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2 Methoxyestrone

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Chantal Guillemette – One of the best experts on this subject based on the ideXlab platform.

  • Urinary oestrogen steroidome as an indicator of the risk of localised prostate cancer progression
    British Journal of Cancer, 2021
    Co-Authors: Jean-philippe Emond, Louis Lacombe, Patrick Caron, Véronique Turcotte, David Simonyan, Armen Aprikian, Fred Saad, Michel Carmel, Simone Chevalier, Chantal Guillemette
    Abstract:

    Background Prostate cancer (PCa) is the most common cancer in North American men. Beyond the established contribution of androgens to disease progprogression, growing evidence suggest that oestrogen-related pathways might also be of clinical importance. The aim of this study was to explore the association of urinary oestrogen levels with clinical outcomes. Methods Urine samples from the prospective multi-institutional PROCURE cohort were collected before RP for discovery ( n  = 259) and validation ( n  = 253). Urinary total oestrogens (unconjugated + conjugated), including oestrone and oestradiol, their bioactive and inactive catechol and methyl derivatives ( n  = 15), were measured using mass spectrometry (MS). Results The median follow-up time for the discovery and replication cohorts was 7.6 and 6.5 years, respectively. Highly significant correlations between urinary oestrogens were observed; however, correlations with circulating oestrogens were modest. Our findings indicate that higher levels of urinary oestriol and 16-ketoestradiol were associated with lower risk of BCR. In contrast, higher levels of 2Methoxyestrone were associated with an increased risk of development of metastasis/deaths. Conclusions Our data suggest that urinary levels of oestriol and 16-ketoestradiol metabolites are associated with a more favourable outcome, whereas those of 2Methoxyestrone are associated with an elevated risk of metastasis after RP. Further studies are required to better understand the impact of oestrogens on disease biology and as easily accessible urine-based risk-stratification markers.

  • Urinary oestrogen steroidome as an indicator of the risk of localised prostate cancer progression.
    British journal of cancer, 2021
    Co-Authors: Jean-philippe Emond, Louis Lacombe, Patrick Caron, Véronique Turcotte, David Simonyan, Armen Aprikian, Fred Saad, Michel Carmel, Simone Chevalier, Chantal Guillemette
    Abstract:

    Prostate cancer (PCa) is the most common cancer in North American men. Beyond the established contribution of androgens to disease progprogression, growing evidence suggest that oestrogen-related pathways might also be of clinical importance. The aim of this study was to explore the association of urinary oestrogen levels with clinical outcomes. Urine samples from the prospective multi-institutional PROCURE cohort were collected before RP for discovery (n = 259) and validation (n = 253). Urinary total oestrogens (unconjugated + conjugated), including oestrone and oestradiol, their bioactive and inactive catechol and methyl derivatives (n = 15), were measured using mass spectrometry (MS). The median follow-up time for the discovery and replication cohorts was 7.6 and 6.5 years, respectively. Highly significant correlations between urinary oestrogens were observed; however, correlations with circulating oestrogens were modest. Our findings indicate that higher levels of urinary oestriol and 16-ketoestradiol were associated with lower risk of BCR. In contrast, higher levels of 2Methoxyestrone were associated with an increased risk of development of metastasis/deaths. Our data suggest that urinary levels of oestriol and 16-ketoestradiol metabolites are associated with a more favourable outcome, whereas those of 2Methoxyestrone are associated with an elevated risk of metastasis after RP. Further studies are required to better understand the impact of oestrogens on disease biology and as easily accessible urine-based risk-stratification markers.

M J Reed – One of the best experts on this subject based on the ideXlab platform.

  • the role of 17β hydroxysteroid dehydrogenases in modulating the activity of 2 methoxyestradiol in breast cancer cells
    Cancer Research, 2006
    Co-Authors: Simon P. Newman, M J Reed, Barry V L Potter, Mathew P. Leese, Christopher R Ireson, Helena J Tutill, Joanna M Day, Michael F C Parsons, Atul Purohit
    Abstract:

    The bis-sulfamoylated derivative of 2-methoxyestradiol (2-MeOE2), 2-methoxyestradiol-3,17-O,O-bis-sulfamate (2-MeOE2bisMATE), has shown potent antiproliferative and antiangiogenic activity in vitro and inhibits tumor growth in vivo. 2-MeOE2bisMATE is bioavailable, in contrast to 2-MeOE2 that has poor bioavailability. In this study, we have examined the role of 17beta-hydroxysteroid dehydrogenase (17beta-HSD) type 2 in the metabolism of 2-MeOE2. In MDA-MB-231 cells, which express high levels of 17beta-HSD type 2, and in MCF-7 cells transfected with 17beta-HSD type 2, high-performance liquid chrochromatography analysis showed that a significant proportion of 2-MeOE2 was metabolized to inactive 2Methoxyestrone. Furthermore, MCF-7 cells transfected with 17beta-HSD type 2 were protected from the cytotoxic effects of 2-MeOE2. In contrast, no significant metabolism of 2-MeOE2bisMATE was detected in transfected cells and 17beta-HSD type 2 transfection did not offer protection against 2-MeOE2bisMATE cytotoxicity. This study may go some way to explaining the poor bioavailability of 2-MeOE2, as the gastrointestinal mucosa expresses high levels of 17beta-HSD type 2. In addition, this study shows the value of synthesizing sulfamoylated derivatives of 2-MeOE2 with C17-position modifications as these compounds have improved bioavailability and potency both in vitro and in vivo.

  • Non-steroidal and steroidal sulfamates: new drugs for cancer therapy.
    Molecular and Cellular Endocrinology, 2001
    Co-Authors: A. Purohit, L. W. L. Woo, D Barrow, Hatem Hejaz, R.i. Nicholson, Barry V L Potter, M J Reed
    Abstract:

    Abstract The development of inhibitors to block the formation of estrone and 5-androstenediol from sulfated precursors is an important new strategy for the treatment of breast cancer. In this study a series of tricyclic coumarin sulfamates (665-668 COUMATE) and a tricyclic oxepin sulfamate have been synthesised and tested for their ability to inhibit estrone sulfatase activity (E1-STS). In addition the effect of the steroid-based E1-STS inhibitor, 2Methoxyestrone-3- O –sulfamate (2-MeOEMATE) on the morphology of MDA-MB-231 cells and breast tumour-derived fibroblasts was also examined. The tricyclic coumarin sulfamates and oxepin sulfamate were potent inhibitors of E1-STS activity with IC 50 s ranging from 8 to 250 nM. Of this series 667 COUMATE was the most potent inhibitor (IC 50  = 8 nM) and was three-times more potent than estrone-3- O –sulfamate (EMATE, IC 50  = 25 nM). 667 COUMATE did not stimulate the growth of MCF-7 breast cancer cells and is therefore devoid of estrogenicity. In vivo, 667 COUMATE inhibited E1-STS activity in rat liver tissue to a similar extent to that of EMATE. 2-MeOEMATE had a marked effect on the morphology of MDA-MB-231 cells and breast tumour-derived fibroblasts causing a significant increase in the number of rounded cells. 667 COUMATE and 2-MeOEMATE therefore offer considerable potential for development for cancer therapy.

  • Inhibition of deoxyglucose uptake in MCF-7 breast cancer cells by 2Methoxyestrone and 2Methoxyestrone-3-O-sulfamate.
    Molecular and cellular endocrinology, 2000
    Co-Authors: A Singh, A. Purohit, Hatem Hejaz, B V Potter, M J Reed
    Abstract:

    Most cancer cells are dependent on glucose uptake to fulfil their energy requirements. In the present investigation we have examined the ability of 2Methoxyestrone (2-MeOE1), 2-methoxyestradiol (2-MeOE2), 2Methoxyestrone-3-O-sulfamate (2-MeOEMATE), and a number of related compounds, to inhibit 2-deoxy-D-[1-(3)H]-glucose uptake in MCF-7 breast cancer cells. Glucose uptake was shown to be linear with respect to cell number and time over a 5-35min period. 2-MeOE2, 2-MeOE1 and 2-MeOEMATE inhibited glucose uptake by 25-49% at 10 microM. 2-Hydroxyestradiol and estrone sulfate had little effect on glucose uptake, whereas estrone glucuronide inhibited uptake by 29%. There is evidence that 2-methoxyestrogens may exert an anti-mitotic effect on cells by stabilizing microtubules in a similar manner to that of paclitaxel. We therefore examined the effect of exposing cells to 2-MeOEMATE or paclitaxel for 24 h on basal or insulin stimulated glucose uptake. Using these conditions, 2-MeOEMATE and paclitaxel inhibited basal glucose uptake by 50 and 22%, respectively, and insulin stimulated uptake by 36 and 51%, respectively. The development of drugs that can inhibit glucose uptake could have therapeutic potential for the treatment of breast cancer.

Jean-philippe Emond – One of the best experts on this subject based on the ideXlab platform.

  • Urinary oestrogen steroidome as an indicator of the risk of localised prostate cancer progression
    British Journal of Cancer, 2021
    Co-Authors: Jean-philippe Emond, Louis Lacombe, Patrick Caron, Véronique Turcotte, David Simonyan, Armen Aprikian, Fred Saad, Michel Carmel, Simone Chevalier, Chantal Guillemette
    Abstract:

    Background Prostate cancer (PCa) is the most common cancer in North American men. Beyond the established contribution of androgens to disease progression, growing evidence suggest that oestrogen-related pathways might also be of clinical importance. The aim of this study was to explore the association of urinary oestrogen levels with clinical outcomes. Methods Urine samples from the prospective multi-institutional PROCURE cohort were collected before RP for discovery ( n  = 259) and validation ( n  = 253). Urinary total oestrogens (unconjugated + conjugated), including oestrone and oestradiol, their bioactive and inactive catechol and methyl derivatives ( n  = 15), were measured using mass spectrometry (MS). Results The median follow-up time for the discovery and replication cohorts was 7.6 and 6.5 years, respectively. Highly significant correlations between urinary oestrogens were observed; however, correlations with circulating oestrogens were modest. Our findings indicate that higher levels of urinary oestriol and 16-ketoestradiol were associated with lower risk of BCR. In contrast, higher levels of 2Methoxyestrone were associated with an increased risk of development of metastasis/deaths. Conclusions Our data suggest that urinary levels of oestriol and 16-ketoestradiol metabolites are associated with a more favourable outcome, whereas those of 2Methoxyestrone are associated with an elevated risk of metastasis after RP. Further studies are required to better understand the impact of oestrogens on disease biology and as easily accessible urine-based risk-stratification markers.

  • Urinary oestrogen steroidome as an indicator of the risk of localised prostate cancer progression.
    British journal of cancer, 2021
    Co-Authors: Jean-philippe Emond, Louis Lacombe, Patrick Caron, Véronique Turcotte, David Simonyan, Armen Aprikian, Fred Saad, Michel Carmel, Simone Chevalier, Chantal Guillemette
    Abstract:

    Prostate cancer (PCa) is the most common cancer in North American men. Beyond the established contribution of androgens to disease progression, growing evidence suggest that oestrogen-related pathways might also be of clinical importance. The aim of this study was to explore the association of urinary oestrogen levels with clinical outcomes. Urine samples from the prospective multi-institutional PROCURE cohort were collected before RP for discovery (n = 259) and validation (n = 253). Urinary total oestrogens (unconjugated + conjugated), including oestrone and oestradiol, their bioactive and inactive catechol and methyl derivatives (n = 15), were measured using mass spectrometry (MS). The median follow-up time for the discovery and replication cohorts was 7.6 and 6.5 years, respectively. Highly significant correlations between urinary oestrogens were observed; however, correlations with circulating oestrogens were modest. Our findings indicate that higher levels of urinary oestriol and 16-ketoestradiol were associated with lower risk of BCR. In contrast, higher levels of 2Methoxyestrone were associated with an increased risk of development of metastasis/deaths. Our data suggest that urinary levels of oestriol and 16-ketoestradiol metabolites are associated with a more favourable outcome, whereas those of 2Methoxyestrone are associated with an elevated risk of metastasis after RP. Further studies are required to better understand the impact of oestrogens on disease biology and as easily accessible urine-based risk-stratification markers.

Herman Adlercreutz – One of the best experts on this subject based on the ideXlab platform.

Armen Aprikian – One of the best experts on this subject based on the ideXlab platform.

  • Urinary oestrogen steroidome as an indicator of the risk of localised prostate cancer progression
    British Journal of Cancer, 2021
    Co-Authors: Jean-philippe Emond, Louis Lacombe, Patrick Caron, Véronique Turcotte, David Simonyan, Armen Aprikian, Fred Saad, Michel Carmel, Simone Chevalier, Chantal Guillemette
    Abstract:

    Background Prostate cancer (PCa) is the most common cancer in North American men. Beyond the established contribution of androgens to disease progression, growing evidence suggest that oestrogen-related pathways might also be of clinical importance. The aim of this study was to explore the association of urinary oestrogen levels with clinical outcomes. Methods Urine samples from the prospective multi-institutional PROCURE cohort were collected before RP for discovery ( n  = 259) and validation ( n  = 253). Urinary total oestrogens (unconjugated + conjugated), including oestrone and oestradiol, their bioactive and inactive catechol and methyl derivatives ( n  = 15), were measured using mass spectrometry (MS). Results The median follow-up time for the discovery and replication cohorts was 7.6 and 6.5 years, respectively. Highly significant correlations between urinary oestrogens were observed; however, correlations with circulating oestrogens were modest. Our findings indicate that higher levels of urinary oestriol and 16-ketoestradiol were associated with lower risk of BCR. In contrast, higher levels of 2Methoxyestrone were associated with an increased risk of development of metastasis/deaths. Conclusions Our data suggest that urinary levels of oestriol and 16-ketoestradiol metabolites are associated with a more favourable outcome, whereas those of 2Methoxyestrone are associated with an elevated risk of metastasis after RP. Further studies are required to better understand the impact of oestrogens on disease biology and as easily accessible urine-based risk-stratification markers.

  • Urinary oestrogen steroidome as an indicator of the risk of localised prostate cancer progression.
    British journal of cancer, 2021
    Co-Authors: Jean-philippe Emond, Louis Lacombe, Patrick Caron, Véronique Turcotte, David Simonyan, Armen Aprikian, Fred Saad, Michel Carmel, Simone Chevalier, Chantal Guillemette
    Abstract:

    Prostate cancer (PCa) is the most common cancer in North American men. Beyond the established contribution of androgens to disease progression, growing evidence suggest that oestrogen-related pathways might also be of clinical importance. The aim of this study was to explore the association of urinary oestrogen levels with clinical outcomes. Urine samples from the prospective multi-institutional PROCURE cohort were collected before RP for discovery (n = 259) and validation (n = 253). Urinary total oestrogens (unconjugated + conjugated), including oestrone and oestradiol, their bioactive and inactive catechol and methyl derivatives (n = 15), were measured using mass spectrometry (MS). The median follow-up time for the discovery and replication cohorts was 7.6 and 6.5 years, respectively. Highly significant correlations between urinary oestrogens were observed; however, correlations with circulating oestrogens were modest. Our findings indicate that higher levels of urinary oestriol and 16-ketoestradiol were associated with lower risk of BCR. In contrast, higher levels of 2Methoxyestrone were associated with an increased risk of development of metastasis/deaths. Our data suggest that urinary levels of oestriol and 16-ketoestradiol metabolites are associated with a more favourable outcome, whereas those of 2Methoxyestrone are associated with an elevated risk of metastasis after RP. Further studies are required to better understand the impact of oestrogens on disease biology and as easily accessible urine-based risk-stratification markers.