Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:3.5.1.4 (
deaminase
)
5,113
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Deamination of the nucleoside analogues
ARA-C
and 5-AZA-CdR by CR
deaminase
results in a loss of antileukemic activity. To prevent the inactivation of these analogues, inhibitors of CR
deaminase
may prove to be useful agents. In the present study we investigated the effects of the
deaminase
inhibitors Zebularine, 5-F-Zebularine, and diazepinone riboside on the deamination of CR,
ARA-C
, and 5-AZA-CdR using highly purified human CR
deaminase
(EC 3.5.4.5). These inhibitors produced a competitive type of inhibition with each substrate, the potency of which followed the patterns diazepinone riboside greater than 5-F-Zebularine and THU greater than Zebularine. 5-AZA-CdR was more sensitive than
ARA-C
to the inhibition produced by these
deaminase
inhibitors. The inhibition constants for diazepinone riboside lay in the range of 5-15 nM, suggesting that this inhibitor could be an excellent candidate for use in combination chemotherapy with either
ARA-C
or 5-AZA-CdR in patients with leukemia.
...
PMID:Potent inhibitors for the deamination of cytosine arabinoside and 5-aza-2'-deoxycytidine by human cytidine deaminase. 137 34
