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- Volume 18, Issue 14, 2012
Current Pharmaceutical Design - Volume 18, Issue 14, 2012
Volume 18, Issue 14, 2012
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Editorial [Hot Topic: The Impact of the G-Quadruplex Conformation in the Development of Novel Therapeutic and Diagnostic Agents Executive (Guest Editor: Stefano Alcaro)]
More LessThe anticancer pharmacological treatment is typically affected by a non optimized therapeutic index. In the last decade several novel molecular targets have been identified and when possible used to design innovative anticancer agents. Among them a special fold of the DNA, known as G-quadruplex conformation, has been found particularly attractive for some important reasons. Firstly, it is exclusive of guanine-rich DNA s Read More
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Cell Cycle Regulation of G-Quadruplex DNA Structures at Telomeres
Authors: Stefan A. Juranek and Katrin PaeschkeDNA and RNA regions containing tracts of guanines can form very stable secondary structures called G-quadruplex (G4). Genomic sequences with the potential to form G4 (G4-motifs) are abundant across species. In all analyzed genomes G4 motifs are found near promoter regions and double strand break sites and at telomeres. Telomeres are very G-rich and prone for G4 formation. Therefore they are routinely used in in vitro Read More
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The Polymorphisms of DNA G-Quadruplex Investigated by Docking Experiments with Telomestatin Enantiomers
Human telomeres are comprised of d(TTAGGG) repeats involved in the formation of G-quadruplex DNA structures. Ligands stabilizing these G-quadruplex DNA structures are potential inhibitors of the cancer cell-associated enzyme telomerase. In human cells, telomerase adds multiple copies of the 5'-GGTTAG-3' motif to the end of the G-strand of the telomere and in the majority of tumor cells it results over-expressed. Read More
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State-of-the-Art Methodologies for the Discovery and Characterization of DNA G-Quadruplex Binders
Nowadays, the molecular basis of interaction between low molecular weight compounds and biological macromolecules is the subject of numerous investigations aimed at the rational design of molecules with specific therapeutic applications. In the last decades, it has been demonstrated that DNA quadruplexes play a critical role in several biological processes both at telomeric and gene promoting levels thus providing a great Read More
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Experimental Methods for Studying the Interactions between G-Quadruplex Structures and Ligands
Authors: Joaquim Jaumot and Raimundo GargalloThe present paper reviews the recent advances in and applications of experimental techniques used to study interactions between G-quadruplex structures and ligands that are potentially of pharmaceutical interest. Several instrumental techniques are used to study such interactions. The application of spectroscopic techniques such as molecular absorption, circular dichroism, molecular fluorescence, mass spectrometry a Read More
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Recent Developments in the Chemistry and Biology of G-Quadruplexes with Reference to the DNA Groove Binders
Authors: Akash K. Jain and Santanu BhattacharyaDNA is the chemotherapeutic target for treating diseases of genetic origin. Besides well-known double-helical structures (A, B, Z, parallel stranded-DNA etc.), DNA is capable of forming several multi-stranded structures (triplex, tetraplex, i-motif etc.) which have unique biological significance. The G-rich 3'-ends of chromosomes, called telomeres, are synthesized by telomerase, a ribonucleoprotein, and over-expression of telo Read More
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Heterocyclic Dications as a New Class of Telomeric G-Quadruplex Targeting Agents
Small molecules that can induce and stabilize G-quadruplex DNA structures represent a novel approach for anti-cancer and anti-parasitic therapy and extensive efforts have been directed towards discovering lead compounds that are capable of stabilizing quadruplexes. The purpose of this study is to explore conformational modifications in a series of heterocyclic dications to discover structural motifs that can selectively bin Read More
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G-Quadruplex Binding Ligands: from Naturally Occurring to Rationally Designed Molecules
Authors: Tuong Vy Thi Le, Sujin Han, Junghyun Chae and Hyun-Ju ParkGuanine-rich nucleic acid sequences are known to form G-quadruplex - four-stranded DNA or RNA structures stabilized by an array of Hoogsteen hydrogen bonds. G-quadruplex structures are involved in the modulation of gene expression at the transcription and translation levels. Accordingly, G-quadruplexes are considered as novel therapeutic targets for anticancer drug development. In this review, the authors provide a brief Read More
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Searching Drug-Like Anti-cancer Compound(s) Based on G-Quadruplex Ligands
Authors: Qian Li, Jun-Feng Xiang, Hong Zhang and Ya-Lin TangG-quadruplex structure is a four-stranded form of DNA, which is associated with cancer cell proliferation. G-quadruplexstabilized ligands have the potential to interfere with telomere replication by blocking the elongation procedure catalyzed by telomerase, and therefore have the potential to be anti-cancer drugs. A considerable number of novel compounds capable of targeting G-quadruplex at high affinity and specificity have Read More
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Targeting DNA G-Quadruplex Structures with Peptide Nucleic Acids
Regulation of genetic functions based on targeting DNA or RNA sequences with complementary oligonucleotides is especially attractive in the post-genome era. Oligonucleotides can be rationally designed to bind their targets based on simple nucleic acid base pairing rules. However, the use of natural DNA and RNA oligonucleotides as targeting probes can cause numerous off-target effects. In addition, natural nucleic acids are p Read More
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Screening of a Chemical Library by HT-G4-FID for Discovery of Selective G-quadruplex Binders
Authors: Eric Largy, Nicolas Saettel, Florian Hamon, Sylvie Dubruille and Marie-Paule Teulade-FichouDue to the lack of structural guidelines about G-quadruplex ligands, rational design cannot be the only approach to discover potent G4-ligands. As a complementary approach, screening of chemical library may provide interesting scaffolds known as hits provided that specific tools are available. In this work, the Institut Curie-CNRS chemical library was firstly screened by chemoinformatics methods. Similarity estimations by comp Read More
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Structure Conversion and Structure Separation of G-Quadruplexes Investigated by Carbazole Derivatives
Authors: Ta-Chau Chang, Jen-Fei Chu, Yu-Lin Tsai and Zi-Fu WangThe challenge of G-quadruplexes is that the G-rich sequences can adopt various G4 structures and possibly interconvert among them, particularly under the change of environmental conditions. Both NMR and circular dichroism (CD) show the spectral conversion of d[AG3(T2AG3)3] (HT22) from Na-form to K-form after Na+/K+ ion exchange. No appreciable change on the induced CD spectra of BMVC molecule and the single mol Read More
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G-quadruplex DNA Aptamers and their Ligands: Structure, Function and Application
Authors: W. O. Tucker, K. T. Shum and J. A. TannerHighly specific and tight-binding nucleic acid aptamers have been selected against a variety of molecular targets for over 20 years. A significant proportion of these oligonucleotides display G-quadruplex structures, particularly for DNA aptamers, that enable molecular recognition of their ligands. G-quadruplex structures couple a common scaffold to varying loop motifs that act in target recognition. Here, we review DNA G- Read More
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Folding Versus Charge: Understanding Selective Target Recognition by the Thrombin Aptamers
Authors: Giuseppe Marson, Manlio Palumbo and Claudia SissiThe use of nucleic acids as drugs represents a consistently growing approach. Different therapeutical strategies take advantage of the biological and biophysical properties of DNA and RNA to properly modulate activity of selected targets. A peculiar characteristic of these molecules is their structural flexibility which allows them to assume distinct foldings depending upon their sequence and/or environment. During the last t Read More
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Thrombin Binding Aptamer, More than a Simple Aptamer: Chemically Modified Derivatives and Biomedical Applications
Authors: Anna Avino, Carme Fabrega, Maria Tintore and Ramon EritjaThe thrombin binding aptamer (TBA) is a well characterized chair-like, antiparallel quadruplex structure that binds specifically to thrombin at nanomolar concentrations and therefore it has interesting anticoagulant properties. In this article we review the research involved in the development of new TBA derivatives with improved anticoagulant properties as well as the use of the TBA as a model compound for the Read More
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G-Quadruplex Based Probes for Visual Detection and Sensing
Authors: J. L. Neo, K. Kamaladasan and M. UttamchandaniRecent advances in colorimetric biosensing have led to rapid methods for target detection, potentially leading to applications on-site, at the point-of-need. This review focuses on one such platform, the G-quadruplex-hemin based DNAzymes, which exhibit peroxidase- like activity. Since their discovery in the late 1990s, various approaches have been adopted in applying the unique catalytic properties of these DNAzymes to de Read More
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Luminescent G-quadruplex Probes
Authors: Dik-Lung Ma, Daniel Shiu-Hin Chan, Hui Yang, Hong-Zhang He and Chung-Hang LeungG-quadruplexes have found increasing potential in applications such as molecular therapeutics, diagnostics, and sensing. As a consequence, small molecules capable of selectively detecting G-quadruplexes have received significant attention in recent literature. Our review here addresses representative advances in the development of luminescent G-quadruplex probes and highlights their potential applications in sensing and imaging.
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G-Quadruplex as Signal Transducer for Biorecognition Events
Authors: Lei Lv, Zhijun Guo, Jiahai Wang and Erkang WangG-rich nucleic acid oligomers can form G-quadruplexes built by G-tetrads stacked upon each other. The basic building block of the G-quadruplexes is similar, but the formation of different quadruplex structures is highly responsive to the strand stoichiometry, strand orientation, guanine glycosidic torsion angle, connecting loops, and the metal coordination. Because of its structural variations and different functions, G-qua Read More
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Human Telomere RNA: A Potential Target for Ligand Recognition
By Yan XuA recent finding demonstrated that telomere DNA is transcribed into telomeric repeat-containing RNA (referred to as TERRA) in mammalian cells. The existence of TERRA RNA may reveal a new level of regulation and protection of chromosome ends that could promote valuable insight into fundamental biological processes such as cancer and aging. Revealing the structure and function of telomere RNA will be essential for u Read More
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RNA G-Quadruplexes: G-quadruplexes with “U” Turns
Authors: Tani Agarwal, Gopal Jayaraj, Satya Prakash Pandey, Prachi Agarwala and Souvik MaitiG-quadruplexes are non canonical secondary structures held together by Hoogsteen bonded planar guanine quartets formed in G-rich sequences in DNA and RNA. Considerable research over the past three decades has contributed to a great deal of understanding of these unusual structures in DNA. Various factors governing the stability of DNA quadruplexes coupled with their in vivo existence have been well documented. RNA Read More
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Volumes & issues
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Volume 31 (2025)
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Volume 30 (2024)
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Volume 29 (2023)
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Volume 28 (2022)
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Volume 27 (2021)
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Volume 26 (2020)
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Volume 25 (2019)
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Volume 24 (2018)
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Volume 23 (2017)
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Volume 22 (2016)
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Volume 21 (2015)
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Volume 20 (2014)
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Volume 19 (2013)
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Volume 18 (2012)
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Volume 17 (2011)
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Volume 16 (2010)
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Volume 15 (2009)
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Volume 14 (2008)
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Volume 13 (2007)
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Volume 12 (2006)
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Volume 11 (2005)
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Volume 10 (2004)
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Volume 9 (2003)
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Volume 8 (2002)
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Volume 7 (2001)
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Volume 6 (2000)
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