EC Number |
Inhibitors |
Structure |
---|
2.1.1.45 | more |
5FU-LV, combination of 5-fluorouracil and leucovorin |
|
2.1.1.45 | more |
combination of 5-FU and leucovorin, enhances the inhibition of thymidylate synthase, 0.001 mM inhibits growth to only 1%, inhibition can be rescued by uridine to an almost normal value of 83% |
|
2.1.1.45 | more |
combination of leucovorin and 5-fluorouracil 5FU-LV, IC50 0.00016 (FM3A/0 cell) |
|
2.1.1.45 | more |
inhibitory effect of antifolate drugs on enzymatic activity, and inhibitory activity of four aporphine alkaloids from Rollinia pittieri and Pseudomalmea boyacana, and some 2,4-diamino-pyrimidine antifolates, overview |
|
2.1.1.45 | more |
analysis of enzyme susceptibility to a range of classical inhibitors normally used in the treatment of cancer, bacterial or protozoal infections, in vivo effects in presence of absence of thymidine and/or folate, overview. Modulating certain medium components can affect drug sensitivity, presumably by either competition for uptake and competition for the active site of DHFR-TS. In the case of one human thymidylate synthase inhibitor raltitrexed, the inhibitor is more potent against the intact parasite. Addition of extra glutamic acid residues not only improves retention in the cell, but also increases potency against thymidylate synthase, as it does in human cells. No inhibition by FdUMP |
|
2.1.1.45 | ATP |
- |
|
2.1.1.45 | Mg2+ |
- |
|
2.1.1.45 | H2O2 |
- |
|
2.1.1.45 | pyridoxal 5'-phosphate |
- |
|
2.1.1.45 | NaCl |
- |
|