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 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. | + | 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 (although this is later added before it is fully converted to 6-TGMP). 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. |
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It can be seen in the above structure that human HGPRT has two identical subunits, shown in green and blue, each of which catalyzes one reaction. <scene name='Sandbox_Reserved_693/Hgprt_helices_and_sheets/1'>This view</scene> highlights the main structural motifs of the enzyme, with helices in green and sheets in blue. | It can be seen in the above structure that human HGPRT has two identical subunits, shown in green and blue, each of which catalyzes one reaction. <scene name='Sandbox_Reserved_693/Hgprt_helices_and_sheets/1'>This view</scene> highlights the main structural motifs of the enzyme, with helices in green and sheets in blue. | ||
Revision as of 00:20, 29 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 (although this is later added before it is fully converted to 6-TGMP). 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.
It can be seen in the above structure that human HGPRT has two identical subunits, shown in green and blue, each of which catalyzes one reaction. highlights the main structural motifs of the enzyme, with helices in green and sheets in blue.
3ns1 - 6mp bound to bovine xanthine oxidase
2bzg - TPMT
