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  1. Article ; Online: Signaling Modulation via Minimal C-Terminal Modifications of Apelin-13.

    Théroux, Léa / Van Den Hauwe, Robin / Trân, Kien / Fournier, Justin / Desgagné, Michael / Meneboo, Nathan / Lavallée, Alexis / Fröhlich, Ulrike / Côté, Jérôme / Hollanders, Charlie / Longpré, Jean-Michel / Murza, Alexandre / Marsault, Eric / Sarret, Philippe / Boudreault, Pierre-Luc / Ballet, Steven

    ACS pharmacology & translational science

    2023  Volume 6, Issue 2, Page(s) 290–305

    Abstract: Apelin is an endogenous peptide that is involved in many diseases such as cardiovascular diseases, obesity, and cancer, which has made it an attractive target for drug discovery. Herein, we explore the penultimate and final sequence positions of [ ... ...

    Abstract Apelin is an endogenous peptide that is involved in many diseases such as cardiovascular diseases, obesity, and cancer, which has made it an attractive target for drug discovery. Herein, we explore the penultimate and final sequence positions of [Pyr
    Language English
    Publishing date 2023-01-26
    Publishing country United States
    Document type Journal Article
    ISSN 2575-9108
    ISSN (online) 2575-9108
    DOI 10.1021/acsptsci.2c00219
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Pharmacodynamic and pharmacokinetic profiles of a neurotensin receptor type 2 (NTS2) analgesic macrocyclic analog.

    Chartier, Magali / Desgagné, Michael / Sousbie, Marc / Rumsby, Charles / Chevillard, Lucie / Théroux, Léa / Haroune, Lounès / Côté, Jérôme / Longpré, Jean-Michel / Boudreault, Pierre-Luc / Marsault, Éric / Sarret, Philippe

    Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

    2021  Volume 141, Page(s) 111861

    Abstract: The current opioid crisis highlights the urgent need to develop safe and effective pain medications. Thus, neurotensin (NT) compounds represent a promising approach, as the antinociceptive effects of NT are mediated by activation of the two G protein- ... ...

    Abstract The current opioid crisis highlights the urgent need to develop safe and effective pain medications. Thus, neurotensin (NT) compounds represent a promising approach, as the antinociceptive effects of NT are mediated by activation of the two G protein-coupled receptor subtypes (i.e., NTS1 and NTS2) and produce potent opioid-independent analgesia. Here, we describe the synthesis and pharmacodynamic and pharmacokinetic properties of the first constrained NTS2 macrocyclic NT(8-13) analog. The Tyr
    MeSH term(s) Analgesics, Non-Narcotic/chemical synthesis ; Analgesics, Non-Narcotic/pharmacokinetics ; Analgesics, Non-Narcotic/pharmacology ; Analgesics, Opioid/pharmacology ; Animals ; CHO Cells ; Cricetinae ; Cricetulus ; Cyclization ; Dose-Response Relationship, Drug ; Drug Design ; Drug Synergism ; Hyperalgesia/drug therapy ; Hyperalgesia/etiology ; Inflammation/complications ; Inflammation/drug therapy ; Macrocyclic Compounds/chemical synthesis ; Macrocyclic Compounds/pharmacokinetics ; Macrocyclic Compounds/pharmacology ; Male ; Morphine/pharmacology ; Pain Measurement/drug effects ; Rats ; Rats, Sprague-Dawley ; Receptors, Neurotensin/drug effects ; Substrate Specificity
    Chemical Substances Analgesics, Non-Narcotic ; Analgesics, Opioid ; Macrocyclic Compounds ; Ntsr2 protein, rat ; Receptors, Neurotensin ; neurotensin type 1 receptor ; Morphine (76I7G6D29C)
    Language English
    Publishing date 2021-07-03
    Publishing country France
    Document type Journal Article
    ZDB-ID 392415-4
    ISSN 1950-6007 ; 0753-3322 ; 0300-0893
    ISSN (online) 1950-6007
    ISSN 0753-3322 ; 0300-0893
    DOI 10.1016/j.biopha.2021.111861
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Ud II Zs.198: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

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  3. Article ; Online: Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile.

    Trân, Kien / Van Den Hauwe, Robin / Sainsily, Xavier / Couvineau, Pierre / Côté, Jérôme / Simard, Louise / Echevarria, Marco / Murza, Alexandre / Serre, Alexandra / Théroux, Léa / Saibi, Sabrina / Haroune, Lounès / Longpré, Jean-Michel / Lesur, Olivier / Auger-Messier, Mannix / Spino, Claude / Bouvier, Michel / Sarret, Philippe / Ballet, Steven /
    Marsault, Éric

    Journal of medicinal chemistry

    2021  Volume 64, Issue 9, Page(s) 5345–5364

    Abstract: Side-chain-constrained amino acids are useful tools to modulate the biological properties of peptides. In this study, we applied side-chain constraints to apelin-13 (Ape13) by substituting the Pro12 and Phe13 positions, affecting the binding affinity and ...

    Abstract Side-chain-constrained amino acids are useful tools to modulate the biological properties of peptides. In this study, we applied side-chain constraints to apelin-13 (Ape13) by substituting the Pro12 and Phe13 positions, affecting the binding affinity and signaling profile on the apelin receptor (APJ). The residues 1Nal, Trp, and Aia were found to be beneficial substitutions for Pro12, and the resulting analogues displayed high affinity for APJ (
    MeSH term(s) Amino Acid Sequence ; Amino Acid Substitution ; Animals ; Apelin Receptors/chemistry ; Apelin Receptors/metabolism ; Blood Pressure/drug effects ; GTP-Binding Protein alpha Subunits, G12-G13/chemistry ; GTP-Binding Protein alpha Subunits, G12-G13/metabolism ; Half-Life ; Humans ; Intercellular Signaling Peptides and Proteins/chemistry ; Intercellular Signaling Peptides and Proteins/metabolism ; Intercellular Signaling Peptides and Proteins/pharmacology ; Male ; Protein Binding ; Protein Stability ; Rats ; Rats, Sprague-Dawley ; Signal Transduction/drug effects
    Chemical Substances Apelin Receptors ; Intercellular Signaling Peptides and Proteins ; apelin-13 peptide ; GTP-Binding Protein alpha Subunits, G12-G13 (EC 3.6.5.1)
    Language English
    Publishing date 2021-02-01
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.0c01941
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
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