Estrogen receptors alpha (ERα) and beta (ERβ): Subtype-selective ligands and clinical potential

被引：544
作者：
Paterni, Ilaria [1 ]
Granchi, Carlotta [1 ]
Katzenellenbogen, John A. [2 ]
Minutolo, Filippo [1 ]
机构：
[1] Univ Pisa, Dipartimento Farm, I-56126 Pisa, Italy
[2] Univ Illinois, Dept Chem, Urbana, IL 61801 USA
来源：
STEROIDS | 2014年 / 90卷
基金：
美国国家卫生研究院;
关键词：
Estrogen receptor subtype alpha; Estrogen receptor subtype beta; Modulators; Agonists; Antagonists; Therapeutic applications; SOY ISOFLAVONE GENISTEIN; ACID PHENETHYL ESTER; BREAST-CANCER CELLS; IN-VIVO; PROSTATE-CANCER; ALZHEIMERS-DISEASE; MULTIFUNCTIONAL MEDICINES; BIOLOGICAL-ACTIVITIES; POSTMENOPAUSAL WOMEN; OVARIECTOMIZED RATS;
D O I：
10.1016/j.steroids.2014.06.012
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Estrogen receptors alpha (ER alpha) and beta (ER beta) are nuclear transcription factors that are involved in the regulation of many complex physiological processes in humans. Modulation of these receptors by prospective therapeutic agents is currently being considered for prevention and treatment of a wide variety of pathological conditions, such as, cancer, metabolic and cardiovascular diseases, neurodegeneration, inflammation, and osteoporosis. This review provides an overview and update of compounds that have been recently reported as modulators of ERs, with a particular focus on their potential clinical applications. (C) 2014 Elsevier Inc. All rights reserved.
引用
收藏
页码：13 / 29
页数：17
相关论文
共 168 条
[1]   Mutation of the palmitoylation site of estrogen receptor α in vivo reveals tissue-specific roles for membrane versus nuclear actions [J].
Adlanmerini, Marine ;
Solinhac, Romain ;
Abot, Anne ;
Fabre, Aurelie ;
Raymond-Letron, Isabelle ;
Guihot, Anne-Laure ;
Boudou, Frederic ;
Sautier, Lucile ;
Vessieres, Emilie ;
Kim, Sung Hoon ;
Liere, Philippe ;
Fontaine, Coralie ;
Krust, Andree ;
Chambon, Pierre ;
Katzenellenbogen, John A. ;
Gourdy, Pierre ;
Shaul, Philip W. ;
Henrion, Daniel ;
Arnal, Jean-Francois ;
Lenfant, Francoise .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2014, 111 (02) :E283-E290
[2]  
Ahmed Marwa A, 2012, Int J Physiol Pathophysiol Pharmacol, V4, P156
[3]   The estradiol pharmacophore: Ligand structure-estrogen receptor binding affinity relationships and a model for the receptor binding site [J].
Anstead, GM ;
Carlson, KE ;
Katzenellenbogen, JA .
STEROIDS, 1997, 62 (03) :268-303
[4]   The Estrogen Receptor-α Is Required and Sufficient to Maintain Physiological Glucose Uptake in the Mouse Heart [J].
Arias-Loza, Paula-Anahi ;
Kreissl, Michael C. ;
Kneitz, Susanne ;
Kaiser, Franz R. ;
Israel, Ina ;
Hu, Kai ;
Frantz, Stefan ;
Bayer, Barbara ;
Fritzemeier, Karl-Heinz ;
Korach, Kenneth S. ;
Pelzer, Theo .
HYPERTENSION, 2012, 60 (04) :1070-+
[5]   Estrogenic hormone action in the heart: regulatory network and function [J].
Babiker, FA ;
De Windt, LJ ;
van Eickels, M ;
Grohe, C ;
Meyer, R ;
Doevendans, PA .
CARDIOVASCULAR RESEARCH, 2002, 53 (03) :709-719
[6]   Genistein ameliorates learning and memory deficits in amyloid β(1-40) rat model of Alzheimer's disease [J].
Bagheri, Maryam ;
Joghataei, Mohammad-Taghi ;
Mohseni, Simin ;
Roghani, Mehrdad .
NEUROBIOLOGY OF LEARNING AND MEMORY, 2011, 95 (03) :270-276
[7]   Neuroprotective effect of silymarin in 6-hydroxydopamine hemi-parkinsonian rat: Involvement of estrogen receptors and oxidative stress [J].
Baluchnejadmojarad, Tourandokht ;
Roghani, Mehrdad ;
Mafakheri, Mehdi .
NEUROSCIENCE LETTERS, 2010, 480 (03) :206-210
[8]   Dietary-induced ERβ upregulation counteracts intestinal neoplasia development in intact male ApcMin/+ mice [J].
Barone, Michele ;
Tanzi, Sabina ;
Lofano, Katia ;
Scavo, Maria Principia ;
Pricci, Maria ;
Demarinis, Lucia ;
Papagni, Samanta ;
Guido, Raffaella ;
Maiorano, Eugenio ;
Ingravallo, Giuseppe ;
Comelli, Maria Cristina ;
Francavilla, Antonio ;
Di Leo, Alfredo .
CARCINOGENESIS, 2010, 31 (02) :269-274
[9]   Selective and potent agonists for estrogen receptor beta derived from molecular refinements of salicylaldoximes [J].
Bertini, Simone ;
De Cupertinis, Andrea ;
Granchi, Carlotta ;
Bargagli, Barbara ;
Tuccinardi, Tiziano ;
Martinelli, Adriano ;
Macchia, Marco ;
Gunther, Jillian R. ;
Carlson, Kathryn E. ;
Katzenellenbogen, John A. ;
Minutolo, Filippo .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2011, 46 (06) :2453-2462
[10]   Medicarpin, a legume phytoalexin, stimulates osteoblast differentiation and promotes peak bone mass achievement in rats: evidence for estrogen receptor β-mediated osteogenic action of medicarpin [J].
Bhargavan, Biju ;
Singh, Divya ;
Gautam, Abnish K. ;
Mishra, Jay Sharan ;
Kumar, Amit ;
Goel, Atul ;
Dixit, Manish ;
Pandey, Rashmi ;
Manickavasagam, Lakshmi ;
Dwivedi, Shailendra D. ;
Chakravarti, Bandana ;
Jain, Girish K. ;
Ramachandran, Ravishankar ;
Maurya, Rakesh ;
Trivedi, Arun ;
Chattopadhyay, Naibedya ;
Sanyal, Sabyasachi .
JOURNAL OF NUTRITIONAL BIOCHEMISTRY, 2012, 23 (01) :27-38
12345678910