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Literature DB >> 17034120

Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia.

Bryan H Norman¹, Jeffrey A Dodge, Timothy I Richardson, Peter S Borromeo, Charles W Lugar, Scott A Jones, Keyue Chen, Yong Wang, Gregory L Durst, Robert J Barr, Chahrzad Montrose-Rafizadeh, Harold E Osborne, Robert M Amos, Sherry Guo, Amechand Boodhoo, Venkatesh Krishnan.

Abstract

Benzopyran selective estrogen receptor beta agonist-1 (SERBA-1) shows potent, selective binding and agonist function in estrogen receptor beta (ERbeta) in vitro assays. X-ray crystal structures of SERBA-1 in ERalpha and beta help explain observed beta-selectivity of this ligand. SERBA-1 in vivo demonstrates involution of the ventral prostate in CD-1 mice (ERbeta effect), while having no effect on gonadal hormone levels (ERalpha effect) at 10x the efficacious dose, consistent with in vitro properties of this molecule.

Entities: Chemical Disease Gene Species

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Year: 2006 PMID： 17034120 DOI： 10.1021/jm060491j

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

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Cited

22 in total

1. Selective estrogen receptor modulators regulate stromal proliferation in human benign prostatic hyperplasia by multiple beneficial mechanisms--action of two new agents.

Authors: Rajeev Kumar; Vikas Verma; Amit Sarswat; J P Maikhuri; Ashish Jain; Rajeev K Jain; V L Sharma; Diwakar Dalela; Gopal Gupta
Journal: Invest New Drugs Date: 2010-12-23 Impact factor: 3.850

2. Selective and potent agonists for estrogen receptor beta derived from molecular refinements of salicylaldoximes.

Authors: Simone Bertini; Andrea De Cupertinis; Carlotta Granchi; Barbara Bargagli; Tiziano Tuccinardi; Adriano Martinelli; Marco Macchia; Jillian R Gunther; Kathryn E Carlson; John A Katzenellenbogen; Filippo Minutolo
Journal: Eur J Med Chem Date: 2011-03-23 Impact factor: 6.514

Review 3. Minireview: Estrogen receptor-beta: mechanistic insights from recent studies.

Authors: Bonnie J Deroo; Adrian V Buensuceso
Journal: Mol Endocrinol Date: 2010-04-02

4. Estrogen receptor beta agonist LY500307 fails to improve symptoms in men with enlarged prostate secondary to benign prostatic hypertrophy.

Authors: C G Roehrborn; M E Spann; S L Myers; C R Serviss; L Hu; Y Jin
Journal: Prostate Cancer Prostatic Dis Date: 2014-11-04 Impact factor: 5.554

5. Estrogen receptor β, a regulator of androgen receptor signaling in the mouse ventral prostate.

Authors: Wan-Fu Wu; Laure Maneix; Jose Insunza; Ivan Nalvarte; Per Antonson; Juha Kere; Nancy Yiu-Lin Yu; Virpi Tohonen; Shintaro Katayama; Elisabet Einarsdottir; Kaarel Krjutskov; Yu-Bing Dai; Bo Huang; Wen Su; Margaret Warner; Jan-Åke Gustafsson
Journal: Proc Natl Acad Sci U S A Date: 2017-04-24 Impact factor: 11.205

6. Coupling of receptor conformation and ligand orientation determine graded activity.

Authors: John B Bruning; Alexander A Parent; German Gil; Min Zhao; Jason Nowak; Margaret C Pace; Carolyn L Smith; Pavel V Afonine; Paul D Adams; John A Katzenellenbogen; Kendall W Nettles
Journal: Nat Chem Biol Date: 2010-10-10 Impact factor: 15.040

7. Bibenzyl- and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta.

Authors: Michael Waibel; Meri De Angelis; Fabio Stossi; Karen J Kieser; Kathryn E Carlson; Benita S Katzenellenbogen; John A Katzenellenbogen
Journal: Eur J Med Chem Date: 2009-02-20 Impact factor: 6.514