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1 to 10 of 18 literature results
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Stopping treatment can reverse acquired resistance to letrozole.
Using the intratumoral aromatase xenograft model, we have observed that despite long-lasting growth inhibition, tumors eventually begin to grow during…
Authors: Gauri J Sabnis, Luciana F Macedo, Olga Goloubeva, Adam Schayowitz, Angela M H Brodie
Source: Cancer research. 2008 Jun 15
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Effects of novel retinoic acid metabolism blocking agent (VN/14-1) on letrozole-insensitive breast cancer cells.
Aromatase inhibitors are proving to be more effective than tamoxifen for postmenopausal estrogen receptor (ER)-positive breast cancer. However, the in…
Authors: Aashvini Belosay, Angela M H Brodie, Vincent C O Njar
Source: Cancer research. 2006 Dec 1
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Regulation of androgen receptor activity by tyrosine phosphorylation.
The androgen receptor (AR) is essential for the growth of prostate cancer cells. Here, we report that tyrosine phosphorylation of AR is induced by gro…
Authors: Zhiyong Guo, Bojie Dai, Tianyun Jiang, Kexin Xu, Yingqiu Xie, Oekyung Kim, Issa Nesheiwat, Xiangtian Kong, Jonathan Melamed, Venkatesh D Handratta,…
Source: Cancer cell. 2006 Oct
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A novel androgen receptor splice variant is up-regulated during prostate cancer progression and promotes androgen depletion-resistant growth.
The androgen receptor (AR) plays a key role in progression to incurable androgen ablation-resistant prostate cancer (PCA). We have identified three no…
Authors: Zhiyong Guo, Xi Yang, Feng Sun, Richeng Jiang, Douglas E Linn, Hege Chen, Hegang Chen, Xiangtian Kong, Jonathan Melamed, Clifford G Tepper,…
Source: Cancer research. 2009 Mar 15
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Additive antitumor effect of aromatase inhibitor letrozole and antiestrogen fulvestrant in a postmenopausal breast cancer model.
Blocking estrogen receptors with antiestrogens and blocking estrogen synthesis with aromatase inhibitors are two strategies currently being used for r…
Authors: Danijela Jelovac, Luciana Macedo, Olga G Goloubeva, Venkatesh Handratta, Angela M H Brodie
Source: Cancer research. 2005 Jun 15
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Activation of mitogen-activated protein kinase in xenografts and cells during prolonged treatment with aromatase inhibitor letrozole.
Ovariectomized mice bearing tumor xenografts grown from aromatase-transfected estrogen receptor (ER)-positive human breast cancer cells (MCF-7Ca) were…
Authors: Danijela Jelovac, Gauri Sabnis, Brian J Long, Luciana Macedo, Olga G Goloubeva, Angela M H Brodie
Source: Cancer research. 2005 Jun 15
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Synergistic effect of a novel antiandrogen, VN/124-1, and signal transduction inhibitors in prostate cancer progression to hormone independence in vitro.
This study was carried out to determine the mechanisms associated with loss of androgen dependency and disease progression in prostate cancer. We inve…
Authors: Adam Schayowitz, Gauri Sabnis, Vincent C O Njar, Angela M H Brodie
Source: Molecular cancer therapeutics. 2008 Jan
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Development and evolution of therapies targeted to the estrogen receptor for the treatment and prevention of breast cancer.
This article describes the origins and evolution of "antiestrogenic" medicines for the treatment and prevention of breast cancer. Developing drugs tha…
Authors: V Craig Jordan, Angela M H Brodie
Source: Steroids. 2007 Jan
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Androgen receptor inactivation contributes to antitumor efficacy of 17{alpha}-hydroxylase/17,20-lyase inhibitor 3beta-hydroxy-17-(1H-benzimidazole-1-yl)androsta-5,16-diene in prostate cancer.
We previously reported that our novel compound 3beta-hydroxy-17-(1H-benzimidazole-1-yl)androsta-5,16-diene (VN/124-1) is a potent 17alpha-hydroxylase/…
Authors: Tadas Vasaitis, Aashvini Belosay, Adam Schayowitz, Aakanksha Khandelwal, Pankaj Chopra, Lalji K Gediya, Zhiyong Guo, Hong-Bin Fang, Vincent C O Njar, Angela M H Brodie
Source: Molecular cancer therapeutics. 2008 Aug
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Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.
New chemical entities, steroidal C-17 benzoazoles (5, 6, 9 and 10) and pyrazines (14 and 15) were rationally designed and synthesized. The key reactio…
Authors: Venkatesh D Handratta, Tadas S Vasaitis, Vincent C O Njar, Lalji K Gediya, Ritesh Kataria, Pankaj Chopra, Donnell Newman, Rena Farquhar, Zhiyong Guo, Yun Qiu,…
Source: Journal of medicinal chemistry. 2005 Apr 21
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