Research Topics
Genomes and Genes | Shiuan ChenSummaryAffiliation: City of Hope National Medical Center Country: USA Publications
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Publications
The aromatase inhibitor letrozole and inhibitors of insulin-like growth factor I receptor synergistically induce apoptosis in in vitro models of estrogen-dependent breast cancerJoanna Lisztwan
Novartis Institutes of Biomedical Research Basel, Oncology Research, Klybeckstrasse 141, CH 4057, Basel, Switzerland
Breast Cancer Res 10:R56. 2008....
Prevention and treatment of breast cancer by suppressing aromatase activity and expressionShiuan Chen
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
Ann N Y Acad Sci 963:229-38. 2002....
Structure-function studies of DT-diaphorase (NQO1) and NRH: quinone oxidoreductase (NQO2)S Chen
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
Free Radic Biol Med 29:276-84. 2000..In addition, functional studies of a natural occurring mutant Pro-187 to Ser (P187S) have been carried out. Results obtained from these investigations are summarized and discussed...
Modulation of aromatase expression in human breast tissueS Chen
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
J Steroid Biochem Mol Biol 79:35-40. 2001..e. toxaphene and chlordane) that have been found to be antagonists of ERRalpha-1 orphan receptor. These compounds reduce ERRalpha-1 activity, resulting in a suppression of aromatase expression...
Modulation of aromatase activity and expression by environmental chemicalsShiuan Chen
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
Front Biosci 7:d1712-9. 2002..This review will summarize and discuss findings from this and other laboratories on the effects of environmental chemicals on aromatase activity and expression...
Transcriptional regulation of aromatase expression in human breast tissueShiuan Chen
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
J Steroid Biochem Mol Biol 83:93-9. 2002....
The HDAC inhibitor LBH589 (panobinostat) is an inhibitory modulator of aromatase gene expressionShiuan Chen
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
Proc Natl Acad Sci U S A 107:11032-7. 2010..3/II. These findings provide an important basis for future clinical evaluations of LBH589 in hormone-dependent breast cancer...
Anti-aromatase activity of phytochemicals in white button mushrooms (Agaricus bisporus)Shiuan Chen
Department of Surgical Research, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
Cancer Res 66:12026-34. 2006..Therefore, our studies illustrate the anticancer activity in vitro and in vivo of mushroom extract and its major fatty acid constituents...
Positive and negative transcriptional regulation of aromatase expression in human breast cancer tissueShiuan Chen
Department of Surgical Research, Beckman Research Institute, City of Hope National Medical Center, Duarte, CA 91006, USA
J Steroid Biochem Mol Biol 95:17-23. 2005..By reviewing findings from our laboratory and other laboratories, a detailed mechanism for the transcriptional regulation of aromatase expression in breast cancer tissue is summarized and discussed...
New experimental models for aromatase inhibitor resistanceShiuan Chen
Department of Surgical Research, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
J Steroid Biochem Mol Biol 106:8-15. 2007..Overall, the information presented in this paper supplements our understanding of AI function, and such information can be valuable for the development of treatment strategies against AI resistant breast cancers...
Molecular basis for the constitutive activity of estrogen-related receptor alpha-1S Chen
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
J Biol Chem 276:28465-70. 2001..These results indicate that Phe-329 in ERRalpha-1 and Ala-350 in ERalpha play important roles in both ligand binding and transactivation function...
What do we know about the mechanisms of aromatase inhibitor resistance?Shiuan Chen
Department of Surgical Research, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
J Steroid Biochem Mol Biol 102:232-40. 2006..We anticipate that our studies will generate important information on the mechanisms of AI resistance. Such information can be valuable for the development of treatment strategies against AI-resistant breast cancers...
An "omics" approach to determine the mechanisms of acquired aromatase inhibitor resistanceShiuan Chen
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, Duarte, California, USA
OMICS 15:347-52. 2011..Our results reveal that growth factor/signal transduction pathways are upregulated after ERα-dependent pathways are suppressed by AIs, and ERα can then be activated through different crosstalk mechanisms...
Structure-function studies of aromatase and its inhibitors: a progress reportShiuan Chen
Divisions of Immunology and Informational Sciences, Beckman Research Institute of the City of Hope, Duarte, CA, USA
J Steroid Biochem Mol Biol 86:231-7. 2003....
Genome-wide analysis of aromatase inhibitor-resistant, tamoxifen-resistant, and long-term estrogen-deprived cells reveals a role for estrogen receptorSelma Masri
Department of Surgical Research, Division of Information Sciences, Beckman Research Institute of the City of Hope, Duarte, California, USA
Cancer Res 68:4910-8. 2008....
MCF-7aro/ERE, a novel cell line for rapid screening of aromatase inhibitors, ERalpha ligands and ERRalpha ligandsKi Lui
Department of Surgical Research, Beckman Research Institute of the City of Hope, 1500 E Duarte Road, Duarte, CA 91010, USA
Biochem Pharmacol 76:208-15. 2008..These results indicate that MCF-7aro/ERE is a novel cell line for rapid screening of AIs, ERalpha ligands and ERRalpha ligands...
Characterization of the weak estrogen receptor alpha agonistic activity of exemestaneSelma Masri
Department of Surgical Research, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
Breast Cancer Res Treat 116:461-70. 2009..e., PGR, pS2 and AREG. These results suggest that EXE does have weak estrogen-like activity...
Transcriptional regulation of the mouse PNRC2 promoter by the nuclear factor Y (NFY) and E2F1Dujin Zhou
Department of Surgical Research, Beckman Research Institute of City of Hope, Duarte, California 91010, USA
Gene 361:89-100. 2005....
The role of microRNA-128a in regulating TGFbeta signaling in letrozole-resistant breast cancer cellsSelma Masri
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, 1500 E Duarte Road, Duarte, CA 91010, USA
Breast Cancer Res Treat 124:89-99. 2010....
Molecular characterization of aromatase inhibitor-resistant, tamoxifen-resistant and LTEDaro cell linesSelma Masri
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, Duarte, CA, USA
J Steroid Biochem Mol Biol 118:277-82. 2010....
AKT-aro and HER2-aro, models for de novo resistance to aromatase inhibitors; molecular characterization and inhibitor response studiesCynthie Wong
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, 1500 East Duarte Road, Duarte, CA 91010, USA
Breast Cancer Res Treat 134:671-81. 2012..Together, these data indicate the possibility that HSP90 inhibitors may be a viable therapy for endocrine therapy resistance although additional clinical evaluation is needed...
Biochemical and biological characterization of a novel anti-aromatase coumarin derivativeShiuan Chen
Department of Surgical Research and Division of Informational Sciences, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
J Biol Chem 279:48071-8. 2004..These results demonstrate that coumarins (a common type of phytochemical) or their derivatives can be potent inhibitors of aromatase and may be useful in suppressing aromataseand ER-positive breast tumors...
A novel crosstalk mechanism between nuclear receptor-mediated and growth factor/Ras-mediated pathways through PNRC-Grb2 interactionDujin Zhou
Department of Surgical Research, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
Oncogene 23:5394-404. 2004..This is a newly identified crosstalk mechanism for modulating these two important types of regulatory pathways...
Blueberry phytochemicals inhibit growth and metastatic potential of MDA-MB-231 breast cancer cells through modulation of the phosphatidylinositol 3-kinase pathwayLynn S Adams
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
Cancer Res 70:3594-605. 2010..These data illustrate the inhibitory effect of blueberry phytochemicals on the growth and metastatic potential of MDA-MB-231 cells through modulation of the PI3K/AKT/NFkappaB pathway...
Letrozole-, anastrozole-, and tamoxifen-responsive genes in MCF-7aro cells: a microarray approachToru Itoh
Department of Surgical Research, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
Mol Cancer Res 3:203-18. 2005....
Growth inhibition of estrogen receptor-positive and aromatase-positive human breast cancer cells in monolayer and spheroid cultures by letrozole, anastrozole, and tamoxifenIkuko Kijima
Department of Surgical Research, Beckman Research Institute of the City of Hope, 1500 E Duarte Road, Duarte, CA 91010, USA
J Steroid Biochem Mol Biol 97:360-8. 2005..Our results demonstrate that MCF-7aro and T-47Daro spheroids could be a suitable model for evaluation of growth-inhibitory effects of agents used in hormonal therapy of breast cancer...
Grape seed extract is an aromatase inhibitor and a suppressor of aromatase expressionIkuko Kijima
Department of Surgical Research, Beckman Research Institute of the City of Hope, Duarte, California, USA
Cancer Res 66:5960-7. 2006..We believe that these results are exciting in that they show GSE to be potentially useful in the prevention/treatment of hormone-dependent breast cancer through the inhibition of aromatase activity as well as its expression...
The molecular basis of the interaction between the proline-rich SH3-binding motif of PNRC and estrogen receptor alphaDujin Zhou
Department of Surgical Research, Beckman Research Institute of City of Hope, 1450 East Duarte Road, Duarte, CA 91010, USA
Nucleic Acids Res 34:5974-86. 2006....
Molecular basis for the aromatization reaction and exemestane-mediated irreversible inhibition of human aromataseYanyan Hong
Department of Surgical Research and Division of Information Sciences, Beckman Research Institute of the City of Hope, 1500 East Duarte Road, Duarte, California 91010, USA
Mol Endocrinol 21:401-14. 2007..These structure-function studies of aromatase would provide useful information to design more effective aromatase inhibitors for the prevention and the treatment of hormone-dependent breast cancer...
Induction of aromatase (CYP19) expression in breast cancer cells through a nongenomic action of estrogen receptor alphaYoshiyuki Kinoshita
Department of Surgical Research, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
Cancer Res 63:3546-55. 2003..These results suggest that E(2) up-regulates aromatase expression by a nongenomic action of ER alpha via cross-talk with growth factor-mediated pathways...
Molecular basis for the interaction of four different classes of substrates and inhibitors with human aromataseYanyan Hong
Department of Surgical Research and Division of Information Sciences, Beckman Research Institute of the City of Hope, 1500 E Duarte Road, Duarte, CA 91010, United States
Biochem Pharmacol 75:1161-9. 2008..These structure-function studies help us to evaluate the structural model of aromatase, and to accelerate the structure-based design for new aromatase inhibitors...
Baicalin increases VEGF expression and angiogenesis by activating the ERR{alpha}/PGC-1{alpha} pathwayKeqiang Zhang
Department of Molecular Medicine, Beckman Research Institute of the City of Hope, 1500 East Duarte Road, Duarte, CA 91010, USA
Cardiovasc Res 89:426-35. 2011..In this report, we studied the modulation of angiogenesis as one possible mechanism by investigating the effects of these agents on expression of vascular endothelial growth factor (VEGF), a critical factor for angiogenesis...
Grape seed extract inhibits VEGF expression via reducing HIF-1alpha protein expressionJianming Lu
Department of Molecular Medicine, Beckman Research Institute of the City of Hope, 1500 East Duarte Road, Duarte, CA 91010, USA
Carcinogenesis 30:636-44. 2009..This finding provides new insight into the mechanisms of anticancer activity of GSE and reveals a novel molecular mechanism underlying the antiangiogenic action of GSE...
SGK3 is an estrogen-inducible kinase promoting estrogen-mediated survival of breast cancer cellsYuanzhong Wang
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, 1550 East Duarte Road, Duarte, CA 91010, USA
Mol Endocrinol 25:72-82. 2011....
Lead optimization of COX-2 inhibitor nimesulide analogs to overcome aromatase inhibitor resistance in breast cancer cellsBin Su
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
Bioorg Med Chem Lett 19:6733-5. 2009..Compared to nimesulide which inhibited LTEDaro cell proliferation with an IC(50) at 170.30 microM, several new compounds showed IC(50) close to 1.0 microM...
Flavone and isoflavone phytoestrogens are agonists of estrogen-related receptorsMasatomo Suetsugi
Department of Surgical Research and Division of Information Sciences, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
Mol Cancer Res 1:981-91. 2003..In addition, our studies have demonstrated that an approach that combines structure-based virtual screening and receptor functional assays can identify novel ligands of orphan nuclear receptors...
Binding features of steroidal and nonsteroidal inhibitorsYanyan Hong
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, 1500 E Duarte Rd, Duarte, CA, USA
Steroids 76:802-6. 2011..Together with previous research from our laboratory, this study confirms that W224, E302, D309 and S478 are important active site residues involved in the suicide mechanism of exemestane against aromatase...
Suppression of estrogen biosynthesis by procyanidin dimers in red wine and grape seedsElizabeth T Eng
City of Hope Graduate School of Biological Science, Department of Surgical Research, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
Cancer Res 63:8516-22. 2003..These in vitro and in vivo studies demonstrated that procyanidin B dimers in red wine and grape seeds could be used as chemopreventive agents against breast cancer by suppressing in situ estrogen biosynthesis...
Different catalytic properties and inhibitor responses of the goldfish brain and ovary aromatase isozymesJ Zhao
Division of Immunology, Beckman Research Institute of the City of the Hope, Duarte, California 91010, USA
Gen Comp Endocrinol 123:180-91. 2001..In addition, differences in the K(i) values of aromatase inhibitors for the two goldfish isoforms suggest structural variance in the active sites of these isozymes...
Epitope characterization of an aromatase monoclonal antibody suitable for the assessment of intratumoral aromatase activityYanyan Hong
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, Duarte, California, United States of America
PLoS ONE 4:e8050. 2009..These results also provide valuable information to identify new aromatase antibodies for immunohistochemical diagnosis of hormone-dependent breast cancer in future...
CCAAT/enhancer binding protein delta up-regulates aromatase promoters I.3/II in breast cancer epithelial cellsIkuko Kijima
Department of Surgical Research, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
Cancer Res 68:4455-64. 2008....
Improvement of sensitivity to tamoxifen in estrogen receptor-positive and Herceptin-resistant breast cancer cellsBin Chen
Department of Surgical Research Division of Molecular Medicine, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
J Mol Endocrinol 41:367-77. 2008....
The role of amphiregulin in exemestane-resistant breast cancer cells: evidence of an autocrine loopXin Wang
Department of Surgical Research, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
Cancer Res 68:2259-65. 2008..AREG then activates the EGFR pathway and leads to the activation of the MAPK pathway that drives cell proliferation...
Regulation of aromatase promoter activity in human breast tissue by nuclear receptorsChun Yang
Beckman Research Institute of the City of Hope, Division of Immunology, 1450 East Duarte Road, Duarte, California, CA 91010-0269, USA
Oncogene 21:2854-63. 2002..By binding to S1, ERalpha down-regulates the aromatase promoter activity. These results demonstrate that nuclear receptors play important roles in modulating aromatase expression in human breast tissue...
Whole blueberry powder modulates the growth and metastasis of MDA-MB-231 triple negative breast tumors in nude miceLynn S Adams
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, Duarte, CA, USA
J Nutr 141:1805-12. 2011..04) and 25% fewer lymph node metastases (P = 0.09) compared to control mice. This study demonstrates the oral antitumor and metastasis activity of whole BB powder against TNBC in mice...
Heat shock protein 90 inhibitors: new mode of therapy to overcome endocrine resistanceCynthie Wong
Graduate School of Biological Sciences and Division of Tumor Cell Biology, Beckman Research Institute of City of Hope, Duarte, California 91010, USA
Cancer Res 69:8670-7. 2009....
PNRC accumulates in the nucleolus by interaction with B23/nucleophosmin via its nucleolar localization sequenceYuanzhong Wang
Division of Tumor Cell Biology, Beckman Research Institute, Duarte, CA 91010, USA
Biochim Biophys Acta 1813:109-19. 2011..Our study also suggests that the stretches of six successive basic residues (lysine and/or arginine) could function as NoLS...
White button mushroom (Agaricus bisporus) exhibits antiproliferative and proapoptotic properties and inhibits prostate tumor growth in athymic miceLynn S Adams
Department of Surgical Research, Beckman Research Institute of the City of Hope, Duarte, CA, USA
Nutr Cancer 60:744-56. 2008....
Molecular characterization of aromataseYanyan Hong
Department of Surgical Research, Beckman Research Institute of City of Hope, Duarte, California 91010, USA
Ann N Y Acad Sci 1155:112-20. 2009..This review presents current knowledge about structural and functional characteristics of aromatase to address unsolved mysteries about this enzyme...
Nuclear receptor coactivator PNRC2 regulates energy expenditure and adiposityDujin Zhou
Department of Surgical Research, Transgenic Mouse Facility, and Animal Resources Center, Beckman Research Institute of City of Hope, Duarte, CA 91010, USA
J Biol Chem 283:541-53. 2008..PNRC2 may be a new target in the treatment of obesity and related metabolic diseases...
White button mushroom phytochemicals inhibit aromatase activity and breast cancer cell proliferationB J Grube
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
J Nutr 131:3288-93. 2001..These results suggest that diets high in mushrooms may modulate the aromatase activity and function in chemoprevention in postmenopausal women by reducing the in situ production of estrogen...
Phytochemicals for breast cancer prevention by targeting aromataseLynn S Adams
Department of Surgical Research, Beckman Research Institute of the City of Hope, 1500 E Duarte Rd Duarte, CA, USA
Front Biosci 14:3846-63. 2009..We will review reported aromatase inhibition, kinetic data and possible structural variations that may inhibit or enhance the interaction of phytochemicals with the aromatase enzyme...
Pomegranate ellagitannin-derived compounds exhibit antiproliferative and antiaromatase activity in breast cancer cells in vitroLynn S Adams
Beckman Research Institute of the City of Hope, Duarte, California, USA
Cancer Prev Res (Phila) 3:108-13. 2010..The remaining test compounds also exhibited antiproliferative activity, but to a lesser degree than UB. These studies suggest that pomegranate ET-derived compounds have potential for the prevention of estrogen-responsive breast cancers...
Sequence-function correlation of aromatase and its interaction with reductaseYanyan Hong
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
J Steroid Biochem Mol Biol 118:203-6. 2010..These studies may lead to a novel field for the development of new inhibitors which interfere with the interaction between aromatase and CPR in order to inhibit the aromatization reaction...
Expression and purification of a recombinant form of human aromatase from Escherichia coliFangming Zhang
Division of Immunology, Beckman Research Institute of the City of Hope, 1450 East Duarte Road, Duarte, CA 91010, USA
Biochem Pharmacol 64:1317-24. 2002..The results indicate that the recombinant aromatase from E. coli has catalytic properties identical to those of the enzyme expressed in human tissue and will be very useful for further structure-function studies of aromatase...
Suppression of aromatase (estrogen synthetase) by red wine phytochemicalsE T Eng
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
Breast Cancer Res Treat 67:133-46. 2001..This is the first report demonstrating that wine, especially red wine, contains phytochemicals that can inhibit aromatase...
Catalytic properties of NAD(P)H:quinone acceptor oxidoreductase: study involving mouse, rat, human, and mouse-rat chimeric enzymesS Chen
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
Mol Pharmacol 47:934-9. 1995..Based on these results, we propose that the carboxyl-terminal portion of the enzyme plays an important role in the reduction of cytotoxic drugs and the binding of flavones...
Protective effects of white button mushroom (Agaricus bisporus) against hepatic steatosis in ovariectomized mice as a model of postmenopausal womenNoriko Kanaya
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, Duarte, California, United States of America
PLoS ONE 6:e26654. 2011..These results suggest that WBM is protective against hepatic steatosis and NAFLD in OVX mice as a model for postmenopausal women...
Aromatase inhibitors: structural features and biochemical characterizationYanyan Hong
Department of Surgical Research, Beckman Research Institute of the City of Hope, 1500 E. Duarte Rd, Duarte, CA 91010, USA
Ann N Y Acad Sci 1089:237-51. 2006..Such information has helped the examination of binding characteristics of AIs, the evaluation of reaction mechanism of aromatase, and the explanation of the molecular basis for a low catalytic activity of the natural variant, M364T...
Aromatase destabilizer: novel action of exemestane, a food and drug administration-approved aromatase inhibitorXin Wang
Department of Surgical Research, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
Cancer Res 66:10281-6. 2006..This is the first report on the evaluation of three FDA-approved AIs on the stability of the aromatase protein. We have found that exemestane, different from letrozole and anastrozole, can destabilize the aromatase protein...
A COX-2 inhibitor nimesulide analog selectively induces apoptosis in Her2 overexpressing breast cancer cells via cytochrome c dependent mechanismsBin Chen
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
Biochem Pharmacol 77:1787-94. 2009..These results suggest that compound 76 selectively induce apoptosis in Her2 overexpressing breast cancer cells through the mitochondria, and could be used as a lead to design more potent derivatives...
Aromatase and breast cancerS Chen
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA schen smtplink coh org
Front Biosci 3:d922-33. 1998....
Down-regulation of promoter 1.3 activity of the human aromatase gene in breast tissue by zinc-finger protein, snail (SnaH)T Okubo
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, California 91010 0269, USA
Cancer Res 61:1338-46. 2001..3. A reduction of the expression of SnaH in breast cancer tissue further suggests a cancer-protective role for this protein in normal breast tissue...
PNRC2 is a 16 kDa coactivator that interacts with nuclear receptors through an SH3-binding motifD Zhou
Division of Immunology, Beckman Research Institute of the City of Hope, 1450 East Duarte Road, Duarte, CA 91010, USA
Nucleic Acids Res 29:3939-48. 2001..Our results reveal that PNRC2 has a structure and function similar to PNRC, a previously characterized coactivator. These two proteins represent a new type of nuclear receptor co-regulatory proteins...
The development, application and limitations of breast cancer cell lines to study tamoxifen and aromatase inhibitor resistanceCynthie Wong
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
J Steroid Biochem Mol Biol 131:83-92. 2012....
Grape seed extract inhibits angiogenesis via suppression of the vascular endothelial growth factor receptor signaling pathwayWei Wen
Department of Molecular Medicine, Beckman Research Institute of the City of Hope, 1500 East Duarte Road, Duarte, CA 91010, USA
Cancer Prev Res (Phila) 1:554-61. 2008..Taken together, this study indicates that GSE is a well-tolerated and inexpensive natural VEGF inhibitor and could potentially be useful in cancer prevention or treatment...
Molecular characterization of binding of substrates and inhibitors to DT-diaphorase: combined approach involving site-directed mutagenesis, inhibitor-binding analysis, and computer modelingS Chen
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, California, USA
Mol Pharmacol 56:272-8. 1999..Our studies generated results that explain why dicoumarol is a potent inhibitor and binds differently from flavones and phenindone in the active site of DT-diaphorase...
Modulation of aromatase expression in the breast tissue by ERR alpha-1 orphan receptorC Yang
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
Cancer Res 58:5695-700. 1998..It is thought that the silencer element in the human aromatase gene may function differently in different tissues because of distinct expression patterns of transcription factors...
Binding characteristics of aromatase inhibitors and phytoestrogens to human aromataseS Chen
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, CA 91010, U S A
J Steroid Biochem Mol Biol 61:107-15. 1997..Furthermore, the investigation reveals that phytoestrogens bind to the active site of aromatase in a different orientation from that in the estrogen receptor...
The stress-activated c-Jun protein kinase (JNK) is stimulated by lipoxygenase pathway product 12-HETE in RIN m5F cellsD Bleich
Division of Diabetes, Endocrinology, and Metabolism, City of Hope National Medical Center, Duarte, California 91010, USA
Biochem Biophys Res Commun 230:448-51. 1997..We demonstrate that 1 nM 12-HETE stimulates JNK activity, while 1 nM 15-HETE, the 15-lipoxygenase pathway product, does not. These results suggest 12-HETE is a novel upstream signal for IL-1beta induced JNK activation in RIN m5F cells...
Molecular basis of the catalytic differences among DT-diaphorase of human, rat, and mouseS Chen
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
J Biol Chem 272:1437-9. 1997..This structural information is very important for designing suitable drugs and approaches for human cancer chemotherapy mediated by DT-diaphorase...
Inhibition of the proliferation of acquired aromatase inhibitor-resistant breast cancer cells by histone deacetylase inhibitor LBH589 (panobinostat)Makoto Kubo
Department of Cancer Biology, Beckman Research Institute of the City of Hope, 1500 East Duarte Road, Duarte, CA 91010, USA
Breast Cancer Res Treat 137:93-107. 2013..In all, our findings strongly support further investigation of LBH589 as a novel therapeutic strategy for patients with AI-resistant breast cancer, in part by suppressing the NF-κB1 pathway...
CCL2 mediates cross-talk between cancer cells and stromal fibroblasts that regulates breast cancer stem cellsAkihiro Tsuyada
Division of Tumor Cell Biology, City of Hope Beckman Research Institute and Medical Center, Duarte, California 91010, USA
Cancer Res 72:2768-79. 2012..Our findings therefore suggest that CCL2 represents a potential therapeutic target that can block the cancer-host communication that prompts CSC-mediated disease progression...
Aromatase, estrone sulfatase, and 17β-hydroxysteroid dehydrogenase: structure-function studies and inhibitor developmentYanyan Hong
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, 1450 E Duarte Road, Duarte, CA 91010, United States
Mol Cell Endocrinol 340:120-6. 2011..Selective and potent inhibitors of the three enzymes have been developed as antiproliferative agents in hormone-dependent breast carcinoma. New treatment strategies for hormone-dependent breast cancer are discussed...
Conjugated linoleic acid reduces body weight gain in ovariectomized female C57BL/6J miceNoriko Kanaya
Division of Tumor Cell Biology, Beckman Research Institute of the City of Hope, Duarte, CA 91010, USA
Nutr Res 30:714-21. 2010..Our results indicate that CLA is functional as an antiobesity supplement in the mouse model for postmenopausal women and that the antiobesity effect of CLA is not estrogen related...
Catalytic properties of NAD(P)H:quinone oxidoreductase-2 (NQO2), a dihydronicotinamide riboside dependent oxidoreductaseK Wu
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
Arch Biochem Biophys 347:221-8. 1997..In addition, the chimeric enzyme is inhibited by quercetin but not dicumarol. These results suggest that additional region(s) in these enzymes is involved in differentiating NRH from NAD(P)H...
Expression of human placental aromatase in Saccharomyces cerevisiaeD Pompon
Beckman Research Institute of the City of Hope, Division of Immunology, Duarte, California 91010
Mol Endocrinol 3:1477-87. 1989..The kinetic results are similar to those determined for human placental aromatase, and suggest that the yeast synthesized aromatase will be useful for further structure-function studies...
PNRC: a proline-rich nuclear receptor coregulatory protein that modulates transcriptional activation of multiple nuclear receptors including orphan receptors SF1 (steroidogenic factor 1) and ERRalpha1 (estrogen related receptor alpha-1)D Zhou
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
Mol Endocrinol 14:986-98. 2000..The exact 23-amino acid sequence was also found in another protein isolated from the same yeast two-hybrid screening study. These two proteins belong to a new family of nuclear receptor coregulatory proteins...
Demonstration of the activation of prodrug CB 1954 using human DT-diaphorase mutant Q104Y-transfected MDA-MB-231 cells and mouse xenograft modelK Wu
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
Arch Biochem Biophys 385:203-8. 2001..These studies reveal that DT-diaphorase can activate CB 1954, and human Q104Y mutant enzyme is more active than the wild-type enzyme in the intracellular reductive activation of CB 1954...
Resistance to type 1 diabetes induction in 12-lipoxygenase knockout miceD Bleich
Division of Diabetes, Endocrinology, and Metabolism, City of Hope National Medical Center, Duarte, California 91010, USA
J Clin Invest 103:1431-6. 1999..In summary, elimination of leukocyte 12-LO in mice ameliorates low dose streptozotocin-induced diabetes by increasing islet resistance to cytokines and decreasing macrophage production of nitric oxide...
Mouse liver NAD(P)H:quinone acceptor oxidoreductase: protein sequence analysis by tandem mass spectrometry, cDNA cloning, expression in Escherichia coli, and enzyme activity analysisS Chen
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, California 91010
Protein Sci 3:1296-304. 1994..abstract truncated at 250 words)..
Anti-aromatase chemicals in red wineE T Eng
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, California 91010, USA
Ann N Y Acad Sci 963:239-46. 2002..Further research is underway to purify and characterize the active compounds in red wine that are responsible for the inhibition of aromatase...
Characterization of the human EPLIN (Epithelial Protein Lost in Neoplasm) gene reveals distinct promoters for the two EPLIN isoformsS Chen
Department of Medicine, Microbiology, Immunology and Molecular Genetics, Jonsson Comprehensive Cancer Center, and Dental Research Institute, UCLA School of Medicine, 10833 Le Conte Avenue, Los Angeles, CA, USA
Gene 248:69-76. 2000..The activity of 0.7kb EPLIN-alpha promoter reporter construct could be enhanced by activated RhoA, indicating that this serum response element is functional...
A two-domain structure for the two subunits of NAD(P)H:quinone acceptor oxidoreductaseS Chen
Division of Immunology, Beckman Research Institute of the City of Hope, Duarte, California 91010
Protein Sci 3:51-7. 1994..Furthermore, based on the data, it is suggested that the binding of substrates involves an interaction between 2 structural domains...
The red wine polyphenol resveratrol displays bilevel inhibition on aromatase in breast cancer cellsYun Wang
Department of Biochemistry and Department of Anatomy, The Chinese University of Hong Kong, Shatin, N.T, Hong Kong
Toxicol Sci 92:71-7. 2006..The present study illustrated that pharmacological dosage of resveratrol inhibited aromatase at both the enzyme and mRNA levels...
Dual inhibition of mTOR and estrogen receptor signaling in vitro induces cell death in models of breast cancerAnne Boulay
Novartis Institutes for BioMedical Research Basel, Oncology Research, Novartis Pharma AG, Basel, Switzerland
Clin Cancer Res 11:5319-28. 2005..Moreover, RAD001-letrozole combinations can act in a synergistic manner to inhibit proliferation and trigger apoptotic cell death. This combination holds promise for the treatment of hormone-dependent breast cancers...
ERRgamma suppresses cell proliferation and tumor growth of androgen-sensitive and androgen-insensitive prostate cancer cells and its implication as a therapeutic target for prostate cancerShan Yu
Department of Anatomy, The Chinese University of Hong Kong, Shatin, China
Cancer Res 67:4904-14. 2007..More importantly, our results suggest that ERRgamma could be a novel therapeutic target for prostate cancer treatment...
The plant polyphenol butein inhibits testosterone-induced proliferation in breast cancer cells expressing aromataseYun Wang
Department of Biochemistry, The Chinese University of Hong Kong, Rm. 507C MMW Bldg, Shatin, N.T, Hong Kong
Life Sci 77:39-51. 2005..The present study illustrated that butein was an aromatase inhibitor and a potential natural alternative for the chemoprevention or therapy of breast cancer...
The red clover (Trifolium pratense) isoflavone biochanin A inhibits aromatase activity and expressionYun Wang
Department of Biochemistry, The Chinese University of Hong Kong, Shatin NT, Hong Kong
Br J Nutr 99:303-10. 2008..Since genistein is a major metabolite of biochanin A, it might contribute to biochanin A's suppressive effect on CYP19 expression. The present study illustrated that biochanin A inhibited CYP19 activity and gene expression...
Modulation of in situ estrogen synthesis by proline-, glutamic acid-, and leucine-rich protein-1: potential estrogen receptor autocrine signaling loop in breast cancer cellsRajib Rajhans
Department of Obstetrics and Gynecology, University of Texas Health Science Center, Floyd Curl Drive, San Antonio, Texas 78229 3900, USA
Mol Endocrinol 22:649-64. 2008....
Pak1 phosphorylation of snail, a master regulator of epithelial-to-mesenchyme transition, modulates snail's subcellular localization and functionsZhibo Yang
Department of Molecular and Cellular Oncology, The University of Texas M D Anderson Cancer Center, 1515 Holcombe Boulevard, Houston, TX 77030, USA
Cancer Res 65:3179-84. 2005..The regulation of phosphorylation and function of Snail by Pak1 represents a novel mechanism by which a signaling kinase might contribute to the process of epithelial-mesenchymal transition...
Fast skeletal muscle troponin I is a co-activator of estrogen receptor-related receptor alphaYuping Li
Department of Biochemistry and Molecular Biology, Third Military Medical University, No 30 Gaotanyan Street, Chongqing 400038, China
Biochem Biophys Res Commun 369:1034-40. 2008..Combining mutagenesis and yeast two-hybrid assays, we mapped the ERRalpha-interacting domain on TNNI2 to a region encompassing amino acids 1-128. These findings reveal a new function for TNNI2 as a co-activator of ERRalpha...
Expression and functional study of estrogen receptor-related receptors in human prostatic cells and tissuesC P Cheung
Department of Anatomy, Faculty of Medicine, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong, China
J Clin Endocrinol Metab 90:1830-44. 2005..Our study shows that ERRs, which are coexpressed with ERs in prostatic cells, could regulate cell growth and modulate ER-mediated pathways via interference on ERalpha transcription in prostatic cells...
Local estrogen formation by nontumoral, cirrhotic, and malignant human liver tissues and cellsLuigi A M Castagnetta
Department of Experimental Oncology and Clinical Application, University Medical School, Palermo, Italy
Cancer Res 63:5041-5. 2003....
Molecular mechanisms of aromatase inhibition by new A, D-ring modified steroidsMargarida Cepa
Serviço de Bioquímica, Faculdade de Farmacia, Universidade do Porto, Rua Anibal Cunha, 164, 4099 030 Porto, Portugal
Biol Chem 389:1183-91. 2008..These findings are important for the elucidation of a structure-activity relationship on aromatase, which may help in the development of new AIs...
Identification and characterization of PNRC splicing variantsYuanzhong Wang
Department of Biochemistry and Molecular Biology, Third Military Medical University, Chonqing, 400038, PR China
Gene 423:116-24. 2008..Our results suggest that PNRC exists as functionally distinct isoforms and alternative splicing serves as a regulatory mechanism of PNRC coactivator activity...
Molecular cloning and functional study of rat estrogen receptor-related receptor gamma in rat prostatic cellsKi Lui
Department of Anatomy, The Chinese University of Hong Kong, Hong Kong, China
Prostate 66:1600-19. 2006..Its co-expression with ERs suggests that besides ERs, ligand-independent ERRgamma is also involved in prostatic growth and functions...
CB 1954: from the Walker tumor to NQO2 and VDEPTRichard J Knox
Enact Pharma PLC, Porton Down Scientific Park, Salisbury, Wiltshire, UK
Curr Pharm Des 9:2091-104. 2003..NQO2 activity is substantially raised in tumor samples from colorectal and hepatoma patients (up to 14-fold). A phase I clinical trial of an NQO2 co-substrate with CB 1954 is scheduled...
