2018年5月18日星期五

Alovudine|POLG inhibitor

Alovudine|POLG inhibitor

DC Chemicals, Website:www.dcchemicals.com

Product Name: Alovudine|CAS: 25526-93-6|Cat No: DC10735|Other Names: Alovudine, MIV-310; CL-184824; MIV310; CL184824; MIV 310; CL 184824

Alovudine is a DNA polymerase subunit gamma-1 (POLG) inhibitor, shows promise for treating AML.

Alovudine is a dideoxynucleoside thymidine analogue, which when phosphorylated shows POLG inhibitory activity. Investigators from Medivir and their collaborators aimed to study the effects of alovudine in acute myeloid leukemia (AML) cells both in vitro and in vivo. The results showed that when OCI-AML2 cells were separately treated with alovudine and AraC, there was a reduction in the biogenesis of mtDNA and oxidative phosphorylation was impaired, as were cell growth and viability in alovudine-treated cells compared to AraC-treated cells. When alovudine was administered to AML mice (n = 10) (dosed at 50 mg/kg b.i.d. p.o.) for 11 days, it was shown that tumor volume was reduced in these mice compared to control mice (n = 10), as was tumor weight, showing a clear antileukemic activity. These results confirm alovudine to be a potent POLG inhibitor that impairs oxidative phosphorylation in AML, decreasing its growth both in vitro an in vivo

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