05476nam 2200733Ia 450 991014624390332120170814170325.01-280-52027-297866105202753-527-60518-53-527-60266-6(CKB)1000000000019310(EBL)481319(OCoLC)68923684(SSID)ssj0000204788(PQKBManifestationID)11172538(PQKBTitleCode)TC0000204788(PQKBWorkID)10191420(PQKB)11550447(MiAaPQ)EBC481319(EXLCZ)99100000000001931020030725d2004 uy 0engur|n|---|||||txtccrMolecular biology in medicinal chemistry[electronic resource] /edited by Th. Dingermann, D. Steinhilber and G. FolkersWeinheim Wiley-VCH20041 online resource (437 p.)Methods and principles in medicinal chemistry ;v. 21Description based upon print version of record.3-527-30431-2 Includes bibliographical references and index.Molecular Biology in Medicinal Chemistry; Contents; Preface; Foreword; Contributors; Part I Molecular Targets; 1 Cellular Assays in Drug Discovery; 1.1 Introduction; 1.1.1 Positioning Cellular Assays; 1.1.2 Impact on Drug Discovery; 1.1.3 Classification of Cellular Assays; 1.1.4 Progress in Tools and Technologies for Cellular Compound Profiling; 1.2 Membrane Proteins and Fast Cellular Responses; 1.2.1 Receptors; 1.2.1.1 FLIPR Technology for Detection of Intracellular Calcium Release; 1.2.1.2 Competitive Immunoassay for Detection of Intracellular cAMP1.2.1.3 Enzyme Fragment Complementation (EFC) Technology1.2.2 Membrane Transport Proteins; 1.2.2.1 Ion Channels; 1.2.2.2 MDR Proteins; 1.3 Gene and Protein Expression Profiling in High-throughput Formats; 1.3.1 Reporter Gene Assays in Lead Finding; 1.3.2 Reporter Gene Assays in Lead Optimization; 1.4 Spatio-temporal Assays and Subpopulation Analysis; 1.4.1 Phosphorylation Stage-specific Antibodies; 1.4.2 Target-protein-specific Antibodies; 1.4.3 Protein-GFP Fusions; 1.4.4 Fluorescence Resonance Energy Transfer (FRET)1.4.5 GPCR Activation using Bioluminescence Resonance Energy Transfer (BRET)1.4.6 Protein Fragment Complementation Assays (PCA); 1.5 Phenotypic Assays; 1.5.1 Proliferation/Respiration/Toxicity; 1.5.2 Apoptosis; 1.5.3 Differentiation; 1.5.4 Monitoring Cell Metabolism; 1.5.5 Other Phenotypic Assays; Acknowledgments; References; 2 Gene Knockout Models; 2.1 Introduction; 2.2 Gene Knockout Mice; 2.2.1 ES Cells; 2.2.2 Targeting Vector; 2.2.3 Selection of Recombinant ES Cells; 2.2.4 Injection of Recombinant ES Cells into Blastocysts and Blastocyst Transfer to Pseudopregnant Recipients2.2.5 Chimeras and F1 and F2 Offspring2.3 Tissue-Specific Gene Expression; 2.3.1 Ligand-Activated CRE Recombinases; 2.3.2 The Tetracycline/Doxycycline-Inducible Expression System; 2.4 Transgenic Mice; 2.5 Targeted Gene Disruption in Drosophila; 2.6 Targeted Gene Knockdown in Zebrafish; 2.7 Targeted Caenorhabditis Elegans Deletion Strains; References; 3 Reporter Gene Assay Systems for the Investigation of G-protein-coupled Receptors; 3.1 Receptors and Cellular Communication; 3.1.1 Ion Channel-linked Receptors; 3.1.2 Enzyme-linked Cell-surface Receptors; 3.1.3 GPCRs3.2 Affinity and Activity of GPCR Ligands3.3 The Role of Transcription Factors in Gene Expression; 3.3.1 CREB; 3.3.2 SRF; 3.3.3 STAT Proteins; 3.3.4 c-Jun; 3.3.5 NF-AT; 3.4 Reporter Genes; 3.4.1 CAT; 3.4.2 β-Gal; 3.4.3 β-Glucuronidase; 3.4.4 AP; 3.4.5 SEAP; 3.4.6 β-Lactamase; 3.4.7 Luciferase; 3.4.8 GFP; 3.5 Reporter Gene Assay Systems for the Investigation of GPCRs; 3.5.1 Application of Luciferase as a Reporter Gene; 3.5.2 Application of other Reporter Genes for the Investigation of GPCRs; References; 4 From the Human Genome to New Drugs: The Potential of Orphan G-protein-coupled Receptors4.1 IntroductionThis readily comprehensible book explains the identification of molecular targets via cellular assays, reporter genes or transgenic models, as well as surveying recent advances in the synthesis, separation and analysis of drugs. A special section is devoted to molecular genetics methods.With its examination of these novel methods and generous practical advice, this is essential reading for all pharmaceutical chemists, molecular biologists and medical researchers using molecular methods to study drugs and their action.Methods and principles in medicinal chemistry ;v. 21.Chiral drugsGenomicsMolecular biologyMolecular pharmacologyPharmacogenomicsElectronic books.Chiral drugs.Genomics.Molecular biology.Molecular pharmacology.Pharmacogenomics.615.19Dingermann Theodor921169Folkers Gerd505529Steinhilber Dieter1959-921170MiAaPQMiAaPQMiAaPQBOOK9910146243903321Molecular biology in medicinal chemistry2066160UNINA