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Instruments / Technical Area	Publication Details	Published	Actions
I03-Macromolecular Crystallography	1,2,6-thiadiazinones as novel narrow spectrum calcium/calmodulin-dependent protein kinase kinase 2 (CaMKK2) inhibitors Christopher Asquith , Paulo Godoi , Rafael M. Counago , Tuomo Laitinen , John W. Scott , Christopher Langendorf , Jonathan S. Oakhill , David Drewry , William Zuercher , Panayiotis Koutentis , Timothy Willson , Andreas Kalogirou Molecules 23 DOI: 10.3390/molecules23051221 Diamond Proposal Number(s): [14664] Open Access Show Abstract ▼ 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.	May 2018

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