cites this paper
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  2018cites this paper
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  2018cites this paper
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  2018cites this paper
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  2018cites this paper
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  2018cites this paper
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  2017cites this paper
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  2017cites this paper
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  2017cites this paper
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  2017cites this paper
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  2017cites this paper
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  2017cites this paper
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  2017cites this paper
• Pallis, Monica and Burrows, Francis and Whittall, Abigail and Boddy, Nicholas and Seedhouse, Claire and Russell, Nigel (2013) Efficacy of RNA polymerase II inhibitors in targeting dormant leukaemia

  2017influential citation
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  2017cites this paper
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  2017cites this paper
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  2017cites this paper
• Qazzaz, Mohannad E. and Raja, Vijay J. and Lim, Kuan- Hon and Kam, Toh-Seok and Lee, Jong Bong and Gershkovich, Pavel and Bradshaw, Tracey D. (2016) In vitro anticancer properties and biological evaluation of novel natural alkaloid jerantinine

  2017cites this paper
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  2016cites this paper
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  2016cites this paper
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  2016cites this paper
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  2016cites this paper
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  2016cites this paper
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  2016cites this paper
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  2016cites this paper
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  2016cites this paper
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  2016cites this paper
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  2016cites this paper
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  2016cites this paper
• Recent progress of cyclin-dependent kinase inhibitors as potential anticancer agents.

  2016cites this paper
• Chronic Lymphocytic Leukemia: Exploiting Vulnerabilities with Targeted Agents

  2016cites this paper
• Potential Use of Flavopiridol in Treatment of Chronic Diseases.

  2016cites this paper