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    1,2,6-Thiadiazinones as Novel Narrow Spectrum Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CaMKK2) Inhibitors.

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    Author
    Asquith, CRM; Godoi, PH; Couñago, RM; Laitinen, T; Scott, JW; Langendorf, CG; Oakhill, JS; Drewry, DH; Zuercher, WJ; Koutentis, PA; ...
    Date
    2018-05-19
    Source Title
    Molecules
    Publisher
    MDPI AG
    University of Melbourne Author/s
    Oakhill, Jonathan; Scott, John; Langendorf, Christopher Grant
    Affiliation
    Medicine and Radiology
    Metadata
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    Document Type
    Journal Article
    Citations
    Asquith, C. R. M., Godoi, P. H., Couñago, R. M., Laitinen, T., Scott, J. W., Langendorf, C. G., Oakhill, J. S., Drewry, D. H., Zuercher, W. J., Koutentis, P. A., Willson, T. M. & Kalogirou, A. S. (2018). 1,2,6-Thiadiazinones as Novel Narrow Spectrum Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CaMKK2) Inhibitors.. Molecules, 23 (5), pp.1221-1221. https://doi.org/10.3390/molecules23051221.
    Access Status
    Open Access
    URI
    http://hdl.handle.net/11343/255244
    DOI
    10.3390/molecules23051221
    Open Access at PMC
    http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6019134
    Abstract
    We demonstrate for the first time that 4H-1,2,6-thiadiazin-4-one (TDZ) can function as a chemotype for the design of ATP-competitive kinase inhibitors. Using insights from a co-crystal structure of a 3,5-bis(arylamino)-4H-1,2,6-thiadiazin-4-one bound to calcium/calmodulin-dependent protein kinase kinase 2 (CaMKK2), several analogues were identified with micromolar activity through targeted displacement of bound water molecules in the active site. Since the TDZ analogues showed reduced promiscuity compared to their 2,4-dianilinopyrimidine counter parts, they represent starting points for development of highly selective kinase inhibitors.

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