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El. knyga: Progress in Medicinal Chemistry

Series edited by (WITNET LTD, Cambridge, UK), Series edited by (St. Ippolyts, Herts, UK)
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Progress in Medicinal Chemistry provides a review of eclectic developments in medicinal chemistry. This volume includes chapters covering recent advances in cancer therapeutics,  fluorine in medicinal chemistry, a  perspective on the next generation of antibacterial agents derived by manipulation of natural products, a  new era for Chagas Disease drug discovery? and imaging in drug development.

    • 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

    Daugiau informacijos

    A review of eclectic developments in medicinal chemistry, with authoritative extended reviews of targets and technologies addressing new therapeutics
    Contributors vii
    Preface ix
    1 Non-systemic Intestine-Targeted Drugs
    1(1)
    Matthew C.T. Fyfe
    1 Introduction
    1(44)
    2 Orally Administered NSIT Drugs
    3(26)
    3 Rectally Administered Non-systemic Intestinal Drugs
    29(3)
    4 Conclusions
    32(13)
    Acknowledgement
    34(1)
    References
    34(11)
    2 Measurement, Interpretation and Use of Free Ligand Solution Conformations in Drug Discovery
    45(104)
    Charles D. Blundell
    Thorsten Nowak
    Martin J. Watson
    1 Introduction
    46(5)
    2 Measurement of Free Ligand Solution Conformational Preferences
    51(11)
    3 Effectors Determining Free Ligand Conformational Preferences
    62(28)
    4 Rationalising and Relating Free Ligand Conformational Preferences
    90(20)
    5 Free Ligand Conformational Design
    110(14)
    6 Outlook and Summary
    124(25)
    Acknowledgements
    129(1)
    Appendix. Lisinopril Structure Determination
    129(2)
    Glossary
    131(1)
    References
    132(17)
    3 Recent Advances in the Discovery of Deubiquitinating Enzyme Inhibitors
    149(44)
    Mark Kemp
    1 Introduction
    149(2)
    2 Function and Structure of DUBs
    151(5)
    3 Assays to Identify DUB Inhibitors
    156(2)
    4 DUB Inhibitors by Target
    158(23)
    5 Summary
    181(12)
    Acknowledgements
    184(1)
    References
    184(9)
    4 The Evolving Role of the Medicinal Chemist
    193(34)
    Geoff Lawton
    Peter Nussbaumer
    1 Introduction
    194(1)
    2 Definition
    195(1)
    3 The Drug Discovery Process
    196(14)
    4 Business Structures for Drug Discovery
    210(3)
    5 Medicinal Chemistry Employers
    213(1)
    6 Education and Professional Development for Medicinal Chemists
    214(4)
    7 The Medicinal Chemistry `Phenotype'
    218(2)
    8 Changing Paradigms
    220(2)
    9 Future Directions
    222(1)
    10 Conclusions
    223(4)
    References
    224(3)
    Index 227(8)
    Cumulative Index of Authors 235(8)
    Cumulative Index of Subject 243
    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 tomorrows antibacterial drugs.He is a founder of INMedD, a new medicines discovery social enterprise. 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.