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  1. Book: The phospholipase C pathway

    Tobin, Andrew B.

    its regulation and desensitization

    (Molecular biology intelligence unit)

    1996  

    Author's details Andrew B. Tobin
    Series title Molecular biology intelligence unit
    Keywords Phospholipase C / metabolism ; G-Proteins / metabolism ; Receptors, Cell Surface / metabolism ; Signal Transduction ; Phospholipase C ; Zellrezeptor ; Signaltransduktion ; GTP-bindende Proteine ; Rezeptor ; Desensibilisierung
    Subject EC 3.1.4.3 ; Lipophosphodiesterase I ; Lecithinase C ; Clostridium welchii alpha-toxin ; Clostridium oedematiens beta-toxin ; Clostridium oedematiens gamma-toxin ; Signalübertragung ; Signalvermittlung ; Guaninnucleotidbindende Proteine ; G-Proteine ; Hyposensibilisierung ; Spezifische Hyposensibilisierung ; Spezifische Immuntherapie ; SIT
    Language English
    Size [14], 223 S. : Ill., graph. Darst.
    Publisher Springer u.a.
    Publishing place New York u.a.
    Publishing country United States
    Document type Book
    HBZ-ID HT007463513
    ISBN 3-540-61447-8 ; 0-412-12461-0 ; 1-57059-386-8 ; 978-3-540-61447-0 ; 978-0-412-12461-7 ; 978-1-57059-386-4
    Database Catalogue ZB MED Medicine, Health

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    In stock of ZB MED Cologne/Königswinter

    Shelf markLoan statusLocation
    1997 A 2607 order for loan Magazin

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  2. Article ; Online: Targeting the M1 muscarinic acetylcholine receptor in Alzheimer's disease.

    Dwomoh, Louis / Tejeda, Gonzalo S / Tobin, Andrew B

    Neuronal signaling

    2022  Volume 6, Issue 1, Page(s) NS20210004

    Abstract: Alzheimer's disease (AD) remains a major cause of morbidity and mortality worldwide, and despite extensive research, only a few drugs are available for management of the disease. One strategy has been to up-regulate cholinergic neurotransmission to ... ...

    Abstract Alzheimer's disease (AD) remains a major cause of morbidity and mortality worldwide, and despite extensive research, only a few drugs are available for management of the disease. One strategy has been to up-regulate cholinergic neurotransmission to improve cognitive function, but this approach has dose-limiting adverse effects. To avoid these adverse effects, new drugs that target specific receptor subtypes of the cholinergic system are needed, and the M1 subtype of muscarinic acetylcholine receptor (M1-mAChR) has been shown to be a good target for this approach. By using several strategies, M1-mAChR ligands have been developed and trialled in preclinical animal models and in human studies, with varying degrees of success. This article reviews the different approaches to targeting the M1-mAChR in AD and discusses the advantages and limitations of these strategies. The factors to consider in targeting the M1-mAChR in AD are also discussed.
    Language English
    Publishing date 2022-04-21
    Publishing country England
    Document type Journal Article ; Review
    ISSN 2059-6553
    ISSN (online) 2059-6553
    DOI 10.1042/NS20210004
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  3. Article ; Online: How Arrestins and GRKs Regulate the Function of Long Chain Fatty Acid Receptors.

    Alharbi, Abdulrahman G / Tobin, Andrew B / Milligan, Graeme

    International journal of molecular sciences

    2022  Volume 23, Issue 20

    Abstract: FFA1 and FFA4, two G protein-coupled receptors that are activated by long chain fatty acids, play crucial roles in mediating many biological functions in the body. As a result, these fatty acid receptors have gained considerable attention due to their ... ...

    Abstract FFA1 and FFA4, two G protein-coupled receptors that are activated by long chain fatty acids, play crucial roles in mediating many biological functions in the body. As a result, these fatty acid receptors have gained considerable attention due to their potential to be targeted for the treatment of type-2 diabetes. However, the relative contribution of canonical G protein-mediated signalling versus the effects of agonist-induced phosphorylation and interactions with β-arrestins have yet to be fully defined. Recently, several reports have highlighted the ability of β-arrestins and GRKs to interact with and modulate different functions of both FFA1 and FFA4, suggesting that it is indeed important to consider these interactions when studying the roles of FFA1 and FFA4 in both normal physiology and in different disease settings. Here, we discuss what is currently known and show the importance of understanding fully how β-arrestins and GRKs regulate the function of long chain fatty acid receptors.
    MeSH term(s) Arrestins/metabolism ; G-Protein-Coupled Receptor Kinases ; beta-Arrestins ; Receptors, G-Protein-Coupled/metabolism ; Fatty Acids
    Chemical Substances Arrestins ; G-Protein-Coupled Receptor Kinases (EC 2.7.11.16) ; beta-Arrestins ; Receptors, G-Protein-Coupled ; Fatty Acids
    Language English
    Publishing date 2022-10-13
    Publishing country Switzerland
    Document type Journal Article ; Review
    ZDB-ID 2019364-6
    ISSN 1422-0067 ; 1422-0067 ; 1661-6596
    ISSN (online) 1422-0067
    ISSN 1422-0067 ; 1661-6596
    DOI 10.3390/ijms232012237
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  4. Article ; Online: Editorial for Advances in G Protein-Coupled Receptor Signal Transduction Special Issue.

    Tobin, Andrew B / Bradley, Sophie J

    ACS pharmacology & translational science

    2020  Volume 3, Issue 2, Page(s) 169–170

    Language English
    Publishing date 2020-04-02
    Publishing country United States
    Document type Editorial
    ISSN 2575-9108
    ISSN (online) 2575-9108
    DOI 10.1021/acsptsci.0c00029
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  5. Article ; Online: Crosstalk between the M

    Thompson, Karen J / Tobin, Andrew B

    Cellular signalling

    2020  Volume 70, Page(s) 109545

    Abstract: Alzheimer's disease (AD) is a neurodegenerative disorder which accounts for 60-70% of the 50 million worldwide cases of dementia and is characterised by cognitive impairments, many of which have long been associated with dysfunction of the cholinergic ... ...

    Abstract Alzheimer's disease (AD) is a neurodegenerative disorder which accounts for 60-70% of the 50 million worldwide cases of dementia and is characterised by cognitive impairments, many of which have long been associated with dysfunction of the cholinergic system. Although the M
    MeSH term(s) Alzheimer Disease/metabolism ; Animals ; Disease Progression ; Endocannabinoids/metabolism ; Humans ; Receptor, Muscarinic M1/metabolism
    Chemical Substances Endocannabinoids ; Receptor, Muscarinic M1
    Language English
    Publishing date 2020-01-21
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 1002702-6
    ISSN 1873-3913 ; 0898-6568
    ISSN (online) 1873-3913
    ISSN 0898-6568
    DOI 10.1016/j.cellsig.2020.109545
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    Zs.A 2579: Show issues Location:
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    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  6. Article: A growing understanding of the role of muscarinic receptors in the molecular pathology and treatment of schizophrenia.

    Dean, Brian / Bakker, Geor / Ueda, Hiroki R / Tobin, Andrew B / Brown, Alastair / Kanaan, Richard A A

    Frontiers in cellular neuroscience

    2023  Volume 17, Page(s) 1124333

    Abstract: Pre-clinical models, postmortem and neuroimaging studies all support a role for muscarinic receptors in the molecular pathology of schizophrenia. From these data it was proposed that activation of the muscarinic M1 and/or M4 receptor would reduce the ... ...

    Abstract Pre-clinical models, postmortem and neuroimaging studies all support a role for muscarinic receptors in the molecular pathology of schizophrenia. From these data it was proposed that activation of the muscarinic M1 and/or M4 receptor would reduce the severity of the symptoms of schizophrenia. This hypothesis is now supported by results from two clinical trials which indicate that activating central muscarinic M1 and M4 receptors can reduce the severity of positive, negative and cognitive symptoms of the disorder. This review will provide an update on a growing body of evidence that argues the muscarinic M1 and M4 receptors have critical roles in CNS functions that are dysregulated by the pathophysiology of schizophrenia. This realization has been made possible, in part, by the growing ability to visualize and quantify muscarinic M1 and M4 receptors in the human CNS using molecular neuroimaging. We will discuss how these advances have provided evidence to support the notion that there is a sub-group of patients within the syndrome of schizophrenia that have a unique molecular pathology driven by a marked loss of muscarinic M1 receptors. This review is timely, as drugs targeting muscarinic receptors approach clinical use for the treatment of schizophrenia and here we outline the background biology that supported development of such drugs to treat the disorder.
    Language English
    Publishing date 2023-02-22
    Publishing country Switzerland
    Document type Journal Article ; Review
    ZDB-ID 2452963-1
    ISSN 1662-5102
    ISSN 1662-5102
    DOI 10.3389/fncel.2023.1124333
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  7. Article ; Online: Parasite and host kinases as targets for antimalarials.

    Ong, Han Wee / Adderley, Jack / Tobin, Andrew B / Drewry, David H / Doerig, Christian

    Expert opinion on therapeutic targets

    2023  Volume 27, Issue 2, Page(s) 151–169

    Abstract: Introduction: The deployment of Artemisinin-based combination therapies and transmission control measures led to a decrease in the global malaria burden over the recent decades. Unfortunately, this trend is now reversing, in part due to resistance ... ...

    Abstract Introduction: The deployment of Artemisinin-based combination therapies and transmission control measures led to a decrease in the global malaria burden over the recent decades. Unfortunately, this trend is now reversing, in part due to resistance against available treatments, calling for the development of new drugs against untapped targets to prevent cross-resistance.
    Areas covered: In view of their demonstrated druggability in noninfectious diseases, protein kinases represent attractive targets. Kinase-focussed antimalarial drug discovery is facilitated by the availability of kinase-targeting scaffolds and large libraries of inhibitors, as well as high-throughput phenotypic and biochemical assays. We present an overview of validated
    Expert opinion: We propose priority research areas, including (i) diversification of
    MeSH term(s) Animals ; Humans ; Antimalarials/pharmacology ; Parasites ; Malaria/drug therapy ; Plasmodium ; Drug Discovery
    Chemical Substances Antimalarials
    Language English
    Publishing date 2023-03-20
    Publishing country England
    Document type Review ; Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, N.I.H., Extramural
    ZDB-ID 2055208-7
    ISSN 1744-7631 ; 1472-8222
    ISSN (online) 1744-7631
    ISSN 1472-8222
    DOI 10.1080/14728222.2023.2185511
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    Zs.A 5244: Show issues Location:
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  8. Article ; Online: Chemogenetic Approaches to Explore the Functions of Free Fatty Acid Receptor 2.

    Milligan, Graeme / Barki, Natasja / Tobin, Andrew B

    Trends in pharmacological sciences

    2021  Volume 42, Issue 3, Page(s) 191–202

    Abstract: Short-chain fatty acids are generated in large amounts by the intestinal microbiota. They activate both the closely related G protein-coupled receptors free fatty acid receptor 2 (FFA2) and free fatty acid receptor 3 (FFA3) that are considered ... ...

    Abstract Short-chain fatty acids are generated in large amounts by the intestinal microbiota. They activate both the closely related G protein-coupled receptors free fatty acid receptor 2 (FFA2) and free fatty acid receptor 3 (FFA3) that are considered therapeutic targets in diseases of immuno-metabolism. Limited and species-selective small-molecule pharmacology has restricted our understanding of the distinct roles of these receptors. Replacement of mouse FFA2 with a designer receptor exclusively activated by designer drug form of human FFA2 (hFFA2-DREADD) has allowed definition of specific roles of FFA2 in pharmacological and physiological studies conducted both ex vivo and in vivo, whilst overlay of murine disease models offers opportunities for therapeutic validation prior to human studies. Similar approaches can potentially be used to define roles of other poorly characterised receptors.
    MeSH term(s) Animals ; Fatty Acids, Nonesterified ; Mice ; Receptors, Cell Surface ; Receptors, G-Protein-Coupled
    Chemical Substances Fatty Acids, Nonesterified ; Receptors, Cell Surface ; Receptors, G-Protein-Coupled
    Language English
    Publishing date 2021-01-22
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 282846-7
    ISSN 1873-3735 ; 0165-6147
    ISSN (online) 1873-3735
    ISSN 0165-6147
    DOI 10.1016/j.tips.2020.12.003
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    Zs.A 1513: Show issues Location:
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    Zs.MG 6: Show issues

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  9. Article ; Online: Fatty airways: a source of good and bad fats?

    Brightling, Christopher E / Tobin, Andrew B / Milligan, Graeme

    The European respiratory journal

    2019  Volume 54, Issue 6

    Language English
    Publishing date 2019-12-12
    Publishing country England
    Document type Editorial ; Comment
    ZDB-ID 639359-7
    ISSN 1399-3003 ; 0903-1936
    ISSN (online) 1399-3003
    ISSN 0903-1936
    DOI 10.1183/13993003.02060-2019
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    Zs.A 2322: Show issues Location:
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    Zs.MO 292: Show issues

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  10. Article ; Online: Design of Next-Generation G Protein-Coupled Receptor Drugs: Linking Novel Pharmacology and In Vivo Animal Models.

    Bradley, Sophie J / Tobin, Andrew B

    Annual review of pharmacology and toxicology

    2016  Volume 56, Page(s) 535–559

    Abstract: Despite the fact that G protein-coupled receptors (GPCRs) are the most successful drug targets in history, this supergene family of cell surface receptors has yet to be fully exploited as targets in the treatment of human disease. Here, we present ... ...

    Abstract Despite the fact that G protein-coupled receptors (GPCRs) are the most successful drug targets in history, this supergene family of cell surface receptors has yet to be fully exploited as targets in the treatment of human disease. Here, we present optimism that this may change in the future by reviewing the substantial progress made in the understanding of GPCR molecular pharmacology that has generated an extensive toolbox of ligand types that include orthosteric, allosteric, and bitopic ligands, many of which show signaling bias. We discuss how combining these advances with recently described transgenic, chemical genetic, and optogenetic animal models will provide the framework to allow for the rational design of next-generation GPCR drugs that possess increased therapeutic efficacy and decreased adverse/toxic responses.
    MeSH term(s) Animals ; Drug Discovery/methods ; Humans ; Ligands ; Models, Animal ; Receptors, G-Protein-Coupled/metabolism
    Chemical Substances Ligands ; Receptors, G-Protein-Coupled
    Language English
    Publishing date 2016-01-06
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 196587-6
    ISSN 1545-4304 ; 0362-1642
    ISSN (online) 1545-4304
    ISSN 0362-1642
    DOI 10.1146/annurev-pharmtox-011613-140012
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