A comparison of 11β-chloromethlylestradiol and tamoxifen aziridine as affinity labeling reagents for estrogen receptors

Steroids ◽  
1988 ◽  
Vol 51 (5-6) ◽  
pp. 499-518
Author(s):  
Thomas Ratajczak ◽  
Vincent Atrache ◽  
Peter Antes ◽  
Mark Comber ◽  
Roland Hähnel
Keyword(s):  
Estrogen Receptors ◽  
Affinity Labeling ◽  
Tamoxifen Aziridine

The synthesis and study of some potential affinity labeling reagents for estrogen receptors

Steroids ◽  
1981 ◽  
Vol 38 (5) ◽  
pp. 537-555 ◽  
Author(s):  
Thomas Ratajczak ◽  
Peter N. Sheppard ◽  
Robert J. Capon ◽  
Roland Hähnel
Keyword(s):  
Estrogen Receptors ◽  
Affinity Labeling

100. Highly selective affinity labeling of the estrogen receptor with tamoxifen aziridine

1982 ◽  
Vol 17 (3) ◽  
pp. xxxiv
Author(s):  
J.A. Katzenellenbogen ◽  
K.E. Carlson ◽  
D.W. Robertson ◽  
D.F. Heiman
Keyword(s):  
Estrogen Receptor ◽  
Affinity Labeling ◽  
Tamoxifen Aziridine

Localization of the estrogen receptor in uterine cells by affinity labeling with [3H]tamoxifen aziridine

1991 ◽  
Vol 39 (1) ◽  
pp. 131-132 ◽  
Author(s):  
Diane M. Ignar-Trowbridge ◽  
Karen G. Nelson ◽  
Kim A. Ross ◽  
Todd F. Washburn ◽  
Kenneth S. Korach ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Affinity Labeling ◽  
Tamoxifen Aziridine

Comparison of Tritiated Estradiol and Tamoxifen Aziridine for Measurement of Estrogen Receptors in Human Breast Cancer Cytosolss

1991 ◽  
Vol 83 (21) ◽  
pp. 1553-1559 ◽  
Author(s):  
Martine J. Piccart ◽  
Carl Muquardt ◽  
Carine Bosman ◽  
Pascale Pirotte ◽  
Stéphane Veenstra ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptors ◽  
Human Breast Cancer ◽  
Human Breast ◽  
Tamoxifen Aziridine

m-[o-(2-Chloro-5-Fluorosulfonylphenylureido)Phenoxybutoxy]Benzamidine: Affinity Labeling Reagent Which Can Identify Secondary Binding Sites of Coagulation Complement and Fibrinolytic Serine Proteases

1979 ◽  
Author(s):  
D Bing ◽  
D Robison ◽  
J Andrews ◽  
R Laura
Keyword(s):  
Binding Sites ◽  
Serine Proteases ◽  
Enzyme Inhibitor ◽  
Molecular Model ◽  
Factor Xa ◽  
Affinity Labeling ◽  
Catalytic Center ◽  
Inhibitor Complex ◽  
Polypeptide Chains ◽  
Kinetics Of

We have determined that m-[o-(2-chloro-5-fluorosulfonylphenylureido)phenoxybutoxy]benza-midine [mCP(PBA)-F] is an affinity labeling reagent which labels both polypeptide chains of thrombin, factor Xa, complement component CIS and plasmin. As this means it is reacting outside of the catalytic center, we have called this reagent an exo-site affinity labeling reagent. Progressive irreversible inhibition of these enzymes by this reagent is rapid (k1st 2.5-4.6 x 10-3sec-1), the kinetics of inactivation are consistent with inhibition proceding via formation of a specific enzyme-inhibitor complex analogous to a Michaelis-Menton complex (KL - 115-26 μM), and diisopropylfluorophosphate or p-amidino-phenylmethanesulfonyfluoride Prevent labeling by [3H]mCP(PBA)-F. A molecular model of mCP(PBA)-F shows that the reactive SO2F group can be 17 A from the cationic amidine. The data are consistent with the hypothesis that both peptide chains are required for the specific proteolytic activity exhibited by these proteases and that the peptide chain which does not contain the active site serine is close to the catalytic center. (Supported by NIH and AHA grants

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