SandboxPKA: Difference between revisions
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- The '''<scene name='Dasatinib/Mact/1'>Activation Loop Movement</scene>''' involves Tyr412 responsible for activation of the kinase activity. | - The '''<scene name='Dasatinib/Mact/1'>Activation Loop Movement</scene>''' involves Tyr412 responsible for activation of the kinase activity. | ||
- In the unactivated, autoinhibited conformation, the Asp-810-Phe-811-Gly-812 (DFG) triad at the beginning of the A-loop is in the “DFG-out” conformation. The DFG motif can <scene name='Dasatinib/Mdfg/3'>move</scene> when | - In the unactivated, autoinhibited conformation, the Asp-810-Phe-811-Gly-812 (DFG) triad at the beginning of the A-loop is in the “DFG-out” conformation. The DFG motif can <scene name='Dasatinib/Mdfg/3'>move</scene> when Tyr412 is phosphorylated, thus promoting the change towards the active conformation. <Ref>PMID: 19164557</Ref> | ||
- The '''myristoyl group''' complements activation loop in turning on and off c-Abl protein. It has been shown to be a key regulator of this kinase. | - The '''myristoyl group''' complements activation loop in turning on and off c-Abl protein. It has been shown to be a key regulator of this kinase. | ||
