05227nam 2200673Ia 450 991014410920332120170809153157.01-281-94720-297866119472003-527-62329-93-527-62330-2(CKB)1000000000552742(EBL)481431(SSID)ssj0000212698(PQKBManifestationID)11175620(PQKBTitleCode)TC0000212698(PQKBWorkID)10139458(PQKB)10124067(MiAaPQ)EBC481431(OCoLC)299046803(PPN)242769438(EXLCZ)99100000000055274220080410d2008 uy 0engur|n|---|||||txtccrNuclear receptors as drug targets /edited by Eckhard Ottow and Hilmar WeinmannWeinheim Wiley-VCHc20081 online resource (524 p.)Methods and principles in medicinal chemistryDescription based upon print version of record.3-527-31872-0 Includes bibliographical references and index.Nuclear Receptors as Drug Targets; Contents; List of Contributors; Preface; A Personal Foreword; 1 Nuclear Receptors as Drug Targets: A Historical Perspective of Modern Drug Discovery; 1.1 Introduction; 1.2 Short Historical Overview on Nuclear Receptors in Pharmacological Research and Drug Discovery; 1.2.1 Glucocorticoid Receptor Research; 1.2.2 Estrogen Receptor Research; 1.2.3 Progesterone Receptor Research; 1.2.4 Other Receptor Research; 1.3 Recent Progress in Nuclear Receptor Drug Discovery; 1.3.1 SERMs; 1.3.2 Selective GR Modulators1.3.3 Other Modulator Efforts: PR, MR, AR, PPAR, FXR and LXR1.4 Modern Methods and Technologies in Nuclear Receptor Drug Discovery; 1.4.1 Cofactor Interaction Screening; 1.4.2 Microarray Technology and Gene Expression Profiling; 1.4.3 Novel Computational Methods; 1.4.4 Structural Biology; 1.5 Summary and Future Developments; References; 2 Targeting the Nuclear Receptor-Cofactor Interaction; 2.1 Introduction; 2.2 Evaluation of the Nuclear Receptor-Cofactor Interaction as a Drug Target; 2.2.1 Evaluation of the ER-Coactivator Interaction; 2.2.2 Evaluation of the AR-Coactivator Interaction2.3 Inhibitors of the Nuclear Receptor-Cofactor Interaction2.3.1 Phage Display Peptides; 2.3.2 Nonnatural Cyclic Peptides; 2.3.3 Small Molecules; 2.4 Perspectives; References; 3 Untangling the Estrogen Receptor Web: Tools to Selectively Study Estrogen-Binding Receptors; 3.1 Physiological Roles of Estrogen and the Challenges in Drug Discovery; 3.2 Possibility of Multiple Targets; 3.3 ERα; 3.3.1 Discovery and Characterization; 3.3.2 Expression Patterns and Response to Known Drugs; 3.3.3 Physiological Roles of ERα; 3.4 ERβ; 3.4.1 Discovery and Characterization3.4.2 Expression Patterns and Response to Known Drugs3.4.3 Possible Physiological Roles of ERβ; 3.5 ERR; 3.5.1 Discovery and Characterization; 3.5.2 Expression Patterns and Response to Known Drugs; 3.5.3 Possible Physiological Roles of ERRs; 3.6 GPR30; 3.6.1 Discovery and Characterization; 3.6.2 Expression Patterns and Response to Known Drugs; 3.6.3 Possible Physiological Roles of GPR30; 3.6.4 Controversies Over GPR30; 3.7 Membrane ERs; 3.8 Integrated Estrogen Signaling; 3.9 Conclusions; References; 4 Subtype-Selective Estrogens; 4.1 Introduction; 4.1.1 Biology of the Estrogen Receptors4.1.2 Interaction of ERα and ERβ with Ligands4.2 Subtype-Selective ER Ligands; 4.2.1 ERα Agonists; 4.2.1.1 Six-Membered Heterocycles; 4.2.1.2 Five-Membered Heterocycles; 4.2.1.3 Bicyclononene Ring Systems; 4.2.1.4 Steroidal ERα Agonists; 4.2.2 ERβ Agonists; 4.2.2.1 Diaryl-Ethylenes, Imidazoles, Isoxazoles and Thiophenes; 4.2.2.2 Bicyclic 6+6 Ring Systems; 4.2.2.3 Bicyclic [6+5]-Ring Systems; 4.2.2.4 Tricycles; 4.2.2.5 Tetracyclics; 4.2.2.6 Steroidal ERβ-Selective Estrogens; 4.2.2.7 Miscellaneous ERβ Ligands; 4.2.3 ERα-Selective Antagonists; 4.2.3.1 Triphenylethylenes; 4.2.3.2 Benzothiophenes4.2.3.3 IndolesEdited by two experts working at the pioneering pharmaceutical company and major global player in hormone-derived drugs, this handbook and reference systematically treats the drug development aspects of all human nuclear receptors, including recently characterized receptors such as PPAR, FXR and LXR. Authors from leading pharmaceutical companies around the world present examples and real-life data from their own work.Methods and principles in medicinal chemistry.Drug receptorsNuclear receptors (Biochemistry)Drug targetingDrug receptors.Nuclear receptors (Biochemistry)Drug targeting.615.7Ottow E(Eckhard),1953-992990Weinmann Hilmar992991MiAaPQMiAaPQMiAaPQBOOK9910144109203321Nuclear receptors as drug targets2273854UNINA