Sandbox Reserved 693
From Proteopedia
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[[Image:Mercaptopurine.png]] | [[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 | + | 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 <scene name='Sandbox_Reserved_693/Gmp/1'>GMP</scene>. Analysis will focus on the <scene name='Sandbox_Reserved_693/Plain_hgprt/1'>structure of HGPRT with GMP bound</scene>, since the structure with the 6-MP derivative 6-TGTP is not readily available. |
Revision as of 22:02, 28 April 2013
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. |
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6-Mercaptopurine activity and targeting
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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