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Effect of Estramustine Phosphate on the Assembly of Isolated Bovine Brain Microtubules and Fast Axonal Transport in the Frog Sciatic Nerve

Kanje, Martin LU ; Ekström, Per LU ; Edström, Anders LU ; Deinum, Johanna; Wallin, Margareta and Hartley-Asp, Beryl (1985) In Cancer Research 45(5). p.2234-2239
Abstract

Estramustine phosphate (0.01 to 0.5 nriM), an estradiol mustard derivative used in the therapy of prostatic carcinoma, inhibited the assembly of brain microtubule proteins in vitro and disassembled preformed microtubules. In the presence of estramustine phosphate, the minimum microtubule-protein concentration sufficient for the assembly of microtubules was increased. Low concentrations of taxoi (20 μM) completely reversed the inhibition of assembly by estramustine phosphate. The effects were specific to estramustine phosphate since neither estradiol 170-phosphate, the hormonal moiety of the drug, nor nornitrogen mustard, the alkylating moiety, had any effect on assembly. Estramustine phosphate (0.1 to 0.5 HIM) was also found to... (More)

Estramustine phosphate (0.01 to 0.5 nriM), an estradiol mustard derivative used in the therapy of prostatic carcinoma, inhibited the assembly of brain microtubule proteins in vitro and disassembled preformed microtubules. In the presence of estramustine phosphate, the minimum microtubule-protein concentration sufficient for the assembly of microtubules was increased. Low concentrations of taxoi (20 μM) completely reversed the inhibition of assembly by estramustine phosphate. The effects were specific to estramustine phosphate since neither estradiol 170-phosphate, the hormonal moiety of the drug, nor nornitrogen mustard, the alkylating moiety, had any effect on assembly. Estramustine phosphate (0.1 to 0.5 HIM) was also found to reversibly inhibit fast axonal transport in the frog sciatic nerve. The nerve content of adenosine triphosphate, adenosine diphosphate, and adenosine monophosphate was not significantly affected by estramustine phosphate. Our results suggest that the cytotoxic action of estramustine phosphate could be dependent partially on an interaction with microtubules, probably via the microtubule-associated proteins.

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author
organization
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type
Contribution to journal
publication status
published
subject
keywords
bovine brain microtubules, axonal transport
in
Cancer Research
volume
45
issue
5
pages
6 pages
publisher
American Association for Cancer Research Inc.
external identifiers
  • scopus:0021809304
ISSN
0008-5472
language
English
LU publication?
yes
id
902852e3-ac31-4d52-810b-aef6655f1cfd
date added to LUP
2016-12-07 14:27:32
date last changed
2017-09-10 05:12:52
@article{902852e3-ac31-4d52-810b-aef6655f1cfd,
  abstract     = {<p>Estramustine phosphate (0.01 to 0.5 nriM), an estradiol mustard derivative used in the therapy of prostatic carcinoma, inhibited the assembly of brain microtubule proteins in vitro and disassembled preformed microtubules. In the presence of estramustine phosphate, the minimum microtubule-protein concentration sufficient for the assembly of microtubules was increased. Low concentrations of taxoi (20 μM) completely reversed the inhibition of assembly by estramustine phosphate. The effects were specific to estramustine phosphate since neither estradiol 170-phosphate, the hormonal moiety of the drug, nor nornitrogen mustard, the alkylating moiety, had any effect on assembly. Estramustine phosphate (0.1 to 0.5 HIM) was also found to reversibly inhibit fast axonal transport in the frog sciatic nerve. The nerve content of adenosine triphosphate, adenosine diphosphate, and adenosine monophosphate was not significantly affected by estramustine phosphate. Our results suggest that the cytotoxic action of estramustine phosphate could be dependent partially on an interaction with microtubules, probably via the microtubule-associated proteins.</p>},
  author       = {Kanje, Martin and Ekström, Per and Edström, Anders and Deinum, Johanna and Wallin, Margareta and Hartley-Asp, Beryl},
  issn         = {0008-5472},
  keyword      = {bovine brain microtubules,axonal transport},
  language     = {eng},
  month        = {05},
  number       = {5},
  pages        = {2234--2239},
  publisher    = {American Association for Cancer Research Inc.},
  series       = {Cancer Research},
  title        = {Effect of Estramustine Phosphate on the Assembly of Isolated Bovine Brain Microtubules and Fast Axonal Transport in the Frog Sciatic Nerve},
  volume       = {45},
  year         = {1985},
}