The scheme depicts a possible mechanism of cross-linking by erbstatin and related analogues. A mechanism of action is proposed which involves initial oxidation to reactive quinone intermediates that subsequently cross-link protein nucleophiles via multiple 1,4-Michael-type additions. Similar alkylation of protein by protein-tyrosine kinase inhibitors, such as herbimycin A, has been invoked.
Lab/Branch/Program:
Chemical Biology Laboratory
Citation:
Caroline Stanwell, Bin Ye, Stuart H Yuspa and Terrence R Burke Jr. in Biochemical Pharmacology 1996, 52 (3), 475-480.
Published Date:
August, 1996