Download e-book for kindle: Quadruplex Nucleic Acids by Stephen Neidle

Pharmacology

By Stephen Neidle

ISBN-10: 0854043748

ISBN-13: 9780854043743

The examine of G-quadruplexes has emerged in recent times as a big concentration of analysis in nucleic acids. this is often now a speedily growing to be region, no longer least due to its capability as a unique method of melanoma therapeutics, and there's a lot present job at the layout of quadruplex-selective small-molecule ligands and the examine in their mobile results. This well timed booklet provides a uniquely built-in view of quadruplex nucleic acids that would be a big source in destiny drug-discovery strategies.

Therapeutic purposes of Quadruplex Nucleic Acids provides a unmarried finished survey that describes and assesses fresh advances in quadruplex therapeutics and focusing on options. It additionally covers the underlying basics of such subject matters as quadruplex constitution, small-molecule attractiveness, organic roles of genomic quadruplexes, and quadruplex informatics.

Written by way of an international chief during this box, this publication is a crucial source for researchers in medicinal chemistry, chemical biology, structural biology, drug discovery, and pharmacology in melanoma and different healing parts, in addition to for chemists and biologists engaged on nucleic acids, and may be necessary for either energetic researchers and scholars in those areas.

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Extra resources for Quadruplex Nucleic Acids

Sample text

2 Location of Ions The smaller Na1 ion is able to reside within the plane of a quartet, whereas ammonium and potassium ions coordinate between two G-quartets. On 40 Chapter 2 the other hand, ‘‘external’’ ions interact with the quadruplex in a much less defined manner, with little, if any, preference for cation nature. Na1 and K1 compete on the same footing for atmospheric binding. For most other nucleic acids structures, there are no ‘‘internal’’ ions, and cations only interact in a relative passive way (‘‘atmospheric binding’’) with no preference for cation nature.

However, a detailed review on the kinetics of these aggregates is beyond the scope of this manuscript and additional information on quartet formation by isolated bases can be found in the chapter by J. Davis and co-workers (also see ref. 15). 2 Thermodynamics Although this review focuses on the kinetics and dynamics of quadruplexes, one cannot avoid a preliminary discussion on the thermodynamics of these structures. 1 Enthalpy and Entropy of Formation The formation of quadruplex structures, whatever their type, is clearly enthalpy driven, with an enthalpy per quartet of À15 to À25 kcal molÀ1.

18 A˚) allows for in-plane coordination. 69 In any case, empty sites between quartets are probably very rare. 5 M KCl. Is it possible to obtain an ‘‘empty’’ quadruplex, whose central cavity is devoid of cations? , self-assembly of 5 0 -GMP, unlike a normal stacking interaction is not determined predominantly by hydrophobic forces. 89 Ions therefore play a strong stabilizing role on the quadruplex, but this does not exclude that a relatively unstable quadruplex stem could be formed in the absence of ions.

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Quadruplex Nucleic Acids by Stephen Neidle


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