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Mechanism-based inhibition of thymidylate synthase by 5-(trifluoromethyl)-2'-deoxyuridine 5'-monophosphate

Authors :
Eckstein, Jens W.
Foster, Paul G.
Finer-Moore, Janet
Wataya, Yusuke
Santi, Daniel V.
Source :
Biochemistry. Dec 20, 1994, Vol. 33 Issue 50, p15086, 9 p.
Publication Year :
1994

Abstract

5-(trifluoromethyl)-2'-deoxyuridine 5'-monophosphate (CF3dUMP) inhibits thymidylate synthase (TS) from Lactobacillus casei. In the absence of 5,10-methylenetetrahydrofolate, CF3dUMP binds to the active site of TS and attacks the catalytic nucleophile cysteine 198 to form a covalent complex. Tyrosine 146 and cysteine 198 of the TS are bound covalently to CF3dUMP in the complex.

Details

ISSN :
00062960
Volume :
33
Issue :
50
Database :
Gale General OneFile
Journal :
Biochemistry
Publication Type :
Academic Journal
Accession number :
edsgcl.16645986