Published in J Med Chem on July 03, 2003
Direct evidence for a G-quadruplex in a promoter region and its targeting with a small molecule to repress c-MYC transcription. Proc Natl Acad Sci U S A (2002) 9.60
Targeting G-quadruplexes in gene promoters: a novel anticancer strategy? Nat Rev Drug Discov (2011) 3.54
The dynamic character of the G-quadruplex element in the c-MYC promoter and modification by TMPyP4. J Am Chem Soc (2004) 3.19
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. Nucleic Acids Res (2005) 3.01
The cationic porphyrin TMPyP4 down-regulates c-MYC and human telomerase reverse transcriptase expression and inhibits tumor growth in vivo. Mol Cancer Ther (2002) 2.39
Structures, folding patterns, and functions of intramolecular DNA G-quadruplexes found in eukaryotic promoter regions. Biochimie (2008) 2.38
Evidence for the presence of a guanine quadruplex forming region within a polypurine tract of the hypoxia inducible factor 1alpha promoter. Biochemistry (2005) 2.27
NMR solution structure of the major G-quadruplex structure formed in the human BCL2 promoter region. Nucleic Acids Res (2006) 2.03
The importance of negative superhelicity in inducing the formation of G-quadruplex and i-motif structures in the c-Myc promoter: implications for drug targeting and control of gene expression. J Med Chem (2009) 2.03
Deconvoluting the structural and drug-recognition complexity of the G-quadruplex-forming region upstream of the bcl-2 P1 promoter. J Am Chem Soc (2006) 1.93
Targeting Axl and Mer kinases in cancer. Mol Cancer Ther (2011) 1.88
Telomestatin and diseleno sapphyrin bind selectively to two different forms of the human telomeric G-quadruplex structure. J Am Chem Soc (2005) 1.87
Telomestatin, a potent telomerase inhibitor that interacts quite specifically with the human telomeric intramolecular g-quadruplex. J Am Chem Soc (2002) 1.82
The role of supercoiling in transcriptional control of MYC and its importance in molecular therapeutics. Nat Rev Cancer (2009) 1.71
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. Nucleic Acids Res (2007) 1.66
Formation of pseudosymmetrical G-quadruplex and i-motif structures in the proximal promoter region of the RET oncogene. J Am Chem Soc (2007) 1.53
A novel G-quadruplex-forming GGA repeat region in the c-myb promoter is a critical regulator of promoter activity. Nucleic Acids Res (2008) 1.49
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. Mol Cancer Ther (2008) 1.44
Formation of a unique end-to-end stacked pair of G-quadruplexes in the hTERT core promoter with implications for inhibition of telomerase by G-quadruplex-interactive ligands. J Am Chem Soc (2009) 1.42
Design and synthesis of an expanded porphyrin that has selectivity for the c-MYC G-quadruplex structure. J Am Chem Soc (2005) 1.40
The c-MYC NHE III(1): function and regulation. Annu Rev Pharmacol Toxicol (2010) 1.31
Targeting MYC Expression through G-Quadruplexes. Genes Cancer (2010) 1.29
Telomerase inhibition and cell growth arrest by G-quadruplex interactive agent in multiple myeloma. Mol Cancer Ther (2003) 1.26
The different biological effects of telomestatin and TMPyP4 can be attributed to their selectivity for interaction with intramolecular or intermolecular G-quadruplex structures. Cancer Res (2003) 1.25
Telomerase inhibition and cell growth arrest after telomestatin treatment in multiple myeloma. Clin Cancer Res (2004) 1.21
Structure of the biologically relevant G-quadruplex in the c-MYC promoter. Nucleosides Nucleotides Nucleic Acids (2006) 1.21
Biophysical studies of the c-MYC NHE III1 promoter: model quadruplex interactions with a cationic porphyrin. Biophys J (2006) 1.20
NM23-H2 may play an indirect role in transcriptional activation of c-myc gene expression but does not cleave the nuclease hypersensitive element III(1). Mol Cancer Ther (2009) 1.19
Solution structure of a 2:1 quindoline-c-MYC G-quadruplex: insights into G-quadruplex-interactive small molecule drug design. J Am Chem Soc (2011) 1.17
Telomere inhibition and telomere disruption as processes for drug targeting. Annu Rev Pharmacol Toxicol (2002) 1.17
Biochemical techniques for the characterization of G-quadruplex structures: EMSA, DMS footprinting, and DNA polymerase stop assay. Methods Mol Biol (2010) 1.16
Intramolecularly folded G-quadruplex and i-motif structures in the proximal promoter of the vascular endothelial growth factor gene. Nucleic Acids Res (2008) 1.16
Specific inhibition of the Akt1 pleckstrin homology domain by D-3-deoxy-phosphatidyl-myo-inositol analogues. Mol Cancer Ther (2003) 1.14
Demonstration that drug-targeted down-regulation of MYC in non-Hodgkins lymphoma is directly mediated through the promoter G-quadruplex. J Biol Chem (2011) 1.14
Telomeres and telomerases as drug targets. Curr Opin Pharmacol (2002) 1.14
A novel EPAS1/HIF2A germline mutation in a congenital polycythemia with paraganglioma. J Mol Med (Berl) (2012) 1.13
Dietary administration of the proapoptotic vitamin E analogue alpha-tocopheryloxyacetic acid inhibits metastatic murine breast cancer. Cancer Res (2006) 1.11
The cationic porphyrin TMPyP4 destabilizes the tetraplex form of the fragile X syndrome expanded sequence d(CGG)n. Nucleic Acids Res (2003) 1.09
The C-terminus of nucleolin promotes the formation of the c-MYC G-quadruplex and inhibits c-MYC promoter activity. Biochemistry (2010) 1.07
The dynamic character of the BCL2 promoter i-motif provides a mechanism for modulation of gene expression by compounds that bind selectively to the alternative DNA hairpin structure. J Am Chem Soc (2014) 1.06
Molecular cloning of the human platelet-derived growth factor receptor beta (PDGFR-beta) promoter and drug targeting of the G-quadruplex-forming region to repress PDGFR-beta expression. Biochemistry (2010) 1.06
The i-motif in the bcl-2 P1 promoter forms an unexpectedly stable structure with a unique 8:5:7 loop folding pattern. J Am Chem Soc (2009) 1.04
Development and molecular characterization of HCT-116 cell lines resistant to the tumor promoter and multiple stress-inducer, deoxycholate. Carcinogenesis (2002) 1.02
Tertiary DNA structure in the single-stranded hTERT promoter fragment unfolds and refolds by parallel pathways via cooperative or sequential events. J Am Chem Soc (2012) 1.02
The transcriptional complex between the BCL2 i-motif and hnRNP LL is a molecular switch for control of gene expression that can be modulated by small molecules. J Am Chem Soc (2014) 1.02
The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796. Bioorg Med Chem (2010) 1.01
UA62784, a novel inhibitor of centromere protein E kinesin-like protein. Mol Cancer Ther (2009) 1.01
High-throughput virtual screening identifies novel N'-(1-phenylethylidene)-benzohydrazides as potent, specific, and reversible LSD1 inhibitors. J Med Chem (2013) 0.98
Retracted Mutations in the G-quadruplex silencer element and their relationship to c-MYC overexpression, NM23 repression, and therapeutic rescue. Proc Natl Acad Sci U S A (2004) 0.97
Orally active alpha-tocopheryloxyacetic acid suppresses tumor growth and multiplicity of spontaneous murine breast cancer. Mol Cancer Ther (2009) 0.95
S110, a 5-Aza-2'-deoxycytidine-containing dinucleotide, is an effective DNA methylation inhibitor in vivo and can reduce tumor growth. Mol Cancer Ther (2010) 0.94
The role of G-quadruplex/i-motif secondary structures as cis-acting regulatory elements. Pure Appl Chem (2010) 0.94
Use of a bacteriophage lysin to identify a novel target for antimicrobial development. PLoS One (2013) 0.93
The vitamin E analog, alpha-tocopheryloxyacetic acid enhances the anti-tumor activity of trastuzumab against HER2/neu-expressing breast cancer. BMC Cancer (2011) 0.93
Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. ACS Med Chem Lett (2011) 0.93
Synthesis of 2,6-diaryl-substituted pyridines and their antitumor activities. Eur J Med Chem (2007) 0.92
Synthetic enantiopure aziridinomitosenes: preparation, reactivity, and DNA alkylation studies. J Am Chem Soc (2003) 0.92
Comparing Aurora A and Aurora B as molecular targets for growth inhibition of pancreatic cancer cells. Mol Cancer Ther (2006) 0.91
High density peptide microarrays. In situ synthesis and applications. Mol Divers (2004) 0.90
Anticancer activity and cellular repression of c-MYC by the G-quadruplex-stabilizing 11-piperazinylquindoline is not dependent on direct targeting of the G-quadruplex in the c-MYC promoter. J Med Chem (2012) 0.89
Binding of G-quadruplex-interactive agents to distinct G-quadruplexes induces different biological effects in MiaPaCa cells. Nucleosides Nucleotides Nucleic Acids (2005) 0.89
A comprehensive strategy to combat colon cancer targeting the adenomatous polyposis coli tumor suppressor gene. Ann N Y Acad Sci (2005) 0.87
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity. J Med Chem (2009) 0.86
Molecular modeling and biophysical analysis of the c-MYC NHE-III1 silencer element. J Mol Model (2007) 0.86
Procyanidin B3, an inhibitor of histone acetyltransferase, enhances the action of antagonist for prostate cancer cells via inhibition of p300-dependent acetylation of androgen receptor. Biochem J (2011) 0.86
Synthesis of new xanthone analogues and their biological activity test--cytotoxicity, topoisomerase II inhibition, and DNA cross-linking study. Bioorg Med Chem Lett (2006) 0.86
Determination of the importance of the stereochemistry of psorospermin in topoisomerase II-induced alkylation of DNA and in vitro and in vivo biological activity. Mol Cancer Ther (2005) 0.85
I-motif structures formed in the human c-MYC promoter are highly dynamic--insights into sequence redundancy and I-motif stability. PLoS One (2010) 0.85
Licochalcone E has an antidiabetic effect. J Nutr Biochem (2011) 0.84
Molecular heterogeneity of glucose-6-phosphate dehydrogenase deficiency in Gaza Strip Palestinians. Blood Cells Mol Dis (2012) 0.84
Effects of novel chalcone derivatives on α-glucosidase, dipeptidyl peptidase-4, and adipocyte differentiation in vitro. BMB Rep (2011) 0.84
Characterization of novel diaryl oxazole-based compounds as potential agents to treat pancreatic cancer. J Pharmacol Exp Ther (2009) 0.84
Chemical genetic screen reveals a role for desmosomal adhesion in mammary branching morphogenesis. J Biol Chem (2012) 0.84
Structure of a quinobenzoxazine--G-quadruplex complex by REDOR NMR. Biochemistry (2004) 0.84
Identification of a novel inhibitor of urokinase-type plasminogen activator. Mol Cancer Ther (2007) 0.84
Identification of a lead small-molecule inhibitor of the Aurora kinases using a structure-assisted, fragment-based approach. Mol Cancer Ther (2006) 0.84
Design, synthesis, and biological evaluation of a series of fluoroquinoanthroxazines with contrasting dual mechanisms of action against topoisomerase II and G-quadruplexes. J Med Chem (2003) 0.83
A direct and nondestructive approach to determine the folding structure of the I-motif DNA secondary structure by NMR. J Am Chem Soc (2009) 0.83
Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of hydroxylated 2,4-diphenyl-6-aryl pyridines. Bioorg Med Chem (2010) 0.83
Structure-based design of novel anti-cancer agents targeting aurora kinases. Curr Med Chem Anticancer Agents (2003) 0.82
Modulating the functional contributions of c-Myc to the human endothelial cell cyclic strain response. J Vasc Res (2009) 0.82
Synthesis of 2-(thienyl-2-yl or -3-yl)-4-furyl-6-aryl pyridine derivatives and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship. Bioorg Med Chem (2010) 0.81
Design, synthesis, and antitumor evaluation of 2,4,6-triaryl pyridines containing chlorophenyl and phenolic moiety. Eur J Med Chem (2012) 0.81
2-Thienyl-4-furyl-6-aryl pyridine derivatives: synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study. Bioorg Med Chem (2009) 0.80
DNA structure: Visualizing the quadruplex. Nat Chem (2013) 0.80
DNA acting like RNA. Biochem Soc Trans (2011) 0.80
In vitro and in vivo characterization of SGI-1252, a small molecule inhibitor of JAK2. Exp Hematol (2010) 0.79
Protective effects of a chalcone derivative against Aβ-induced oxidative stress and neuronal damage. BMB Rep (2011) 0.79
Synthesis, biological evaluation, and molecular docking study of 3-(3'-heteroatom substituted-2'-hydroxy-1'-propyloxy) xanthone analogues as novel topoisomerase IIα catalytic inhibitor. Eur J Med Chem (2011) 0.79
Synthesis and investigation of dihydroxychalcones as calpain and cathepsin inhibitors. Bioorg Chem (2013) 0.78