Nuclear Receptors

Author : Mostafa Z. Badr
Publisher : Springer Nature
Page : 676 pages
File Size : 40,8 Mb
Release : 2021-09-28
Category : Medical
ISBN : 9783030783150

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Nuclear Receptors by Mostafa Z. Badr Pdf

Nuclear receptors are ligand activated transcription factors that control numerous biological functions. Consequently, altering activity of these receptors is proposed, and indeed documented, to affect many physiological and pathological conditions in experimental animals and humans. Thus, nuclear receptors have become a major target in the effort to treat numerous diseases. This book will shed light on and emphasize intricate processes involved in designing as well as discovering physiological and pharmacological modulators of these important proteins. World-renowned scientists will share with the reader their professional expertise and extensive experience acquired through decades working with nuclear receptors. Chapters address the various means and consequences of modulating nuclear receptor activity will be presented and discussed. These modulators cover a wide span of moieties ranging from synthetic chemicals to natural products. In addition, the classification of these chemicals ranges from pan agonists to selective agonists and inverse agonists to antagonists. They also include proteolytic means to obliterate the receptor in the event that modulating its activity through canonical pharmacological agents becomes less effective and/or less desirable due to anticipated or experienced toxicities. Modulation of receptor activity may also take place in the absence of a ligand or through manipulating the structure of the receptor itself by controlling posttranslational events.

Author : Iain J. McEwan,Raj Kumar
Publisher : Springer
Page : 236 pages
File Size : 46,7 Mb
Release : 2015-08-20
Category : Medical
ISBN : 9783319187297

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Nuclear Receptors: From Structure to the Clinic by Iain J. McEwan,Raj Kumar Pdf

Nuclear Receptors focuses on the structural analysis of nuclear receptors from the initial work using isolated protein domains to the more recent exciting developments investigating the conformational shape of full-length receptor complexes. The book also reviews the structure of key nuclear receptor co-regulatory proteins. It brings together, for the first time, a comprehensive review of nuclear receptor structure and the importance of receptor conformation underpinning allosteric regulation by different ligands (hormone, drugs, DNA response elements, protein-protein interactions) and receptor activity. The nuclear receptor superfamily, including receptors for steroid hormones and non-steroid ligands, are pivotal to normal physiology, regulating processes as diverse as reproduction, metabolism, the immune system and brain development. The first members of the family were cloned over 25 years ago, which heralded in the idea of a superfamily of intracellular receptor proteins that bound small molecule ligands: classical steroid hormones, vitamins, fatty acids and other products of metabolism. These signals are then transmitted through multiprotein receptor-DNA complexes, leading to the regulation of target genes, often in a cell-selective manner. The cloning of the receptor cDNAs also ushered in an era of unparalleled analysis of the mechanisms of action of these ligand-activated transcription factors. ​

Author : Didier Picard
Publisher : OUP Oxford
Page : 306 pages
File Size : 47,8 Mb
Release : 1999-07-08
Category : Science
ISBN : 9780191565922

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Nuclear Receptors by Didier Picard Pdf

The steroid / nuclear receptor superfamily is a large and growing group of transcription factors that are studied by a large and varied number of basic and clinical researchers. The first two chapters describe the evolutionary biology of the superfamily and explain how to clone and characterize new receptors. Chapter 3 shows how to identify the ligands of novel receptors and chapter 4 explains the kinetic analysis of receptor interactions. In chapter 5, the reader is guided through the functional characterization of coactivators using microinjection. The next section covers receptor phosphorylation, ligand regulated transcription, and hormone resistance syndromes. Chapter 9 describes the in vitro assembly of Hsp90 complexes and chapter 10 explains yeast as a model system for looking at receptor function. The final chapter shows how heterologous proteins can be regulated by fusion to the hormone binding domain of a receptor. Nuclear Receptors: A Practical Approach is a comprehensive guide to studying members of the superfamily and will be invaluable to all researchers old and new.

Author : Chris M. Bunce,Moray J. Campbell
Publisher : Springer Science & Business Media
Page : 456 pages
File Size : 46,7 Mb
Release : 2010-03-11
Category : Medical
ISBN : 9789048133031

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Nuclear Receptors by Chris M. Bunce,Moray J. Campbell Pdf

In 1890 a case of myxedema was treated in Lisbon by the implantation of a sheep thyroid gland with the immediate improvement in the patient’s condition. A few years later, medications for the then ill-explained condition of the menopause included tablets made from cow ovaries. In the first quarter of the 20th century the identification of vitamin D, and its sunlight driven production in skin, paved the way to the elimination of rickets as a major medical problem. Twenty years or so later, Sir Vincent Wigglesworth established the endocrine basis of developmental moulting in insects, arguably the most commonly performed animal behaviour on Planet Earth. A paradigm that would unify these disparate observations arose between 1985 and 1987 beginning with the identification of the glucocorticoid receptor and the nuclear receptor super-family. What follows is a timely and positive manifestation of the capacity, productivity and value of international human scientific endeavour. Based on intrigue, lively competition and cooperation a global effort has rapidly fostered a school of biology with widespread ramifications for the understanding of metazoan animals, the human condition and the state of the planet. This book is the first this century to try and capture the spirit of this endeavour, to depict where the field is now and to identify some of the challenges and opportunities for the future.

Author : Anonim
Publisher : Elsevier
Page : 601 pages
File Size : 46,7 Mb
Release : 2003-11-25
Category : Science
ISBN : 9780080497075

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Nuclear Receptors by Anonim Pdf

Nuclear Receptors are inducible transcription factors that mediate complex effects on development, differentiation and homeostasis. They regulate the transcription of their target genes through binding to DNA sequences. *Analysis of Nuclear Receptor Ligands*Structure/Function Analysis of Nuclear Receptors*Analysis of Nuclear Receptor Co-Factors and Chromatin Remodeling

Author : Anonim
Publisher : Unknown
Page : 128 pages
File Size : 55,7 Mb
Release : 2024-06-29
Category : Electronic
ISBN : 9789814476058

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Nuclear Receptor Coregulators and Human Diseases by Anonim Pdf

Author : Vincent Laudet,Hinrich Gronemeyer
Publisher : Gulf Professional Publishing
Page : 486 pages
File Size : 53,5 Mb
Release : 2002
Category : Medical
ISBN : 0124377351

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The Nuclear Receptor FactsBook by Vincent Laudet,Hinrich Gronemeyer Pdf

The FactsBook Series has established itself as the best source of easily accessible and accurate facts about protein groups. They use an easy-to-follow format and are researched and compiled by experts in the field. This Factsbook is devoted to nuclear receptors. The first section presents an introduction and describes the mode of action of the receptors in general. The second section of the book contains detailed entries covering each type of receptor. Entries provide information on: Nomenclature and structure, Isolation, DNA binding properties, Ligands, Expression, Target genes, Knockouts, Disease association, Gene structure, promoter and isoforms, Chromosomal location, Amino acid sequences, Key references

Author : Mostafa Z. Badr
Publisher : Unknown
Page : 314 pages
File Size : 43,9 Mb
Release : 2019
Category : Ligands
ISBN : 1493991965

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Nuclear Receptors by Mostafa Z. Badr Pdf

This volume presents valuable techniques for studying the class of ligand-activated transcription factors known as nuclear receptors. After a brief overview of the history of the field, chapters cover methods to detect the receptors and their mRNAs in various tissues, protocols to characterize nuclear receptor modulators and activities, their signaling and roles in certain pathogenesis, molecular modeling of nuclear receptor-ligand interactions, as well as the utility of informatics in the field of nuclear receptors. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Authoritative and cutting-edge, Nuclear Receptors: Methods and Experimental Protocols seeks to aid researchers working toward furthering our understanding of these vital receptors and their role in numerous pathological conditions.

Author : Anonim
Publisher : Academic Press
Page : 420 pages
File Size : 52,7 Mb
Release : 2017-05-17
Category : Science
ISBN : 9780128021965

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Nuclear Receptors in Development and Disease by Anonim Pdf

Nuclear Receptors in Development and Disease, Volume 125, the latest volume in the Current Topics in Developmental Biology series, covers nuclear receptors in development and disease, and includes contributions from an international board of authors. The book's chapters provide a comprehensive set of reviews that cover such topics as nuclear differentiation and remodeling, evolution of receptors, ligand signaling and neural development. Covers the area of nuclear receptors in development and disease Includes contributions from an International board of authors Provides a comprehensive set of reviews on topics as nuclear differentiation and remodeling, evolution of receptors, ligand signaling and neural developments

Author : Anonim
Publisher : Elsevier
Page : 448 pages
File Size : 44,8 Mb
Release : 2006-11-07
Category : Science
ISBN : 9780080469409

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Nuclear Receptors in Development by Anonim Pdf

A superb compilation of reviews from leading experts in the field of nuclear receptors, volume 16 in the Advances in Developmental Biology series covers the role of different nuclear receptor subfamilies in development, physiology and metabolism. This volume brilliantly reviews how genetic defects in the function of nuclear receptors leads to various developmental defects. Receptors discussed include: thyroid receptors, peroxisome proliferators activated receptors, and retinoic acid receptors. Additionaly, this volume offers an indespesable chapter on the orphan receptors Ftz-F1, COUPs, and RORs in embryonic and postnatal development. * Provides a compilation of reviews of several nuclear receptor subfamilies - such as TRs, PPARs, RARs, the orphan receptors COUP-TFs, RORs, and Ftz-F1 in embryonic and postnatal development. * Offers a detailed section on retinoid receptor signaling * Covers the role of co-repressors and co-activators in modulation of nuclear receptor functions

Author : Thomas P. Burris,Edward R.B. McCabe
Publisher : Academic Press
Page : 437 pages
File Size : 47,5 Mb
Release : 2000-09-06
Category : Medical
ISBN : 9780080917146

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Nuclear Receptors and Genetic Disease by Thomas P. Burris,Edward R.B. McCabe Pdf

Nuclear Receptors and Genetic Disease provides the first compilation of the role of nuclear hormones in health and disease and incorporates the latest breakthroughs in the field. It provides comprehensive reviews of the major receptors prepared by the acknowledged experts in each area. Each chapter provides information on the history, physiology, structure, mechanism of action, genetics, pathophysiology, disease diagnosis, and disease treatment for a particular nuclear receptor. Each chapter also includes a table showing all the known mutations of the respective nuclear receptor with the corresponding clinical disorder. Receptors included in this book are: The Nuclear Receptor Superfamily Thyroid Hormone Receptors Estrogen and Progesterone Receptors The Androgen Receptor DAX-1 and Related Orphan Receptors The Vitamin D Receptor Retinoid Receptors Mineralocorticoid and Glucocorticoid Receptors Hepatocyte Nuclear Factor 4 a Peroxisome Proliferator Activated Receptors Coactivators and Corepressors

Author : Leonard Freedman
Publisher : Springer Science & Business Media
Page : 330 pages
File Size : 41,8 Mb
Release : 2012-12-06
Category : Science
ISBN : 9781461217640

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Molecular Biology of Steroid and Nuclear Hormone Receptors by Leonard Freedman Pdf

Intracellular Receptors: New Instruments for a Symphony of Signals In the late eighteenth century, it was proposed on theoretical grounds that each of the body's organs, beginning with the brain, must be "a factory and laboratory of a specific humor which it returns to the blood", and that these circulating signals "are indispensable for the life of the whole" (Bordeu 1775). During the nineteenth cen tury, some remarkable physiological experiments revealed the actions of humoral factors that affected the for and function of multiple tissues, organs and organ sys tems within the body (Berthold 1849); much later, the chemical and molecular na ture of some of those factors was determined. Against this deep historical backdrop of the founding studies of intercellular signaling, molecular biology sprang into existence a mere forty years ago, rooted in the revelation of regulable gene expression in bacteria. But contemporaneous with those classical analyses of transcriptional regulation of the lactose operon, the mod em era of signal transduction was inaugurated by the identification of cAMP as a second messenger -- an intracellular mediator of hormonal activation of glycogen catabolism (Sutherland and RaIl 1960). Later in that same decade, it emerged that cAMP is a critical signal not only in metazoans, but even in bacteria, where it serves an analogous function as a critical switch that activates expression of genes re quired for catabolism of complex carbon sources, including those of the lactose operon.

Author : Moray J. Campbell,Charlotte L. Bevan
Publisher : Springer Nature
Page : 338 pages
File Size : 52,5 Mb
Release : 2022-09-15
Category : Medical
ISBN : 9783031118364

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Nuclear Receptors in Human Health and Disease by Moray J. Campbell,Charlotte L. Bevan Pdf

This book addresses and dissects the roles and crosstalk mechanisms for the 48 human nuclear receptors (NR) in human health and disease. After a State-of-the-Art introduction by an undisputed and celebrated field leader to provide an overview of the field and its significance, chapters are organized into six sections. The first three sections discuss NR roles in Reproduction & Development, Metabolism and Central Systems. These present to the reader our current understanding of NR signaling in the development and functioning of the reproductive system; the roles in the regulation of energy metabolism; and how NR signaling is more widely integrated into systemic functions from calcium flux to circadian rhythm. The subsequent three sections dissect how aberrant NR functions drive Cancer; how new insights into Genomic Interaction are helping to reveal how NR disruption drives disease; and finally, how Translational Efforts are exploiting this understanding from developing novel NR ligands to establishing how underlying genetic variation impacts NR function. Within these sections the chapters also illustrate emerging understanding of how the epigenome and non-coding genome combine to regulate NR function and impact dysfunction. Increasingly these insights cross-fertilize over cell and disease boundaries and it is unsurprising that NR are being explored in novel and new arenas such as the context of neurological disorders and depression. Thus, there is wide scope for re-purposing of licensed drugs and development of new NR-targeting therapies for a host of conditions and diseases. This unique book brings together many of the leading figures in NR research from across the globe, to discuss emerging roles and their implications for human health and disease. It summarizes the state of the art and shows signposts for future research to further shape this influential field.

Author : Pietro Cozzini,Glen E. Kellogg
Publisher : Royal Society of Chemistry
Page : 191 pages
File Size : 43,5 Mb
Release : 2012
Category : Medical
ISBN : 9781849733649

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Computational Approaches to Nuclear Receptors by Pietro Cozzini,Glen E. Kellogg Pdf

Nuclear receptors (NR) are ligand-induced activated transcription factors that are involved in numerous biological processes. Since the 1990's when the first structures were determined by means of X ray diffraction, the number of NR structures has increased considerably. Moreover several "omics" projects (genomics, pharmcogenomics and proteomics) have opened up great opportunities for the discovery of new targets, the characterization of abnormal protein patterns, the selection of "tailored" drugs and the evaluation of drug efficacy even with a lack of structural data. Furthermore, structure-based drug design, computational methods for in silico screening and nanobiotechnology- based tools are simplifying this time-consuming and money-intensive research of lead compounds and, possibly, new drugs. Biological interactions such as those that occur between a protein and ligand are concerted events where flexible molecules interact. Thus understanding flexibility of large molecules or biological complexes is of primary importance to help define the right model to approximate the reality for drug discovery, virtual screening, food safety analysis, etc. NRs are known as flexible targets, with many structural similarities, in particular for their Ligand Binding Domain: these similarities could be assumed to share behavioural qualities that belong to this class of compounds. Thus to supply a possible, complete and exhaustive answer to questions about the behaviour of NRs, their interactions with new potential drugs, endocrine disruptors such as animal and human food toxins, food additives or industry residuals, it is mandatory to approach the problem from a different point of view: a molecular modelling approach, steered synthesis, and in vitro and in vivo tests, etc. The aim of this book is to provide a state of the art review on investigations into Nuclear Receptors.

Author : Kazuwa Nakao,Nagahiro Minato,Shinji Uemoto
Publisher : Springer
Page : 330 pages
File Size : 52,6 Mb
Release : 2015-10-13
Category : Science
ISBN : 9784431556510

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Innovative Medicine by Kazuwa Nakao,Nagahiro Minato,Shinji Uemoto Pdf

This book is devoted to innovative medicine, comprising the proceedings of the Uehara Memorial Foundation Symposium 2014. It remains extremely rare for the findings of basic research to be developed into clinical applications, and it takes a long time for the process to be achieved. The task of advancing the development of basic research into clinical reality lies with translational science, yet the field seems to struggle to find a way to move forward. To create innovative medical technology, many steps need to be taken: development and analysis of optimal animal models of human diseases, elucidation of genomic and epidemiological data, and establishment of “proof of concept”. There is also considerable demand for progress in drug research, new surgical procedures, and new clinical devices and equipment. While the original research target may be rare diseases, it is also important to apply those findings more broadly to common diseases. The book covers a wide range of topics and is organized into three complementary parts. The first part is basic research for innovative medicine, the second is translational research for innovative medicine, and the third is new technology for innovative medicine. This book helps to understand innovative medicine and to make progress in its realization.