Literature DB >> 21921919

Development of subtype-selective oestrogen receptor-based therapeutics.

Stefan Nilsson1, Konrad F Koehler, Jan-Åke Gustafsson.   

Abstract

The two oestrogen receptor subtypes α and β are hormone-regulated modulators of intracellular signalling and gene expression. Regulation of oestrogen receptor activity is crucial not only for development and homeostasis but also for the treatment of various diseases and symptoms. Classical selective oestrogen receptor modulators are well established in the treatment of breast cancer and osteoporosis, but emerging data suggest that the development of subtype-selective ligands that specifically target either oestrogen receptor-α or oestrogen receptor-β could be a more optimal approach for the treatment of cancer, cardiovascular disease, multiple sclerosis and Alzheimer's disease.

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Year:  2011        PMID： 21921919     DOI： 10.1038/nrd3551

Source DB:  PubMed          Journal:  Nat Rev Drug Discov        ISSN： 1474-1776            Impact factor:   84.694


  137 in total

Review 1.  Principles for modulation of the nuclear receptor superfamily.

Authors:  Hinrich Gronemeyer; Jan-Ake Gustafsson; Vincent Laudet
Journal:  Nat Rev Drug Discov       Date:  2004-11       Impact factor: 84.694

2.  Estrogen induces vascular wall dilation: mediation through kinase signaling to nitric oxide and estrogen receptors alpha and beta.

Authors:  Xiaomei Guo; Mahnaz Razandi; Ali Pedram; Ghassan Kassab; Ellis R Levin
Journal:  J Biol Chem       Date:  2005-03-11       Impact factor: 5.157

3.  Abnormal vascular function and hypertension in mice deficient in estrogen receptor beta.

Authors:  Yan Zhu; Zhao Bian; Ping Lu; Richard H Karas; Lin Bao; Daniel Cox; Jeffrey Hodgin; Philip W Shaul; Peter Thoren; Oliver Smithies; Jan-Ake Gustafsson; Michael E Mendelsohn
Journal:  Science       Date:  2002-01-18       Impact factor: 47.728

4.  On the size of the active site in proteases. I. Papain.

Authors:  I Schechter; A Berger
Journal:  Biochem Biophys Res Commun       Date:  1967-04-20       Impact factor: 3.575

5.  Striatin assembles a membrane signaling complex necessary for rapid, nongenomic activation of endothelial NO synthase by estrogen receptor alpha.

Authors:  Qing Lu; David C Pallas; Howard K Surks; Wendy E Baur; Michael E Mendelsohn; Richard H Karas
Journal:  Proc Natl Acad Sci U S A       Date:  2004-11-29       Impact factor: 11.205

6.  Genistein induced apoptotic cell death in adult T-cell leukemia cells through estrogen receptors.

Authors:  Masao Yamasaki; Ayako Mukai; Masayo Ohba; Yoshihiro Mine; Yoichi Sakakibara; Masahito Suiko; Kazuhiro Morishita; Kazuo Nishiyama
Journal:  Biosci Biotechnol Biochem       Date:  2010-10-07       Impact factor: 2.043

7.  Estrogen receptor beta-selective agonists stimulate calcium oscillations in human and mouse embryonic stem cell-derived neurons.

Authors:  Lili Zhang; Brigitte E Blackman; Marcus D Schonemann; Tatjana Zogovic-Kapsalis; Xiaoyu Pan; Mary Tagliaferri; Heather A Harris; Isaac Cohen; Renee A Reijo Pera; Synthia H Mellon; Richard I Weiner; Dale C Leitman
Journal:  PLoS One       Date:  2010-07-27       Impact factor: 3.240

8.  Response-specific and ligand dose-dependent modulation of estrogen receptor (ER) alpha activity by ERbeta in the uterus.

Authors:  Jonna Frasor; Daniel H Barnett; Jeanne M Danes; Rex Hess; Albert F Parlow; Benita S Katzenellenbogen
Journal:  Endocrinology       Date:  2003-07       Impact factor: 4.736

9.  Serum heat shock protein 70 levels predict the development of atherosclerosis in subjects with established hypertension.

Authors:  Alan G Pockley; Anastasia Georgiades; Thomas Thulin; Ulf de Faire; Johan Frostegård
Journal:  Hypertension       Date:  2003-08-04       Impact factor: 10.190

10.  Oestrogen receptor beta ligand: a novel treatment to enhance endogenous functional remyelination.

Authors:  Daniel K Crawford; Mario Mangiardi; Bingbing Song; Rhusheet Patel; Sienmi Du; Michael V Sofroniew; Rhonda R Voskuhl; Seema K Tiwari-Woodruff
Journal:  Brain       Date:  2010-09-21       Impact factor: 13.501
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  90 in total

1.  Nonsteroidal selective androgen receptor modulators and selective estrogen receptor β agonists moderate cognitive deficits and amyloid-β levels in a mouse model of Alzheimer's disease.

Authors:  Sonia George; Géraldine H Petit; Gunnar K Gouras; Patrik Brundin; Roger Olsson
Journal:  ACS Chem Neurosci       Date:  2013-09-25       Impact factor: 4.418

Review 2.  Insights into rapid modulation of neuroplasticity by brain estrogens.

Authors:  Deepak P Srivastava; Kevin M Woolfrey; Peter Penzes
Journal:  Pharmacol Rev       Date:  2013-09-27       Impact factor: 25.468

Review 3.  Minireview: dynamic structures of nuclear hormone receptors: new promises and challenges.

Authors:  S Stoney Simons; Dean P Edwards; Raj Kumar
Journal:  Mol Endocrinol       Date:  2013-11-27

Review 4.  Perimenopause as a neurological transition state.

Authors:  Roberta D Brinton; Jia Yao; Fei Yin; Wendy J Mack; Enrique Cadenas
Journal:  Nat Rev Endocrinol       Date:  2015-05-26       Impact factor: 43.330

5.  Targeted estrogen delivery reverses the metabolic syndrome.

Authors:  Brian Finan; Bin Yang; Nickki Ottaway; Kerstin Stemmer; Timo D Müller; Chun-Xia Yi; Kirk Habegger; Sonja C Schriever; Cristina García-Cáceres; Dhiraj G Kabra; Jazzminn Hembree; Jenna Holland; Christine Raver; Randy J Seeley; Wolfgang Hans; Martin Irmler; Johannes Beckers; Martin Hrabě de Angelis; Joseph P Tiano; Franck Mauvais-Jarvis; Diego Perez-Tilve; Paul Pfluger; Lianshan Zhang; Vasily Gelfanov; Richard D DiMarchi; Matthias H Tschöp
Journal:  Nat Med       Date:  2012-11-11       Impact factor: 53.440

6.  Synthesis and biological evaluation of two agents for imaging estrogen receptor β by positron emission tomography: challenges in PET imaging of a low abundance target.

Authors:  Jae Hak Lee; Olaf Peters; Lutz Lehmann; Carmen S Dence; Terry L Sharp; Kathryn E Carlson; Dong Zhou; M Jeyakumar; Michael J Welch; John A Katzenellenbogen
Journal:  Nucl Med Biol       Date:  2012-06-30       Impact factor: 2.408

7.  In silico prediction of chemical mechanism of action via an improved network-based inference method.

Authors:  Zengrui Wu; Weiqiang Lu; Dang Wu; Anqi Luo; Hanping Bian; Jie Li; Weihua Li; Guixia Liu; Jin Huang; Feixiong Cheng; Yun Tang
Journal:  Br J Pharmacol       Date:  2016-11-01       Impact factor: 8.739

8.  In search of novel drug target sites on estrogen receptors using RNA aptamers.

Authors:  Daiying Xu; Vamsee-Krishna Chatakonda; Antonis Kourtidis; Douglas S Conklin; Hua Shi
Journal:  Nucleic Acid Ther       Date:  2014-03-03       Impact factor: 5.486

9.  Thiophene-core estrogen receptor ligands having superagonist activity.

Authors:  Jian Min; Pengcheng Wang; Sathish Srinivasan; Jerome C Nwachukwu; Pu Guo; Minjian Huang; Kathryn E Carlson; John A Katzenellenbogen; Kendall W Nettles; Hai-Bing Zhou
Journal:  J Med Chem       Date:  2013-04-15       Impact factor: 7.446

10.  Interaction of 14-3-3 proteins with the estrogen receptor alpha F domain provides a drug target interface.

Authors:  Ingrid J De Vries-van Leeuwen; Daniel da Costa Pereira; Koen D Flach; Sander R Piersma; Christian Haase; David Bier; Zeliha Yalcin; Rob Michalides; K Anton Feenstra; Connie R Jiménez; Tom F A de Greef; Luc Brunsveld; Christian Ottmann; Wilbert Zwart; Albertus H de Boer
Journal:  Proc Natl Acad Sci U S A       Date:  2013-05-15       Impact factor: 11.205
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