Clozapine is an antipsychotic drug which is unusual in that it has no dopamine receptor-blocking activity. Previous studies gave conflicting results whether administration of clozapine induces hyperprolactinemia. In the present study it was shown that a wide concentration range of clozapine does not interfere with dopamine-mediated inhibition of prolactin (PRL) secretion by normal cultured rat ...

The cellular targets for estramustine, an antitumor drug used in the treatment of hormone-refractory prostate cancer, are believed to be the spindle microtubules responsible for chromosome separation at mitosis. Estramustine only weakly inhibits polymerization of purified tubulin into microtubules by binding to tubulin (Kd, approximately 30 microM) at a site distinct from the colchicine or the ...

The antiparasitic effect of a collection of compounds with antimitotic activity has been tested on a mammalian cell line infected with Encephalitozoon intestinalis, a microsporidian causing intestinal and systemic infection in immunocompromised patients. The antiparasitic effect was evaluated by counting the number of parasitophorous vacuoles detected by immunofluorescence. Out of 526 compounds...

Microtubule stabilizers are powerful antimitotic compounds and represent a proven cancer treatment strategy. Several classes of compounds in clinical use or trials, such as the taxanes and epothilones, bind to the same region of β-tubulin. Determining how these molecules interact with tubulin and stabilize microtubules is important both for understanding the mechanism of action and enhancing ch...

Chelation reactions of the antimitotic drug, 6-amino-purine (adenine; abbr. ADN) with the metal ions: Be ( I I ) , AI ( I II ) , Cr ( I I I ) , M n ( I I ) , Fe ( I I I ) , Co (II ) , N i ( I I ) , C u ( I I ) , P b ( I I ) , and U 0 2 ( I I ) have been investigated in aqueous solution at 3 0 ° using B j e r r u m C a l v i n pH titration technique. The formation constants have been determined ...

Compounds that selectively disrupt fungal mitosis have proven to be effective in controlling agricultural pests, but no specific mitotic inhibitor is available for the treatment of systemic mycoses in mammalian hosts. In an effort to identify novel mitotic inhibitors, we used a cell-based screening strategy that exploited the hypersensitivity of a yeast alpha-tubulin mutant strain to growth inh...

Under restricted culture conditions, the growth and division of Saccharomyces cerevisiae was inhibited by the antimitotic drug Colcemid; in contrast, the related drug colchicine had no effect. The difference in the sensitivity of yeast to these two agents was not dependent on their ability to permeate the cell but rather reflected an inherent difference in the affinity of the two drugs for a ce...

Localized treatment of the limb buds of the frog, Xenopus laevis, and the salamander, Ambystoma mexicanum, with the mitotic inhibitor colchicine results in limbs that, when compared with the contralateral control, are smaller in size and have lost skeletal elements. There is a very well defined pattern in terms of what elements are most likely to be lost. For example, frogs that have lost a toe...

PURPOSE OF REVIEW Tumor treating fields (TTFields), an external therapeutic device with antimitotic properties, is a Food and Drug Administration approved treatment for recurrent glioblastoma (GBM) that has been reported to be efficacious in newly diagnosed GBM as well. RECENT FINDINGS Preclinical data show that TTFields is an antimitotic agent that additionally augments response to alkylator...