TABLE 2.
Inhibition constants (Ki) of enzymes involved in nucleotide biosynthesis for MTX and its polyglutamates (Allegra et al., 1985a,b; Drake et al., 1987; Baram et al., 1988; Sant et al., 1992)
Ki | MTX-PG1 | MTX-PG2 | MTX-PG3 | MTX-PG4 | MTX-PG5 |
---|---|---|---|---|---|
µM | |||||
DHFR | 11.0 × 10−5 | 17.0 × 10−5 | 8.0 × 10−5 | 8.0 × 10−5 | |
TS | 13.0 | 0.17 | 0.14 | 0.13 | 0.047 |
AICART | 143.9 | 5.47 | 0.56 | 0.056 | 0.057 |
GART | 80 | 57 | 7.1 | 5.1 | 2.5 |
ATase | ND | 550 |
ND, no inhibition was detected.