Crystal structure of the major quadruplex formed in the promoter region of the human c-MYC oncogene

Stump, Sascha; Mou, Tung-Chung; Sprang, Stephen R.; Natale, Nicholas R.; Beall, Howard D.

doi:10.1371/journal.pone.0205584

Title: Crystal structure of the major quadruplex formed in the promoter region of the human c-MYC oncogene

Abstract

The c-MYC oncogene mediates multiple tumor cell survival pathways and is dysregulated or overexpressed in the majority of human cancers. The NHE III₁ region of the c-MYC promoter forms a DNA quadruplex. Stabilization of this structure with small molecules has been shown to reduce expression of c-MYC, and targeting the c-MYC quadruplex has become an emerging strategy for development of antitumor compounds. Previous solution NMR studies of the c-MYC quadruplex have assigned the major conformer and topology of this important target, however, regions outside the G-quartet core were not as well-defined. Here, we report a high-resolution crystal structure (2.35 Å) of the major quadruplex formed in the NHE III₁ region of the c-MYC promoter. The crystal structure is in general agreement with the solution NMR structure, however, key differences are observed in the position of nucleotides outside the G-quartet core. The crystal structure provides an alternative model that, along with comparisons to other reported quadruplex crystal structures, will be important to the rational design of selective compounds. This work will aid in development of ligands to target the c-MYC promoter quadruplex with the goal of creating novel anticancer therapies.

Authors:

Stump, Sascha ^[1]; Mou, Tung-Chung ^[1]; Sprang, Stephen R. ^[1];

^[1];

^[1]

Univ. of Montana, Missoula, MT (United States)

Publication Date:: Fri Oct 12 00:00:00 EDT 2018

Research Org.:: SLAC National Accelerator Laboratory (SLAC), Menlo Park, CA (United States)

Sponsoring Org.:: USDOE Office of Science (SC), Basic Energy Sciences (BES)

OSTI Identifier:: 1627869

Grant/Contract Number:: AC02-76SF00515

Resource Type:: Accepted Manuscript

Journal Name:: PLoS ONE

Additional Journal Information:: Journal Volume: 13; Journal Issue: 10; Journal ID: ISSN 1932-6203

Publisher:: Public Library of Science

Country of Publication:: United States

Language:: English

Subject:: 59 BASIC BIOLOGICAL SCIENCES; 60 APPLIED LIFE SCIENCES; 37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY; Crystal structure; Potassium; Nucleotides; Guanine; Crystallization; Small molecules; Oncogenes; Oligonucleotides

Citation Formats


                    Stump, Sascha, Mou, Tung-Chung, Sprang, Stephen R., Natale, Nicholas R., and Beall, Howard D. Crystal structure of the major quadruplex formed in the promoter region of the human c-MYC oncogene.  United States: N. p., 2018. 
Web.  doi:10.1371/journal.pone.0205584.

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                    Stump, Sascha, Mou, Tung-Chung, Sprang, Stephen R., Natale, Nicholas R., & Beall, Howard D. Crystal structure of the major quadruplex formed in the promoter region of the human c-MYC oncogene.  United States.  https://doi.org/10.1371/journal.pone.0205584

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                    Stump, Sascha, Mou, Tung-Chung, Sprang, Stephen R., Natale, Nicholas R., and Beall, Howard D. Fri .  
"Crystal structure of the major quadruplex formed in the promoter region of the human c-MYC oncogene".  United States.  https://doi.org/10.1371/journal.pone.0205584.  https://www.osti.gov/servlets/purl/1627869.

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@article{osti_1627869,

  title        = {Crystal structure of the major quadruplex formed in the promoter region of the human c-MYC oncogene},

  author       = {Stump, Sascha and Mou, Tung-Chung and Sprang, Stephen R. and Natale, Nicholas R. and Beall, Howard D.},

  abstractNote = {The c-MYC oncogene mediates multiple tumor cell survival pathways and is dysregulated or overexpressed in the majority of human cancers. The NHE III1 region of the c-MYC promoter forms a DNA quadruplex. Stabilization of this structure with small molecules has been shown to reduce expression of c-MYC, and targeting the c-MYC quadruplex has become an emerging strategy for development of antitumor compounds. Previous solution NMR studies of the c-MYC quadruplex have assigned the major conformer and topology of this important target, however, regions outside the G-quartet core were not as well-defined. Here, we report a high-resolution crystal structure (2.35 Å) of the major quadruplex formed in the NHE III1 region of the c-MYC promoter. The crystal structure is in general agreement with the solution NMR structure, however, key differences are observed in the position of nucleotides outside the G-quartet core. The crystal structure provides an alternative model that, along with comparisons to other reported quadruplex crystal structures, will be important to the rational design of selective compounds. This work will aid in development of ligands to target the c-MYC promoter quadruplex with the goal of creating novel anticancer therapies.},

  doi          = {10.1371/journal.pone.0205584},

  journal      = {PLoS ONE},

  number       = 10,

  volume       = 13,

  place        = {United States},

  year         = {Fri Oct 12 00:00:00 EDT 2018},

  month        = {Fri Oct 12 00:00:00 EDT 2018}

}

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Figures / Tables:

Fig 1: Topology of the c-MYC promoter quadruplex. Diagram showing fully parallel topology of the c-MYC promoter quadruplex crystal structure with all reversal loops continuing in the right to left direction (5’ to 3’). Thymines are represented in yellow, adenines in blue, and guanines in green. Sequence modifications in Pu22more »

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Agrawal, Prashansa; Lin, Clement; Mathad, Raveendra I.
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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
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Sun, Daekyu; Hurley, Laurence H.
Journal of Medicinal Chemistry, Vol. 52, Issue 9
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Parkinson, Gary N.; Lee, Michael P. H.; Neidle, Stephen
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Structure of the Biologically Relevant G-Quadruplex in The c-MYC Promoter
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Sun, D.
Nucleic Acids Research, Vol. 33, Issue 18
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Structure of two intramolecular G-quadruplexes formed by natural human telomere sequences in K + solution †
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Phan, Anh Tuân; Kuryavyi, Vitaly; Luu, Kim Ngoc
Nucleic Acids Research, Vol. 35, Issue 19
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A non-canonical DNA structure is a binding motif for the transcription factor SP1 in vitro
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Raiber, Eun-Ang; Kranaster, Ramon; Lam, Enid
Nucleic Acids Research, Vol. 40, Issue 4
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Wei, D.; Parkinson, G. N.; Reszka, A. P.
Nucleic Acids Research, Vol. 40, Issue 10
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Flexibility and structural conservation in a c-KIT G-quadruplex
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Wei, Dengguo; Husby, Jarmila; Neidle, Stephen
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Metal Cations in G-Quadruplex Folding and Stability
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Bhattacharyya, Debmalya; Mirihana Arachchilage, Gayan; Basu, Soumitra
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Carabet, Lavinia A.; Rennie, Paul S.; Cherkasov, Artem
Multidisciplinary Digital Publishing Institute
DOI: 10.14288/1.0379338

Solution Structure of a MYC Promoter G-Quadruplex with 1:6:1 Loop Length
journal, February 2019

Dickerhoff, Jonathan; Onel, Buket; Chen, Luying
ACS Omega, Vol. 4, Issue 2
DOI: 10.1021/acsomega.8b03580

Therapeutic Inhibition of Myc in Cancer. Structural Bases and Computer-Aided Drug Discovery Approaches
text, January 2019

Carabet, Lavinia A.; Rennie, Paul S.; Cherkasov, Artem
Multidisciplinary Digital Publishing Institute
DOI: 10.14288/1.0379338

Evaluation of an Analogue of the Marine ε-PLL Peptide as a Ligand of G-quadruplex DNA Structures
journal, January 2020

Marzano, Maria; Falanga, Andrea Patrizia; Marasco, Daniela
Marine Drugs, Vol. 18, Issue 1
DOI: 10.3390/md18010049

Developing Novel G-Quadruplex Ligands: from Interaction with Nucleic Acids to Interfering with Nucleic Acid–Protein Interaction
journal, January 2019

Sun, Zhi-Yin; Wang, Xiao-Na; Cheng, Sui-Qi
Molecules, Vol. 24, Issue 3
DOI: 10.3390/molecules24030396

Figures / Tables found in this record:

Figures/Tables have been extracted from DOE-funded journal article accepted manuscripts.

Similar Records in DOE PAGES and OSTI.GOV collections:

NM23-H2 may play an indirect role in transcriptional activation of c-myc gene expression but does not cleave the nuclease hypersensitive element III[subscript 1]

Journal Article Dexheimer, Thomas S ; Carey, Steven S ; Zuohe, Song ; ... - Mol. Cancer Ther.

The formation of G-quadruplex structures within the nuclease hypersensitive element (NHE) III{sub 1} region of the c-myc promoter and the ability of these structures to repress c-myc transcription have been well established. However, just how these extremely stable DNA secondary structures are transformed to activate c-myc transcription is still unknown. NM23-H2/nucleoside diphosphate kinase B has been recognized as an activator of c-myc transcription via interactions with the NHE III{sub 1} region of the c-myc gene promoter. Through the use of RNA interference, we confirmed the transcriptional regulatory role of NM23-H2. In addition, we find that further purification of NM23-H2 resultsmore »« less
https://doi.org/10.1158/1535-7163.MCT-08-1093
Constitutive CCND1/CDK2 Activity Substitutes for p53 Loss, or MYC or Oncogenic RAS Expression in the Transformation of Human Mammary Epithelial Cells

Journal Article Junk, Damian J. ; Cipriano, Rocky ; Stampfer, Martha ; ... - PLoS ONE

Cancer develops following the accumulation of genetic and epigenetic alterations that inactivate tumor suppressor genes and activate proto-oncogenes. Dysregulated cyclin-dependent kinase (CDK) activity has oncogenic potential in breast cancer due to its ability to inactivate key tumor suppressor networks and drive aberrant proliferation. Accumulation or overexpression of cyclin D1 (CCND1) occurs in a majority of breast cancers and over-expression of CCND1 leads to accumulation of activated CCND1/CDK2 complexes in breast cancer cells. We describe here the role of constitutively active CCND1/CDK2 complexes in human mammary epithelial cell (HMEC) transformation. A genetically-defined, stepwise HMEC transformation model was generated by inhibiting p16more »« less
https://doi.org/10.1371/journal.pone.0053776

Full Text Available
Enforced expression of the c-myc oncogene inhibits cell differentiation by precluding entry into a distinct predifferentiation state in G/sub 0//G/sub 1/

Journal Article Freytag, S O - Mol. Cell. Biol.; (United States)

A broad base of data has implicated a role for the c-myc proto-oncogene in the control of the cell cycle and cell differentiation. To further define the role of myc in these processes, the authors examined the effect of enforced myc expression on several events that are thought to be important steps leading to the terminally differentiated state: (i) the ability to arrest growth in G/sub 0//G/sub 1/, (ii) the ability to replicate the genome upon initiation of the differentiation program, and (iii) the ability to loose responsiveness to mitogens and withdraw from the cell cycle. 3T3-L1 preadipocyte cell linesmore »« less
https://doi.org/10.1128/MCB.8.4.1614
Biophysical and X-ray structural studies of the (GGGTT)3GGG G-quadruplex in complex with N-methyl mesoporphyrin IX

Journal Article Lin, Linda Yingqi ; McCarthy, Sawyer ; Powell, Barrett M. ; ... - PLoS ONE

The G-quadruplex (GQ) is a well-studied non-canonical DNA structure formed by G-rich sequences found at telomeres and gene promoters. Biological studies suggest that GQs may play roles in regulating gene expression, DNA replication, and DNA repair. Small molecule ligands were shown to alter GQ structure and stability and thereby serve as novel therapies, particularly against cancer. In this work, we investigate the interaction of a G-rich sequence, 5’-GGGTTGGGTTGGGTTGGG-3’ (T1), with a water-soluble porphyrin, N- methyl mesoporphyrin IX (NMM) via biophysical and X-ray crystallographic studies. UV-vis and fluorescence titrations, as well as a Job plot, revealed a 1:1 binding stoichiometry withmore »« less
https://doi.org/10.1371/journal.pone.0241513
Crystallization and Characterization of the Thallium Form of the Oxytricha Nova G-Quadruplex

Journal Article Gill, M ; Strobel, S ; Loria, J - Nucleic Acids Research

The crystal structure of the Tl{sup +} form of the G-quadruplex formed from the Oxytricha nova telomere sequence, d(G{sub 4}T{sub 4}G{sub 4}), has been solved to 1.55 {angstrom}. This G-quadruplex contains five Tl{sup +} ions, three of which are interspersed between adjacent G-quartet planes and one in each of the two thymine loops. The structure displays a high degree of similarity to the K{sup +} crystal structure [Haider et al. (2002), J. Mol. Biol., 320, 189-200], including the number and location of the monovalent cation binding sites. The highly isomorphic nature of the two structures, which contain such a largemore »« less
https://doi.org/10.1093/nar/gkl616

Similar Records

Title: Crystal structure of the major quadruplex formed in the promoter region of the human c-MYC oncogene

Abstract

Citation Formats

Figures / Tables:

Putative DNA Quadruplex Formation within the Human c-kit Oncogene journal, August 2005

Linking Crystallographic Model and Data Quality journal, May 2012

Flexibility and structural conservation in a c-KIT G-quadruplex journal, December 2014

Structural basis of G-quadruplex unfolding by the DEAH/RHA helicase DHX36 journal, June 2018

Solution Structure of a 2:1 Quindoline–c-MYC G-Quadruplex: Insights into G-Quadruplex-Interactive Small Molecule Drug Design journal, November 2011

PHENIX: a comprehensive Python-based system for macromolecular structure solution. text, January 2010

Crystallographic studies of quadruplex nucleic acids journal, December 2007

The Protein Data Bank journal, May 2002

Crystal structure of a c-kit promoter quadruplex reveals the structural role of metal ions and water molecules in maintaining loop conformation journal, January 2012

Structure of the Biologically Relevant G-Quadruplex in The c-MYC Promoter journal, September 2006

Structure of the Human Telomere in K + Solution: An Intramolecular (3 + 1) G-Quadruplex Scaffold journal, August 2006

Deconvoluting the Structural and Drug-Recognition Complexity of the G-Quadruplex-Forming Region Upstream of the bcl-2 P1 Promoter journal, April 2006

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 journal, October 2005

Targeting G-quadruplexes in gene promoters: a novel anticancer strategy? journal, April 2011

Structure of an Unprecedented G-Quadruplex Scaffold in the Human c-kit Promoter journal, April 2007

Metal Cations in G-Quadruplex Folding and Stability journal, September 2016

The Major G-Quadruplex Formed in the Human BCL-2 Proximal Promoter Adopts a Parallel Structure with a 13-nt Loop in K + Solution journal, January 2014

The role of supercoiling in transcriptional control of MYC and its importance in molecular therapeutics journal, November 2009

Quadruplex nucleic acids as targets for anticancer therapeutics journal, May 2017

XDS journal, January 2010

Human Telomeric DNA Forms Parallel-Stranded Intramolecular G-Quadruplex in K + Solution under Molecular Crowding Condition journal, September 2007

Evidence for the Presence of a Guanine Quadruplex Forming Region within a Polypurine Tract of the Hypoxia Inducible Factor 1α Promoter † journal, December 2005

Crystal structure of parallel quadruplexes from human telomeric DNA journal, May 2002

Structure of two intramolecular G-quadruplexes formed by natural human telomere sequences in K + solution † journal, September 2007

Quadruplex DNA: sequence, topology and structure journal, September 2006

PARP1 exhibits enhanced association and catalytic efficiency with γH2A.X-nucleosome journal, December 2019

Optimized End-Stacking Provides Specificity of N -Methyl Mesoporphyrin IX for Human Telomeric G-Quadruplex DNA journal, December 2012

Solution structure of the human telomeric repeat d[AG3(T2AG3)3] G-tetraplex journal, December 1993

Cavin1 intrinsically disordered domains are essential for fuzzy electrostatic interactions and caveola formation journal, February 2021

Demonstration that Drug-targeted Down-regulation of MYC in Non-Hodgkins Lymphoma Is Directly Mediated through the Promoter G-quadruplex journal, September 2011

Features and development of Coot journal, March 2010

Solution Structure of the Biologically Relevant G-Quadruplex Element in the Human c-MYC Promoter. Implications for G-Quadruplex Stabilization † journal, February 2005

PHENIX: a comprehensive Python-based system for macromolecular structure solution journal, January 2010

Design, synthesis and biological evaluation of a novel class of anticancer agents: Anthracenylisoxazole lexitropsin conjugates journal, February 2009

Propeller-Type Parallel-Stranded G-Quadruplexes in the Human c-myc Promoter journal, July 2004

Structural basis of G-quadruplex unfolding by the DEAH/RHA helicase DHX36. text, January 2018

Stabilization of G-Quadruplex DNA and Down-Regulation of Oncogene c - myc by Quindoline Derivatives journal, April 2007

Direct evidence for a G-quadruplex in a promoter region and its targeting with a small molecule to repress c-MYC transcription journal, August 2002

A Conserved Quadruplex Motif Located in a Transcription Activation Site of the Human c-kit Oncogene journal, June 2006

Structure of Human Telomeric DNA in Crowded Solution journal, June 2011

The Protein Data Bank journal, January 2000

A non-canonical DNA structure is a binding motif for the transcription factor SP1 in vitro journal, October 2011

MYC on the Path to Cancer journal, March 2012

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 journal, May 2009

AIMing towards improved antitumor efficacy journal, April 2015

Circular dichroism of quadruplex DNAs: Applications to structure, cation effects and ligand binding journal, December 2007

Mechanistic studies on the anticancer activity of 2,4-disubstituted quinazoline derivative journal, October 2014

Design, synthesis and biological evaluation of a novel class of anticancer agents: Anthracenylisoxazole lexitropsin conjugates journal, February 2009

AIMing towards improved antitumor efficacy journal, April 2015

MYC on the Path to Cancer journal, March 2012

Circular dichroism of quadruplex DNAs: Applications to structure, cation effects and ligand binding journal, December 2007

Crystallographic studies of quadruplex nucleic acids journal, December 2007

Discovery of a New Four-Leaf Clover-Like Ligand as a Potent c-MYC Transcription Inhibitor Specifically Targeting the Promoter G-Quadruplex journal, February 2018

Evidence for the Presence of a Guanine Quadruplex Forming Region within a Polypurine Tract of the Hypoxia Inducible Factor 1α Promoter † journal, December 2005

A Conserved Quadruplex Motif Located in a Transcription Activation Site of the Human c-kit Oncogene journal, June 2006

Putative DNA Quadruplex Formation within the Human c-kit Oncogene journal, August 2005

Deconvoluting the Structural and Drug-Recognition Complexity of the G-Quadruplex-Forming Region Upstream of the bcl-2 P1 Promoter journal, April 2006

Structure of the Human Telomere in K + Solution: An Intramolecular (3 + 1) G-Quadruplex Scaffold journal, August 2006

Structure of an Unprecedented G-Quadruplex Scaffold in the Human c-kit Promoter journal, April 2007

Human Telomeric DNA Forms Parallel-Stranded Intramolecular G-Quadruplex in K + Solution under Molecular Crowding Condition journal, September 2007

Structure of Human Telomeric DNA in Crowded Solution journal, June 2011

Solution Structure of a 2:1 Quindoline–c-MYC G-Quadruplex: Insights into G-Quadruplex-Interactive Small Molecule Drug Design journal, November 2011

The Major G-Quadruplex Formed in the Human BCL-2 Proximal Promoter Adopts a Parallel Structure with a 13-nt Loop in K + Solution journal, January 2014

Stabilization of G-Quadruplex DNA and Down-Regulation of Oncogene c - myc by Quindoline Derivatives journal, April 2007

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 journal, May 2009

Crystal structure of parallel quadruplexes from human telomeric DNA journal, May 2002

Targeting G-quadruplexes in gene promoters: a novel anticancer strategy? journal, April 2011

Programmable RNA targeting by bacterial Argonaute nucleases with unconventional guide binding and cleavage specificity journal, August 2022

Direct evidence for a G-quadruplex in a promoter region and its targeting with a small molecule to repress c-MYC transcription journal, August 2002

Structure of the Biologically Relevant G-Quadruplex in The c-MYC Promoter journal, September 2006

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 journal, October 2005

Structure of two intramolecular G-quadruplexes formed by natural human telomere sequences in K + solution † journal, September 2007

A non-canonical DNA structure is a binding motif for the transcription factor SP1 in vitro journal, October 2011

Crystal structure of a c-kit promoter quadruplex reveals the structural role of metal ions and water molecules in maintaining loop conformation journal, January 2012

Flexibility and structural conservation in a c-KIT G-quadruplex journal, December 2014

The PDB_REDO server for macromolecular structure model optimization journal, May 2014

Putative DNA Quadruplex Formation within the Human c-kit Oncogene
journal, August 2005

Linking Crystallographic Model and Data Quality
journal, May 2012

Flexibility and structural conservation in a c-KIT G-quadruplex
journal, December 2014

Structural basis of G-quadruplex unfolding by the DEAH/RHA helicase DHX36
journal, June 2018

Solution Structure of a 2:1 Quindoline–c-MYC G-Quadruplex: Insights into G-Quadruplex-Interactive Small Molecule Drug Design
journal, November 2011

PHENIX: a comprehensive Python-based system for macromolecular structure solution.
text, January 2010

Crystallographic studies of quadruplex nucleic acids
journal, December 2007

The Protein Data Bank
journal, May 2002

Crystal structure of a c-kit promoter quadruplex reveals the structural role of metal ions and water molecules in maintaining loop conformation
journal, January 2012

Structure of the Biologically Relevant G-Quadruplex in The c-MYC Promoter
journal, September 2006

Structure of the Human Telomere in K ⁺ Solution: An Intramolecular (3 + 1) G-Quadruplex Scaffold
journal, August 2006

Deconvoluting the Structural and Drug-Recognition Complexity of the G-Quadruplex-Forming Region Upstream of the bcl-2 P1 Promoter
journal, April 2006

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
journal, October 2005

Targeting G-quadruplexes in gene promoters: a novel anticancer strategy?
journal, April 2011

Structure of an Unprecedented G-Quadruplex Scaffold in the Human c-kit Promoter
journal, April 2007

Metal Cations in G-Quadruplex Folding and Stability
journal, September 2016

The Major G-Quadruplex Formed in the Human BCL-2 Proximal Promoter Adopts a Parallel Structure with a 13-nt Loop in K ⁺ Solution
journal, January 2014

The role of supercoiling in transcriptional control of MYC and its importance in molecular therapeutics
journal, November 2009

Quadruplex nucleic acids as targets for anticancer therapeutics
journal, May 2017

XDS
journal, January 2010

Human Telomeric DNA Forms Parallel-Stranded Intramolecular G-Quadruplex in K ⁺ Solution under Molecular Crowding Condition
journal, September 2007

Evidence for the Presence of a Guanine Quadruplex Forming Region within a Polypurine Tract of the Hypoxia Inducible Factor 1α Promoter ^†
journal, December 2005

Crystal structure of parallel quadruplexes from human telomeric DNA
journal, May 2002

Structure of two intramolecular G-quadruplexes formed by natural human telomere sequences in K + solution †
journal, September 2007

Quadruplex DNA: sequence, topology and structure
journal, September 2006

PARP1 exhibits enhanced association and catalytic efficiency with γH2A.X-nucleosome
journal, December 2019

Optimized End-Stacking Provides Specificity of N -Methyl Mesoporphyrin IX for Human Telomeric G-Quadruplex DNA
journal, December 2012

Solution structure of the human telomeric repeat d[AG3(T2AG3)3] G-tetraplex
journal, December 1993

Cavin1 intrinsically disordered domains are essential for fuzzy electrostatic interactions and caveola formation
journal, February 2021

Demonstration that Drug-targeted Down-regulation of MYC in Non-Hodgkins Lymphoma Is Directly Mediated through the Promoter G-quadruplex
journal, September 2011

Features and development of Coot
journal, March 2010

Solution Structure of the Biologically Relevant G-Quadruplex Element in the Human c-MYC Promoter. Implications for G-Quadruplex Stabilization ^†
journal, February 2005

PHENIX: a comprehensive Python-based system for macromolecular structure solution
journal, January 2010

Design, synthesis and biological evaluation of a novel class of anticancer agents: Anthracenylisoxazole lexitropsin conjugates
journal, February 2009

Propeller-Type Parallel-Stranded G-Quadruplexes in the Human c-myc Promoter
journal, July 2004

Structural basis of G-quadruplex unfolding by the DEAH/RHA helicase DHX36.
text, January 2018

Stabilization of G-Quadruplex DNA and Down-Regulation of Oncogene c - myc by Quindoline Derivatives
journal, April 2007

Direct evidence for a G-quadruplex in a promoter region and its targeting with a small molecule to repress c-MYC transcription
journal, August 2002

A Conserved Quadruplex Motif Located in a Transcription Activation Site of the Human c-kit Oncogene
journal, June 2006

Structure of Human Telomeric DNA in Crowded Solution
journal, June 2011

The Protein Data Bank
journal, January 2000

A non-canonical DNA structure is a binding motif for the transcription factor SP1 in vitro
journal, October 2011

MYC on the Path to Cancer
journal, March 2012

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
journal, May 2009

AIMing towards improved antitumor efficacy
journal, April 2015

Circular dichroism of quadruplex DNAs: Applications to structure, cation effects and ligand binding
journal, December 2007

Mechanistic studies on the anticancer activity of 2,4-disubstituted quinazoline derivative
journal, October 2014

Design, synthesis and biological evaluation of a novel class of anticancer agents: Anthracenylisoxazole lexitropsin conjugates
journal, February 2009

AIMing towards improved antitumor efficacy
journal, April 2015

MYC on the Path to Cancer
journal, March 2012

Circular dichroism of quadruplex DNAs: Applications to structure, cation effects and ligand binding
journal, December 2007

Crystallographic studies of quadruplex nucleic acids
journal, December 2007

Discovery of a New Four-Leaf Clover-Like Ligand as a Potent c-MYC Transcription Inhibitor Specifically Targeting the Promoter G-Quadruplex
journal, February 2018

Evidence for the Presence of a Guanine Quadruplex Forming Region within a Polypurine Tract of the Hypoxia Inducible Factor 1α Promoter ^†
journal, December 2005

A Conserved Quadruplex Motif Located in a Transcription Activation Site of the Human c-kit Oncogene
journal, June 2006

Putative DNA Quadruplex Formation within the Human c-kit Oncogene
journal, August 2005

Deconvoluting the Structural and Drug-Recognition Complexity of the G-Quadruplex-Forming Region Upstream of the bcl-2 P1 Promoter
journal, April 2006

Structure of the Human Telomere in K ⁺ Solution: An Intramolecular (3 + 1) G-Quadruplex Scaffold
journal, August 2006

Structure of an Unprecedented G-Quadruplex Scaffold in the Human c-kit Promoter
journal, April 2007

Human Telomeric DNA Forms Parallel-Stranded Intramolecular G-Quadruplex in K ⁺ Solution under Molecular Crowding Condition
journal, September 2007

Structure of Human Telomeric DNA in Crowded Solution
journal, June 2011

Solution Structure of a 2:1 Quindoline–c-MYC G-Quadruplex: Insights into G-Quadruplex-Interactive Small Molecule Drug Design
journal, November 2011

The Major G-Quadruplex Formed in the Human BCL-2 Proximal Promoter Adopts a Parallel Structure with a 13-nt Loop in K ⁺ Solution
journal, January 2014

Stabilization of G-Quadruplex DNA and Down-Regulation of Oncogene c - myc by Quindoline Derivatives
journal, April 2007

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
journal, May 2009

Crystal structure of parallel quadruplexes from human telomeric DNA
journal, May 2002

Targeting G-quadruplexes in gene promoters: a novel anticancer strategy?
journal, April 2011

Programmable RNA targeting by bacterial Argonaute nucleases with unconventional guide binding and cleavage specificity
journal, August 2022

Direct evidence for a G-quadruplex in a promoter region and its targeting with a small molecule to repress c-MYC transcription
journal, August 2002

Structure of the Biologically Relevant G-Quadruplex in The c-MYC Promoter
journal, September 2006

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
journal, October 2005

Structure of two intramolecular G-quadruplexes formed by natural human telomere sequences in K + solution †
journal, September 2007

A non-canonical DNA structure is a binding motif for the transcription factor SP1 in vitro
journal, October 2011

Crystal structure of a c-kit promoter quadruplex reveals the structural role of metal ions and water molecules in maintaining loop conformation
journal, January 2012

Flexibility and structural conservation in a c-KIT G-quadruplex
journal, December 2014

The PDB_REDO server for macromolecular structure model optimization
journal, May 2014

PHENIX: a comprehensive Python-based system for macromolecular structure solution.
text, January 2010

Metal Cations in G-Quadruplex Folding and Stability
journal, September 2016

Therapeutic Inhibition of Myc in Cancer. Structural Bases and Computer-Aided Drug Discovery Approaches
journal, December 2018

Developing Novel G-Quadruplex Ligands: from Interaction with Nucleic Acids to Interfering with Nucleic Acid–Protein Interaction
journal, January 2019