Title : Efforts in redesigning the antileukemic drug 6-thiopurine: decreasing toxic side effects while maintaining efficacy.

Pub. Date : 2019 Jan 1

PMID : 30774864






3 Functional Relationships(s)
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1 We have previously reported in vitro that the oxidative metabolites of 6TP, specifically 6-thiouric acid (6TU, K i 7 muM), are potent inhibitors of UDP-glucose dehydrogenase (UDPGDH), an enzyme that is responsible for the formation of UDP-glucuronic acid (UDPGA), an essential substrate that is used in detoxification processes in the liver. Mercaptopurine UDP-glucose 6-dehydrogenase Homo sapiens
2 We have previously reported in vitro that the oxidative metabolites of 6TP, specifically 6-thiouric acid (6TU, K i 7 muM), are potent inhibitors of UDP-glucose dehydrogenase (UDPGDH), an enzyme that is responsible for the formation of UDP-glucuronic acid (UDPGA), an essential substrate that is used in detoxification processes in the liver. Mercaptopurine UDP-glucose 6-dehydrogenase Homo sapiens
3 Efforts were undertaken for the construction of 6TP analogs, substituted at the C8 position, to reduce inhibition of UDPGDH while retaining therapeutic efficacy. Mercaptopurine UDP-glucose 6-dehydrogenase Homo sapiens