Functional Desensitization Of Calcitonin Gene Related Peptide Cgrp Receptors In Sk N Mc Cells
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Functional Desensitization Of Calcitonin Gene Related Peptide Cgrp Receptors In Sk N Mc Cells
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Author : Sokhom Steven Pin
language : en
Publisher:
Release Date : 2007
Functional Desensitization Of Calcitonin Gene Related Peptide Cgrp Receptors In Sk N Mc Cells written by Sokhom Steven Pin and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2007 with Electronic dissertations categories.
The receptor for calcitonin gene-related peptide (CGRP) has been cloned and well studied, but the mechanism of CGRP receptor desensitization has not been fully elucidated. This study is aimed at elucidating the desensitization of CGRP receptors by measuring agonist-mediated activation of adenylate cyclase in a model system employing human neuroblastoma-derived SK-N-MC cells. In these cells, pre-incubation with αCGRP or Î2CGRP induced a rapid desensitization of CGRP signaling. Î2CGRP was 4-600 times more potent at desensitizing the CAMP production as compared to the other receptor-activating ligands. The desensitized receptors exhibited slow re-sensitization upon removal of the pre-incubated ligand, with significant recovery of function achieved within 4 h after the washout procedure. Additional agonists within the calcitonin/CGRP family of peptides and the linear CGRP analogs were also compared to CGRP with regard to their ability to activate and desensitize CGRP receptors. Adrenomedullin and adrenomedullin2 produced desensitization but at a slower rate and with a weaker desensitization potency than CGRP-induced desensitization. Calcitonin and amylin did not produce desensitization. The two linear CGRP analogs Cys(Acm) 2,7αCGRP and cys(Et)2,7αCGRP have high binding affinity to CGRP receptors, but only cys(Et)2,7αCGRP could activate and desensitize the receptors. Cys(Et)2,7αCGRP produced desensitization at a slower rate and with much lower desensitization potency (DC50) than either αCGRP or Î2CGRP. Next it was tested whether the desensitizing effects of the distinct peptides involve protein kinase C (PKC) or protein kinase A (PKA). A PKC inhibitor, Ro 31-8220, concentration-dependently reduced the desensitization induced by αCGRP, Î2CGRP, cys(Et)2,7αCGRP, adrenomedullin, and adrenomedullin2, while having little effect on their desensitization potencies. PKA inhibitors, KT-5720 and H-89, on the other hand, showed little effect on the induced level of desensitization. Desensitization induced by all of the agonists tested were blocked by CGRP receptor antagonist CGRP8-37, indicating they were mediated through CGRP receptors. The findings indicate that functional desensitization is produced by distinct peptides acting through the active site of CGRP receptors, and involves the activation of PKC as a common component necessary to achieve maximal desensitization of receptor signaling.
Desensitisation Of Calcitonin Gene Related Peptide And Adrenomedullin Receptors In Vascular Smooth Muscle And Sk N Mc Cells
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Author : William Martyn Drake
language : en
Publisher:
Release Date : 2002
Desensitisation Of Calcitonin Gene Related Peptide And Adrenomedullin Receptors In Vascular Smooth Muscle And Sk N Mc Cells written by William Martyn Drake and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2002 with Adrenomedullin categories.
Desensitisation Of The Cgrp Receptor In Sk N Mc Cells
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Author : Ka Man Emily Chu
language : en
Publisher:
Release Date : 2008
Desensitisation Of The Cgrp Receptor In Sk N Mc Cells written by Ka Man Emily Chu and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2008 with categories.
The Cgrp Family
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Author : David Poyner
language : en
Publisher: CRC Press
Release Date : 1999-10-01
The Cgrp Family written by David Poyner and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 1999-10-01 with Science categories.
This book is based on presentations given at CGRP '98, the Third International Meeting on CGRP and related peptides held in the UK in May 1998. The principal speakers have each contributed a chapter and many of the short and poster communications will also be found here. This book follows from the tradition set by the First and Second Meetings in 1
Ramps
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Author : William S. Spielman
language : en
Publisher: Springer Science & Business Media
Release Date : 2012-03-21
Ramps written by William S. Spielman 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 2012-03-21 with Medical categories.
Among the many GPCRs discovered, the calcitonin family of receptors comprise of members that regulate a number of physiological processes and are involved in many pathological conditions. Therefore, understanding how these receptors function is a critical question in the field. When Foord and his colleagues discovered that a single transmembrane protein called Receptor Activity Modifying Proteins (RAMPs) could modulate the surface expression of GPCRs of the calcitonin family, it widely opened the field of receptor life cycle. Hundreds of studies have confirmed the importance of RAMPs in the life cycle of this receptor family. Receptor biology is a rapidly expanding field and with the advances in cell and molecular biology and in vivo techniques, it is very likely that the field of RAMPs will explode further and many unanswered questions will be answered with in the next few years.
Neurobiology Of Trp Channels
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Author : Tamara Luti Rosenbaum Emir
language : en
Publisher: CRC Press
Release Date : 2017-08-09
Neurobiology Of Trp Channels written by Tamara Luti Rosenbaum Emir and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2017-08-09 with Science categories.
During the last two decades, there has been an explosion of research pertaining to the molecular mechanisms that allow for organisms to detect different stimuli that is an essential feature for their survival. Among these mechanisms, living beings need to be able to respond to different temperatures as well as chemical and physical stimuli. Thermally activated ion channels were proposed to be present in sensory neurons in the 1980s, but it was not until 1997 that a heat- and capsaicin- activated ion channel, TRPV1, was cloned and its function described in detail. This groundbreaking discovery led to the identification and characterization of several more proteins of the family of Transient Receptor Potential (TRP) ion channels. Intensive research has provided us with the atomic structures of some of these proteins, as well as understanding of their physiological roles, both in normal and pathological conditions. With chapters contributed by renowned experts in the field, Neurobiology of TRP Channels contains a state- of- the- art overview of our knowledge of TRP channels, ranging from structure to their functions in organismal physiology. Features: • Contains chapters on the roles of several TRP ion channels with a diversity of physiological functions, providing a complete picture of the widespread importance of these proteins. • Presents an overview of the structure of TRP channels, including the roles of these proteins in different physiological processes. • Discusses the roles of TRP channels in pathophysiological processes, further highlighting their importance. • Features several full color illustrations to allow the reader better comprehension of TRP channels. A volume in the Frontiers in Neuroscience series
Peptide Receptors
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Author : A. Bjorklund
language : en
Publisher: Elsevier
Release Date : 2000-06-08
Peptide Receptors written by A. Bjorklund and has been published by Elsevier this book supported file pdf, txt, epub, kindle and other format this book has been release on 2000-06-08 with Science categories.
During the last few years, the pace of research in the field of neuropeptide receptors has increased steadily: new neuropeptides were discovered, and the classification of receptor subtypes has been refined. It thus appeared essential to update the information. Peptide Receptors Part I summarizes current knowledge on ten distinct peptide families. This volume integrates photomontages and maps of quantitative receptor autoradiography, in situ hybridization histochemistry, and immunocytochemistry images. Application of these classical techniques and of new approaches such as transgenic and knock-out animals has revealed a distinct species and tissue specific variation in receptor subtypes expression and pharmacology in the mammalian central nervous system. The functional role of neuropeptides and their receptors in the CNS has been investigated thanks to the development of potent and selective receptor antagonists and agonists. The development of specific neuropeptide-related molecules will help to get a better understanding of receptor subtype physiology and neuronal distribution and may lead to innovative treatments in a variety of brain disorders.
Canadian Journal Of Physiology And Pharmacology
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Author :
language : en
Publisher:
Release Date : 1995
Canadian Journal Of Physiology And Pharmacology written by and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 1995 with categories.
Role For Receptor Activity Modifying Proteins Ramps In The Trafficking Of The Adrenomedullin Receptor
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Author : Jennifer Melinda Bomberger
language : en
Publisher:
Release Date : 2005
Role For Receptor Activity Modifying Proteins Ramps In The Trafficking Of The Adrenomedullin Receptor written by Jennifer Melinda Bomberger and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2005 with Adrenomedullin categories.
Cumulated Index Medicus
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Author :
language : en
Publisher:
Release Date : 2000
Cumulated Index Medicus written by and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2000 with Medicine categories.