Structure-based drug discovery exploits the knowledge of the three-dimensional framework of biological molecules to enhance the process and outcome of drug design and development. Scientists can utilize modern structural biology techniques to characterize new therapeutic targets and develop efficient new drugs. Over the last few years, there have been significant improvements and advances in the field, leading to faster and more effective drug development at the preclinical stage. Today, a number of drugs have been derived from structure-based design programs and scientists continue to discover breakthrough methods in this fast-growing field.
With the most comprehensive and up-to-date overview of structure-based drug discovery covering mostly experimental but also computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field.
The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that:
- Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology
- Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design
- Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures
- Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins
From the Back Cover
Structure-based drug discovery exploits the knowledge of the three-dimensional framework of biological molecules to enhance the process and outcome of drug design and development. Scientists can utilize modern structural biology techniques to characterize new therapeutic targets and develop efficient new drugs. Over the last few years, there have been significant improvements and advances in the field, leading to faster and more effective drug development at the preclinical stage. Today, a number of drugs have been derived from structure-based design programs and scientists continue to discover breakthrough methods in this fast-growing field.
With the most comprehensive and up-to-date overview of structure-based drug discovery covering mostly experimental but also computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field.
The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that:
- Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology
- Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design
- Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures
- Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins
About the Author
JEAN-PAUL RENAUD, PhD, is cofounder and President & Chief Scientific Officer at Urania Therapeutics (formerly RiboStruct), which focuses on rational drug design targeting the human ribosome. Previously, he was cofounder and Chief Scientific Officer at NovAliX and CNRS Research Director in the Structural Biology and Genomics Department at the Institute of Genetics and Molecular and Cellular Biology. Dr Renaud has over 30 years of research experience, along with 48 articles, 4 book chapters and 3 patents to his credit. He also initiated and is the Chairman and Scientific Organizer of the NovAliX Conferences “Biophysics in Drug Discovery”.
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