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  1. Article ; Online: Strengthening Peptoid Helicity through Sequence Site-Specific Positioning of Amide

    Rzeigui, Maha / Traikia, Mounir / Jouffret, Laurent / Kriznik, Alexandre / Khiari, Jameleddine / Roy, Olivier / Taillefumier, Claude

    The Journal of organic chemistry

    2020  Volume 85, Issue 4, Page(s) 2190–2201

    Abstract: The synthesis of biomimetic helical secondary structures is sought after for the construction of innovative nanomaterials and applications in medicinal chemistry such as the development of protein-protein interaction modulators. Peptoids, a sequence- ... ...

    Abstract The synthesis of biomimetic helical secondary structures is sought after for the construction of innovative nanomaterials and applications in medicinal chemistry such as the development of protein-protein interaction modulators. Peptoids, a sequence-defined family of oligomers, enable a peptidomimetic strategy, especially considering the easily accessible monomer diversity and peptoid helical folding propensity. However,
    Language English
    Publishing date 2020-01-13
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 123490-0
    ISSN 1520-6904 ; 0022-3263
    ISSN (online) 1520-6904
    ISSN 0022-3263
    DOI 10.1021/acs.joc.9b02916
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 4473: Show issues Location:
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  2. Article: Strengthening Peptoid Helicity through Sequence Site-Specific Positioning of Amide cis-Inducing NtBu Monomers

    Rzeigui, Maha / Traikia, Mounir / Jouffret, Laurent / Kriznik, Alexandre / Khiari, Jameleddine / Roy, Olivier / Taillefumier, Claude

    Journal of organic chemistry. 2019 Dec. 24, v. 85, no. 4

    2019  

    Abstract: The synthesis of biomimetic helical secondary structures is sought after for the construction of innovative nanomaterials and applications in medicinal chemistry such as the development of protein–protein interaction modulators. Peptoids, a sequence- ... ...

    Abstract The synthesis of biomimetic helical secondary structures is sought after for the construction of innovative nanomaterials and applications in medicinal chemistry such as the development of protein–protein interaction modulators. Peptoids, a sequence-defined family of oligomers, enable a peptidomimetic strategy, especially considering the easily accessible monomer diversity and peptoid helical folding propensity. However, cis–trans isomerization of the backbone tertiary amides may impair the peptoid’s adoption of stable secondary structures, notably the all-cis polyproline I-like helical conformation. Here, we show that cis-inducing NtBu achiral monomers strategically positioned within chiral sequences may reinforce the degree of peptoid helicity, although with a reduced content of chiral side chains. The design principles presented here will undoubtedly help achieve more conformationally stable helical peptoids with desired functions.
    Keywords N-substituted glycines ; amides ; biomimetics ; chemical structure ; cis-trans isomerism ; nanomaterials ; organic chemistry ; protein-protein interactions
    Language English
    Dates of publication 2019-1224
    Size p. 2190-2201.
    Publishing place American Chemical Society
    Document type Article
    ZDB-ID 123490-0
    ISSN 1520-6904 ; 0022-3263
    ISSN (online) 1520-6904
    ISSN 0022-3263
    DOI 10.1021/acs.joc.9b02916
    Database NAL-Catalogue (AGRICOLA)

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  3. Article ; Online: New pyrido[3,4-g]quinazoline derivatives as CLK1 and DYRK1A inhibitors: synthesis, biological evaluation and binding mode analysis.

    Tazarki, Helmi / Zeinyeh, Wael / Esvan, Yannick J / Knapp, Stefan / Chatterjee, Deep / Schröder, Martin / Joerger, Andreas C / Khiari, Jameleddine / Josselin, Béatrice / Baratte, Blandine / Bach, Stéphane / Ruchaud, Sandrine / Anizon, Fabrice / Giraud, Francis / Moreau, Pascale

    European journal of medicinal chemistry

    2019  Volume 166, Page(s) 304–317

    Abstract: Cdc2-like kinase 1 (CLK1) and dual specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) are involved in the regulation of alternative pre-mRNA splicing. Dysregulation of this process has been linked to cancer progression and ... ...

    Abstract Cdc2-like kinase 1 (CLK1) and dual specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) are involved in the regulation of alternative pre-mRNA splicing. Dysregulation of this process has been linked to cancer progression and neurodegenerative diseases, making CLK1 and DYRK1A important therapeutic targets. Here we describe the synthesis of new pyrido[3,4-g]quinazoline derivatives and the evaluation of the inhibitory potencies of these compounds toward CDK5, CK1, GSK3, CLK1 and DYRK1A. Introduction of aminoalkylamino groups at the 2-position resulted in several compounds with low nanomolar affinity and selective inhibition of CLK1 and/or DYRK1A. Their evaluation on several immortalized or cancerous cell lines showed varying degree of cell viability reduction. Co-crystal structures of CLK1 with two of the most potent compounds revealed two alternative binding modes of the pyrido[3,4-g]quinazoline scaffold that can be exploited for future inhibitor design.
    MeSH term(s) Cell Line, Tumor ; Chemistry Techniques, Synthetic ; Drug Design ; Humans ; Molecular Docking Simulation ; Protein Binding ; Protein Conformation ; Protein Kinase Inhibitors/chemical synthesis ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/metabolism ; Protein Kinase Inhibitors/pharmacology ; Protein Serine-Threonine Kinases/antagonists & inhibitors ; Protein Serine-Threonine Kinases/chemistry ; Protein Serine-Threonine Kinases/metabolism ; Protein-Tyrosine Kinases/antagonists & inhibitors ; Protein-Tyrosine Kinases/chemistry ; Protein-Tyrosine Kinases/metabolism ; Quinazolines/chemical synthesis ; Quinazolines/chemistry ; Quinazolines/metabolism ; Quinazolines/pharmacology ; Structure-Activity Relationship ; Dyrk Kinases
    Chemical Substances Protein Kinase Inhibitors ; Quinazolines ; Clk dual-specificity kinases (EC 2.7.1.-) ; Protein-Tyrosine Kinases (EC 2.7.10.1) ; Protein Serine-Threonine Kinases (EC 2.7.11.1)
    Language English
    Publishing date 2019-01-26
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2019.01.052
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.B 784: Show issues Location:
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