Journal ArticleDOI
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 2: structure-activity relationship studies on the benzopyran scaffold.
Timothy Ivo Richardson,Bryan H. Norman,Charles Willis Lugar,Scott Alan Jones,Yong Wang,Jim D. Durbin,Venkatesh Krishnan,Jeffrey Alan Dodge +7 more
Reads0
Chats0
TLDR
X-ray crystal structures of 5b and a non-selective analog 5c in ERalpha help explain the observed selectivity of the benzopyran platform.About:
This article is published in Bioorganic & Medicinal Chemistry Letters.The article was published on 2007-07-01. It has received 35 citations till now. The article focuses on the topics: Estrogen receptor beta & Benzopyrans.read more
Citations
More filters
Journal ArticleDOI
Evolution And Synthetic Applications Of The Heck-matsuda Reaction: The Return Of Arenediazonium Salts To Prominence
TL;DR: In this paper, the authors highlight the potential and the versatility of arenediazonium salts as viable alternatives to conventional aryl halides and oxygen-based electrophiles for Pd-catalyzed Heck reactions.
Journal ArticleDOI
Estrogen receptor β ligands: Recent advances and biomedical applications
TL;DR: This study provides a detailed review of selective ERβ ligands that have been developed recently and discusses the potential therapeutic applications of these agents in biomedicine.
Journal ArticleDOI
Development and Scale-Up of a Continuous, High-Pressure, Asymmetric Hydrogenation Reaction, Workup, and Isolation
Martin D. Johnson,Scott A. May,Joel R. Calvin,Jacob R. Remacle,James R. Stout,William D. Diseroad,Nikolay Zaborenko,Brian D. Haeberle,Wei-Ming Sun,Michael Miller,John Brennan +10 more
TL;DR: In this paper, a fully continuous process including an asymmetric hydrogenation reaction operating at 70 bar hydrogen, aqueous extraction, and crystallization was designed, developed, and demonstrated at pilot scale.
Journal ArticleDOI
Hormonal Action of Plant Derived and Anthropogenic Non-Steroidal Estrogenic Compounds: Phytoestrogens and Xenoestrogens
Tamás Lóránd,E. Vigh,János Garai +2 more
TL;DR: The endocrine effects of known phytoestrogens and xenoestrogens with special emphasis on molecular structure-activity relationships are reviewed and pharmaceutical estrogen analogues with similar properties (selective estrogen receptor modulators, SERMs) are discussed.
Patent
Nuclear receptor binding agents
James T. Dalton,Christina M. Barrett,Yali He,Seoung-Soo Hong,Duane D. Miller,Michael L. Mohler,Ramesh Narayanan,Zhongzhi Wu +7 more
TL;DR: In this paper, a novel class of selective estrogen receptor modulators (SERMs) were proposed for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.
References
More filters
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
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
ERβ: Identification and characterization of a novel human estrogen receptor
TL;DR: A novel estrogen receptor (hereinafter referred to as ERβ) was cloned using degenerate PCR primers and revealed that ERβ is expressed in human thymus, spleen, ovary and testis, and the level of transactivation by 17β‐estradiol is higher for ERα than for ERβ, which may reflect suboptimal conditions for ER β at thelevel of the ligand, responsive element or cellular context.
Journal ArticleDOI
Structure of the Ligand-Binding Domain of Oestrogen Receptor Beta in the Presence of a Partial Agonist and a Full Antagonist
Ashley C. W. Pike,Andrzej M. Brzozowski,Roderick E. Hubbard,Tomas Bonn,Ann Gerd Thorsell,Owe Engström,Jan Ljunggren,Jan-Åke Gustafsson,Mats Carlquist +8 more
TL;DR: The three‐dimensional structure of the oestrogen receptor beta isoform (ERβ) ligand‐binding domain (LBD) in the presence of the phyto‐oestrogen genistein and the antagonist raloxifene is reported.
Journal ArticleDOI
Tissue Distribution and Quantitative Analysis of Estrogen Receptor-α (ERα) and Estrogen Receptor-β (ERβ) Messenger Ribonucleic Acid in the Wild-Type and ERα-Knockout Mouse
TL;DR: The optimization and use of an RNase protection assay able to detect and distinguish messenger RNA (mRNA) transcripts from both the ERalpha and ERbeta genes in the mouse suggest that the biological functions of the ERbeta protein may be dependent on the presence of ERalpha in certain cell types and tissues.