The Nuclear Receptor Facts: Book PDF
Preview The Nuclear Receptor Facts: Book
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SanDiego San Francisco New York Boston London Sydney Tokyo This bookis printedonacid-freepaper. Copyright©2002 byACADEMIC PRESS All Rights Reserved. No partof this publicationmaybe reproduced ortransmittedin any form orby any means, electronicormechanical, includingphotocopying, recording, orany information storageand retrieval system, withoutpermissionin writingfrom the publisher. AcademicPress A division ofHarcourt, Inc. Harcourt Place, 32Jamestown Road, London NW1 7BY, UK http://www.academicpress.com AcademicPress A division ofHarcourt, Inc. 525 BStreet, Suite 1900, SanDiego, California92101-4495, USA http://www.academicpress.com ISBN0-12-437735-1 Acataloguerecordfor thisbookis availablefrom the British Library LibraryofCongress CatalogCard Number: 2001096534 Typeset byMackrethMedia Services, HemelHempstead, UK PrintedinGreat BritainbyCPIBookcraft 01 02 03 04 05 BC 9 8 7 6 5 4 3 2 1 Preface Multicellular organisms require specific intercellular communication to organize properly the complex body plan during embryogenesis, and maintain the physiological properties and functions during the entire life. Signaling through nuclear receptors is a major signal transduction paradigm invented by metazoans to provide a plethora of intra- and intercellular communication networks. Nuclear receptors constitute a large family of ligand-inducible transcription factors that regulate gene-initiated programs at the basis ofa multitude of (patho)physiological phenomena. They act by (1) responding directly to a large variety of hormonal and metabolic signals; (2) integrating diverse signaling pathways as nuclear receptors are themselves targets of post-translational modifications; and (31 regulating the activities ofothermajorsignallingcascades (calledsignal transduction crosstalk). This book is intended to provide a comprehensive summary of the current knowledge of the mechanism(s) of action of this important class of transcription regulatory receptors which are of major importance for research in a large number of areas related to animal development and physiology, medicine, and pharmacological drug development. The introductory section is conceptual whilst the major part of the book is an in-depth discussion of each nuclear receptor that provides the readerwith virtuallyall of the data presentlyavailable. Compilation of this book was hard work as the field is vast and evolving rapidly. We are grateful to Pierre Chambon for his critical interest and suggestions. We apologize to all colleagues whose recent data are not considered in this book or whosework is, in spiteofallefforts, mentionedorcitedinadequately. V.L. would like to thank deeply all the members of his laboratory for their patience, kindness and knowledge of nuclear receptors that was extremely useful during the preparation of this book. The help of Jacques Samarut, Frederic Flamant, Pierre Jurdic, Bart Staels, Jamshed Tata, Barbara Demeneix, Gunther Schutz and Frances Sladek for information, criticisms and sharing of unpublished data is also acknowledged. Last but not least, thanks to Catherine Hanni and Palomafor the numerous days ofabsence and to Deniseand EdmondHannifor the old table and the fresh garden of La Bastide where this book was written. Work from V.L.'s laboratory is supported by the Centre National de la Recherche Scientifique, Ecole Normale Superieure de Lyon, Ministere de l'Education Nationale, de la Recherche et de laTechnologie, Association pourla Recherche sur Ie Cancer, Fondation pour la Recherche Medicale, Ligue Nationale contre Ie Cancer, and Region Rhone-Alpes. V.L. also thanks the Institut Universitaire de Francefor support. H.G. thanks all the members of his laboratory for their patience, support and help while this book was being prepared. Work in the laboratory was supportedby the Association for International Cancer Research, Association pour la Recherche surIe Cancer, Fondation pour la Recherche Medicale, Institut National de la Sante et de la Recherche Medicale, the Centre National de la Recherche Scientifique, the HopitalUniversitaire deStrasbourgand Bristol-Myers Squibb. The authors hope that there are a minimum of omissions and inaccuracies and that these can be recitified in later editions. We would appreciate if such points • -==-------- ----------------- were forwarded to the Editor, Nuclear Receptor FactsBook, Academic Press, 32 Jamestown Road, London NWI 7BY, UK. Vincent Lauder • Abbreviations 4-ABB 4-amino butyl benzoate AD activatingdomain ADH alcoholdehydrogenase 3-AEB 3-amino ethylbenzoate AEV avian erythroblastosisvirus AF activationfunction AHC adrenal hypoplasiacongenita AlB amplifiedinbreastcancer AML acute myeloidleukemia AP activatingprotein aP2 adipocytefatty acid-bindingprotein2 APC adenomatous polyposis coli APL acutepromyelocyticleukemia ApoB apolipoprotein B AR androgen receptor ARC activator-recruitedcofactor ARE androgenresponse element ARF adipocyte regulatoryfactor Arp apoAI regulatoryprotein ASC-2 activatingsignal cointegrator-2 ATF-2 activatingtranscriptionfactor 2 BAR bileacid receptor bp basepair BCAR breast cancerantiestrogen resistance BMP bonemorphogeneticprotein BRL49653 rosiglitazone CaMKIV Ca2+/calmodulin-dependentprotein kinase IV CAR constitutivelyactive receptor, constitutive androstane receptor CARLA coactivator-dependentreceptorligandassay CBP CREB-bindingprotein CDK cyclin-dependent kinase C/EBP CAAT/enhancerbindingprotein CEF chicken embryo fibroblasts CGP52608 1-(3-ally1-4-oxothiazolidine-2-ylidene)-4-methylthio semicarbazone CIP CBP-interactingprotein CMV cytomegalovirus CNS centralnervous system CoRNRbox corepressornuclear receptorbox COUP-TF chickenovalbuminupstreampromotertranscriptionfactor COX-2 cyclooxygenase-2 9C-RA 9-cis retinoicacid CRABP cellularretinoicacidbindingprotein CRALBP cellularretinaldehydebindingprotein • _L _ ~ I CRBPI cellularretinalbindingproteinI CREB cyclicAMP response elementbindingfactor CREM cyclicAMP response elementmodulatorprotein CRH corticotrophin-releasingprotein CRSP cofactorrequired for Spi activation CTE C-terminal extension CYP cytochrome P450 3D three-dimensional DBD DNA-bindingdomain p,p'-DDE 1,I-dichloro-2,2-bis(p-chlorophenyl)ethylene DES diethylstilbestrol DHEA dihydroepiandrosterone DHR Drosophila hormone receptor DHT dihydrotestosterone DIMIT 3,5-dimethyl-3'-isopropylthyronine dpc days post-coitum DR direct repeat DRIP vitamin D receptor interactingproteincomplement DSF dissatisfaction DSS dosage-sensitive sex reversal 20E 20-hydroxyecdysone E2F E2factor EBI089 I-25-dihyroxy-22,24-diene-24,27-trihomovitaminD EBV Epstein-Barrvirus EC embryonal carcinoma EcR ecdysone receptor EcRE ecdysone receptorresponse element EGF epidermalgrowthfactor ELP embryonal LTR-bindingprotein EMS ethylmethanesulfonate EMSA electrophoretic mobilityshift assay ER estrogen receptor, evertedrepeat ERA-I early retinoicacid-inducedF9 teratocarcinomastem cellgenel ERE estrogen response element ERM ets related member ERR estrogen receptorrelatedreceptor ES embryonicstem EST expressedsequencetag FAAR fatty acid-activated receptor FGR familial glucocorticoidresistance FISH fluorescent in situ hybridization FPPS farnesyl pyrophosphatesynthase FRET fluorescence energy transfer FSH follicle-stimulating hormone FTF a-fetoprotein transcriptionfactor FTZ-FI fushi tarazu-factor 1 FXR farnesoid receptor GAL galactose GCNF germ cellnuclearfactor • - - ---------------------------' G-CSF granulocytecolony-stimulatingfactor GM-CSF granulocyte-macrophagecolony-stimulatingfactor GFP greenfluorescent protein GH growth hormone GHF growthhormone-specific transcriptionfactor GnRH gonadotrophin-releasinghormone GR glucocorticoidreceptor GRE glucocorticoidresponse element GRF GCNF-relatedfactor GRIP glucocorticoidreceptor interactingprotein GST glutathione S-transferase HAT histone acetyltransferase HBV hepatitisBvirus HDAC histone deacetylase HETE hydroxyeicosatetraenoicacid HHG hypogonadotropichypogonadism HIV humanimmunodeficiencyvirus HMG high motilitygroup proteins HNF4 hepatocytenuclearfactor 4 HODE hydroxyoctadecadienoicacid HPA hypothalamic-pituitary-adrenal hpf hours post-fertilization HPV humanpapillomavirus H-2RIIBP H-2 region IIbindingprotein HRE hormone receptorresponse element Hsp heat-shockprotein HSV herpes simplexvirus IBABP ilealbile acidbindingprotein IGF insulin-likegrowthfactor IGFBP insulin-likegrowthfactor bindingprotein IL interleukin IR3 3 bp-spacedinvertedrepeats IKB inhibitorofNFKB JAK Janus kinase JH juvenilehormone JNK Jun N-terminal kinase LBD ligand-bindingdomain LBP ligand-bindingpocket LH luteinizinghormone LPL lipoproteinlipase LRH liverreceptorhomologous protein LT leukotriene LTR longterminalrepeat LXR liverX receptor MAP mitogen-activatedprotein MAPK mitogen-activatedproteinkinase MCAD medium-chainacylcoenzymeAdehydroenase MED mediator (multiproteincomplexinvolvedin transcription activation) • _L-- _ MHC majorhistocompatibility complex mHMG-CoAS mitochondrial hydroxymethylglutaryl-CoAsynthase MIS Mullerianinhibitingsubstance MKK mitogen-activatedproteinkinase MLP majorlatepromoter MMTV mouse mammary tumorvirus MoMLV Moloney murineleukaemiavirus MOZ monocyticzincfinger MR mineralocorticoidreceptor NAT negative regulator ofactivated transcription NBFI-B nervegrowthfactor-induced B NBRE NGFI-B response element NCNF neuronalcellnuclearfactor NCoR nuclearreceptorcorepressor NFAT nuclearfactor ofactivatedcells NFKB nuclearfactor KB (a transcriptionfactor) NHR nuclearhormone receptor NIDDM non-insulin-dependentdiabetes mellitus NIX neural interactingfactor NLS nuclearlocalizationsignal NMDA N-methyl-D-asparticacid NMR nuclearmagnetic resonance NPM nuclearphosphoproteinnucleophosmin. NR nuclearreceptor NRE negative regulatory element NRIF3 nuclearreceptorinteractingfactor3 NRRE nuclearreceptorresponsive element NSAID non-steroidalanti-inflammatorydrug NSD-l NR-bindingSET-domaincontainingprotein NTCP Na+/taurocholate-cotransportingpeptide NUT subunitof the yeast mediatorcomplex OCT 22-oxa-la,25-dihydroxyvitaminD 3 Oct octamer-bindingprotein 1,25(OHh-D l,25-dihydroxyvitaminD 3 3 OHT hydroxy-tamoxifen OR orphanreceptor p300 paralogofCBP PAL palindrome pal palindromicelement PAR pregnane-activatedreceptor PARP poly(ADP-ribose) polymerase PB phenobarbital PBP PPAR-bindingprotein PC2 positivecoactivator2 P/CAF p300/CREBbindingprotein [CBP]-associatedfactor P/CIP p300/CBP/co-integrator-associatedprotein PCN pregnenolone 16-carbonitrile PCR polymerase chainreaction PDB protein database in Brookhaven III - - - - - - - - - PEPCK phosphoenolpyruvatecarboxykinase PCC peroxisomeproliferator-activatedreceptorgammacoactivator PKA proteinkinase A PKB proteinkinase B PLTP phospholipidtransferprotein PML promyelocyticleukemia PNMT phenylethanolamineN-methyltransferase PNR photoreceptor-specificnuclearreceptor PNRC proline-richnuclearreceptorcoregulatoryprotein POD PMLoncogenic domain POMC pro-opiomelanocortine PPAR peroxisomeproliferator-activatedreceptor PPARE peroxisomeproliferator-activatedreceptorresponse element PPRE peroxisomeproliferatorresponse element PR progesteronereceptor PRF pre-fingerregion PSA prostate-specificantigen PSU petmutantsuppressor PTH parathyroidhormone PTHrP parathyroidhormone-relatedpeptide PXR pregnaneXreceptor RA retinoicacid RAC3 receptor-associatedcoactivator3 RACE rapid amplificationofcDNAends RAP250 nuclearreceptoractivatingprotein250 RAR retinoicacidreceptor RARE retinoicacidreceptorresponse element Rb retinoblastoma RE response element RevRE Rev-erb response element RIP receptorinteractingprotein RLD rat liver-derived RNR retina-specific nuclearreceptor ROR RAR-relatedorphanreceptor RORE ROR response element RT reverse transcriptase RTR retinoidreceptor-relatedtestis-associatedreceptor RU Roussel-Uclafcompound (RUisfollowedbyanumber) RXR retinoidXreceptor RXRE retinoidXreceptorresponse element SERM selective estrogenreceptor modulators SET homologous domain inSu(var)3-9, enhancerofzesteand trithorax SF steroidogenicfactor SFRE SF-I response element SHP shortheterodimerpartner SMCC Srband mediatorprotein-containingcomplex SMRT silencingmediatorofrepressedtranscription SRA steroidreceptorRNA activator StAR steroidogenicacute regulatoryprotein •
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