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  1. Article ; Online: Novel Cocrystal Structures of Peptide Antagonists Bound to the Human Melanocortin Receptor 4 Unveil Unexplored Grounds for Structure-Based Drug Design.

    Gimenez, Luis E / Martin, Charlotte / Yu, Jing / Hollanders, Charlie / Hernandez, Ciria C / Wu, Yiran / Yao, Deqiang / Han, Gye Won / Dahir, Naima S / Wu, Lijie / Van der Poorten, Olivier / Lamouroux, Arthur / Mannes, Morgane / Zhao, Suwen / Tourwé, Dirk / Stevens, Raymond C / Cone, Roger D / Ballet, Steven

    Journal of medicinal chemistry

    2024  Volume 67, Issue 4, Page(s) 2690–2711

    Abstract: Melanocortin 4 receptor (MC4-R) antagonists are actively sought for treating cancer cachexia. We determined the structures of complexes ... ...

    Abstract Melanocortin 4 receptor (MC4-R) antagonists are actively sought for treating cancer cachexia. We determined the structures of complexes with
    MeSH term(s) Humans ; Receptor, Melanocortin, Type 4 ; Peptides/pharmacology ; Ligands ; Drug Design ; Receptor, Melanocortin, Type 3 ; Receptors, Melanocortin
    Chemical Substances Receptor, Melanocortin, Type 4 ; Peptides ; Ligands ; Receptor, Melanocortin, Type 3 ; Receptors, Melanocortin
    Language English
    Publishing date 2024-02-12
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.3c01822
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Efficient Synthesis of Polysubstituted 1,5-Benzodiazepinone Dipeptide Mimetics via an Ugi-4CR-Ullmann Condensation Sequence

    Van Den Hauwe, Robin / Elsocht, Mathias / Hollanders, Charlie / Ballet, Steven

    Synlett

    2021  Volume 32, Issue 17, Page(s) 1719–1724

    Abstract: An efficient three-step synthesis towards 3-amino-1,4-benzodiazepin-2-one derivatives is presented. The versatile Ugi-4-component reaction (Ugi-4CR) and Boc deprotection is followed by a ligand-free Ullmann condensation. This protocol allows the rapid ... ...

    Abstract An efficient three-step synthesis towards 3-amino-1,4-benzodiazepin-2-one derivatives is presented. The versatile Ugi-4-component reaction (Ugi-4CR) and Boc deprotection is followed by a ligand-free Ullmann condensation. This protocol allows the rapid construction of a diverse array of substituted 1,5-benzodiazepinones. Since Ugi-based products are typically limited by their ‘inert’ C -terminal amides, the use of a convertible (‘cleavable’) isocyanide was envisaged and resulted in building blocks that can be made SPPS compatible. To demonstrate the potential of this novel synthetic route, the design and preparation of novel phenylurea-1,5-benzodiazepin-4(5 H )-one dipeptide mimetics with potential CCK2-antagonist properties is reported.
    Keywords 1,5-benzodiazepinone ; Ugi multicomponent reaction ; Cu-catalyzed Ullmann cyclization ; constrained dipeptides.
    Language English
    Publishing date 2021-07-06
    Publisher Georg Thieme Verlag KG
    Publishing place Stuttgart ; New York
    Document type Article
    ZDB-ID 2042012-2
    ISSN 1437-2096 ; 0936-5214
    ISSN (online) 1437-2096
    ISSN 0936-5214
    DOI 10.1055/a-1545-2860
    Database Thieme publisher's database

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  3. Article: 3-Substituted 2-isocyanopyridines as versatile convertible isocyanides for peptidomimetic design

    Hollanders, Charlie / Elsocht, Mathias / Van der Poorten, Olivier / Jida, Mouhamad / Renders, Evelien / Maes, Bert U. W. / Ballet, Steven

    Chemical communications. 2021 July 13, v. 57, no. 56

    2021  

    Abstract: We report the use of 3-substituted 2-isocyanopyridines as convertible isocyanides in Ugi four-component reactions. The N-(3-substituted pyridin-2-yl)amide Ugi products can be cleaved by amines, alcohols, and water with Zn(OAc)₂ as a catalyst. In addition, ...

    Abstract We report the use of 3-substituted 2-isocyanopyridines as convertible isocyanides in Ugi four-component reactions. The N-(3-substituted pyridin-2-yl)amide Ugi products can be cleaved by amines, alcohols, and water with Zn(OAc)₂ as a catalyst. In addition, the applicability of the method was demonstrated in constrained di-/tripeptides bearing acid and base sensitive protective groups obtained via Ugi-4CR post-condensation modifications.
    Keywords Ursidae ; acids ; alcohols ; amines ; catalysts ; chemical communication ; cyanides ; methodology
    Language English
    Dates of publication 2021-0713
    Size p. 6863-6866.
    Publishing place The Royal Society of Chemistry
    Document type Article
    ZDB-ID 1472881-3
    ISSN 1364-548X ; 1359-7345 ; 0009-241X
    ISSN (online) 1364-548X
    ISSN 1359-7345 ; 0009-241X
    DOI 10.1039/d1cc01701b
    Database NAL-Catalogue (AGRICOLA)

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  4. Article ; Online: 3-Substituted 2-isocyanopyridines as versatile convertible isocyanides for peptidomimetic design.

    Hollanders, Charlie / Elsocht, Mathias / Van der Poorten, Olivier / Jida, Mouhamad / Renders, Evelien / Maes, Bert U W / Ballet, Steven

    Chemical communications (Cambridge, England)

    2021  Volume 57, Issue 56, Page(s) 6863–6866

    Abstract: We report the use of 3-substituted 2-isocyanopyridines as convertible isocyanides in Ugi four-component reactions. The N-(3-substituted pyridin-2-yl)amide Ugi products can be cleaved by amines, alcohols, and water with Zn(OAc)2 as a catalyst. In addition, ...

    Abstract We report the use of 3-substituted 2-isocyanopyridines as convertible isocyanides in Ugi four-component reactions. The N-(3-substituted pyridin-2-yl)amide Ugi products can be cleaved by amines, alcohols, and water with Zn(OAc)2 as a catalyst. In addition, the applicability of the method was demonstrated in constrained di-/tripeptides bearing acid and base sensitive protective groups obtained via Ugi-4CR post-condensation modifications.
    MeSH term(s) Molecular Structure ; Nitriles/chemical synthesis ; Nitriles/chemistry ; Peptidomimetics/chemical synthesis ; Pyridines/chemical synthesis ; Pyridines/chemistry
    Chemical Substances Nitriles ; Peptidomimetics ; Pyridines
    Language English
    Publishing date 2021-06-16
    Publishing country England
    Document type Journal Article
    ZDB-ID 1472881-3
    ISSN 1364-548X ; 1359-7345 ; 0009-241X
    ISSN (online) 1364-548X
    ISSN 1359-7345 ; 0009-241X
    DOI 10.1039/d1cc01701b
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Genome-Based Characterization of a Plasmid-Associated Micrococcin P1 Biosynthetic Gene Cluster and Virulence Factors in Mammaliicoccus sciuri IMDO-S72.

    Van der Veken, David / Hollanders, Charlie / Verce, Marko / Michiels, Chris / Ballet, Steven / Weckx, Stefan / Leroy, Frédéric

    Applied and environmental microbiology

    2021  Volume 88, Issue 4, Page(s) e0208821

    Abstract: Analysis of ... ...

    Abstract Analysis of the
    MeSH term(s) Animals ; Bacteriocins ; Mammals ; Microbial Sensitivity Tests ; Multigene Family ; Plasmids/genetics ; Virulence Factors/genetics
    Chemical Substances Bacteriocins ; Virulence Factors ; micrococcin (1392-45-6)
    Language English
    Publishing date 2021-12-22
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 223011-2
    ISSN 1098-5336 ; 0099-2240
    ISSN (online) 1098-5336
    ISSN 0099-2240
    DOI 10.1128/AEM.02088-21
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. 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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  7. Article ; Online: Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.

    Martin, Charlotte / Gimenez, Luis E / Williams, Savannah Y / Jing, Yu / Wu, Yiran / Hollanders, Charlie / Van der Poorten, Olivier / Gonzalez, Simon / Van Holsbeeck, Kevin / Previti, Santo / Lamouroux, Arthur / Zhao, Suwen / Tourwé, Dirk / Stevens, Raymond C / Cone, Roger D / Ballet, Steven

    Journal of medicinal chemistry

    2020  Volume 64, Issue 1, Page(s) 357–369

    Abstract: The melanocortin receptors (MC1R-MC5R) belong to class A G-protein-coupled receptors (GPCRs) and are known to have receptor-specific roles in normal and diseased states. Selectivity for MC4R is of particular interest due to its involvement in various ... ...

    Abstract The melanocortin receptors (MC1R-MC5R) belong to class A G-protein-coupled receptors (GPCRs) and are known to have receptor-specific roles in normal and diseased states. Selectivity for MC4R is of particular interest due to its involvement in various metabolic disorders, including obesity, feeding regulation, and sexual dysfunctions. To further improve the potency and selectivity of MC4R (ant)agonist peptide ligands, we designed and synthesized a series of cyclic peptides based on the recent crystal structure of MC4R in complex with the well-characterized antagonist
    MeSH term(s) Crystallography, X-Ray ; Humans ; Ligands ; Molecular Structure ; Receptor, Melanocortin, Type 4/chemistry ; Receptor, Melanocortin, Type 4/drug effects
    Chemical Substances Ligands ; MC4R protein, human ; Receptor, Melanocortin, Type 4
    Language English
    Publishing date 2020-11-14
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; 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.0c01620
    Database MEDical Literature Analysis and Retrieval System OnLINE

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