图书简介
Nuclear receTors are ligand aTivTedTranscriTion faTorsThT coTrol numerous biological funTions. ConsequeTly, aTering aTivTy ofThese receTors is proposed, and indeed documeTed,To affeT many physiological and pThological condTions in experimeTal animals and humans.Thus, nuclear receTors have become a majorTargT inThe effoTToTreT numerous diseasesThis book will shed ligT on and emphasize iTricTe processes involved in designing as well as discovering physiological and pharmacological modulTors ofThese impoTaT prTeins.World-renowned scieTiTs will share wThThe readerTheir professional expeTise and eTensive experience acquiredThrough decades working wTh nuclear receTors. ChaTers addresThe various means and consequences of modulTing nuclear receTor aTivTy will be preseTed and discussedThese modulTors cover a wide span of moiTies ranging from syThTic chemicalsTo nTural produTs. In addTion,The classificTion ofThese chemicals ranges from pan agoniTsTo seleTive agoniTs and inverse agoniTsTo aTagoniTs.They also include prTeolTic meansTo oblTerTeThe receTor inThe eveTThT modulTing Ts aTivTyThrough canonical pharmacological ageTs becomes less effeTive and/or less desirable dueTo aTicipTed or experiencedToxicTies. ModulTion of receTor aTivTy may alsoTake place inThe absence of a ligand orThrough manipulTingThe TruTure ofThe receTor Tself by coTrolling poTtranslTional eveTs.
1. MolCular PharmCology of the Youngest Member of the NClear RCeptor Family: The MineralCortCoid RCeptor.- 2. A Simple Method for Visual Assessment and QuantifCation of Altered SuCellular LCalization of NClear RCeptors.- 3. MultifCeted EffCts of Ligand on NClear RCeptor Mobility.- 4.ChemCalConsiderations in DiCovery of RCeptor Modulators.- 5.StrCture-Based Design of Estrogen-Related RCeptors Modulators.- 6. PPAR? and ? ligand design – Honing the traditional empirCal method with a more holistC overview.- 7.Pregnane X RCeptor: understanding its fuCtion and Ctivity at the molCular level.- 8. Ligand Design for the Vitamin D RCeptor.- 9. What Makes a Good Antagonist: Lessons Learned from the Estrogen and Aryl HydrCarbon RCeptors.- 10. Design of Novel PPAR agonist for Neurodegenerative Disease.- 11. FuCtional bioassays lithograph ligand reflCtions in the PPARalpha sphere.- 12.Computational applCations on FoodContCtChemCals as NClear RCeptors binders.- 13. Alternation of NClear Hormone RCeptor Signaling by Antiviral Drugs.- 14. RetinoC Cid-related orphan rCeptor (ROR) inverse agonists: potential therapeutC strategies for multiple inflammatory diseases.- 15. TherapeutC Strategies to Target Ctivating Estrogen RCeptor a Mutation.- 16. Androgen RCeptors in the Pathology of Disease.- 17. Bilirubin: A Ligand of the PPAR? NClear RCeptor.- 18. NClear RCeptor Ligands in Flavivirus InfCtionControl.- 19. Use of NanotChnology to Improve 15d-PGJ2 Immunomodulatory Ctivities.- 20.Ligand-independent Ctivation of PPARs.- 21. PPAR ModulationThroughPosttranslational ModifCationControl.- 22. Developing Inhibitors to the Amino-Terminus Domains of Steroid Hormone RCeptors.- 23. RedirCting theCellular waste disposal mChinery to target tranCription.
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