Computational Characterization and Prediction of Estrogen Receptor Coactivator Binding Site Inhibitors

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ISBN 13 :
Total Pages : 52 pages
Book Rating : 4.:/5 (316 download)

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Book Synopsis Computational Characterization and Prediction of Estrogen Receptor Coactivator Binding Site Inhibitors by : Brian J. Bennion

Download or read book Computational Characterization and Prediction of Estrogen Receptor Coactivator Binding Site Inhibitors written by Brian J. Bennion and published by . This book was released on 2005 with total page 52 pages. Available in PDF, EPUB and Kindle. Book excerpt: Many carcinogens have been shown to cause tissue specific tumors in animal models. The mechanism for this specificity has not been fully elucidated and is usually attributed to differences in organ metabolism. For heterocyclic amines, potent carcinogens that are formed in well-done meat, the ability to either bind to the estrogen receptor and activate or inhibit an estrogenic response will have a major impact on carcinogenicity. Here we describe our work with the human estrogen receptor alpha (hERa) and the mutagenic/carcinogenic heterocyclic amines PhIP, MeIQx, IFP, and the hydroxylated metabolite of PhIP, N2-hydroxy-PhIP. We found that PhIP, in contrast to the other heterocyclic amines, increased cell-proliferation in MCF-7 human breast cancer cells and activated the hERa receptor. We show mechanistic data supporting this activation both computationally by homology modeling and docking, and by NMR confirmation that PhIP binds with the ligand binding domain (LBD). This binding competes with estradiol (E2) in the native E2 binding cavity of the receptor. We also find that other heterocyclic amines and N2-hydroxy-PhIP inhibit ER activation presumably by binding into another cavity on the LBD. Moreover, molecular dynamics simulations of inhibitory heterocyclic amines reveal a disruption of the surface of the receptor protein involved with protein-protein signaling. We therefore propose that the mechanism for the tissue specific carcinogenicity seen in the rat breast tumors and the presumptive human breast cancer associated with the consumption of well-done meat maybe mediated by this receptor activation.

Characterization and Coloning of an Estrogen Receptor Coactivator

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Publisher :
ISBN 13 :
Total Pages : 252 pages
Book Rating : 4.:/5 (392 download)

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Book Synopsis Characterization and Coloning of an Estrogen Receptor Coactivator by : Shlomit Halachmi

Download or read book Characterization and Coloning of an Estrogen Receptor Coactivator written by Shlomit Halachmi and published by . This book was released on 1996 with total page 252 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Design and Synthesis of Estrogen Receptor Coactivator Binding Inhibitors

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ISBN 13 :
Total Pages : pages
Book Rating : 4.:/5 (931 download)

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Book Synopsis Design and Synthesis of Estrogen Receptor Coactivator Binding Inhibitors by :

Download or read book Design and Synthesis of Estrogen Receptor Coactivator Binding Inhibitors written by and published by . This book was released on 2004 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:

Chemoinformatics Approaches to Structure- and Ligand-Based Drug Design, Volume II

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Publisher : Frontiers Media SA
ISBN 13 : 2889766314
Total Pages : 325 pages
Book Rating : 4.8/5 (897 download)

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Book Synopsis Chemoinformatics Approaches to Structure- and Ligand-Based Drug Design, Volume II by : Adriano D. Andricopulo

Download or read book Chemoinformatics Approaches to Structure- and Ligand-Based Drug Design, Volume II written by Adriano D. Andricopulo and published by Frontiers Media SA. This book was released on 2022-07-27 with total page 325 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Nuclear Hormone Receptors

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Publisher :
ISBN 13 :
Total Pages : 434 pages
Book Rating : 4.3/5 (91 download)

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Book Synopsis Nuclear Hormone Receptors by : Malcolm G. Parker

Download or read book Nuclear Hormone Receptors written by Malcolm G. Parker and published by . This book was released on 1991 with total page 434 pages. Available in PDF, EPUB and Kindle. Book excerpt: An overview of the supergene family made up of those nuclear hormone receptors which recognize thyroid and steroid hormones, vitamen D and retinoic acid and which are characterized by their ability to bind both ligands and the genes which respond to them.

The Heterogeneity of Cancer Metabolism

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Publisher : Springer
ISBN 13 : 331977736X
Total Pages : 186 pages
Book Rating : 4.3/5 (197 download)

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Book Synopsis The Heterogeneity of Cancer Metabolism by : Anne Le

Download or read book The Heterogeneity of Cancer Metabolism written by Anne Le and published by Springer. This book was released on 2018-06-26 with total page 186 pages. Available in PDF, EPUB and Kindle. Book excerpt: Genetic alterations in cancer, in addition to being the fundamental drivers of tumorigenesis, can give rise to a variety of metabolic adaptations that allow cancer cells to survive and proliferate in diverse tumor microenvironments. This metabolic flexibility is different from normal cellular metabolic processes and leads to heterogeneity in cancer metabolism within the same cancer type or even within the same tumor. In this book, we delve into the complexity and diversity of cancer metabolism, and highlight how understanding the heterogeneity of cancer metabolism is fundamental to the development of effective metabolism-based therapeutic strategies. Deciphering how cancer cells utilize various nutrient resources will enable clinicians and researchers to pair specific chemotherapeutic agents with patients who are most likely to respond with positive outcomes, allowing for more cost-effective and personalized cancer therapeutic strategies.

Glucocorticoid Signaling

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Publisher : Springer
ISBN 13 : 1493928953
Total Pages : 387 pages
Book Rating : 4.4/5 (939 download)

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Book Synopsis Glucocorticoid Signaling by : Jen-Chywan Wang

Download or read book Glucocorticoid Signaling written by Jen-Chywan Wang and published by Springer. This book was released on 2015-07-27 with total page 387 pages. Available in PDF, EPUB and Kindle. Book excerpt: This timely volume provides a comprehensive overview of glucocorticoids and their role in regulating many aspects of physiology and their use in the treatment of disease. The book is broken into four sections that begin by giving a general introduction to glucocorticoids and a brief history of the field. The second section will discuss the effects of glucocorticoids on metabolism, while the third section will cover the effects of glucocorticoids on key tissues. The final section will discuss general topics, such as animal models in glucocorticoid research and clinical implications of glucocorticoid research. Featuring chapters from leaders in the field, this volume will be of interest to both researchers and clinicians.

Resveratrol in Health and Disease

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Publisher : CRC Press
ISBN 13 : 142002647X
Total Pages : 714 pages
Book Rating : 4.4/5 (2 download)

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Book Synopsis Resveratrol in Health and Disease by : Bharat B. Aggarwal

Download or read book Resveratrol in Health and Disease written by Bharat B. Aggarwal and published by CRC Press. This book was released on 2005-11-01 with total page 714 pages. Available in PDF, EPUB and Kindle. Book excerpt: Practicing evidenced-based medicine some 25 centuries ago, Hippocrates proclaimed "Let food be thy medicine and medicine be thy food." This advice parallels the common American saying, "You are what you eat," and is supported by a National Institute of Health recommendation to consume as many as eight servings of fruits and vegetables daily to prev

The Fish Oocyte

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Publisher : Springer Science & Business Media
ISBN 13 : 1402062354
Total Pages : 513 pages
Book Rating : 4.4/5 (2 download)

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Book Synopsis The Fish Oocyte by : Patrick J. Babin

Download or read book The Fish Oocyte written by Patrick J. Babin and published by Springer Science & Business Media. This book was released on 2007-08-17 with total page 513 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents a comprehensive overview on egg production in fish, from the standpoint of the oocyte. It covers oocyte development, maturation, hydration and fertilization. The book places special emphasis on using state-of-the-art tools for discerning the ultra-structure of the follicle and genomic/proteomic tools to fully understand biological basis of fish reproduction.

Computer-assisted Drug Design

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Publisher :
ISBN 13 :
Total Pages : 648 pages
Book Rating : 4.3/5 (91 download)

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Book Synopsis Computer-assisted Drug Design by : Edward C. Olson

Download or read book Computer-assisted Drug Design written by Edward C. Olson and published by . This book was released on 1979 with total page 648 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Molecular Docking

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Publisher : BoD – Books on Demand
ISBN 13 : 1789233542
Total Pages : 190 pages
Book Rating : 4.7/5 (892 download)

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Book Synopsis Molecular Docking by : Dimitrios Vlachakis

Download or read book Molecular Docking written by Dimitrios Vlachakis and published by BoD – Books on Demand. This book was released on 2018-07-11 with total page 190 pages. Available in PDF, EPUB and Kindle. Book excerpt: Molecular docking has always been and will be on the forefront of developments in the eminent field of drug design and medicinal chemistry. At the early days, drug discovery was based on blackboard drawings and expert intuition. However, as times move on, the amount of available information and overall knowledge base that needs to be analyzed cannot be processed manually. This, coupled by the rapid growth in computational infrastructure and processing power, has allowed for the efficient use of molecular docking tools and algorithms to be considered in the greater field of drug discovery. In the postgenomic era, molecular docking has become the key player for the screening of hundreds of thousands of compounds against a repertoire of pharmacological targets.

Cyclized Helical Peptides

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Publisher : John Wiley & Sons
ISBN 13 : 3527343423
Total Pages : 242 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Cyclized Helical Peptides by : Zigang Li

Download or read book Cyclized Helical Peptides written by Zigang Li and published by John Wiley & Sons. This book was released on 2021-08-23 with total page 242 pages. Available in PDF, EPUB and Kindle. Book excerpt: An important and timely guide to the progress being made on constrained helical peptides Constraint helical peptides have emerged as a solution to target previously undruggable protein-protein interactions, which feature large and complex surfaces. Cyclized Helical Peptides: Synthesis, Properties and Therapeutic Applications offers a review of the most current methodologies of constructing constrained helices. The authors noted experts on the topic include the information on the fundamental features of cyclized helical peptides and discuss their limitations. The book summarizes and explores the effects of chemical methods constructing helical peptides on helicity, binding affinity, cell penetration, and nonspecific toxicity. The book examines the therapeutic applications of the constraint helices and includes comparison with existing small molecule modulators or antibodies. Designed as a useful resource for both those outside and inside the field. Those new to the field will find a comprehensive introduction to cyclized helical peptide and those inside the field will find a deeper understanding of the topic. This important book: Offers a practical introduction to constrained helical peptides Includes all aspects of constrained helical peptides Includes information on the most recent methods that have emerged Presents a guide to help solve practical problems in the field Written for academics, pharmaceutical professional, Cyclized Helical Peptides is a comprehensive guide to the developments of constrained helical peptides.

The Female Brain

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Publisher : Harmony
ISBN 13 : 0767928415
Total Pages : 306 pages
Book Rating : 4.7/5 (679 download)

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Book Synopsis The Female Brain by : Louann Brizendine, MD

Download or read book The Female Brain written by Louann Brizendine, MD and published by Harmony. This book was released on 2007-08-07 with total page 306 pages. Available in PDF, EPUB and Kindle. Book excerpt: Since Dr. Brizendine wrote The Female Brain ten years ago, the response has been overwhelming. This New York Times bestseller has been translated into more than thirty languages, has sold nearly a million copies between editions, and has most recently inspired a romantic comedy starring Whitney Cummings and Sofia Vergara. And its profound scientific understanding of the nature and experience of the female brain continues to guide women as they pass through life stages, to help men better understand the girls and women in their lives, and to illuminate the delicate emotional machinery of a love relationship. Why are women more verbal than men? Why do women remember details of fights that men can’t remember at all? Why do women tend to form deeper bonds with their female friends than men do with their male counterparts? These and other questions have stumped both sexes throughout the ages. Now, pioneering neuropsychiatrist Louann Brizendine, M.D., brings together the latest findings to show how the unique structure of the female brain determines how women think, what they value, how they communicate, and who they love. While doing research as a medical student at Yale and then as a resident and faculty member at Harvard, Louann Brizendine discovered that almost all of the clinical data in existence on neurology, psychology, and neurobiology focused exclusively on males. In response to the overwhelming need for information on the female mind, Brizendine established the first clinic in the country to study and treat women’s brain function. In The Female Brain, Dr. Brizendine distills all her findings and the latest information from the scientific community in a highly accessible book that educates women about their unique brain/body/behavior. The result: women will come away from this book knowing that they have a lean, mean, communicating machine. Men will develop a serious case of brain envy.

Estrogen Receptor and Breast Cancer

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Publisher : Humana Press
ISBN 13 : 9783030075934
Total Pages : 432 pages
Book Rating : 4.0/5 (759 download)

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Book Synopsis Estrogen Receptor and Breast Cancer by : Xiaoting Zhang

Download or read book Estrogen Receptor and Breast Cancer written by Xiaoting Zhang and published by Humana Press. This book was released on 2019-11-08 with total page 432 pages. Available in PDF, EPUB and Kindle. Book excerpt: The discovery of ER by Dr. Elwood Jensen exactly 60 years ago has not only led to the birth of a whole new vital nuclear receptor research field but also made a rapid, direct and lasting impact on the treatment and prevention of breast cancer. Since that landmark discovery, tremendous progress has been made in our understanding of the molecular functions of ER and development of targeted therapies against ER pathways for breast cancer treatment. However, there is currently no book available addressing these discoveries and recent advancement in a historical and systematic fashion. This book is intended to provide comprehensive, most up-to-date information on the history and recent advancement of ER and breast cancer by world renowned leaders in the field. These chapters include the history of the discovery of ER; physiological and pathological roles of ER; recent discovery of ER cistrome, transcriptome and its regulation of noncoding RNAs such as microRNAs and enhancer RNAs in breast cancer; development and clinical practices of the first targeted therapy Tamoxifen and other antiestrogens for breast cancer treatment; structural basis of ER and antiestrogen actions; molecular insights into endocrine resistance; the role of ER mutants, ER-beta and environmental estrogens in breast cancer; and emerging state-of-the-art therapeutic approaches currently in development to overcome treatment resistance and future perspectives. The book will provide undergraduate and graduate students, basic scientists and clinical cancer researchers, residents, fellows, as well as clinicians, oncology educators and the general public a thorough and authoritative review of these exciting topics.

Mechanisms of Insulin Action

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Publisher : Springer Science & Business Media
ISBN 13 : 0387722041
Total Pages : 223 pages
Book Rating : 4.3/5 (877 download)

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Book Synopsis Mechanisms of Insulin Action by : Alan R. Saltiel

Download or read book Mechanisms of Insulin Action written by Alan R. Saltiel and published by Springer Science & Business Media. This book was released on 2007-10-05 with total page 223 pages. Available in PDF, EPUB and Kindle. Book excerpt: More than 18 million people in the United States have diabetes mellitus, and about 90% of these have the type 2 form of the disease. This book attempts to dissect the complexity of the molecular mechanisms of insulin action with a special emphasis on those features of the system that are subject to alteration in type 2 diabetes and other insulin resistant states. It explores insulin action at the most basic levels, through complex systems.

Index Medicus

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Publisher :
ISBN 13 :
Total Pages : 1436 pages
Book Rating : 4.:/5 (319 download)

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Book Synopsis Index Medicus by :

Download or read book Index Medicus written by and published by . This book was released on 2002 with total page 1436 pages. Available in PDF, EPUB and Kindle. Book excerpt: Vols. for 1963- include as pt. 2 of the Jan. issue: Medical subject headings.

Natural Products Isolation

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Publisher : Springer Science & Business Media
ISBN 13 : 1592599559
Total Pages : 518 pages
Book Rating : 4.5/5 (925 download)

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Book Synopsis Natural Products Isolation by : Satya D. Sarker

Download or read book Natural Products Isolation written by Satya D. Sarker and published by Springer Science & Business Media. This book was released on 2008-02-05 with total page 518 pages. Available in PDF, EPUB and Kindle. Book excerpt: The term “natural products” spans an extremely large and diverse range of chemical compounds derived and isolated from biological sources. Our interest in natural products can be traced back thousands of years for their usefulness to humankind, and this continues to the present day. Compounds and extracts derived from the biosphere have found uses in medicine, agriculture, cosmetics, and food in ancient and modern societies around the world. Therefore, the ability to access natural products, understand their usefulness, and derive applications has been a major driving force in the field of natural product research. The first edition of Natural Products Isolation provided readers for the first time with some practical guidance in the process of extraction and isolation of natural products and was the result of Richard Cannell’s unique vision and tireless efforts. Unfortunately, Richard Cannell died in 1999 soon after completing the first edition. We are indebted to him and hope this new edition pays adequate tribute to his excellent work. The first edition laid down the “ground rules” and established the techniques available at the time. Since its publication in 1998, there have been significant developments in some areas in natural product isolation. To capture these developments, publication of a second edition is long overdue, and we believe it brings the work up to date while still covering many basic techniques known to save time and effort, and capable of results equivalent to those from more recent and expensive techniques.