Intramolecular cyclization of N-phenyl N′(2-chloroethyl)ureas leads to active N-phenyl-4,5-dihydrooxazol-2-amines alkylating β-tubulin Glu198 and prohibitin Asp40
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چکیده
منابع مشابه
Characterization of the Covalent Binding of N-Phenyl-N -(2-chloroethyl)ureas to -Tubulin: Importance of Glu198 in Microtubule Stability
N-Phenyl-N -(2-chloroethyl)ureas (CEUs) are antimicrotubule agents interacting covalently with -tubulin near the colchicine-binding site (C-BS). Glutamyl 198 residue in -tubulin (Glu198), which is adjacent to the C-BS behind the two potent nucleophilic residues, Cys239 and Cys354, has been shown to covalently react with 1-(2-chloroethyl)-3-(4iodophenyl)urea (ICEU). By use of mass spectrometry, ...
متن کاملCharacterization of the covalent binding of N-phenyl-N'-(2-chloroethyl)ureas to {beta}-tubulin: importance of Glu198 in microtubule stability.
N-Phenyl-N'-(2-chloroethyl)ureas (CEUs) are antimicrotubule agents interacting covalently with β-tubulin near the colchicine-binding site (C-BS). Glutamyl 198 residue in β-tubulin (Glu198), which is adjacent to the C-BS behind the two potent nucleophilic residues, Cys239 and Cys354, has been shown to covalently react with 1-(2-chloroethyl)-3-(4-iodophenyl)urea (ICEU). By use of mass spectrometr...
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ژورنال
عنوان ژورنال: Biochemical Pharmacology
سال: 2011
ISSN: 0006-2952
DOI: 10.1016/j.bcp.2011.02.014