Nuclear Receptors
Nuclear Receptors

Author: Mostafa Z. Badr

Publisher: Springer Nature

Published: 2021-09-28

Total Pages: 676

ISBN-13: 3030783154

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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.

The Nuclear Receptor FactsBook
The Nuclear Receptor FactsBook

Author: Vincent Laudet

Publisher: Gulf Professional Publishing

Published: 2002

Total Pages: 486

ISBN-13: 9780124377356

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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

Nuclear Hormone Receptors
Nuclear Hormone Receptors

Author: Malcolm G. Parker

Publisher:

Published: 1991

Total Pages: 434

ISBN-13:

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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.

Nuclear Receptors in Drug Metabolism
Nuclear Receptors in Drug Metabolism

Author: Wen Xie

Publisher: John Wiley & Sons

Published: 2008-11-03

Total Pages: 352

ISBN-13: 0470409053

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This book gives you an updated and expert overview of nuclear hormone receptors in drug metabolism and drug development and equips you with the interdisciplinary understanding of these receptors and how they can be regulated. Pharmaceutical researchers will find this extremely useful in developing drugs for cancer, heart disease, and diabetes treatment. This comprehensive resource collects scattered materials into one handy, informative volume.

Hormone Signaling
Hormone Signaling

Author: Vincent Goffin

Publisher: Springer Science & Business Media

Published: 2002-03-31

Total Pages: 340

ISBN-13: 9780792376606

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Multicellular organisms require a means of intracellular communication to organize and develop the complex body plan that occurs during embryogenesis and then for cell and organ systems to access and respond to an ever changing environmental milieu. Mediators of this constant exchange of information are growth factors, neurotransmmitters, peptide and protein hormones which bind to cell surface receptors and transduce their signals from the extracellular space to the intracellular compartment. Via multiple signaling pathways, receptors of this general class affect growth, development and differentiation. Smaller hydrophobic signaling molecules, such as steroids and non-steroid hormones, vitamins and metabolic mediators interact with a large family of nuclear receptors. These receptors function as transcription factors affecting gene expression, to regulate the multiple aspects of animal and human physiology, including development, reproduction and homeostasis. The aim of this book is to cover various aspects of intracellular signaling involving hormone receptors.

Innovative Medicine
Innovative Medicine

Author: Kazuwa Nakao

Publisher: Springer

Published: 2015-10-13

Total Pages: 330

ISBN-13: 4431556516

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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.

Computational Approaches to Nuclear Receptors
Computational Approaches to Nuclear Receptors

Author: Pietro Cozzini

Publisher: Royal Society of Chemistry

Published: 2012-11-30

Total Pages: 191

ISBN-13: 1849735352

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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.

Receptor Regulation
Receptor Regulation

Author: R. J. Lefkowitz

Publisher: Springer Science & Business Media

Published: 2013-03-09

Total Pages: 258

ISBN-13: 9400958226

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ROBERT J. LEFKOWITZ, M. D. Receptor Regulation (Receptors and Recognition, Series B, Volume 13) Edited by R. J. Lefkowitz Published in 1981 by Chapman and Hall, 11 New Fetter Lane, London EC4P 4EE © 1981 Chapman and Hall The study of hormone and drug receptors has become one of the most excit ing and rapidly moving areas of biomedical research. Elucidation of receptor mechanisms and receptor structure has become the common goal of many scientists from diverse backgrounds. The rapid advances achieved have been due, in large part, to the concentrated effort of workers from a variety of disciplines including classical pharmacology, biochemistry, endocrinology, cell biology, genetics' and molecular biology, among others. Hormone and drug receptors appear to be of three major types, which may be classified by their cellular locations. Found in the plasma membranes of cells are the receptors for a wide variety of polypeptide hormones, catecholamines and a variety of neurotransmitters. Included within this group are those receptors coupled to the enzyme adenylate cyclase. The second group of receptors are the soluble cytoplasmic receptors for the steroid hormones. A third type of hormone receptor is the receptor for the thyroid hormones which appears to be confined to the nucleus. Not only may these different types of receptor be distinguished in terms of their cellular locations but also by their mechanisms of action.

Biased Signaling in Physiology, Pharmacology and Therapeutics
Biased Signaling in Physiology, Pharmacology and Therapeutics

Author: Brian J Arey

Publisher: Elsevier

Published: 2014-06-05

Total Pages: 317

ISBN-13: 0124115071

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Biased Signaling in Physiology, Pharmacology and Therapeutics is a unique and essential reference for the scientific community concerning how conformational-dependent activation is a common phenomenon across many classes of receptors or signaling molecules. It discusses the role of conformational dynamics in leading to signaling bias across different classes of receptors and signaling molecules. By providing a broader view of signaling bias, this resource helps to explain common mechanisms shared across receptor classes and how this can be utilized to elucidate their cellular activity and better understand their therapeutic potential. Written for both new and established scientists in pharmacology, cell biology, biochemistry, and signal transduction, as well as physicians, this book clearly illustrates how biased receptor signaling can be utilized to develop and understand complex pharmacology. Chapters are each focused on a specific class of receptor or other important topic and make use of real-world examples illustrating how the latest research in signal transduction has led to a better understanding of pharmacology and cell biology. This structure creates a basis for understanding that physiological signalling bias has been selected by nature in order to provide complex and tissue- specific biological responses in the face of limited receptors and signaling pathways. This book provides a framework to reveal that these physiological mechanisms are not restricted to one receptor type or family and thus presents receptor signaling from a newer, more global perspective. - Offers a unique and valuable resource on biased receptor signaling that provides a global view for better understanding pharmacology across many receptor families - Integrates biased receptor signaling, physiology, and pharmacology to place this emerging science within the context of treating disease - Includes important chapters on both the pharmaceutical and therapeutic implications of biased signaling