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The interaction of 5-ethynyl-2'-deoxyuridylate (5-ethynyl-dUMP; 1) with thymidylate (dTMP) synthetase has been investigated. The compound was an inhibitor of the enzyme, competitive with 2'-deoxyuridylate (dUMP) when the reaction was initiated by addition of enzyme (Ki = 2.7 X 10(-6) M). However, upon preincubation of 1 with dTMP synthetase, the inhibition pattern became noncompetitive. The time course of the enzyme reaction in the presence of 1 was nonlinear, indicating an increase in binding with time. Irreversible inactivation of the enzyme did not occur. The compound did not appear to become altered structurally as a result of interaction with the enzyme. A ternary complex was formed among dTMP synthetase, compound 1, and 5,10-methylenetetrahydrofolate, which was stable enough to survive Sephadex G-25 filtration but dissociated upon denaturation of the enzyme.
P V Danenberg, and
R S Bhatt, and
N G Kundu, and
K Danenberg, and
C Heidelberger
March 1983,
Biochemistry,
P V Danenberg, and
R S Bhatt, and
N G Kundu, and
K Danenberg, and
C Heidelberger
June 1980,
The Journal of biological chemistry,
P V Danenberg, and
R S Bhatt, and
N G Kundu, and
K Danenberg, and
C Heidelberger
July 1975,
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P V Danenberg, and
R S Bhatt, and
N G Kundu, and
K Danenberg, and
C Heidelberger
July 1972,
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P V Danenberg, and
R S Bhatt, and
N G Kundu, and
K Danenberg, and
C Heidelberger
January 1977,
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P V Danenberg, and
R S Bhatt, and
N G Kundu, and
K Danenberg, and
C Heidelberger
September 1972,
Biochemical and biophysical research communications,
P V Danenberg, and
R S Bhatt, and
N G Kundu, and
K Danenberg, and
C Heidelberger
November 1983,
The Journal of biological chemistry,
P V Danenberg, and
R S Bhatt, and
N G Kundu, and
K Danenberg, and
C Heidelberger
January 1974,
Methods in enzymology,
P V Danenberg, and
R S Bhatt, and
N G Kundu, and
K Danenberg, and
C Heidelberger
March 1971,
Biochemical and biophysical research communications,
P V Danenberg, and
R S Bhatt, and
N G Kundu, and
K Danenberg, and
C Heidelberger
November 1975,
Biochemical and biophysical research communications,
