A practice-oriented overview of ligand binding modes for medicinal chemists, this handbook systematically surveys classical and non-classical binders and their mechanisms for the most relevant drug target classes, including enzyme, receptors and channels.
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PART I: INTRODUCTION
Basic principles of enzymology
Basic principles of receptor pharmacology
Pharmacological advantages/disadvantages of different interaction modes
Capturing inactive conformations
Suppression of transient conformations
Databases of allosteric protein sites
PART II: RECEPTORS
Ion Channels
GPCRs
mGluRs
Other receptor types
PART III: ENZYMES
Allosteric inhibition: Caspases, secretases, kinases
Covalent reversible inhibitors: proteases, kinases
Covalent irreversible inhibitors: historical and recent examples
Interfacial inhibitors
Enzyme Activators
Basic principles of enzymology
Basic principles of receptor pharmacology
Pharmacological advantages/disadvantages of different interaction modes
Capturing inactive conformations
Suppression of transient conformations
Databases of allosteric protein sites
PART II: RECEPTORS
Ion Channels
GPCRs
mGluRs
Other receptor types
PART III: ENZYMES
Allosteric inhibition: Caspases, secretases, kinases
Covalent reversible inhibitors: proteases, kinases
Covalent irreversible inhibitors: historical and recent examples
Interfacial inhibitors
Enzyme Activators
Les mer
Produktdetaljer
ISBN
9783527338023
Publisert
2022-01-10
Utgiver
Vendor
Wiley-VCH Verlag GmbH
Høyde
244 mm
Bredde
170 mm
Aldersnivå
P, 06
Språk
Product language
Engelsk
Format
Product format
Innbundet
Antall sider
480
Biografisk notat
Gerhard Müller is Senior Vice President at Mercachem (Nijmegen, The Netherlands), where he is in charge of all drug discovery projects. Before joining Mercachem, he held several managerial research positions within the Biotech industry (CSO of Axxima Pharmaceuticals AG, Vice President Drug Discovery at GPC Biotech AG), as well as in the pharmaceutical industry (Section Head Chemistry at Organon, Research Scientist at Bayer AG and at Glaxo). He is an expert in structure-based design, utilizing protein crystallography, NMR spectroscopy, and direct and indirect molecular modelling technologies. His current focus is on target-family centric medicinal chemistry approaches for Lead Finding and Optimization, applied to inhibitor design against kinases and epigenetic targets. He has authored more than 75 scientific publications and many patent applications from his academic and industrial research.Beat Ernst heads the Institute of Molecular Pharmacy at the University of Basel (Switzerland). Prior to his academic appointment, he was in charge of the carbohydrate section of Ciba-Geigy and later the selectin project at Novartis. His research interests are focused on carbohydrate-protein interactions. In a joint project with the biotechnology company GlycoMimetics he developed the glycomimetic GMI-1070, a selectin antagonist that recently successfully finished phase II clinical trials for the treatment of the sickle cell disease. He has authored more than 170 scientific publications, patent applications and books from his academic and industrial research.