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Receptor Regulation


Receptor Regulation
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Receptor Regulation


Receptor Regulation
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Author : R. J. Lefkowitz
language : en
Publisher: Springer Science & Business Media
Release Date : 2013-03-09

Receptor Regulation written by R. J. Lefkowitz and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2013-03-09 with Science categories.


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.



Mechanisms Of Receptor Regulation


Mechanisms Of Receptor Regulation
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Author : George Poste
language : en
Publisher: Springer Science & Business Media
Release Date : 2013-11-11

Mechanisms Of Receptor Regulation written by George Poste and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2013-11-11 with Medical categories.


It is less than 80 years since John Newport Langley first proposed the role of "receptive substances" as the site of drug action from his obser vations on the effects of nicotine and curare at the myoneural junction. The many advances in our understanding of receptor biology that have occurred during the intervening period mirror the extraordinary growth of knowledge in the biological sciences and in cell and molecular biology in particular. Receptor biology, in common with many other topics in contemporary biology, is on the threshold of a transition from being a descriptive, phenomenological discipline to one in which underlying mechanisms and regulatory principles can be defined with increasing pre cision. This change, together with the evolution of powerful analytical techniques and timely convergence of ideas from a number of previously separate fields of inquiry, is generating an increasingly unified theoretical and experimental framework for the study of receptor function. These themes, and the mood of anticipation that a real understanding of receptor function in health and disease is emerging, are reflected in in this volume, which summarizes the proceedings of the Sec the papers ond Smith Kline & French Research Symposium on New Horizons in Therapeutics held in Philadelphia in 1984.



Regulation Of G Protein Coupled Receptor Function And Expression


Regulation Of G Protein Coupled Receptor Function And Expression
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Author : Jeffrey L. Benovic
language : en
Publisher:
Release Date : 2000

Regulation Of G Protein Coupled Receptor Function And Expression written by Jeffrey L. Benovic and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2000 with Medical categories.


This comprehensive text describes many techniques that are used to define the molecular mechanisms involved in receptor regulation. It covers a broad range of important concepts and methodologies in the study of G protein-coupled receptors.



5 Ht0 Receptor Regulation And Function


5 Ht0 Receptor Regulation And Function
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Author : Delyth A. Clemett
language : en
Publisher:
Release Date : 1998

5 Ht0 Receptor Regulation And Function written by Delyth A. Clemett and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 1998 with Biochemistry categories.




Dopamine Receptor Regulation


Dopamine Receptor Regulation
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Author : Paul Richard Russell
language : en
Publisher:
Release Date : 1982

Dopamine Receptor Regulation written by Paul Richard Russell and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 1982 with categories.




Death Receptors In Cancer Therapy


Death Receptors In Cancer Therapy
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Author : Wafik S. El-Deiry
language : en
Publisher: Springer Science & Business Media
Release Date : 2007-11-15

Death Receptors In Cancer Therapy written by Wafik S. El-Deiry and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2007-11-15 with Medical categories.


An in depth review of our latest understanding of the molecular events that regulate cell death and those molecules that provide targets for developing agonists or antagonists to modulate death signaling for therapeutic purposes. The authors focus on the extrinsic system of death receptors, their regulation and function, and their abnormalities in cancer. Topics of particular interest include resistance to apoptosis, TRAIL signaling, death receptors in embryonic development, mechanisms of caspase activation, and death receptor mutations in cancer. Additional chapters address death signaling in melanoma, synthetic retinoids and death receptors, the role of p53 in death receptor regulation, immune suppression of cancer, and combination therapy with death ligands.



Gaba Receptors Transporters And Metabolism


Gaba Receptors Transporters And Metabolism
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Author : Chikako Tanaka
language : en
Publisher: Birkhäuser
Release Date : 2012-12-06

Gaba Receptors Transporters And Metabolism written by Chikako Tanaka and has been published by Birkhäuser this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012-12-06 with Medical categories.


Highlighting the current developments and future directions in GABA research, the ambitious aim of this topical volume is to cover GABA from the molecular mechanisms of its transmission to new targets for pharmaceutical research. Distinguished scientists at the forefront of GABA research were invited to contribute reviews on glutamate decarboxylase and autoimmunity, molecular structure and functional regulation of GABA transporters, transmitter release and GABA receptor regulation, GABA receptor subtypes and functional regulation, and GABA receptor ligands and their therapeutic application. Describing the latest advances in what has become a rapidly-evolving field, this volume will prove immensely valuable to neuroscientists, pharmacologists, biochemists, and physiologists working in the field of GABA research.



Pharmacological Regulation Of Gene Expression In The Cns Towards An Understanding Of Basal Ganglial Functions


Pharmacological Regulation Of Gene Expression In The Cns Towards An Understanding Of Basal Ganglial Functions
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Author : Kalpana Merchant
language : en
Publisher: CRC Press
Release Date : 1996-09-13

Pharmacological Regulation Of Gene Expression In The Cns Towards An Understanding Of Basal Ganglial Functions written by Kalpana Merchant and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 1996-09-13 with Science categories.


This book focuses on dopamine-mediated regulation of gene expression within the striatum and associated regions of the central nervous system. It is an excellent review of experimental data on interactions between neuronal systems at systemic, cellular, and molecular levels. Each of the chapters, written by the world's leading scientists, provides an understanding of anatomy, neurochemistry, and cellular and molecular effects. Such an understanding sheds light on the pathophysiology of central disorders involving the basal ganglia and leads to new approaches for the treatment of diseases such as Parkinson's disease and schizophrenia, and also addictions to psychostimulants such as cocaine and amphetamines.



Intracellular Receptor Regulation Of Nf Kappa B Transcriptional Activation Activity


Intracellular Receptor Regulation Of Nf Kappa B Transcriptional Activation Activity
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Author : Robert Michael Nissen
language : en
Publisher:
Release Date : 2000

Intracellular Receptor Regulation Of Nf Kappa B Transcriptional Activation Activity written by Robert Michael Nissen and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2000 with categories.




Nuclear Receptor Regulation Of The Udp Glucuronosyltransferase 1 Locus And The Role Of The Pregnane X Receptor As A Tissue Specific Master Regulator


Nuclear Receptor Regulation Of The Udp Glucuronosyltransferase 1 Locus And The Role Of The Pregnane X Receptor As A Tissue Specific Master Regulator
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Author : Erin Janine Sinnokrak
language : en
Publisher:
Release Date : 2012

Nuclear Receptor Regulation Of The Udp Glucuronosyltransferase 1 Locus And The Role Of The Pregnane X Receptor As A Tissue Specific Master Regulator written by Erin Janine Sinnokrak and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012 with categories.


The UDP-glucuronosyltransferases (UGTs) represent the most significant family of Phase II drug metabolism enzymes and assist in the detoxification and removal of endogenous and exogenous compounds from the body. Using UDP-glucuronic acid as a cosubstrate, the UGTs catalyze the transfer of a polar glucuronic acid moiety to a substrate, thereby increasing its size and hydrophilicity, facilitating excretion. The UGTs are subject to regulation by several nuclear receptors (NRs), including the aryl hydrocarbon receptor (AhR), pregnane x receptor (PXR), constitutive androstane receptor (CAR), and peroxisome-proliferators activated receptor (PPAR). Using a Tg-UGT1 mouse line that expresses all nine functional human UGT1A proteins, it was demonstrated that many of the UGT1 genes are regulated by these nuclear receptors in vivo. In ex vivo primary Tg-UGT1 hepatocyte cultures, PPAR[alpha] was shown to regulate UGT1A1, and promoter analysis experiments were undertaken to identify a PPAR[alpha]-responsive element on the UGT1A1 promoter. A DR1 element at -3272 was characterized as the PPAR[alpha]-responsive sequence. UGT1A4 was also shown to be upregulated by the nuclear receptors in vivo. Experiments to characterize nuclear receptor response elements in the UGT1A4 regulatory region resulted in the identification of an AhR-responsive sequence at -3086 and a PPAR[alpha]-responsive sequence at -366. A putative PXR-responsive element was identified at -212, and although deletion past or mutation of this element resulted in loss of PXR inducibility, basal transcriptional levels increased dramatically, suggesting that in the absence of an agonist, PXR may act through this element to suppress transcription. Regulation of the UGTs during hormonal events such as development and pregnancy has been well demonstrated in humans and rats, and pregnant Tg-UGT1 mice exhibit dramatic upregulation of UGT1A protein during pregnancy. Although the hormonal changes that occur during the human menstrual or the mouse estrus cycles are much less severe than in pregnancy, UGT1 regulation was shown to occur during estrus. PXR was hypothesized to be the mediator of the hormonal regulation, and experiments were undertaken to examine the contribution of PXR to UGT1 induction. A Tg-UGT1-PXRnull mouse line was generated and was demonstrated to have no functional PXR. It was expected that induction during pregnancy and estrus would be lost in the absence of PXR, however, induction was maintained. Basal levels of UGT1 transcription were elevated in the Tg-UGT1-PXRnull mice, and it was hypothesized that this could be due to the impact of PXR on cross-talk with other nuclear receptors. Induction studies were performed in Tg-UGT1 and Tg-UGT1-PXRnull mice using CAR and AhR agonists. Induction of CAR and AhR control genes was unaffected by the loss of PXR, but basal expression and inducibility of the UGT1 genes were dramatically different in the PXRnull background.