Sandbox E20: Difference between revisions
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==Conclusions== | ==Conclusions== | ||
The X-ray structure shows, a posteriori, that the design of E2020 took advantage of several important features of the active-site gorge of AChE, to produce a drug with both high affinity for AChE and a high degree of selectivity for AChE versus butyrylcholinesterase (BChE). It also delineates voids within the gorge that are not occupied by E2020 and could provide sites for potential modification of E2020 to produce drugs with improved pharmacological profiles. | The X-ray structure shows, a posteriori, that the design of E2020 took advantage of several important features of the active-site gorge of AChE, to produce a drug with both high affinity for AChE and a high degree of selectivity for AChE versus butyrylcholinesterase (BChE). It also delineates voids within the gorge that are not occupied by E2020 and could provide sites for potential modification of E2020 to produce drugs with improved pharmacological profiles. | ||
<scene name='90/902074/Cartoon_and_e20/1'>cartoon_and_E2020</scene> | |||
<jmol> | |||
<jmolCheckbox> | |||
<scriptWhenUnChecked>hide E20 or hidden | |||
</scriptWhenUnChecked> | |||
<scriptWhenchecked>hide hidden and not (E20) | |||
</scriptWhenchecked> | |||
<checked>true</checked> | |||
<text>ligand</text> | |||
</jmolCheckbox> | |||
</jmol> | |||
<scene name='90/902074/T/1'>residues near E2020</scene> | |||
==About this Structure== | ==About this Structure== | ||
