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5(ALPHA-BROMOACETYL)-2'-DEOXYURIDINE 5'-PHOSPHATE - MECHANISM BASED AFFINITY LABEL FOR THYMIDYLATE SYNTHETASE

被引：9
作者：
BROUILLETTE, CB
CHANG, CTC
MERTES, MP
机构：
[1] Department of Medicinal Chemistry, School of Pharmacy, University of Kansas, Lawrence
来源：
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1979年 / 87卷 / 02期
关键词：
D O I：
10.1016/0006-291X(79)91838-2
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
5(α-Bromoacetyl)-2′-deoxyuridine 5′-phosphate is an active site-directed irreversible inhibitor of thymidylate synthetase from Lactobacillus casei. The reversible inhibition (KI4uM) is competitive with substrate and on incubation the reversible enzyme-inhibitor complex is converted to the irreversible complex with a first order rate constant (k2) of 0.15 min-1. © 1979.
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收藏
页码：613 / 618
页数：6
相关论文
共 11 条
[1]   5-IODOACETAMIDOMETHYL-2'-DEOXYURIDINE 5'-PHOSPHATE - SELECTIVE INHIBITOR OF MAMMALIAN THYMIDYLATE SYNTHETASES [J].
BARFKNECHT, RL ;
HUETROSE, RA ;
KAMPF, A ;
MERTES, MP .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1976, 98 (16) :5041-5043
[2]  
CHANG CC, UNPUBLISHED
[3]   STRUCTURES OF REVERSIBLE AND IRREVERSIBLE COMPLEXES OF THYMIDYLATE SYNTHETASE AND FLUORINATED PYRIMIDINE NUCLEOTIDES [J].
DANENBER.PV ;
LANGENBA.RJ ;
HEIDELBE.C .
BIOCHEMISTRY, 1974, 13 (05) :926-933
[4]   THYMIDYLATE SYNTHETASE - TARGET ENZYME IN CANCER CHEMOTHERAPY [J].
DANENBERG, PV .
BIOCHIMICA ET BIOPHYSICA ACTA, 1977, 473 (02) :73-92
[5]  
FRIEDKIN M, 1973, ADV ENZYMOL RAMB, V38, P235
[6]  
KITZ R, 1962, J BIOL CHEM, V237, P3245
[7]  
LOMAX MIS, 1967, J BIOL CHEM, V242, P109
[8]   5-NITRO-2'-DEOXYURIDYLATE - MECHANISM-BASED INHIBITOR OF THYMIDYLATE SYNTHETASE [J].
MATSUDA, A ;
WATAYA, Y ;
SANTI, DV .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1978, 84 (03) :654-659
[9]   5-NITRO-2'-DEOXYURIDINE 5'-MONOPHOSPHATE IS A POTENT IRREVERSIBLE INHIBITOR OF LACTOBACILLUS-CAESI THYMIDYLATE SYNTHETASE [J].
MERTES, MP ;
CHANG, CTC ;
DECLERCQ, E ;
HUANG, GF ;
TORRENCE, PF .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1978, 84 (04) :1054-1059
[10]   AN ISOTOPIC ASSAY FOR THYMIDYLATE SYNTHETASE [J].
ROBERTS, D .
BIOCHEMISTRY, 1966, 5 (11) :3546-&
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