The realisation that human, animal, viral and bacterial genomes all contain over-representation of higher-order quadruplex structures in regulatory and other pharmacologically-useful regions, has led to a large number of studies aimed at exploiting this findings for therapeutic and diagnostic purposes. Quadruplex-binding small molecules are starting to be evaluated in human clinical trials. Provides the authority and expertise of leading contributors from an international board of authors Presents the latest release in the Annual Reports in Medicinal Chemistry series

Complete, up-to-date coverage of the broad area of nucleic acid chemistry and biology Assembling contributions from a collection of authors with expertise in all areas of nucleic acids, medicinal chemistry, and therapeutic applications, Medicinal Chemistry of Nucleic Acids presents a thorough overview of nucleic acid chemistry—a rapidly evolving and highly challenging discipline directly responsible for the development of antiviral and antitumor drugs. This reliable resource delves into a multitude of subject areas involving the study of nucleic acids—such as the new advances in genome sequencing, and the processes for creating RNA interference (RNAi) based drugs—to assist pharmaceutical researchers in removing roadblocks that hinder their ability to predict drug efficacy. Offering the latest cutting-edge science in this growing field, Medicinal Chemistry of Nucleic Acids includes: In-depth coverage of the development and application of modified nucleosides and nucleotides in medicinal chemistry A close look at a large range of current topics on nucleic acid chemistry and biology Essential information on the use of nucleic acid drugs to treat diseases like cancer A thorough exploration of siRNA for RNAi and the regulation of microRNA, non-coding RNA (ncRNA), a newly developing and exciting research area Thorough in its approach and promising in its message, Medicinal Chemistry of Nucleic Acids probes the new domains of pharmaceutical research—and exposes readers to a wealth of new drug discovery opportunities emerging in the dynamic field of nucleic acid chemistry.

Guanine rich DNA has been known for decades to form unusual structures, although their biological relevance was little understood. Recent advances have demonstrated that quadruplex structures can play a role in gene expression and provide opportunities for a new class of anticancer therapeutics. A number of quadruplex-specific proteins have also been discovered. Quadruplex Nucleic Acids discusses all aspects of the fundamentals of quadruplex structures, including their structure in solution and the crystalline state, the kinetics of quadruplex folding, and the role of cations in structure and stability. The biology of quadruplexes and G-rich genomic regions and G-quartets in supramolecular chemistry and nanoscience are also considered. Surveying the current state of knowledge, and with contributions from leading experts, this is the first comprehensive review of this rapidly growing area. Quadruplex Nucleic Acids is ideal for researchers interested in areas related to chemistry, chemical biology, medicinal chemistry, molecular pharmacology, and structural and molecular biology.

"Therapeutic applications of quadruplex nucleic acids provides a single comprehensive survey that describes and assesses recent advances in quadruplex therapeutics and targeting strategies. It also covers the underlying fundamentals of such topics as quadruplex structure, small-molecule recognition, biological roles of genomic quadruplexes, and quadruplex informatics"--P. [4] of cover.

Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors.

Gaining Insights into the Small Molecule Targeting of the G-Quadruplex in the c-MYC Promoter Using NMR and an Allele-Specific Transcriptional Assay, by Christine E. Kaiser, Vijay Gokhale, Danzhou Yang and Laurence H. Hurley.- Higher-Order Quadruplex Structures, by Luigi Petraccone.- Investigation of Quadruplex Structure Under Physiological Conditions Using In-Cell NMR, by Robert Hänsel, Silvie Foldynová-Trantírková, Volker Dötsch and Lukás Trantírek.- Circular Dichroism of Quadruplex Structures, by Antonio Randazzo, Gian Piero Spada and Mateus Webba da Silva.- Molecular Crowding and Hydration Regulating of G-Quadruplex Formation, by Daisuke Miyoshi, Takeshi Fujimoto and Naoki Sugimoto.- Visualizing the Quadruplex: From Fluorescent Ligands to Light-Up Probes, by Eric Largy, Anton Granzhan, Florian Hamon, Daniela Verga and Marie-Paule Teulade-Fichou.- Calculation of Hydrodynamic Properties for G-Quadruplex Nucleic Acid Structures from in silico Bead Models, by Huy T. Le, Robert Buscaglia, William L. Dean, Jonathan B. Chaires and John O. Trent.- Energetics of Ligand Binding to G-Quadruplexes, Concetta Giancola and Bruno Pagano.- Tetramolecular Quadruplex Stability and Assembly, by Phong Lan Thao Tran, Anne De Cian, Julien Gros, Rui Moriyama and Jean-Louis Mergny.

Life in all its forms is based on nucleic acids which store and transfer genetic information. The book addresses main aspects of synthesis, hydrolytic stability and solution equilibria of nucleosides, nucleotides and oligonucleotides, as well as synthesis of their structural analogs that are of interest in chemotherapy. In addition, recent achievements in chemistry of catalytic nucleic acids, development of oligonucleotide based drugs and novel strategies for their targeting and delivery are discussed. The central theme always is the correlation of structure and function.