BioNMR in Drug Research. Methods and Principles in Medicinal Chemistry

  • ID: 2179494
  • Book
  • 502 Pages
  • John Wiley and Sons Ltd
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The vast progress made in the investigation of biomolecules using NMR has only recently been rewarded with the Nobel Prize for Kurt Wuthrich. Editied by a former coworker of Wuthrich, this book presents the theoretical background on NMR of biomolecules, plus the use of NMR techniques in determining the structures of proteins and nucleic acids.

BioNMR spectroscopy offers a universal tool for examining the binding of an active substance to its target protein. Its use thereby benefits the rational development of drugs. This interaction can now be investigated in a hitherto unparalleled precision and displayed in 3D–an important prerequisite for the targeted development of new active substances, The latest methods for characterizing substance–receptor complexes are demonstrated backed by many case studies from pharmaceutical reseach. Thus it comes as no surprise that a large number of the authors are working for leading pharmaceutical companies.

With its successful mixture of basic information and application strategies, coupled with many real–life examples, this is an invaluable guide for both NMR spectroscopists and pharmaceutical researchers.

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BASIC TECHNIQUES

Modern Methods for Expression of Proteins in Isotopically Enriched Form

Structure Calculation Using Automated Techniques

Achieving Better Sensitivity, Less Noise and Less Artifacts in NMR Spectra

NMR OF BIOMOLECULES

NMR Strategies for Protein Assignment

NMR of Membrane–Associated Peptides and Proteins

NMR of Nucleic Acids

MODERN SPECTROSCOPIC TECHNIQUES

Methods for the Measurement of Angle Restraints from Scalar and Dipolar Couplings as well as from Cross Correlated Relaxation: Application to Biomolecules

Orientational Restraints

Scalar Coupling Across Hydrogen Bonds

TROSY:Transverse Relaxation–Optimized Spectroscopy

MAS Solid–State NMR of Isotopically Enriched Biological Samples

Determination of Protein Dynamics Using 15N Relaxation Measurements

TOOLS FOR INVESTIGATION OF DRUG–RECEPTOR COMPLEXES AND FOR LIGAND SCREENING

The Determination of Equilibrium Dissociation Constants of Protein–Ligand Complexes by NMR

Experiments in NMR–based Screening

The Use of Spin–Labels in NMR–supported Lead Finding and Optimization

NMR of Weakly Binding Ligands

Isotope Filter and Editing Techniques

STRATEGIES FOR DRUG DEVELOPMENT USING NMR

Strategies for NMR Screening and Library Design

Strategies for Hit Finding Using NMR

Strategies for Drug Discovery Using NMR

NMR–based Drug Design: Approaches for Very Large Proteins

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"The editor has managed to recruit a team of well–recognized experts as authors for this book, thereby ensuring a high standard of reliable and objective reporting. The book is not only of interest to specialists in pharmaceutical research and development, but will certainly also be a valuable resource for everyone concerned with the latest methods of NMR spectroscopy and their application to biomolecules"

(Angewandte Chemie Int. Ed.)

"The book presents a good overview of state–of–the–art NMR techniques in drug discovery. [...] It is suggested reading for people involved in pharmaceutical research as well as academic researchers with an interest in drug discovery."

(ChemBioChem)

"...certainly a valuable resource for everyone concerned with the latest methods of NMR spectroscopy and their applications..." Angewandte Chemie Int. Edition
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