A paper in Nature reveals the high-resolution cryoEM structure of DNA-PKcs in complex with inhibitors, providing insights into their mode of action and specificity, to help the discovery of new cancer drugs targeting DNA-PKcs
. The PIKK regulatory domain of mTOR is lifted and removed completely from the substrate-binding site while the PRD of DNA-PKcs still docks there, although it is lifted compared to apo DNA-PKcs. DNA-PKcs/ATPγS-Mgis coloured orange. PRDs of DNA-PKcs and mTOR are circled in dashed lines., Close-up view of the ligand-binding pocket of DNA-PKcs and mTOR. Residues contributing to the pocket are highly conserved between DNA-PKcs and mTOR.
, Comparison of mTOR in complex with specific inhibitor Torin2 and pp242 and DNA-PKcs in complex with specific inhibitor AZD7648 and M3814 and close-up view. The major differences are in the p-loop conformations. Moreover, among the few residues that differ, Met3729 of DNA-PKcs is more extended compared to the Ile2163 of mTOR at the equivalent position and acts as the gatekeeper. Moreover, it affects the conformation of DNA-PKcs p-loop when different ligands bind.
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