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Träfflista för sökning "WFRF:(Wallin B G) srt2:(1990-1994)"

Sökning: WFRF:(Wallin B G) > (1990-1994)

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  • Moraga, D, et al. (författare)
  • Estramustine-phosphate binds to a tubulin binding domain on microtubule-associated proteins MAP-2 and tau.
  • 1992
  • Ingår i: Biochimica et biophysica acta. - 0006-3002. ; 1121:1-2, s. 97-103
  • Tidskriftsartikel (refereegranskat)abstract
    • Estramustine-phosphate (EMP), a phosphorylated conjugate of estradiol and nor-nitrogen mustard binds to microtubule-associated proteins MAP-2 and tau. It was shown that this estramustine derivative inhibits the binding of the C-terminal tubulin peptide beta-(422-434) to both MAP-2 and tau. This tubulin segment constitutes a main binding domain for these microtubule-associated proteins. Interestingly, estramustine-phosphate interacted with the synthetic tau peptides V187-G204 and V218-G235, representing two major repeats within the conserved microtubule-binding domain on tau and also on MAP-2. This observation was corroborated by the inhibitory effects of estramustine-phosphate on the tau peptide-induced tubulin assembly into microtubules. On the other hand, the nonphosphorylated drug estramustine failed to block the MAP peptide-induced assembly, indicating that the negatively charged phosphate moiety of estramustine-phosphate is of importance for its inhibitory effect. These findings suggest that the molecular sites for the action of estramustine-phosphate are located within the microtubule binding domains on tau and MAP-2.
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