LEADER 05227nam 2200673Ia 450 001 9910144109203321 005 20170809153157.0 010 $a1-281-94720-2 010 $a9786611947200 010 $a3-527-62329-9 010 $a3-527-62330-2 035 $a(CKB)1000000000552742 035 $a(EBL)481431 035 $a(SSID)ssj0000212698 035 $a(PQKBManifestationID)11175620 035 $a(PQKBTitleCode)TC0000212698 035 $a(PQKBWorkID)10139458 035 $a(PQKB)10124067 035 $a(MiAaPQ)EBC481431 035 $a(OCoLC)299046803 035 $a(PPN)242769438 035 $a(EXLCZ)991000000000552742 100 $a20080410d2008 uy 0 101 0 $aeng 135 $aur|n|---||||| 181 $ctxt 182 $cc 183 $acr 200 00$aNuclear receptors as drug targets /$fedited by Eckhard Ottow and Hilmar Weinmann 210 $aWeinheim $cWiley-VCH$dc2008 215 $a1 online resource (524 p.) 225 1 $aMethods and principles in medicinal chemistry 300 $aDescription based upon print version of record. 311 $a3-527-31872-0 320 $aIncludes bibliographical references and index. 327 $aNuclear 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 Modulators 327 $a1.3.3 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 Interaction 327 $a2.3 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 ER?; 3.3.1 Discovery and Characterization; 3.3.2 Expression Patterns and Response to Known Drugs; 3.3.3 Physiological Roles of ER?; 3.4 ER?; 3.4.1 Discovery and Characterization 327 $a3.4.2 Expression Patterns and Response to Known Drugs3.4.3 Possible Physiological Roles of ER?; 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 Receptors 327 $a4.1.2 Interaction of ER? and ER? with Ligands4.2 Subtype-Selective ER Ligands; 4.2.1 ER? 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 ER? Agonists; 4.2.2 ER? 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 ER?-Selective Estrogens; 4.2.2.7 Miscellaneous ER? Ligands; 4.2.3 ER?-Selective Antagonists; 4.2.3.1 Triphenylethylenes; 4.2.3.2 Benzothiophenes 327 $a4.2.3.3 Indoles 330 $aEdited by two experts working at the pioneering pharmaceutical company and major global player in hormone-derived drugs, this handbook and reference systematically treats the drug development aspects of all human nuclear receptors, including recently characterized receptors such as PPAR, FXR and LXR. Authors from leading pharmaceutical companies around the world present examples and real-life data from their own work. 410 0$aMethods and principles in medicinal chemistry. 606 $aDrug receptors 606 $aNuclear receptors (Biochemistry) 606 $aDrug targeting 615 0$aDrug receptors. 615 0$aNuclear receptors (Biochemistry) 615 0$aDrug targeting. 676 $a615.7 701 $aOttow$b E$g(Eckhard),$f1953-$0992990 701 $aWeinmann$b Hilmar$0992991 801 0$bMiAaPQ 801 1$bMiAaPQ 801 2$bMiAaPQ 906 $aBOOK 912 $a9910144109203321 996 $aNuclear receptors as drug targets$92273854 997 $aUNINA