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. Author manuscript; available in PMC: 2019 May 8.
Published before final editing as: Curr Pharm Des. 2017 Nov 8:10.2174/1381612823666171109101851. doi: 10.2174/1381612823666171109101851

Table 6.

Substrate activity of various MeP prodrugs with M64V PNP

Compound wild-type M64V M64V/wt
nmoles/mg-hr
9-β-D-ribofuranosyl-6-methylpurine (MeP-R) 84,000 176,000 2
9-(2-deoxy-β-D-ribofuranosyl)-6-methylpurine (MeP-dR) 528,000 593,000 1
9-(α-L-lyxofuranosyl)-MeP 218 10,200 47
9-(5-deoxy-α-L-lyxofuranosyl)-MeP 20 3,500 175
9-(6-deoxy-β-D-allofuranosyl)-6-methylpurine 47 316 7
9-(6-deoxy-α-L-talofuranosyl)-6-methylpurine (5’-methyl (talo) MeP-R) 1,440 86,000 60
9-(2,6-dideoxy-β-D-talofuranosyl)-6-methylpurine 3,600 264,000 73
9-(5,5-dimethyl-β-D-ribofuranosyl)-6-methylpurine - 280 >280
F-dAdo 435,000 1,595,000 4
9-β-D-arabinofuranosyl-2-F-adenine (F-araA) 1,250 1,000 1
9-α-L-lyxofuranosyl-2-F-adenine 7,800 244,000 31
9-(6-deoxy-β-D-allofuranosyl)-2-F-adenine 2,700 92,000 34
9-(6-deoxy-β-D-talofuranosyl)-2-F-adenine (5’-methyl (talo) F-Ado) 34,000 1,360,000 40

Enzymes were incubated with 100 µM of each substrate and the rate of cleavage was determined by HPLC separation of the base form the nucleoside. Each value is the average of at least two experiments that were in good agreement.