Drug Discovery Strategies and MethodsCRC Press, 2003 M11 4 - 348 pages Navigate the complex and multidisciplinary path of drug discovery procedures with Drug Discovery Strategies and Methods-a well-organized and timely reference that analyzes methods in target identification and validation, lead detection, compound optimization, and biological testing. This volume addresses challenges encountered during the discovery of new pharmaceutical candidates including the use of cutting-edge techniques utilized in drug design and development. It considers key elements in the drug design cycle ranging from appropriateness of targets and disease models to compound characterization, safety, and efficacy and the role of protein crystallography in structure-based drug design. |
Contents
1 Protein Crystallography in StructureBased Drug Design | 1 |
2 Src Homology2 Domains and StructureBased SmallMolecule Library Approaches to Drug Discovery | 19 |
3 ThreeDimensional Structure of the Inhibited Catalytic Domain of Human Stromelysin1 by Heteronuclear NMR Spectroscopy | 53 |
Old and New Therapeutic Possibilities | 77 |
5 Development of PET and SPECT Radioligands for Cannabinoid Receptors | 111 |
6 Structural and Pharmacological Aspects of Peptidomimetics | 126 |
7 Linkers and Resins for SolidPhase Synthesis | 149 |
Implications for Drug Action | 189 |
Therapeutic Opportunities | 212 |
10 Uncoating and Adsorption Inhibitors of Rhinovirus Replication | 239 |
11 Profiles of Prototype Antiviral Agents Interfering with the Initial Stages of HIV Infection | 269 |
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Common terms and phrases
Acad Sci USA acid action activity addition adenosine affinity agents agonist allosteric amide amino amyloid analogues analysis anandamide antagonist assay atoms binding Biol bond brain cannabimimetics cannabinoid receptor CB1 receptor cells Chem Clercq complex compounds concentration conformational Congo Red containing crystal dependence derivatives determined discovery disease domain drug effects endogenous enhanced experiments fibril Figure formation function highly human important increased indicated inhibition inhibitors interactions involved lead Lett ligand linker mechanism method molecular molecules mutation Natl Acad Sci Nature novel observed opioid peptide Pharmacol phase position possible potent present produced properties protein reaction released residues resin resistance reverse ring role Scheme selective SH2 domain showed shown solid solid-phase specific Src SH2 stromelysin structure studies suggested synthesis therapeutic treatment virus vitro x-ray