Turning off transcription of the bcl-2 gene by stabilizing the bcl-2 promoter quadruplex with quindoline derivatives.

No abstract is available for this paper.

• Publication year

  2010

• Venue

  Journal of Medicinal Chemistry

• Publication date

  2010-05-18

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1021/jm100445ePMID 20481493
• 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.

• A small molecule that disrupts G-quadruplex DNA structure and enhances gene expression.

  2009cited by this paper
• Isaindigotone derivatives: a new class of highly selective ligands for telomeric G-quadruplex DNA.

  2009cited by this paper
• A G-rich sequence within the c-kit oncogene promoter forms a parallel G-quadruplex having asymmetric G-tetrad dynamics.

  2009cited by this paper
• Spectroscopy probing of the formation, recognition, and conversion of a G-quadruplex in the promoter region of the bcl-2 oncogene.

  2009cited by this paper
• Targeting the G-quadruplex-forming region near the P1 promoter in the human BCL-2 gene with the cationic porphyrin TMPyP4 and with the complementary C-rich strand.

  2009cited by this paper
• Evidence of genome-wide G4 DNA-mediated gene expression in human cancer cells

  2009cited by this paper
• 5-N-methylated quindoline derivatives as telomeric g-quadruplex stabilizing ligands: effects of 5-N positive charge on quadruplex binding affinity and cell proliferation.

  2008cited by this paper
• Exploring the differential recognition of DNA G-quadruplex targets by small molecules using dynamic combinatorial chemistry.

  2008cited by this paper
• A novel G-quadruplex-forming GGA repeat region in the c-myb promoter is a critical regulator of promoter activity

  2008cited by this paper
• Genome-wide computational and expression analyses reveal G-quadruplex DNA motifs as conserved cis-regulatory elements in human and related species.

  2008cited by this paper
• Intramolecularly folded G-quadruplex and i-motif structures in the proximal promoter of the vascular endothelial growth factor gene

  2008cited by this paper
• The proximal promoter region of the human vascular endothelial growth factor gene has a G-quadruplex structure that can be targeted by G-quadruplex–interactive agents

  2008cited by this paper
• Characterization of the G-quadruplexes in the duplex nuclease hypersensitive element of the PDGF-A promoter and modulation of PDGF-A promoter activity by TMPyP4

  2007cited by this paper
• Formation of pseudosymmetrical G-quadruplex and i-motif structures in the proximal promoter region of the RET oncogene.

  2007cited by this paper
• Structure of an unprecedented G-quadruplex scaffold in the human c-kit promoter.

  2007cited by this paper
• Stabilization of G-quadruplex DNA and down-regulation of oncogene c-myc by quindoline derivatives.

  2007cited by this paper
• Inhibition of myc promoter and telomerase activity and induction of delayed apoptosis by SYUIQ-5, a novel G-quadruplex interactive agent in leukemia cells

  2007cited by this paper
• Deconvoluting the structural and drug-recognition complexity of the G-quadruplex-forming region upstream of the bcl-2 P1 promoter.

  2006cited by this paper
• Senescence and telomere shortening induced by novel potent G-quadruplex interactive agents, quindoline derivatives, in human cancer cell lines

  2006cited by this paper
• An intramolecular G-quadruplex structure with mixed parallel/antiparallel G-strands formed in the human BCL-2 promoter region in solution.

  2006cited by this paper
• G-quadruplex formation within the promoter of the KRAS proto-oncogene and its effect on transcription

  2006cited by this paper
• Synthesis and evaluation of quindoline derivatives as G-quadruplex inducing and stabilizing ligands and potential inhibitors of telomerase.

  2005cited by this paper
• Facilitation of a structural transition in the polypurine/polypyrimidine tract within the proximal promoter region of the human VEGF gene by the presence of potassium and G-quadruplex-interactive agents

  2005cited by this paper
• Evidence for the presence of a guanine quadruplex forming region within a polypurine tract of the hypoxia inducible factor 1alpha promoter.

  2005cited by this paper
• Telomestatin and diseleno sapphyrin bind selectively to two different forms of the human telomeric G-quadruplex structure.

  2005cited by this paper
• An inhibitor of Bcl-2 family proteins induces regression of solid tumours

  2005cited by this paper
• Design and synthesis of an expanded porphyrin that has selectivity for the c-MYC G-quadruplex structure.

  2005cited by this paper
• Overexpression of Bcl-2 is associated with apoptotic resistance to the G-quadruplex ligand 12459 but is not sufficient to confer resistance to long-term senescence

  2005cited by this paper
• A G-quadruplex-interactive agent, telomestatin (SOT-095), induces telomere shortening with apoptosis and enhances chemosensitivity in acute myeloid leukemia.

  2004cited by this paper
• Determining the folding and unfolding rate constants of nucleic acids by biosensor. Application to telomere G-quadruplex.

  2004cited by this paper
• Activation of Apoptosis in Vivo by a Hydrocarbon-Stapled BH3 Helix

  2004cited by this paper
• Biological Activity of the G-Quadruplex Ligand RHPS4 (3,11-Difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridinium methosulfate) Is Associated with Telomere Capping Alteration

  2004cited by this paper
• Stabilization of the c-myc gene promoter quadruplex by specific ligands' inhibitors of telomerase.

  2004cited by this paper
• Synthesis and evaluation of analogues of 10H-indolo[3,2-b]quinoline as G-quadruplex stabilising ligands and potential inhibitors of the enzyme telomerase.

  2004cited by this paper
• Interactions of cryptolepine and neocryptolepine with unusual DNA structures.

  2003cited by this paper
• Selective recognition of G-qQuadruplex telomeric DNA by a bis(quinacridine) macrocycle.

  2003cited by this paper
• Direct evidence for a G-quadruplex in a promoter region and its targeting with a small molecule to repress c-MYC transcription

  2002cited by this paper
• Poly(ADP-ribose) polymerase-1 cleavage during apoptosis: An update

  2002cited by this paper
• Oblimersen Bcl-2 Antisense: Facilitating Apoptosis in Anticancer Treatment

  2002cited by this paper
• Secondary DNA structures as molecular targets for cancer therapeutics.

  2001cited by this paper
• Structure-based design of selective and potent G quadruplex-mediated telomerase inhibitors

  2001cited by this paper
• Morphologic and biochemical hallmarks of apoptosis.

  2000cited by this paper
• A novel inhibitor of human telomerase derived from 10H-indolo[3,2-b]quinoline.

  2000cited by this paper
• Apoptosis in cancer.

  2000cited by this paper
• Antiapoptotic bcl-2 and bcl-xL in advanced malignant melanoma

  2000cited by this paper
• Activation of the Bcl-2 promoter by nerve growth factor is mediated by the p42/p44 MAPK cascade.

  1999cited by this paper
• Bax and Bcl-2 expressions predict response to radiotherapy in human cervical cancer

  1998cited by this paper
• Expression of Bcl-2 family of proteins in fresh myeloma cells

  1998cited by this paper
• The WT1 Protein Is a Negative Regulator of the Normalbcl-2 Allele in t(14;18) Lymphomas*

  1997cited by this paper
• Apoptosis: Bcl-2-related proteins get connected

  1997cited by this paper
• High prevalence of bcl-2 oncoprotein expression in small cell lung cancer.

  1995cited by this paper
• Apoptosis of lung cancer cells caused by some anti-cancer agents (MMC, CPT-11, ADM) is inhibited by bcl-2.

  1993cited by this paper
• Alternative promoters and exons, somatic mutation and deregulation of the Bcl‐2‐Ig fusion gene in lymphoma.

  1988cited by this paper
• RAPID, SIMULTANEOUS MEASUREMENT OF DNA, PROTEIN, AND CELL VOLUME IN SINGLE CELLS FROM LARGE MAMMALIAN CELL POPULATIONS

  1973cited by this paper

• Tetrahydroberberine Targets the bcl-2 Promoter G-Quadruplex to Trigger Mitochondrial Apoptosis and Inhibit Nasopharyngeal Carcinoma Progression.

  2026cites this paper
• Design, Synthesis and Bioactive Evaluation of Topo I/c-MYC Dual Inhibitors to Inhibit Oral Cancer via Regulating the PI3K/AKT/NF-κB Signaling Pathway

  2025cites this paper
• From unearthing to an intriguing cancer-fighting target: the human BCL-2 promoter G-quadruplex and i-motif.

  2025cites this paper
• Structure–activity relationships for the G-quadruplex-targeting experimental drug QN-302 and two analogues probed with comparative transcriptome profiling and molecular modeling

  2024cites this paper
• G-quadruplexes in cancer-related gene promoters: from identification to therapeutic targeting

  2023cites this paper
• Bioactive nutraceuticals as G4 stabilizers: potential cancer prevention and therapy—a critical review

  2023cites this paper
• Design, synthesis and bioactivity of novel naphthalimide-benzotriazole conjugates against A549 cells via targeting BCL2 G-quadruplex and inducing autophagy.

  2022cites this paper
• High-throughput techniques enable advances in the roles of DNA and RNA secondary structures in transcriptional and post-transcriptional gene regulation

  2022cites this paper
• High-affinity binding at quadruplex–duplex junctions: rather the rule than the exception

  2022cites this paper
• The Dynamic Regulation of G-Quadruplex DNA Structures by Cytosine Methylation

  2022cites this paper
• BCL2 G quadruplex-binding small molecules: current status and prospects for the development of next-generation anticancer therapeutics.

  2022cites this paper
• Synthesis, Anti-tumour Activity, and Mechanism of Benzoyl hydrazine Schiff base-copper complexes

  2022cites this paper
• Strong In Vitro And Vivo Cytotoxicity Of Two Platinum(II) Complexes With Cryptolepine Derivatives

  2021cites this paper
• Role of basic aminoalkyl chains in the lead optimization of Indoloquinoline alkaloids.

  2021cites this paper
• Rapid and practical access to diverse quindolines by catalyst-free and regioselectivity-reversed Povarov reaction

  2021cites this paper
• Quinoline anticancer agents active on DNA and DNA-interacting proteins: From classical to emerging therapeutic targets.

  2021cites this paper
• Interaction analysis of anti-cancer drug Methotrexate with bcl-2 promoter stabilization and its transcription regulation

  2021cites this paper
• Oxidative lesions modulate G-quadruplex stability and structure in the human BCL2 promoter

  2021cites this paper
• Unraveling the binding characteristics of small ligands to telomeric DNA by pressure modulation

  2021cites this paper
• Quantitative characterization of human oncogene promoter G‐quadruplex DNA‐ligand interactions using a combination of mass spectrometry and capillary electrophoresis

  2021cites this paper
• Structured Waters Mediate Small Molecule Binding to G-Quadruplex Nucleic Acids

  2021cites this paper
• Modulating gene expression in breast cancer via DNA secondary structure and the CRISPR toolbox

  2021cites this paper
• Regulation of PDGFR-β gene expression by targeting the G-vacancy bearing G-quadruplex in promoter

  2021cites this paper
• Targeting Oncogene Promoters and Ribosomal RNA Biogenesis by G-Quadruplex Binding Ligands Translate to Anticancer Activity

  2021cites this paper
• Topologies of G-quadruplex: Biological functions and regulation by ligands.

  2020cites this paper
• Ligand-Mediated G-Quadruplex Induction in a Double-Stranded DNA Context by Cyclic Imidazole/Lysine Polyamide

  2020cites this paper
• Introduction

  2020cites this paper
• Mitochondria-localizing curcumin-cryptolepine Zn(II) complexes and their antitumor activity.

  2020cites this paper
• Challenges in developing small-molecule quadruplex therapeutics

  2020cites this paper
• Click and combinatorial approaches to quadruplex ligand discovery

  2020cites this paper
• Imaging and therapeutic applications of Zn(ii)-cryptolepine-curcumin molecular probes in cell apoptosis detection and photodynamic therapy.

  2020cites this paper
• Recent Progress of Targeted G-Quadruplex-Preferred Ligands Toward Cancer Therapy

  2019cites this paper
• Non-duplex G-Quadruplex Structures Emerge as Mediators of Epigenetic Modifications.

  2019cites this paper
• Developing Novel G-Quadruplex Ligands: From Interaction with Nucleic Acids to Interfering with Nucleic Acid–Protein Interaction

  2019cites this paper
• Probing G-quadruplex topologies and recognition concurrently in real time and 3D using a dual-app nucleoside probe

  2019cites this paper
• Folding/unfolding kinetics of G-quadruplexes upstream of the P1 promoter of the human BCL-2 oncogene

  2019cites this paper
• Synthesis and in vitro antitumor activity evaluation of copper(II) complexes with 5-pyridin-2-yl-[1,3]dioxolo[4,5-g]isoquinoline derivatives.

  2019cites this paper
• Targeting multiple G-quadruplex-forming DNA sequences: Design, biophysical and biological evaluations of indolo-naphthyridine scaffold derivatives.

  2019cites this paper
• G-Quadruplex DNA and RNA

  2019cites this paper
• Regulation at the schizophrenia-associated MIR137 locus and repetitive DNA in the regulation and evolution of brain-related pathway

  2018cites this paper
• Study on the polymorphism of G-quadruplexes by reversed-phase HPLC and LC-MS.

  2018cites this paper
• Studies on interactions of carbazole derivatives with DNA, cell image, and cytotoxicity.

  2018cites this paper
• Design, Synthesis, and Evaluation of Novel p-(Methylthio)styryl Substituted Quindoline Derivatives as Neuroblastoma RAS (NRAS) Repressors via Specific Stabilizing the RNA G-Quadruplex.

  2018cites this paper
• Targeting the BCL2 Gene Promoter G‐Quadruplex with a New Class of Furopyridazinone‐Based Molecules

  2018cites this paper
• A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line.

  2018cites this paper
• A Dual-App Nucleoside Probe Provides Structural Insights into the Human Telomeric Overhang in Live Cells.

  2018cites this paper
• Whole-Transcriptome Profiling of Canine and Human in Vitro Models Exposed to a G-Quadruplex Binding Small Molecule

  2018cites this paper
• Microwave-Assisted Synthesis of Imidazo[4,5-f][1,10]phenanthroline Derivatives as Apoptosis Inducers in Chemotherapy by Stabilizing Bcl-2 G-quadruplex DNA

  2017cites this paper
• Targeting glioma stem cells in vivo by a G-quadruplex-stabilizing synthetic macrocyclic hexaoxazole

  2017cites this paper
• SVA retrotransposons as potential modulators of neuropeptide gene expression

  2017cites this paper
• Identification of G-quadruplex structures that possess transcriptional regulating functions in the Dele and Cdc6 CpG islands

  2017cites this paper
• G-Quadruplex surveillance in BCL-2 gene: a promising therapeutic intervention in cancer treatment.

  2017cites this paper
• Targeting Promoter Quadruplex Nucleic Acids for Cancer Therapy

  2017cites this paper
• Synthesis and evaluation of 7-substituted-5,6-dihydrobenzo[c]acridine derivatives as new c-KIT promoter G-quadruplex binding ligands.

  2017cites this paper
• Synthesis and antitumor mechanism of a new iron(iii) complex with 5,7-dichloro-2-methyl-8-quinolinol as ligands.

  2017cites this paper
• Specific Binding Constant and Stoichiometry Determination in Free Solution by Mass Spectrometry and Capillary Electrophoresis Frontal Analysis.

  2017cites this paper
• Emerging Role of G-quadruplex DNA as Target in Anticancer Therapy.

  2017cites this paper
• Discovery of Novel 11-Triazole Substituted Benzofuro[3,2-b]quinolone Derivatives as c-myc G-Quadruplex Specific Stabilizers via Click Chemistry.

  2017cites this paper
• Stabilization of G-quadruplex DNA and inhibition of Bcl-2 expression by a pyridostatin analog.

  2016cites this paper
• AWARD NUMBER: W81XWH-14-1-0219 TITLE: Novel Molecular Targets for kRAS Downregulation: Promoter G-Quadruplexes PRINCIPAL INVESTIGATOR: CONTRACTING ORGANIZATION:

  2016cites this paper
• Novel FeII and CoII Complexes of Natural Product Tryptanthrin: Synthesis and Binding with G-Quadruplex DNA

  2016cites this paper
• Blocking the binding of WT1 to bcl-2 promoter by G-quadruplex ligand SYUIQ-FM05

  2016cites this paper
• A New G-Quadruplex with Hairpin Loop Immediately Upstream of the Human BCL2 P1 Promoter Modulates Transcription.

  2016cites this paper
• Identification and characterization of a new G-quadruplex forming region within the kRAS promoter as a transcriptional regulator.

  2016cites this paper
• Preparation of 6/8/11-Amino/Chloro-Oxoisoaporphine and Group-10 Metal Complexes and Evaluation of Their in Vitro and in Vivo Antitumor Activity

  2016cites this paper
• Ligand‐Mediated G‐Quadruplex Induction in a Double‐Stranded DNA Context by Cyclic Imidazole/Lysine Polyamide

  2016cites this paper
• A Comparative Docking Strategy to Identify Polyphenolic Derivatives as Promising Antineoplastic Binders of G‐quadruplex DNA c‐myc and bcl‐2 Sequences

  2016cites this paper
• Quadruplex Nucleic Acids as Novel Therapeutic Targets.

  2016cites this paper
• Evaluation of the effect of iodine substitution of 8-hydroxyquinoline on its platinum(II) complex: cytotoxicity, cell apoptosis and telomerase inhibition

  2016cites this paper
• Promoter G-quadruplexes and their Interactions with Ligands and Proteins

  2016cites this paper
• DIFFERENTIAL REGULATION OF TYROSINE HYDROXYLASE TRANSCRIPTION THROUGH HIGHLY CONSERVED G- QUADRUPLEX FORMING SEQUENCE IN THE PROMOTER

  2016cites this paper
• Microwave-assisted Synthesis of Imidazole

  2016cites this paper
• Targeting G-quadruplex nucleic acids with heterocyclic alkaloids and their derivatives.

  2015cites this paper
• A G-quadruplex-binding compound showing anti-tumour activity in an in vivo model for pancreatic cancer

  2015cites this paper
• Assessment of gene promoter G‑quadruplex binding and modulation by a naphthalene diimide derivative in tumor cells.

  2015cites this paper
• Stabilization of G-quadruplex DNA, inhibition of telomerase activity, and tumor cell apoptosis by organoplatinum(II) complexes with oxoisoaporphine.

  2015cites this paper
• Fluorescence reporting of G-quadruplex structures and modulating their DNAzyme activity using polyethylenimine-pyrene conjugate.

  2015cites this paper
• Water-Soluble Ruthenium(II) Complexes with Chiral 4-(2,3-Dihydroxypropyl)-formamide Oxoaporphine (FOA): In Vitro and in Vivo Anticancer Activity by Stabilization of G-Quadruplex DNA, Inhibition of Telomerase Activity, and Induction of Tumor Cell Apoptosis.

  2015cites this paper
• Tetraphenylethene Derivatives with Different Numbers of Positively Charged Side Arms have Different Multimeric G-Quadruplex Recognition Specificity.

  2015cites this paper
• Identification of a selective G-quadruplex DNA binder using a multistep virtual screening approach.

  2015cites this paper
• Novel molecular targets for kRAS downregulation: promoter G-quadruplexes

  2015cites this paper
• Synthesis of Macrocyclic Penta- and Tetraoxazoles as G-Quadruplex Ligands

  2015cites this paper
• Novel interaction of the Z-DNA binding domain of human ADAR1 with the oncogenic c-Myc promoter G-quadruplex.

  2014cites this paper
• Systems biology brings new dimensions for structure-based drug design.

  2014cites this paper
• Nonlinear optical dye TSQ1 as an efficiently selective fluorescent probe for G-quadruplex DNA

  2014cites this paper
• Mixed-ligand ruthenium polypyridyl complexes as apoptosis inducers in cancer cells, the cellular translocation and the important role of ROS-mediated signaling.

  2014cites this paper
• Stabilization of VEGF G-quadruplex and inhibition of angiogenesis by quindoline derivatives.

  2014cites this paper
• Biophysical and functional studies of potential G-quadruplex motifs from the proximal GATA4 gene promoter

  2014cites this paper
• In the sense of transcription regulation by G-quadruplexes: asymmetric effects in sense and antisense strands.

  2014cites this paper
• Natural products and their derivatives as G-quadruplex binding ligands

  2013cites this paper
• 5-Methyl-Benzofuro[3,2-b]quinoline Derivatives as DNA Binders

  2013cites this paper
• The G-quadruplex ligand, SYUIQ-FM05, targets proto-oncogene c-kit transcription and induces apoptosis in K562 cells

  2013cites this paper
• Structure-based design of flavone derivatives as c-myc oncogene down-regulators.

  2013cites this paper
• Ruthenium (II) polypyridyl complexes stabilize the bcl-2 promoter quadruplex and induce apoptosis of Hela tumor cells

  2013influential citation
• Co-transcriptional formation of DNA:RNA hybrid G-quadruplex and potential function as constitutional cis element for transcription control

  2013cites this paper
• Novel platinum complexes as efficient G-quadruplex DNA binders and telomerase inhibitors.

  2013cites this paper
• Synthesis and binding studies of novel di-substituted phenanthroline compounds with genomic promoter and human telomeric DNA G-quadruplexes.

  2013cites this paper
• G-Quadruplex Structures in the Human Genome as Novel Therapeutic Targets

  2013cites this paper
• Guanidino anthrathiophenediones as G-quadruplex binders: uptake, intracellular localization, and anti-Harvey-Ras gene activity in bladder cancer cells.

  2013cites this paper
• Anticancer Activity of Platinum (II) Complex as G-Quadruplex DNA Binders

  2013cites this paper