Orphan G Protein Coupled Receptors And Novel Neuropeptides
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Author | : Olivier Civelli |
Publisher | : Springer Science & Business Media |
Total Pages | : 267 |
Release | : 2008-05-15 |
Genre | : Science |
ISBN | : 3540783512 |
Over the last decade it has been shown that orphan G protein-coupled receptors (GPCRs) can be used as targets to discover novel neuropeptides. A dozen neuropeptides have been identified through this approach. Each of these neuropeptides has opened new doors for our understanding of fundamental physiological or behavioral responses. For example the orexins, MCH and ghrelin carry fundamental roles in regulating food intake while neuropeptide S, neuromedin S, the prokineticins and the orexins are major players in modulating sleep and circadian rhythms. The chapters of this book review the latest research in the field, most of them are written by the original discoverers of the respective novel neuropeptide. Emphasis is set not only on their discovery but also on their functional significance. Since many of these neuropeptides are part of drug discovery programs, this book impacts academic as well as pharmaceutical research.
Author | : Olivier Civelli |
Publisher | : Springer |
Total Pages | : 259 |
Release | : 2009-08-29 |
Genre | : Science |
ISBN | : 9783540849155 |
Over the last decade it has been shown that orphan G protein-coupled receptors (GPCRs) can be used as targets to discover novel neuropeptides. A dozen neuropeptides have been identified through this approach. Each of these neuropeptides has opened new doors for our understanding of fundamental physiological or behavioral responses. For example the orexins, MCH and ghrelin carry fundamental roles in regulating food intake while neuropeptide S, neuromedin S, the prokineticins and the orexins are major players in modulating sleep and circadian rhythms. The chapters of this book review the latest research in the field, most of them are written by the original discoverers of the respective novel neuropeptide. Emphasis is set not only on their discovery but also on their functional significance. Since many of these neuropeptides are part of drug discovery programs, this book impacts academic as well as pharmaceutical research.
Author | : Ivone Gomes |
Publisher | : Biota Publishing |
Total Pages | : 169 |
Release | : 2013-04-01 |
Genre | : Medical |
ISBN | : 1615044698 |
Neuropeptides mediate their effects by binding and activating receptors that are responsible for converting these extracellular stimuli into intracellular responses. Most neuropeptides interact with G protein-coupled receptors that transduce the signal by activating heterotrimeric G proteins leading to alterations in second messenger systems to amplify the signal and elicit the intracellular response. In this review, we describe the general structure of G protein-coupled receptors including the information obtained from crystal structure determination that has given an insight into the activation mechanism of these receptors. In addition, we summarize the components of the signal transduction system (including G proteins, effectors and second messengers generally activated by the neuropeptide receptors). Using select examples of neuropeptide-receptor systems, we highlight the neuropeptides and corresponding receptors involved in modulation of pain and analgesia, body weight regulation, and hormonal regulation. Finally, we discuss the enzyme-linked tyrosine kinase receptors activated by growth factors and discuss the emerging concepts in targeting neuropeptide receptors for the identification of novel therapeutics targeting these systems. Table of Contents: Abbreviations / Overview of Neuropeptide Receptors / G Protein-Coupled Receptors: General Structure & Function / G Protein-Coupled Receptor Signaling / Neuropeptide Processing and Regulation / Neuropeptide Receptors / Perspectives / References
Author | : Adriano Marchese |
Publisher | : |
Total Pages | : 0 |
Release | : 1998 |
Genre | : |
ISBN | : |
G protein-coupled receptors (GPCRs) are integral membrane proteins that mediate signals to the interior of the cell via activation of heterotrimeric G proteins, which subsequently interact with and activate various effector proteins, ultimately resulting in a physiological response. GPCRs are involved in a number of behaviours, and have been implicated in such processes as drug addiction and neuropsychiatric diseases. To further our understanding of the molecular mechanisms involved beyond the known GPCR-endogenous ligand systems we endeavored to discover novel GPCRs, in particular opioid and opioid related receptors, potentially involved in these processes. In order to achieve this we applied two distinct homology cloning strategies to identify the DNA sequences encoding novel GPCRs. Firstly, PCR amplification of human genomic DNA and cDNA using degenerate oligonucleotides derived from the transmembrane domains (TMs) of the opioid and the related somatostatin receptors, and secondly, querying publicly available sequence databases using the amino add sequence of known GPCRs. We have discovered a novel family comprised of two receptors, named 'GPR7' and 'GPR8', and a third receptor, named 'GPR14', that are most closely related to the opioid receptors. Our experiments also led to the cloning and successful ligand assignment of a novel P2 receptor subtype, named P2Y4, that selectively binds uridine nucleotides. We also report the discovery of three P2Y4 related receptors, ' GPR20, GPR34', and 'GPR35'. We also successfully identified an additional novel family comprised of three receptors, 'GPR3, GPR6 ', and 'GPR12', most closely related to the cannabinoid receptors. We also identified a novel GPCR, named GPR26, which is activated by high LPA concentrations (EC50 = 0.5 [mu]M). The other receptors we isolated, ' GPR1, GPR30, GPR32, GPR33' are all related to chemoattractant receptors, and we have identified two related GPCR pseudogenes, 4 GPR32 and 4 GPR33. The endogenous ligands for most of these receptors have not been assigned, hence they are referred to as orphan receptors, and are useful targets for endogenous ligand discovery. Examination of the mRNA tissue expression patterns by Northern blot and 'in situ' hybridization revealed that most are abundantly and discretely expressed in the brain, suggesting a unique role for each of these receptors in the central nervous system (CNS). Fluorescence in situ hybridization (FISH) was performed to assign each gene to a human chromosome. The cloning and identification of these novel GPCRs provide a unique opportunity for ligand discovery, and is the critical first step in the identification of many novel endogenous ligand-receptor systems.
Author | : Lakshmi A. Devi |
Publisher | : Springer Science & Business Media |
Total Pages | : 414 |
Release | : 2008-03-01 |
Genre | : Medical |
ISBN | : 1592599192 |
A comprehensive survey of the many recent advances in the field of G protein-coupled receptors (GPCR). The authors describe the current knowledge of GPCR receptor structure and function, the different mechanisms involved in the regulation of GPCR function, and the role of pharmacological chaperones in GPCR folding and maturation. They also present new findings about how GPCR dimerization/oligomerization modifies the properties of individual receptors and show how recent developments are leading to significant advances in drug discovery, such as the detection of ligands for orphan GPCRs. Also discussed are the most recent developments that could lead to new drug discoveries: the role of GPCRs in mediating pain, the development of receptor-type selective drugs based on the structural plasticity of receptor activation, and the identification of natural ligands of orphan GPCRs (deorphanization) as possible drug targets.
Author | : Kenneth H. Lundstrom |
Publisher | : CRC Press |
Total Pages | : 384 |
Release | : 2005-07-11 |
Genre | : Medical |
ISBN | : 9781420028218 |
The broad range of G protein-coupled receptors (GPCRs) encompasses all areas of modern medicine and have an enormous impact on the process of drug development. Using disease-oriented methods to cover everything from screening to expression and crystallization, G Protein-Coupled Receptors in Drug Discovery describes the physiological roles of GPCRs
Author | : Rigers Bakiu |
Publisher | : GRIN Verlag |
Total Pages | : 114 |
Release | : 2016-12-13 |
Genre | : Science |
ISBN | : 366836155X |
Document from the year 2016 in the subject Biology - Evolution, grade: -, Agricultural University of Tirana, language: English, abstract: G protein-coupled receptors (GPCRs) are members of a large protein family that share common structural motifs, including seven transmembrane helices, and play pivotal roles in cell-to-cell communications and in the regulation of cell functions. GPR103 is an orphan GPCR that shows similarities with orexin, neuropeptide FF, and cholecystokinin receptors. In humans, 26RFa/QRFP has been found to be an endogenous ligand for the orphan receptor, GPR103 and it is one of the RFamide peptides, which have been shown to exert important neuroendocrine, behavioural, sensory and autonomic functions. All the information we have till know couldn’ be available if we didn’t know the evolution of this important proteins and the relative interactions, which were discovered recently to be important for the regulation of locomotor activity, sleep and these neuropeptides and receptors exert neuroprotective effect in Alzheimer’s Disease. Anyway, there is a long way to be walked on, because there is a need of additional information, while studing the molecular evolution of these proteins and peptides. What is the Molecular Evolution? In the First chapter the readers can find all about this branch of science and the problems this branch had overcomed in order to bring to the scientific community the molecularisation of the evolution concepts. In the following chapter to the readers is presented a descriptive overview of G-proteins and G-protein coupled receptor. In the other chapters it is also presented 26RFA/QRFP and pyroglutamylated RFamide peptide receptor (QRFPR) molecular evolution, where it is described the molecular phylogeny and the functional implication. It is even shown the unique study regarding the presence on natural selection (positive or negative selection) during the evolution of QRFPRs in mammals and fish species. In the end of the book are shown the recent important finding regarding the function and the role of QRFP and its receptor, together with the experimental approach applied to zebrafish and rodents. Anyway, it is imperative to mention that all the available knowledge from experiments to these animals can be useful for the curation of disorders and other deseases like Alzheimer’s Disease, only if we could understand well their molecular evolution.
Author | : Dietmar Richter |
Publisher | : Springer Science & Business Media |
Total Pages | : 370 |
Release | : 2013-06-05 |
Genre | : Science |
ISBN | : 3540494219 |
In the last two decades, our knowledge on regulatory peptides and their cognate receptors, most of which are members of the seven transmembrane receptor families, has increased enormously. Regulatory peptides are small proteins which, besides their hormonal functions in regulating cellular metabolism in various tissues, may also act as neurotransmitters, and thus they often carry the prefix "neuro." Many of the cognate receptors involved in transducing the peptidergic signal across the cell membrane via a family of G proteins exist in multiple forms, the number of which frequently exceeds that of the corresponding peptide ligands. In this book, various peptide-receptor systems are discussed, e.g. CRF, somatostatin, TRH, opioid peptides, vasopressin, and oxytocin. It also discusses new strategies such as "reverse physiology" to uncover new peptides and orphan receptors.
Author | : Jiyoung Heo |
Publisher | : |
Total Pages | : 390 |
Release | : 2007 |
Genre | : Electronic dissertations |
ISBN | : |
Author | : Tatsuya Haga |
Publisher | : CRC Press |
Total Pages | : 336 |
Release | : 2005-08-04 |
Genre | : Medical |
ISBN | : 1420038273 |
This book provides a broad base of knowledge of G-protein-coupled receptors. Useful at both the university and industrial levels, this book is of particular interest to those who are developing therapeutic approaches to diseases using drugs that influence receptor activation.