Selective Estrogen Receptor Modulators for BPH: New Factors on the Ground
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Supporting Materials for Reappointment of Rong Di for 2004
CURRICULUM VITAE Rong Di Associate Research Professor Department of Plant Biology School of Environmental and Biological Sciences Rutgers University 222B Foran Hall, 59 Dudley Rd., New Brunswick, NJ 08901 Ph. (848)-932-6350, Fax (732)-932-9377 [email protected] http://plantbiology.rutgers.edu/faculty/di/Rong_Di.html July 2017 Appointments 2017-Present Associate Research Professor, Department of Plant Biology, School of Environmental and Biological Sciences, Rutgers University, New Brunswick, NJ 2011-2017 Assistant Research Professor, Department of Plant Biology and Pathology, School of Environmental and Biological Sciences, Rutgers University, New Brunswick, NJ 2014-Present Adjunct Professor, Hainan University, Hainan, China 2003-2011 Assistant Research Professor, Biotechnology Center for Agriculture and the Environment, School of Environmental and Biological Sciences, Rutgers University, New Brunswick, NJ 1997- 2002 Research Associate, Biotechnology Center for Agriculture and the Environment, School of Environmental and Biological Sciences, Rutgers University, New Brunswick, NJ 1992-1996 Postdoctoral Scholar, Dept. of Plant Pathology, and Dept. of Agronomy, University of Kentucky, Lexington, KY 1986-1992 Graduate Research Assistant, Dept. of Plant Pathology, Iowa State University, Ames, IA 1983-1985 Assistant Lecturer, Dept. of Plant Protection, South China College of Tropical Crops (SCCTC), Hainan, P. R. China Education Ph.D. 1992 Plant Virology, Iowa State University, Iowa (Advisor: W Allen Miller) M.S. 1989 Plant Virology, Iowa State University, Iowa (Advisor: John Hill) B.S. 1983 Plant Protection, South China College of Tropical Crops, Hainan, P.R. China Honors and Awards 1985 Selected as the only one among 45 graduates in the Dept. of Plant Protection from SCCTC China to study abroad. -
Tanibirumab (CUI C3490677) Add to Cart
5/17/2018 NCI Metathesaurus Contains Exact Match Begins With Name Code Property Relationship Source ALL Advanced Search NCIm Version: 201706 Version 2.8 (using LexEVS 6.5) Home | NCIt Hierarchy | Sources | Help Suggest changes to this concept Tanibirumab (CUI C3490677) Add to Cart Table of Contents Terms & Properties Synonym Details Relationships By Source Terms & Properties Concept Unique Identifier (CUI): C3490677 NCI Thesaurus Code: C102877 (see NCI Thesaurus info) Semantic Type: Immunologic Factor Semantic Type: Amino Acid, Peptide, or Protein Semantic Type: Pharmacologic Substance NCIt Definition: A fully human monoclonal antibody targeting the vascular endothelial growth factor receptor 2 (VEGFR2), with potential antiangiogenic activity. Upon administration, tanibirumab specifically binds to VEGFR2, thereby preventing the binding of its ligand VEGF. This may result in the inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. VEGFR2 is a pro-angiogenic growth factor receptor tyrosine kinase expressed by endothelial cells, while VEGF is overexpressed in many tumors and is correlated to tumor progression. PDQ Definition: A fully human monoclonal antibody targeting the vascular endothelial growth factor receptor 2 (VEGFR2), with potential antiangiogenic activity. Upon administration, tanibirumab specifically binds to VEGFR2, thereby preventing the binding of its ligand VEGF. This may result in the inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. VEGFR2 is a pro-angiogenic growth factor receptor -
Medicinal Properties of Selected Asparagus Species: a Review Polo-Ma-Abiele Hildah Mfengwana and Samson Sitheni Mashele
Chapter Medicinal Properties of Selected Asparagus Species: A Review Polo-Ma-Abiele Hildah Mfengwana and Samson Sitheni Mashele Abstract Asparagus species are naturally distributed along Asia, Africa, and Europe and are known to have numerous biological properties. This review article was aimed to provide an organized summary of current studies on the traditional uses, phy- tochemistry, and pharmacological and toxicological studies of Asparagus laricinus Burch., Asparagus africanus Lam., Asparagus officinalis L., Asparagus racemosus Willd., and Asparagus densiflorus (Kunth) Jessop to attain and establish new insights for further researches. Information used in this review was obtained from electronic database including PubMed central, Google scholars, Science direct, Scopus, and Sabinet. Based on the present findings, the existing literature still presents some breaches about the mechanism of action of various constituents of these plants, and their relation to other plant compounds in poly-herbal formulations, as well as their long-term use and safety. More in-depth studies are still needed for active compounds and biological activities of Asparagus laricinus, Asparagus africanus, and Asparagus densiflorus. Therefore, innumerable opportunities and possibilities for investigation are still available in novel areas of these plants for future research stud¬ies. It can be concluded that all selected Asparagus species have tremendous potential to improve human health and the pharmacological activities of these plants can be attributed to bioactive phytochemicals they possess. Keywords: Asparagaceae, Asparagus africanus lam., Asparagus densiflorus (kunth) Jessop, Asparagus laricinus Burch., Asparagus officinalis L., Asparagus racemosus Willd., pharmacological actions, phytochemistry 1. Introduction Historically, plants were used for numerous purposes for mankind in general, inter alia, feeding and catering, culinary spices, medicine, various forms of cosmetics, symbols in worship and for a variety of ornamental goods. -
In Vitro Estrogenic Actions in Rat and Human Cells of Hydroxylated Derivatives of D16726 (Zindoxifene), an Agent with Known Antimammary Cancer Activity in Vivo1
[CANCER RESEARCH 48, 784-787, February 15, 1988] In Vitro Estrogenic Actions in Rat and Human Cells of Hydroxylated Derivatives of D16726 (Zindoxifene), an Agent with Known Antimammary Cancer Activity in Vivo1 S. P. Robinson, R. Koch, and V. C. Jordan2 Department of Human Oncology, University of Wisconsin Clinical Cancer Center, Madison, Wl 53792 ABSTRACT derivative D15414, (compound I, Fig. 1) in vitro (17, 19). This is of particular interest if the tumor inhibitory activity of A series of 2-phenyl-l-ethyl-3-methylindoles with or without a hy- D16726 is by estrogen antagonism as this compound does not droxyl group in the para position of the phenyl ring and the 5 or 6 position of the indole nucleus were compared with 17/3-estradiol in the have a structural equivalent of the alkylaminoethoxy side chain. We now report the activity of a series of 2-phenylindole stimulation of (a) prolactin production in rat pituitary cells in primary culture, (b) progesterone receptor synthesis in MCF-7 cells, and (c) derivatives, including D15414, in the stimulation of prolactin proliferation of MCF-7 cells. All compounds were less active than production in rat pituitary cells in primary culture and the i-stradini but all derivatives including 1)15414, the hydroxylated metab stimulation of progesterone receptor synthesis and growth of olite of D16726 (zindoxifene, a known antitumor agent against mammary MCF-7 cells. cancer) were fully estrogenic. Hydroxyl groups at the para position of the phenyl ring and 6 position of the indole nucleus conferred the highest estrogen potency [ED»(drug MATERIALS AND METHODS concentration producing 50% of maximum activity) in all assays around 10 "' M|. -
(12) United States Patent (10) Patent No.: US 9,687,458 B2 Podolski Et Al
US009687458B2 (12) United States Patent (10) Patent No.: US 9,687,458 B2 Podolski et al. (45) Date of Patent: Jun. 27, 2017 (54) TRANS-CLOMIPHENE FOR USE IN 6,143,353 A 1 1/2000 Oshlack CANCER THERAPY 6,190,591 B1 2/2001 Van Lengerich 6,221,399 B1 4/2001 Rolfes 6,248,363 B1 6, 2001 Patel (71) Applicant: REPROS THERAPEUTICS INC., 6,291,505 B1 9/2001 Huebner et al. The Woodlands, TX (US) 6,342,250 B1 1/2002 Masters 6,391920 B1 5, 2002 Fisch (72) Inventors: Joseph S. Podolski. The Woodlands, 6,511.986 B2 1/2003 Zhang et al. TX (US); Ronald D. Wiehle, Houston, 826 R $398 Ma'al TX (US); Kuang Hsu, The Woodlands, 6,638,528s- ww. B1 10/2003 KaniosaO ( a. TX (US); Greg Fontenot, The 6,645,974 B2 11/2003 Hutchinson et al. Woodlands, TX (US) 6,653,297 B1 11/2003 Hodgen 6,685,957 B1 2/2004 Bezemer et al. (73) Assignee: Repros Therapeutics Inc., The $33. R: 3. ErSC Woodlands, TX (US) 7,105,679 B2 9/2006 Kanojia et al. 7,354,581 B2 4/2008 Cedarb tal. (*) Notice: Subject to any disclaimer, the term of this 7,799,782 B2 9/2010 T al patent is extended or adjusted under 35 8,247456 B2 8/2012 Podolski U.S.C. 154(b) by 0 days. 8,377,991 B2 2/2013 Van AS 2002/O1200 12 A1 8, 2002 Fisch (21) Appl. No.: 14/440,007 (Continued) (22) PCT Filed: Oct. -
Effect of Estrogens on Skin Aging and the Potential Role of Selective Estrogen Receptor Modulators
CLIMACTERIC 2007;10:289–297 Effect of estrogens on skin aging and the potential role of selective estrogen receptor modulators S. Verdier-Se´vrain Bio-Hybrid, LLC, West Palm Beach, Florida, USA Key words: SKIN AGING, HORMONE REPLACEMENT THERAPY, TOPICAL ESTROGEN, PHYTOESTROGENS, SELECTIVE ESTROGEN RECEPTOR MODULATORS ABSTRACT Estrogens have a profound influence on skin. The relative hypoestrogenism that accom- panies menopause exacerbates the deleterious effects of both intrinsic and environ- mental aging. Estrogens prevent skin aging. They increase skin thickness and improve skin moisture. Beneficial effects of hormone replacement therapy (HRT) on skin aging have been well documented, but HRT cannot obviously be recommended solely to treat skin aging in menopausal women. Topical estrogen application is highly effective and safe if used by a dermatologist with expertise in endocrinology. The question of whether estrogen alternatives such as phytoestrogens and selective estrogen receptor modulators are effective estrogens for the prevention of skin aging in postmenopausal women remains unanswered. However, preliminary data indicate that such treatment may be of benefit for skin aging treatment. For personal use only. INTRODUCTION There are approximately 40 million postmeno- Intrinsic aging is characterized by smooth, pale, pausal women in the United States, contributing finely wrinkled skin and dryness2. Photoaging is to 17% of the total population1. As the popula- characterized by severe wrinkling and pigmentary tion of older women continues to grow at a rapid changes such as solar lentigo and mottled pig- rate, the challenges of learning more about the mentation3. Estrogens affect several skin functions health-care concerns and priorities of this group of and the estrogen deprivation that accompanies Climacteric Downloaded from informahealthcare.com by University of Washington on 05/23/13 patients become apparent. -
Regulation of Specific Target Genes and Biological Responses by Estrogen Receptor Subtype Agonists Leitman Et Al
COPHAR-861; NO. OF PAGES 8 Available online at www.sciencedirect.com Regulation of specific target genes and biological responses by estrogen receptor subtype agonists Dale C Leitman1, Sreenivasan Paruthiyil2, Omar I Vivar1, Elise F Saunier2, Candice B Herber1, Isaac Cohen2, Mary Tagliaferri2 and Terence P Speed3,4 Estrogenic effects are mediated through two estrogen receptor adverse effects. The most troublesome side-effect of (ER) subtypes, ERa and ERb. Estrogens are the most estrogens is the increased risk of breast and endometrial commonly prescribed drugs to treat menopausal conditions, cancer [1,2]. Estrogens also increase blood clotting that but by non-selectively triggering both ERa and ERb pathways can lead to venous thromboembolisms, and possibly in different tissues they can cause serious adverse effects. The strokes and heart disease, particularly in older women different sizes of the binding pockets and sequences of their [1]. activation function domains indicate that ERa and ERb should have different specificities for ligands and biological responses Estrogens in hormone therapy (HT) were formulated that can be exploited for designing safer and more selective long before there was a significant understanding of estrogens. ERa and ERb regulate different genes by binding to the mechanism of action of estrogens. The identification different regulatory elements and recruiting different of ERa and ERb (Figure 1) and the crystal structures of transcription and chromatin remodeling factors that are their ligand binding domain (LBD), the discovery of a expressed in a cell-specific manner. ERa-selective and ERb- variety of coregulatory proteins involved in the genomic selective agonists have been identified that demonstrate that pathway and the demonstration of the nongenomic the two ERs produce distinct biological effects. -
Anticancer Activity of <Emphasis Type="Italic">Asparagus
J. Korean Soc. Appl. Biol. Chem. 54(2), 188-193 (2011) Article Anticancer Activity of Asparagus cochinchinensis Extract and Fractions in HepG2 Cells Mikyung Park1†, Myeong Sook Cheon2†, Seong Hwan Kim1, Jin Mi Chun2, A Yeong Lee2, Byeong Cheol Moon2, Taesook Yoon2, Byung Kil Choo3, and Ho Kyoung Kim2* 1Laboratory of Chemical Genomics, Pharmacology Research Center, Korea Research Institute of Chemical Technology, P.O.Box 107, Yuseong-gu, Daejeon 305-600, Republic of Korea 2Center of Herbal Resources Research, Korea Institute of Oriental Medicine, 483 Exporo, Daejeon 305-811, Republic of Korea 3Department of Crop Agriculture & Life Science, College of Agriculture & Life Science, Chonbuk National University, Jeonju 561-756, Republic of Korea Received October 18, 2010; Accepted January 4, 2010 Asparagus cochinchinensis Merrill (Liliaceae) has been traditionally used for the treatment of cancer in Korea and China, but its anticancer activity and underlying mechanism remain to be defined. Anticancer activities were investigated on fractions obtained from A. cochinchinensis 70% ethanol extract (ACE-EtOH) in human hepatocellular carcinoma HepG2 cells. Ethylacetate fraction from A. cochinchinensis extract (ACE-EA), more effective than other fractions, induced apoptosis of HepG2 (IC50=72.33±0.34 μg/mL), as revealed by apoptotic feature observation, increased capase-3 activity and Poly ADP ribose polymerase cleavage, and decreased expression of X-linked inhibitor of apoptosis protein in a dose-dependent manner. Protein levels of autophagy- related molecules, microtubule-associated protein 1 light chain 3 α and beclin 1, appeared to be induced by ACE-EA, suggesting ACE-EA exhibits anti-cancer activity with induction via both apoptosis and autophagy signaling pathways in HepG2 cells. -
Multistage Delivery of Active Agents
111111111111111111111111111111111111111111111111111111111111111111111111111111 (12) United States Patent (io) Patent No.: US 10,143,658 B2 Ferrari et al. (45) Date of Patent: Dec. 4, 2018 (54) MULTISTAGE DELIVERY OF ACTIVE 6,355,270 B1 * 3/2002 Ferrari ................. A61K 9/0097 AGENTS 424/185.1 6,395,302 B1 * 5/2002 Hennink et al........ A61K 9/127 (71) Applicants:Board of Regents of the University of 264/4.1 2003/0059386 Al* 3/2003 Sumian ................ A61K 8/0241 Texas System, Austin, TX (US); The 424/70.1 Ohio State University Research 2003/0114366 Al* 6/2003 Martin ................. A61K 9/0097 Foundation, Columbus, OH (US) 424/489 2005/0178287 Al* 8/2005 Anderson ............ A61K 8/0241 (72) Inventors: Mauro Ferrari, Houston, TX (US); 106/31.03 Ennio Tasciotti, Houston, TX (US); 2008/0280140 Al 11/2008 Ferrari et al. Jason Sakamoto, Houston, TX (US) FOREIGN PATENT DOCUMENTS (73) Assignees: Board of Regents of the University of EP 855179 7/1998 Texas System, Austin, TX (US); The WO WO 2007/120248 10/2007 Ohio State University Research WO WO 2008/054874 5/2008 Foundation, Columbus, OH (US) WO WO 2008054874 A2 * 5/2008 ............... A61K 8/11 (*) Notice: Subject to any disclaimer, the term of this OTHER PUBLICATIONS patent is extended or adjusted under 35 U.S.C. 154(b) by 0 days. Akerman et al., "Nanocrystal targeting in vivo," Proc. Nad. Acad. Sci. USA, Oct. 1, 2002, 99(20):12617-12621. (21) Appl. No.: 14/725,570 Alley et al., "Feasibility of Drug Screening with Panels of Human tumor Cell Lines Using a Microculture Tetrazolium Assay," Cancer (22) Filed: May 29, 2015 Research, Feb. -
A Dissertation Submitted to the Faculty of the Graduate School of Arts And
MOLECULAR MODULATION OF ESTROGEN -INDUCED APOPTOSIS IN LONG -TERM ESTROGEN - DEPRIVED BREAST CANCER CELLS A Dissertation submitted to the Faculty of the Graduate School of Arts and Sciences of Georgetown University in partial fulfillment of the requirements for the degree of Doctor of Philosophy in Tumor Biology By Elizabeth E. Sweeney, B.S. Washington, DC March 31, 2014 Copyright 2014 by Elizabeth E. Sweeney All Rights Reserved ii MOLECULAR MODULATION OF ESTROGEN -INDUCED APOPTOSIS IN LONG -TERM ESTROGEN - DEPRIVED BREAST CANCER CELLS Elizabeth E. Sweeney, B.S. Thesis Advisor: V. Craig Jordan , O.B.E., Ph.D., D.Sc., F.Med.Sci . ABSTRACT Estrogen receptor (ER)-positive breast cancer cell lines have been instrumental in modeling breast cancer and providing an opportunity to document the development and evolution of acquired anti-hormone resistance. Models of long-term estrogen-deprived breast cancer cells are utilized in the laboratory to mimic clinical aromatase inhibitor-resistant breast cancer and serve as a tool to discover new therapeutic strategies. The MCF-7:5C and MCF-7:2A subclones were generated through long-term estrogen deprivation of ER-positive MCF-7 cells, and represent anti-hormone resistant breast cancer. MCF-7:5C cells paradoxically undergo estrogen-induced apoptosis within seven days of estrogen (estradiol, E 2) treatment; MCF-7:2A cells also experience E2-induced apoptosis but evade dramatic cell death until approximately 14 days of treatment. Our data suggest that MCF-7:2A cells employ stronger antioxidant defense mechanisms than do MCF-7:5C cells, and that oxidative stress is ultimately required for MCF- 7:2A cells to die in response to E2 treatment. -
Dr. Duke's Phytochemical and Ethnobotanical Databases List of Chemicals for Dry Mouth / Xerostomia
Dr. Duke's Phytochemical and Ethnobotanical Databases List of Chemicals for Dry Mouth / Xerostomia Chemical Activity Count (+)-CATECHIN 2 (+)-EPIPINORESINOL 1 (-)-ANABASINE 1 (-)-EPICATECHIN 2 (-)-EPIGALLOCATECHIN 2 (-)-EPIGALLOCATECHIN-GALLATE 2 (Z)-1,3-BIS(4-HYDROXYPHENYL)-1,4-PENTADIENE 1 1,8-CINEOLE 2 10-METHOXYCAMPTOTHECIN 1 16-HYDROXY-4,4,10,13-TETRAMETHYL-17-(4-METHYL-PENTYL)-HEXADECAHYDRO- 1 CYCLOPENTA[A]PHENANTHREN-3-ONE 2,3-DIHYDROXYBENZOIC-ACID 1 3'-O-METHYL-CATECHIN 1 3-ACETYLACONITINE 1 3-O-METHYL-(+)-CATECHIN 1 4-O-METHYL-GLUCURONOXYLAN 1 5,7-DIHYDROXY-2-METHYLCHROMONE-8-C-BETA-GLUCOPYRANOSIDE 1 5-HYDROXYTRYPTAMINE 1 5-HYDROXYTRYPTOPHAN 1 6-METHOXY-BENZOLINONE 1 ACEMANNAN 1 ACETYL-CHOLINE 1 ACONITINE 2 ADENOSINE 2 AFFINISINE 1 AGRIMONIIN 1 ALANTOLACTONE 2 ALKANNIN 1 Chemical Activity Count ALLANTOIN 1 ALLICIN 2 ALLIIN 2 ALLOISOPTEROPODINE 1 ALLOPTEROPODINE 1 ALLOPURINOL 1 ALPHA-LINOLENIC-ACID 1 ALPHA-TERPINEOL 1 ALPHA-TOCOPHEROL 2 AMAROGENTIN 1 AMELLIN 1 ANABASINE 1 ANDROMEDOTOXIN 1 ANETHOLE 1 ANTHOCYANIDINS 1 ANTHOCYANINS 1 ANTHOCYANOSIDE 1 APIGENIN 1 APOMORPHINE 1 ARABINO-3,6-GALACTAN-PROTEIN 1 ARABINOGALACTAN 1 ARACHIDONIC-ACID 1 ARCTIGENIN 2 ARECOLINE 1 ARGLABRIN 1 ARISTOLOCHIC-ACID 1 ARISTOLOCHIC-ACID-I 1 2 Chemical Activity Count ARMILLARIEN-A 1 ARTEMISININ 1 ASCORBIC-ACID 4 ASTRAGALAN-I 1 ASTRAGALAN-II 1 ASTRAGALAN-III 1 ASTRAGALIN 1 AURICULOSIDE 1 BAICALEIN 1 BAICALIN 1 BAKUCHIOL 1 BENZALDEHYDE 1 BERBAMINE 1 BERBERASTINE 3 BERBERINE 3 BERBERINE-CHLORIDE 1 BERBERINE-IODIDE 1 BERBERINE-SULFATE 1 BETA-AMYRIN-PALMITATE