Drug Discovery Strategies and Methods
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.
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1 Protein Crystallography in StructureBased Drug Design
2 Src Homology2 Domains and StructureBased SmallMolecule Library Approaches to Drug Discovery
3 ThreeDimensional Structure of the Inhibited Catalytic Domain of Human Stromelysin1 by Heteronuclear NMR Spectroscopy
Old and New Therapeutic Possibilities
5 Development of PET and SPECT Radioligands for Cannabinoid Receptors
6 Structural and Pharmacological Aspects of Peptidomimetics
7 Linkers and Resins for SolidPhase Synthesis
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Acad Sci USA activity adenosine A1 receptor agents agonist allosteric Alzheimer’s disease amide amines amino acid analogues anandamide antagonist assay atoms Biochem Biol Chem biological C-terminal cannabimimetics cannabinoid receptor carboxylic acid catalytic domain CB1 receptor cells Chem cleavage compounds concentration conformational crystal structure crystallography diffraction drug discovery effects endocannabinoid endogenous enhanced fibril formation Figure function human hydrogen bonds hydrophobic inhibition inhibitors interactions isoxazole ligand linker Makriyannis marijuana Mechoulam membrane metabolic mice molecular molecules muscarinic receptors mutation Natl Acad Sci neuronal NNRTIs nonpeptide novel opioid peptides opioid receptor pep tide Pertwee phase synthesis phenyl potent prion Proc Natl Acad protein pTyr pY+3 radioligand reaction residues resin Scheme Schiller PW selective SH2 domain signal transduction solid-phase synthesis specific Src SH2 stromelysin-1 structure-based drug design studies target Tetrahedron Lett therapeutic TIPP virus vitro vivo Weltrowska x-ray