SandboxPKA: Difference between revisions
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- The '''<scene name='Dasatinib/Mact/1'>Activation Loop Movement</scene>''' contains Tyr412 responsible of activation of kinase activity. | - The '''<scene name='Dasatinib/Mact/1'>Activation Loop Movement</scene>''' contains Tyr412 responsible of activation of kinase activity. | ||
- The unactivated, autoinhibited conformation [in which the Asp-810-Phe-811-Gly-812 (DFG) triad at the beginning of the A-loop is in the “DFG-out”, can <scene name='Dasatinib/Mdfg/3'>move</scene> when ATP Tyr412 is phosphorlated, rising an active conformation. | - The unactivated, autoinhibited conformation [in which the Asp-810-Phe-811-Gly-812 (DFG) triad at the beginning of the A-loop is in the “DFG-out”, can <scene name='Dasatinib/Mdfg/3'>move</scene> when ATP Tyr412 is phosphorlated, rising an active conformation. <Ref>KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients<\Ref> | ||
- The '''myristoyl group''' complement activation loop in turning on and off c-abl protein. It has been shown to be the key regulator of this kinase. | - The '''myristoyl group''' complement activation loop in turning on and off c-abl protein. It has been shown to be the key regulator of this kinase. | ||