Journal ArticleDOI
Estrogen Signaling through the Transmembrane G Protein–Coupled Receptor GPR30
Eric R. Prossnitz,Jeffrey B. Arterburn,Jeffrey B. Arterburn,Harriet O. Smith,Tudor I. Oprea,Larry A. Sklar,Helen J. Hathaway +6 more
TLDR
An overview of the evidence for the cellular and physiological actions of GPR30 in estrogen-dependent processes and the relationship of G PR30 with classical estrogen receptors is provided.Abstract:
Steroids play an important role in the regulation of normal physiology and the treatment of disease. Steroid receptors have classically been described as ligand-activated transcription factors mediating long-term genomic effects in hormonally regulated tissues. It is now clear that steroids also mediate rapid signaling events traditionally associated with growth factor receptors and G protein–coupled receptors. Although evidence suggests that the classical steroid receptors are capable of mediating many of these events, more recent discoveries reveal the existence of transmembrane receptors capable of responding to steroids with cellular activation. One such receptor, GPR30, is a member of the G protein–coupled receptor superfamily and mediates estrogen-dependent kinase activation as well as transcriptional responses. In this review, we provide an overview of the evidence for the cellular and physiological actions of GPR30 in estrogen-dependent processes and discuss the relationship of GPR30 with classica...read more
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Thresholds for therapies: highlights of the St Gallen International Expert Consensus on the Primary Therapy of Early Breast Cancer 2009
TL;DR: The 11th St Gallen expert consensus meeting on the primary treatment of early breast cancer in March 2009 maintained an emphasis on targeting adjuvant systemic therapies according to subgroups defined by predictive markers, acknowledging the role of risk factors with the caveat that risk per se is not a target.
Journal ArticleDOI
The G-protein-coupled estrogen receptor GPER in health and disease
TL;DR: The physiological roles of GPER are highlighted in the reproductive, nervous, endocrine, immune and cardiovascular systems, as well as its pathological roles in a diverse array of disorders including cancer, for which GPER is emerging as a novel therapeutic target and prognostic indicator.
Journal ArticleDOI
The mammalian ovary from genesis to revelation
TL;DR: Two major functions of the mammalian ovary are the production of germ cells (oocytes), which allow continuation of the species, and the generation of bioactive molecules, primarily steroids and progestins and peptide growth factors, which are critical for ovarian function, regulation of the hypothalamic-pituitary-ovarian axis, and development of secondary sex characteristics.
Journal ArticleDOI
Hypertension Renin–Angiotensin–Aldosterone System Alterations
TL;DR: Animal studies support the existence of protective aminopeptidase A-Ang III-Ang II type 2 receptor and ACE2-Ang-(1 to 7)-Mas receptor arms, paving the way for multiple new treatment options for resistant hypertension.
Journal ArticleDOI
In vivo effects of a GPR30 antagonist
Megan K. Dennis,Ritwik Burai,Chinnasamy Ramesh,Whitney K. Petrie,Sara N Alcon,Tapan K. Nayak,Cristian Bologa,Andrei Leitão,Eugen Brailoiu,Elena Deliu,Nae J. Dun,Larry A. Sklar,Helen J. Hathaway,Jeffrey B. Arterburn,Jeffrey B. Arterburn,Tudor I. Oprea,Eric R. Prossnitz +16 more
TL;DR: In vivo administration of G15 reveals that GPR30 contributes to both uterine and neurological responses initiated by estrogen, and the identification and characterization of a G-1 analog, G15, that binds to G PR30 with high affinity and acts as an antagonist of estrogen signaling through GPR28.
References
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Journal ArticleDOI
Effects of chemotherapy and hormonal therapy for early breast cancer on recurrence and 15-year survival: an overview of the randomised trials
O. Abe,R. Abe,K. Enomoto,K. Kikuchi,H. Koyama,H. Masuda,Y. Nomura,K. Sakai,K. Sugimachi,T. Tominaga,J. Uchino,M. Yoshida,J. L. Haybittle,C Davies,V. J. Harvey,T. M. Holdaway,R. G. Kay,B. H. Mason,John F. Forbes,Nicholas Wilcken,M. Gnant,Raimund Jakesz,M. Ploner,H. M. A. Yosef,C. Focan,J. P. Lobelle,U. Peek,G. D. Oates,Janet T. Powell,M. Durand,L. Mauriac,A. Di Leo,Stella Dolci,M.J. Piccart,M. B. Masood,D. Parker,J. J. Price,Pierre Hupperets,Sue Jackson,Joseph Ragaz,Donna L. Berry,Gloria Broadwater,C. Cirrincione,Hyman B. Muss,Larry Norton,Raymond B. Weiss,H. Abu-Zahra,S. M. Portnoj,Michael J. Baum,Jack Cuzick,Joan Houghton,David Riley,N. H. Gordon,H. L. Davis,A. Beatrice,J. Mihura,A. Naja,Y. Lehingue,P. Romestaing,J. B. Dubois,Thierry Delozier,J. Mace-Lesec'h,P. Rambert,O. Andrysek,J. Barkmanova,Julie Owen,P. Meier,A Howell,G. C. Ribeiro,R. Swindell,R Alison,J Boreham,Matthew Clarke,Rory Collins,Sarah C. Darby,P. Elphinstone,Vaughan Evans,Jon Godwin,Richard Gray,C. S. Harwood,C. Hicks,Spencer L. James,Elizabeth MacKinnon,Paul McGale,Theresa McHugh,Graham M. Mead,Richard Peto,Yisong Wang,J. Albano,C. F. de Oliveira,H. Gervasio,J. Gordilho,H Johansen,Henning T. Mouridsen,Rebecca Gelman,J.R. Harris,I. C. Henderson,Charles L. Shapiro,K. W. Andersen,C. K. Axelsson,M. Blichert-Toft,S. Moller,Jens Overgaard,Marie Overgaard,Carsten Rose,B. Cartensen,T. Palshof,H. J. Trampisch,Otilia Dalesio,E.G.E. de Vries,Sjoerd Rodenhuis,H. van Tinteren,R. L. Comis,Nancy E. Davidson,Nicholas J. Robert,George W. Sledge,Douglass C. Tormey,William C. Wood,David Cameron,Udi Chetty,P. Forrest,W. Jack,J. Rossbach,Jan G. M. Klijn,A. D. Treurniet-Donker,W. L. J. van Putten,Alberto Costa,Umberto Veronesi,H. Bartelink,L. Duchateau,C. Legrand,RJ Sylvester,J.A. van der Hage,C.J.H. van de Velde,M. P. Cunningham,R. Catalano,R. H. Creech,Jacques Bonneterre,P. Fargeot,Pierre Fumoleau,Pierre Kerbrat,Moïse Namer,Walter Jonat,Manfred Kaufmann,Martin Schumacher,G. von Minckwitz,G. Bastert,H. Rauschecker,R. Sauer,Willi Sauerbrei,A.J. Schauer,A. de Schryver,L. Vakaet,M. Belfiglio,A. Nicolucci,F. Pellegrini,M. Sacco,M. Valentini,C. S. McArdle,D. C. Smith,E. Galligioni,Francesco Boccardo,AU Rubagotti,D. M. Dent,C. A. Gudgeon,A. Hacking,A. Erazo,J. Y. Medina,M. Izuo,Y. Morishita,H. Takei,I.S. Fentiman,John L. Hayward,R D Rubens,D. Skilton,H. Graeff,Fritz Jänicke,C. Meisner,H. R. Scheurlen,D. von Fournier,Urania Dafni,G. Fountzilas,P. Klefstrom,Carl Blomqvist,T. Saarto,R. Margreiter,Bernard Asselain,R. J. Salmon,J. R. Vilcoq,Rodrigo Arriagada,Christopher Hill,A. Laplanche,M. G. Le,M. Spielmann,Paolo Bruzzi,E. Montanaro,R. Rosso,M. R. Sertoli,M. Venturini,Dino Amadori,J. Benraadt,M. Kooi,A. O. van de Velde,J. A. van Dongen,J. B. Vermorken,Monica Castiglione,F. Cavalli,A. S. Coates,J. Collins,JF Forbes,Richard D. Gelber,A. Goldhirsch,J. Lindtner,Karen N. Price,C. M. Rudenstam,H.-J. Senn,Judith M Bliss,Clair Chilvers,R. C. Coombes,Emma Hall,Michel Marty,R. V. Borovik,G. Brufman,H. Hayat,E. Robinson,N. Wigler,Gianni Bonadonna,T. Camerini,G. De Palo,M. Del Vecchio,F. Formelli,Pinuccia Valagussa,A Martoni,F. Pannuti,G. Cocconi,A. Colozza,R. Camisa,K. Aogi,S. Takashima,T. Ikeda,K. Inokuchi,K. Sawa,H. Sonoo,S. Korzeniowski,J. Skolyszewski,M. Ogawa,J. Yamashita,J. Bonte,R. Christiaens,Robert Paridaens,W. Van den Boegart,P. Martin,S. Romain,T. Hakes,Clifford A. Hudis,R. Wittes,G. Giokas,D. Kondylis,B. Lissaios,R. de la Huerta,M. G. Sainz,R. Altemus,K. Cowan,David N. Danforth,Allen S. Lichter,Marc E. Lippman,Joyce A. O'Shaughnessy,Lori J. Pierce,Seth M. Steinberg,D. Venzon,JoAnne Zujewski,A. Paradiso,M. De Lena,F. Schittulli,J. Myles,J. L. Pater,Kathleen I. Pritchard,Stewart J. Anderson,G. Bass,Anna Brown,John Bryant,J. Costantino,James J. Dignam,Bernard Fisher,C Redmond,Sam Wieand,Norman Wolmark,I. M. Jackson,Mike K. Palmer,JN Ingle,Vera J. Suman,Nils-Olof Bengtsson,H. Jonsson,Lars-Gunnar Larsson,J. P. Lythgoe,M. Kissin,Bjørn Erikstein,E Hannisdal,A. B. Jacobsen,J. E. Varhaug,S. Gundersen,Martin Hauer-Jensen,H. Host,R. Nissen-Meyer,Roger W. Blamey,A. Mitchell,Morgan Da,J.F.R. Robertson,M. Di Palma,G. Mathe,J. L. Misset,R. M. Clark,Mitch Levine,K Morimoto,Y. Takatsuka,E. Crossley,Al Harris,Denis Talbot,Mark Taylor,B. di Blasio,V. Ivanov,Vladimir Semiglazov,J. Brockschmidt,M. R. Cooper,H. Ueo,Carla I. Falkson,Roger A'Hern,Stanley W. Ashley,T. J. Powles,Ian E. Smith,John Yarnold,J.-C. Gazet,N. Cocoran,N. Deshpande,L. di Martino,P. Douglas,A. Lindtner,G Notter,A. J. S. Bryant,G. H. Ewing,L. A. Firth,J. L. Krushen-Kosloski,L. Foster,W.D. George,Helen J. Stewart,P. Stroner,Per-Uno Malmström,Torgil Möller,Stefan Rydén,Ingrid Tengrup,Lena Tennvall-Nittby,J. Carstenssen,M. Dufmats,Thomas Hatschek,Bo Nordenskjöld,Martin Söderberg,John T. Carpenter,KS Albain,J. Crowley,Stuart A. Green,Silvana Martino,CK Osborne,Peter M. Ravdin,U. Glas,Ulla Johansson,L E Rutqvist,T. Singnomklao,Arne Wallgren,Rudolf Maibach,Beat Thürlimann,Hermann Brenner,A. Hercbergs,M Yoshimoto,Gerrit DeBoer,Alexander H.G. Paterson,JW Meakin,T. Panzarella,Y. Shan,Y. F. Shao,X. Wang,D. B. Zhao,Z. M. Chen,H. C. Pan,J. Bahi,M. Reid,M. Spittle,G. P. Deutsch,F. Senanayake,D. L. W. Kwong,Angelo Raffaele Bianco,Chiara Carlomagno,M. De Laurentiis,S. De Placido,Aman U. Buzdar,Tae C Smith,Jonas Bergh,Lars Holmberg,Göran Liljegren,Jan Nilsson,M. Seifert,P. Sevelda,C. C. Zielinsky,R. B. Buchanan,M. Cross,G.T. Royle,Janet A. Dunn,Robert Kerrin Hills,Michael Lee,J. M. Morrison,D. Spooner,A. Litton,Rowan T. Chlebowski,H. Caffier +412 more
TL;DR: The 10-year and 15-year effects of various systemic adjuvant therapies on breast cancer recurrence and survival are reported and it is found that the cumulative reduction in mortality is more than twice as big at 15 years as at 5 years after diagnosis.
Journal ArticleDOI
Cloning of a novel receptor expressed in rat prostate and ovary.
TL;DR: It is concluded that clone 29 cDNA encodes a novel rat ER, which is suggested be named rat ERbeta to distinguish it from the previously cloned ER (ERalpha) from rat uterus.
Journal ArticleDOI
Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta
George G.J.M. Kuiper,Bo Carlsson,Kaj Grandien,Eva Enmark,Johan Häggblad,Stefan K. Nilsson,Jan-Åke Gustafsson +6 more
TL;DR: The messenger RNA expression of both ER subtypes in rat tissues by RT-PCR is investigated and the ligand binding specificity of the ER sub types is compared, revealing a single binding component for 16β-estradiol with high affinity.
Journal ArticleDOI
Molecular basis of agonism and antagonism in the oestrogen receptor.
Andrzej M. Brzozowski,Ashley C. W. Pike,Zbigniew Dauter,Roderick E. Hubbard,Tomas Bonn,Owe Engström,Lars Öhman,Geoffrey L. Greene,Jan-Åke Gustafsson,Mats Carlquist +9 more
TL;DR: The crystal structures of the LBD of ER in complex with the endogenous oestrogen, 17β-oestradiol, and the selective antagonist raloxifene provide a molecular basis for the distinctive pharmacophore of the ER and its catholic binding properties.
Journal ArticleDOI
A transmembrane intracellular estrogen receptor mediates rapid cell signaling.
TL;DR: It is found that of all G protein–coupled receptors characterized to date, GPR30 is uniquely localized to the endoplasmic reticulum, where it specifically binds estrogen and fluorescent estrogen derivatives.