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  1. Book: Receptor binding techniques

    Davenport, Anthony P.

    (Methods in molecular biology ; 897 ; Springer protocols)

    2012  

    Author's details ed. by Anthony P. Davenport
    Series title Methods in molecular biology ; 897
    Springer protocols
    Collection
    Keywords Binding Sites ; Receptors, Drug / isolation & purification ; Radioligand Assay / methods ; Wirkstoff-Rezeptor-Bindung ; Biochemische Methode
    Subject Rezeptor-Ligand-Wechselwirkung
    Language English
    Size XII, 309 S. : Ill., graph. Darst.
    Edition 3. ed.
    Publisher Humana Press
    Publishing place New York
    Publishing country United States
    Document type Book
    HBZ-ID HT017306337
    ISBN 978-1-61779-908-2 ; 9781617799099 ; 1-61779-908-4 ; 1617799092
    Database Catalogue ZB MED Medicine, Health

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    In stock of ZB MED Cologne/Königswinter

    Shelf markLoan statusLocation
    2012 A 2927 order for loan Magazin

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  2. Article ; Online: From ABCD to E for endothelin in resistant hypertension.

    Abraham, George R / Davenport, Anthony P

    Cell

    2023  Volume 186, Issue 2, Page(s) 240–242

    Abstract: The potent vasoconstrictor peptide endothelin-1 has long been recognized as a physiological regulator of vascular tone. However, pharmacological blockade of the endothelin-1 pathway has few proven indications thus far. A recent clinical trial for ... ...

    Abstract The potent vasoconstrictor peptide endothelin-1 has long been recognized as a physiological regulator of vascular tone. However, pharmacological blockade of the endothelin-1 pathway has few proven indications thus far. A recent clinical trial for resistant hypertension published in The Lancet may yet herald a new era for endothelin receptor antagonists into the clinical mainstream.
    MeSH term(s) Humans ; Endothelin-1/physiology ; Hypertension/drug therapy ; Hypertension/metabolism ; Endothelins/physiology ; Endothelin Receptor Antagonists/therapeutic use
    Chemical Substances Endothelin-1 ; Endothelins ; Endothelin Receptor Antagonists
    Language English
    Publishing date 2023-01-04
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Comment
    ZDB-ID 187009-9
    ISSN 1097-4172 ; 0092-8674
    ISSN (online) 1097-4172
    ISSN 0092-8674
    DOI 10.1016/j.cell.2022.12.014
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 1167: Show issues Location:
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  3. Book: Receptor binding techniques

    Davenport, Anthony P.

    (Methods in molecular biology ; 306)

    2005  

    Author's details ed. by Anthony P. Davenport
    Series title Methods in molecular biology ; 306
    Collection
    Keywords Binding Sites ; Receptors, Drug / isolation & purification ; Radioligand Assay / methods ; Wirkstoff-Rezeptor-Bindung ; Biochemische Methode
    Subject Rezeptor-Ligand-Wechselwirkung
    Language English
    Size X, 240 S. : Ill., graph. Darst.
    Edition 2. ed.
    Publisher Humana Press
    Publishing place Totowa, NJ
    Publishing country United States
    Document type Book
    HBZ-ID HT014380767
    ISBN 1-58829-420-X ; 978-1-58829-420-3
    Database Catalogue ZB MED Medicine, Health

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    In stock of ZB MED Cologne/Königswinter

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    2005 A 2575 order for loan Magazin

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  4. Article: The biased apelin receptor agonist, MM07, reverses Sugen/hypoxia-induced pulmonary arterial hypertension as effectively as the endothelin antagonist macitentan.

    Williams, Thomas L / Nyimanu, Duuamene / Kuc, Rhoda E / Foster, Richard / Glen, Robert C / Maguire, Janet J / Davenport, Anthony P

    Frontiers in pharmacology

    2024  Volume 15, Page(s) 1369489

    Abstract: Introduction: ...

    Abstract Introduction:
    Language English
    Publishing date 2024-04-09
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2587355-6
    ISSN 1663-9812
    ISSN 1663-9812
    DOI 10.3389/fphar.2024.1369489
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article: Editorial: Recent Advances in G Protein-Coupled Receptor Signalling: Impact of Intracellular Location, Environment and Biased Agonism.

    Halls, Michelle L / Davenport, Anthony P / Summers, Roger J

    Frontiers in pharmacology

    2021  Volume 12, Page(s) 707393

    Language English
    Publishing date 2021-05-28
    Publishing country Switzerland
    Document type Editorial
    ZDB-ID 2587355-6
    ISSN 1663-9812
    ISSN 1663-9812
    DOI 10.3389/fphar.2021.707393
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: Targeting the apelin system for the treatment of cardiovascular diseases.

    Chapman, Fiona A / Maguire, Janet J / Newby, David E / Davenport, Anthony P / Dhaun, Neeraj

    Cardiovascular research

    2023  Volume 119, Issue 17, Page(s) 2683–2696

    Abstract: Cardiovascular disease is the leading cause of death worldwide. Its prevalence is rising due to ageing populations and the increasing incidence of diseases such as chronic kidney disease, obesity, and diabetes that are associated with elevated ... ...

    Abstract Cardiovascular disease is the leading cause of death worldwide. Its prevalence is rising due to ageing populations and the increasing incidence of diseases such as chronic kidney disease, obesity, and diabetes that are associated with elevated cardiovascular risk. Despite currently available treatments, there remains a huge burden of cardiovascular disease-associated morbidity for patients and healthcare systems, and newer treatments are needed. The apelin system, comprising the apelin receptor and its two endogenous ligands apelin and elabela, is a broad regulator of physiology that opposes the actions of the renin-angiotensin and vasopressin systems. Activation of the apelin receptor promotes endothelium-dependent vasodilatation and inotropy, lowers blood pressure, and promotes angiogenesis. The apelin system appears to protect against arrhythmias, inhibits thrombosis, and has broad anti-inflammatory and anti-fibrotic actions. It also promotes aqueous diuresis through direct and indirect (central) effects in the kidney. Thus, the apelin system offers therapeutic promise for a range of cardiovascular, kidney, and metabolic diseases. This review will discuss current cardiovascular disease targets of the apelin system and future clinical utility of apelin receptor agonism.
    MeSH term(s) Humans ; Apelin/metabolism ; Apelin Receptors/metabolism ; Cardiovascular Diseases/drug therapy ; Cardiovascular Diseases/metabolism ; Cardiovascular System/metabolism ; Heart
    Chemical Substances Apelin ; Apelin Receptors
    Language English
    Publishing date 2023-11-13
    Publishing country England
    Document type Review ; Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 80340-6
    ISSN 1755-3245 ; 0008-6363
    ISSN (online) 1755-3245
    ISSN 0008-6363
    DOI 10.1093/cvr/cvad171
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 565: Show issues Location:
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  7. Article ; Online: The IUPHAR/BPS Guide to PHARMACOLOGY in 2024.

    Harding, Simon D / Armstrong, Jane F / Faccenda, Elena / Southan, Christopher / Alexander, Stephen P H / Davenport, Anthony P / Spedding, Michael / Davies, Jamie A

    Nucleic acids research

    2023  Volume 52, Issue D1, Page(s) D1438–D1449

    Abstract: The IUPHAR/BPS Guide to PHARMACOLOGY (GtoPdb; https://www.guidetopharmacology.org) is an open-access, expert-curated, online database that provides succinct overviews and key references for pharmacological targets and their recommended experimental ... ...

    Abstract The IUPHAR/BPS Guide to PHARMACOLOGY (GtoPdb; https://www.guidetopharmacology.org) is an open-access, expert-curated, online database that provides succinct overviews and key references for pharmacological targets and their recommended experimental ligands. It includes over 3039 protein targets and 12 163 ligand molecules, including approved drugs, small molecules, peptides and antibodies. Here, we report recent developments to the resource and describe expansion in content over the six database releases made during the last two years. The database update section of this paper focuses on two areas relating to important global health challenges. The first, SARS-CoV-2 COVID-19, remains a major concern and we describe our efforts to expand the database to include a new family of coronavirus proteins. The second area is antimicrobial resistance, for which we have extended our coverage of antibacterials in partnership with AntibioticDB, a collaboration that has continued through support from GARDP. We discuss other areas of curation and also focus on our external links to resources such as PubChem that bring important synergies to the resources.
    MeSH term(s) Databases, Pharmaceutical ; Ligands ; Proteins ; Drug Discovery
    Chemical Substances Ligands ; Proteins
    Language English
    Publishing date 2023-10-27
    Publishing country England
    Document type Journal Article
    ZDB-ID 186809-3
    ISSN 1362-4962 ; 1362-4954 ; 0301-5610 ; 0305-1048
    ISSN (online) 1362-4962 ; 1362-4954
    ISSN 0301-5610 ; 0305-1048
    DOI 10.1093/nar/gkad944
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 1067: Show issues Location:
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  8. Article: Expanding the apelin receptor pharmacological toolbox using novel fluorescent ligands.

    Williams, Thomas L / Macrae, Robyn G C / Kuc, Rhoda E / Brown, Alastair J H / Maguire, Janet J / Davenport, Anthony P

    Frontiers in endocrinology

    2023  Volume 14, Page(s) 1139121

    Abstract: Introduction: The apelin receptor binds two distinct endogenous peptides, apelin and ELA, which act in an autocrine/paracrine manner to regulate the human cardiovascular system. As a class A GPCR, targeting the apelin receptor is an attractive ... ...

    Abstract Introduction: The apelin receptor binds two distinct endogenous peptides, apelin and ELA, which act in an autocrine/paracrine manner to regulate the human cardiovascular system. As a class A GPCR, targeting the apelin receptor is an attractive therapeutic strategy. With improvements in imaging techniques, and the stability and brightness of dyes, fluorescent ligands are becoming increasingly useful in studying protein targets. Here, we describe the design and validation of four novel fluorescent ligands; two based on [Pyr1]apelin-13 (apelin488 and apelin647), and two based on ELA-14 (ELA488 and ELA647).
    Methods: Fluorescent ligands were pharmacologically assessed using radioligand and functional in vitro assays. Apelin647 was validated in high content imaging and internalisation studies, and in a clinically relevant human embryonic stem cell-derived cardiomyocyte model. Apelin488 and ELA488 were used to visualise apelin receptor binding in human renal tissue.
    Results: All four fluorescent ligands retained the ability to bind and activate the apelin receptor and, crucially, triggered receptor internalisation. In high content imaging studies, apelin647 bound specifically to CHO-K1 cells stably expressing apelin receptor, providing proof-of-principle for a platform that could screen novel hits targeting this GPCR. The ligand also bound specifically to endogenous apelin receptor in stem cell-derived cardiomyocytes. Apelin488 and ELA488 bound specifically to apelin receptor, localising to blood vessels and tubules of the renal cortex.
    Discussion: Our data indicate that the described novel fluorescent ligands expand the pharmacological toolbox for studying the apelin receptor across multiple platforms to facilitate drug discovery.
    MeSH term(s) Cricetinae ; Animals ; Humans ; Apelin Receptors/metabolism ; Ligands ; Peptide Hormones/metabolism ; Cricetulus ; Protein Binding
    Chemical Substances Apelin Receptors ; Ligands ; Peptide Hormones
    Language English
    Publishing date 2023-03-09
    Publishing country Switzerland
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2592084-4
    ISSN 1664-2392
    ISSN 1664-2392
    DOI 10.3389/fendo.2023.1139121
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article ; Online: International Union of Basic and Clinical Pharmacology CIII: Chemerin Receptors CMKLR1 (Chemerin

    Kennedy, Amanda J / Davenport, Anthony P

    Pharmacological reviews

    2017  Volume 70, Issue 1, Page(s) 174–196

    Abstract: Chemerin, a chemoattractant protein and adipokine, has been identified as the endogenous ligand for a G protein-coupled receptor encoded by the ... ...

    Abstract Chemerin, a chemoattractant protein and adipokine, has been identified as the endogenous ligand for a G protein-coupled receptor encoded by the gene
    MeSH term(s) Amino Acid Sequence ; Animals ; Humans ; Receptors, Chemokine/agonists ; Receptors, Chemokine/antagonists & inhibitors ; Receptors, Chemokine/chemistry ; Receptors, Chemokine/metabolism ; Receptors, G-Protein-Coupled/agonists ; Receptors, G-Protein-Coupled/antagonists & inhibitors ; Receptors, G-Protein-Coupled/chemistry ; Receptors, G-Protein-Coupled/metabolism ; Terminology as Topic
    Chemical Substances Receptors, Chemokine ; Receptors, G-Protein-Coupled
    Language English
    Publishing date 2017-12-26
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 209898-2
    ISSN 1521-0081 ; 0031-6997
    ISSN (online) 1521-0081
    ISSN 0031-6997
    DOI 10.1124/pr.116.013177
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article ; Online: Trans-myocardial Extraction of Endothelin-1 Correlates with Increased Microcirculatory Resistance following Percutaneous Coronary Intervention.

    Abraham, George R / Nyimanu, Duuamene / Kuc, Rhoda E / Maguire, Janet J / Davenport, Anthony P / Hoole, Stephen P

    Journal of interventional cardiology

    2022  Volume 2022, Page(s) 9154048

    Abstract: Objective: Coronary microvascular dysfunction (CMD) can complicate successful percutaneous coronary intervention (PCI). The potent endogenous vasoconstrictor peptide Endothelin-1 (ET-1) may be an important mediator. To investigate the mechanism, we ... ...

    Abstract Objective: Coronary microvascular dysfunction (CMD) can complicate successful percutaneous coronary intervention (PCI). The potent endogenous vasoconstrictor peptide Endothelin-1 (ET-1) may be an important mediator. To investigate the mechanism, we sought to define the peri-procedural trans-myocardial gradient (TMG-coronary sinus minus aortic root levels) of ET-1 and its precursor peptide - Big ET-1. We then assessed correlation with pressure-wire indices of CMD: coronary flow reserve (CFR) and index of microvascular resistance (IMR).
    Methods: Paired blood samples from the guide catheter and coronary sinus were collected before and after pressure-wire-guided PCI from patients with stable angina. Plasma was analysed using a specific enzyme-linked immunosorbent assay for quantification of ET-1 peptides and correlated with pressure-wire data. Non normally distributed continuous variables are presented as median [IQR].
    Results: ET-1 and Big ET-1 increased post-PCI in the aorta (ET-1: 0.98 [0.76-1.26] pg/ml to 1.20 [1.03-1.67] pg/ml,
    Conclusions: Circulating ET-1 increases post-PCI and upregulated ET-1 trans-myocardial extraction contributes to increased microcirculatory resistance.
    MeSH term(s) Humans ; Percutaneous Coronary Intervention ; Microcirculation ; Endothelin-1 ; Angina, Stable ; Vasoconstrictor Agents ; Vascular Resistance ; Coronary Circulation
    Chemical Substances Endothelin-1 ; Vasoconstrictor Agents
    Language English
    Publishing date 2022-09-19
    Publishing country United States
    Document type Journal Article
    ZDB-ID 1036325-7
    ISSN 1540-8183 ; 0896-4327
    ISSN (online) 1540-8183
    ISSN 0896-4327
    DOI 10.1155/2022/9154048
    Database MEDical Literature Analysis and Retrieval System OnLINE

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