Sandbox southuniversity6: Difference between revisions
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The structure to the right is the first HIV integrase inhibitor approved in the US, raltegravir (Isentress). Compare its structure to that of the prototype DKA shown above. Can you see a hydrophobic group at one end of the molecule, with hydrogen bond donor, acceptor, and donor functional groups next to each other? | The structure to the right is the first HIV integrase inhibitor approved in the US, raltegravir (Isentress). Compare its structure to that of the prototype DKA shown above. Can you see a hydrophobic group at one end of the molecule, with hydrogen bond donor, acceptor, and donor functional groups next to each other? | ||
<StructureSection load='RLT' size='500' side='right' caption='Structure of the first HIV integrase inhibitor to market, raltegravir (PDB entry [[RLT]])' scene=''> | <StructureSection load='RLT' size='500' side='right' caption='Structure of the first HIV integrase inhibitor to market, raltegravir (PDB entry [[RLT]])' scene=''>Compare the 3D structure at the right to that of the 2D depiction above. Note the 4-fluoro phenyl group, the hydrogen bond donor, and the 2 hydrogen bond acceptors that are part of the pharmacophore. | ||
HIV integrase is the enzyme that is responsible for inserting viral DNA into host (human) DNA. The next interactive structure shows raltegravir bound to a viral integrase enzyme. The viral and host DNA are also shown | |||
<scene name='Sandbox_southuniversity6/3oya_trim/1'>TextToBeDisplayed</scene> | |||
</StructureSection> | </StructureSection> | ||