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Chapter One: Structure-Based Drug Design for G Protein-Coupled Receptors
- 1 Introduction
- 2 Structural Architecture of GPCRs
- 3 GPCR Protein–Ligand X-Ray Structures
- 4 Mechanisms of Activation: Agonist Bound Structures
- 5 Biased Agonism
- 6 Traditional Approaches to GPCR Drug Discovery and the Need for Change
- 7 Potential of SBDD and FBDD for GPCR Drug Discovery
- 8 Conclusions and Outlook
- Chapter Two: P2X7 Antagonists as Potential Therapeutic Agents for the Treatment of CNS Disorders
- 1 Introduction
- 2 P2X7 in the CNS
- 3 P2X7 Modulators in Clinical Trials
- 4 P2X7 Receptor Antagonists
- 5 Conclusion
- Chapter Three: γ-Secretase Modulators: Current Status and Future Directions
- 1 Introduction
- 2 GSMs: Chemical Classes
- 3 Chemical Biology
- 4 Outlook
- 5 Clinical Studies
- 6 Conclusions
- Chapter Four: Recent Progress in the Discovery and Development of N-Type Calcium Channel Modulators for the Treatment of Pain
- 1 Introduction
- 2 Voltage-Gated Calcium Channels
- 3 N-Type Calcium Channels
- 4 N-Type Clinical Landscape and Emerging Pipeline
- 5 Concluding Remarks
- Subject Index
Cumulative Index of Authors for Volumes 1–53
Cumulative Index of Subjects for Volumes 1–53
Progress in Medicinal Chemistry provides a review of eclectic developments in medicinal chemistry. This volume continues in the serial's tradition of providing an insight into the skills required of the modern medicinal chemist; in particular, the use of an appropriate selection of the wide range of tools now available to solve key scientific problems, including g-secretase modulators, P2X7 antagonists as therapeutic agents for CNS disorders, N-type calcium channel modulators for the treatment of pain, and more.
- Extended timely reviews of topics in medicinal chemistry
- Targets and technologies relevant to the discovery of tomorrow’s drugs
- Analyses of successful drug discovery programmes
Everyone interested in the strategy and practice of the preclinical phases of the creation of new medicines. Those wishing to understand the drivers of drug design or expand their knowledge of therapeutic target classes
- No. of pages:
- © Elsevier 2014
- 1st March 2013
- Hardcover ISBN:
- eBook ISBN:
Dr Geoff Lawton has extensive experience in new medicine discovery across many therapeutic areas in both large and small companies and is a co-inventor of a marketed drug (Cilazapril). He is a former Director of Chemistry at Roche UK, and Vice-president Chemistry and Preclinical Sciences within Roche Bioscience, Palo Alto, USA. He was for five years the research member of a global therapy area strategy planning team for inflammatory diseases, aligning research with the clinical development and marketing parts of the business.
From 2003 to 2007 he was founding Research Director with Lectus Therapeutics building from start-up a drug discovery organisation; generating the team, facilities and project portfolio targeting the next generation of ion channel modulating medicines.
Since 2001 Geoff has provided scientific and strategic evaluation and advice on drug discovery as an independent consultant for a number small and medium sized biotech companies, CROs, VCs, academic groups and medical research charities.
Geoff serves on the Board of Antabio, a French biotech company developing tomorrow’s antibacterial drugs.
He is a founder of INMedD, a new medicines discovery social enterprise.
St. Ippolyts, Herts, UK
Dr David Witty has more than 20 years experience in the pharmaceutical industry as a medicinal chemist and project leader working principally in areas of anti-infectives, metabolic diseases, cognition and pain, delivering clinical candidates for several conditions. He led IT Strategy within the Neurology division of GSK, developing and deploying the first Electronic Notebooks for drug discovery to sites in the UK and Singapore. He has contributed more than 90 scientific papers, reviews, patents and books on medicinal and synthetic chemistry.
In 2010 David and several colleagues successfully raised $35M in venture funding to found Convergence Pharmaceuticals, a specialist ion channel company focused on the development of novel treatments for pain, based in Cambridge UK. David presently leads their discovery programme and manages scientific operations within the business.
David is chairman of the Fine Chemicals Group of the Society of Chemical Industry, with responsibility for the delivery of conferences, seminars and training courses for chemists throughout the UK and Europe, and advising parliamentary bodies on matters of relevance to the UK chemical industry.
Since 2008 David has been a STEM ambassador for SETPOINT, introducing school students at both primary and secondary level to the excitement and possibilities of pursuing scientific careers, through workshops, lectures and competitions.
WITNET LTD, Cambridge, UK