Uptake of Estramustine Phosphate (Estracyt) Metabolites in Prostatic Cancer

Norlén, Bo Johan; Andersson, Sven-Börje; Björk, Per; Gunnarsson, Per Olov; Fritjofsson, Å

doi:10.1016/s0022-5347(17)41926-4

Cited by 37 publications

(24 citation statements)

References 22 publications

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“…play an important role in the mechanism of action of estramustine by concentrating the active metabolites of this drug in prostatic tumors [5]. Recently, an immunoreactive protein to rat EMBP, which binds to 3H-estramustine with the same affinity, was detected in human pros tate [6], By means of a radioimmunoassay (RIA) using an antibody raised against rat EMBP, we found that: (i) human prostate contained immunoreactive EMBP [7], and (ii) in human benign prostatic hyperplasia (BPH) EMBP was found to be predominantly localized in the epithelial fraction [8].…”

Section: Introductionmentioning

confidence: 99%

Estramustine-Binding Protein in Carcinoma and Benign Hyperplasia of the Human Prostate

Shiina

Urakami²,

Shirakawa³

et al. 1996

Eur Urol

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Section: Introductionmentioning

confidence: 99%

Estramustine-Binding Protein in Carcinoma and Benign Hyperplasia of the Human Prostate

Shiina

Urakami²,

Shirakawa³

et al. 1996

Eur Urol

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“…It appears that the presence of EMBP in tumor tissue may be important for drug uptake and accumulation in specific tissues. For prostatic carcinoma it has been proposed that EMBP may be a prerequisite for antitumor activity [34][35][36][37][38]. EMBP binds EaM with a binding affinity of K d = 10-30 nM [39,40].…”

Section: General Pharmacology and Binding Characteristicsmentioning

confidence: 99%

Estramustine in malignant glioma

Henriksson

et al. 1996

J Neuro-Oncol

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Estramustine, a carbamate ester combining 17 beta-estradiol and nornitrogen mustard, has primarily been employed in the treatment of advanced prostatic carcinoma. However, a significant amount of preclinical investigation has been directed toward estramustine's activity against human malignant glioma. These studies have demonstrated that estramustine has potent antiproliferative effects against malignant glioma both in vitro and in vivo. Similar antimitotic effects also have been demonstrated for other carbamate esters. Estramustine does not impair proliferation of nonneoplastic astrocytes at concentrations that inhibit glioma cells. Although the reasons for this selective activity remain to be determined, it has been shown that malignant gliomas expresses an estramustine-specific binding site, estramustine-binding protein, more than brain tissue. In the clinical situation, an uptake and accumulation of estramustine in human glioma tissue have been demonstrated. Estramustine has been shown to enhance the cytotoxic effects of irradiation in relatively radioresistant glioma cells both in cell culture and in a rat glioma model. Estramustine has been regarded as mainly an anti-mitotic drug but recently other effects such as inhibition of DNA synthesis, induction of apoptosis, and membrane alterations have been shown. This report summarizes the preclinical observations concerning the effects of estramustine and related compounds on human malignant gliomas. These findings form the basis for proposing further laboratory and clinical investigation regarding estramustine and human malignant gliomas.

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“…Its expression and/or concentration was profoundly affected by extrinsic androgen administration, suggesting that EMBP in rat prostate is an androgendependent protein [5]. In the human prostate, EMBP was also detectable using an antibody raised against rat EMBP by means of radioimmunoassay (RIA) and/ or immunohistochemistry [6,7], suggesting that EMBP plays an important role in picking up the estramustine from general circulation into PC cells [8]. Recently, an EMBP-like protein has been reported to be expressed in the tumors originating from organs other than androgen target tissues such as brain tumor [9,10], lung cancer [11,12], and melanocytic tumor [13].…”

Section: Introductionmentioning

confidence: 99%