Sandbox Reserved 693

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This Sandbox is Reserved from 30/01/2013, through 30/12/2013 for use in the course "Biochemistry II" taught by Hannah Tims at the Messiah College. This reservation includes Sandbox Reserved 686 through Sandbox Reserved 700.
To get started:
  • Click the edit this page tab at the top. Save the page after each step, then edit it again.
  • Click the 3D button (when editing, above the wikitext box) to insert Jmol.
  • show the Scene authoring tools, create a molecular scene, and save it. Copy the green link into the page.
  • Add a description of your scene. Use the buttons above the wikitext box for bold, italics, links, headlines, etc.

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6-Mercaptopurine activity and targeting

GMP bound to HGPRT

Drag the structure with the mouse to rotate

Image:Mercaptopurine.png

6-Mercaptopurine (6-MP) is an anti-cancer drug used for decades to treat acute lymphoblastic leukemia, and in recent years for other conditions such as inflammatory bowel disease. The drug is a purine derivative that resembles guanine, except that it has a thiol on the C6 of the base ring structure instead of a carbonyl, and is missing the amine on C2. Within the cell, 6-MP is converted to 6-thioguanosine monophosphate (6-TGMP) via hypoxanthine-guanine phosphoribosyltransferase (HGPRT) because it fits into the same active site as guanine, which is converted by the same enzyme to . Analysis will focus on the , since the structure with the 6-MP derivative 6-TGTP is not readily available.




3ns1 - 6mp bound to bovine xanthine oxidase 2bzg - TPMT



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