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Synthesis and Evaluation of a Library of Trifunctional Scaffold-Derived Compounds as Modulators of the Insulin Receptor

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F16%3A00469437" target="_blank" >RIV/61388963:_____/16:00469437 - isvavai.cz</a>

  • Result on the web

    <a href="http://pubs.acs.org/doi/full/10.1021/acscombsci.6b00132" target="_blank" >http://pubs.acs.org/doi/full/10.1021/acscombsci.6b00132</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1021/acscombsci.6b00132" target="_blank" >10.1021/acscombsci.6b00132</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Synthesis and Evaluation of a Library of Trifunctional Scaffold-Derived Compounds as Modulators of the Insulin Receptor

  • Original language description

    We designed a combinatorial library of trifunctional scaffold-derived compounds, which were derivatized with 30 different in-house-made azides. The compounds were proposed to mimic insulin receptor (IR)-binding epitopes in the insulin molecule and bind to and activate this receptor. This work has enabled us to test our synthetic and biological methodology and to prove its robustness and reliability for the solid-phase synthesis and testing of combinatorial libraries of the trifunctional scaffold-derived compounds. Our effort resulted in the discovery of two compounds, which were able to weakly induce the autophosphorylation of IR and weakly bind to this receptor at a 0.1 mM concentration. Despite these modest biological results, which well document the well-known difficulty in modulating protein protein interactions, this study represents a unique example of targeting the IR with a set of nonpeptide compounds that were specifically designed and synthesized for this purpose. We believe that this work can open new perspectives for the development of next-generation insulin mimetics based on the scaffold structure.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

  • CEP classification

    CE - Biochemistry

  • OECD FORD branch

Result continuities

  • Project

    <a href="/en/project/GA14-17305S" target="_blank" >GA14-17305S: Insulin mimetics</a><br>

  • Continuities

    I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Others

  • Publication year

    2016

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    ACS Combinatorial Science

  • ISSN

    2156-8952

  • e-ISSN

  • Volume of the periodical

    18

  • Issue of the periodical within the volume

    12

  • Country of publishing house

    US - UNITED STATES

  • Number of pages

    13

  • Pages from-to

    710-722

  • UT code for WoS article

    000389787300003

  • EID of the result in the Scopus database

    2-s2.0-85006024527