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https://www.readbyqxmd.com/read/28430646/immunotherapeutic-target-expression-on-breast-tumors-can-be-amplified-by-hormone-receptor-antagonism-a-novel-strategy-for-enhancing-efficacy-of-targeted-immunotherapy
#1
Ritika Jaini, Matthew G Loya, Charis Eng
Immunotherapy has historically been successful in highly antigenic tumors but has shown limited therapeutic efficacy in non-antigenic tumors such as breast cancers. Our previous studies in autoimmunity have demonstrated that increased antigen load within a tissue enhances immune reactivity against it. We therefore hypothesized that enhancing expression of target proteins on breast tumors can increase efficacy of targeted immunotherapy. We hypothesized that antagonism of the estrogen receptor (ER) can increase expression of targets that are hormonally regulated and facilitate enhanced tumor recognition by targeted immunotherapy...
March 1, 2017: Oncotarget
https://www.readbyqxmd.com/read/28426931/lead-optimization-of-benzoxepin-type-selective-estrogen-receptor-er-modulators-and-downregulators-with-subtype-specific-er%C3%AE-and-er%C3%AE-activity
#2
Niamh Mary O'Boyle, Irene Barrett, Lisa M Greene, Miriam Carr, Darren Fayne, Brendan Twamley, Andrew J S Knox, Niall O Keely, Daniela M Zisterer, Mary Jane Meegan
Estrogen receptor (ER) is an important target for the design of drugs such as tamoxifen (2a) and fulvestrant (5). Three series of ER-ligands based on the benzoxepin scaffold structure were synthesised - series I containing an acrylic acid, series II with an acrylamide and series III with an acid substuent. These compounds were shown to be high affinity ligands for the ER with nanomolar IC50 binding values. Series I acrylic acid ligands were generally ERα selective. In particular, compound 13e featuring a phenylpenta-2,4-dienoic acid substituent was shown to be antiproliferative and downregulated ERα and ERβ expression in MCF-7 breast cancer cells...
April 20, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28422740/involvement-of-mir-106b-in-tumorigenic-actions-of-both-prolactin-and-estradiol
#3
Kuan-Hui Ethan Chen, Karissa Bustamante, Vi Nguyen, Ameae M Walker
Prolactin promotes a variety of cancers by an array of different mechanisms. Here, we have investigated prolactin's inhibitory effect on expression of the cell cycle-regulating protein, p21. Using a miRNA array, we identified a number of miRNAs upregulated by prolactin treatment, but one in particular that was strongly induced by prolactin and predicted to bind to the 3'UTR of p21 mRNA, miR-106b. By creating a p21 mRNA 3'UTR-luciferase mRNA construct, we demonstrated degradation of the construct in response to prolactin in human breast, prostate and ovarian cancer cell lines...
March 31, 2017: Oncotarget
https://www.readbyqxmd.com/read/28383555/zeb1-induces-er-%C3%AE-promoter-hypermethylation-and-confers-antiestrogen-resistance-in-breast-cancer
#4
Jianbo Zhang, Chen Zhou, Huimin Jiang, Lin Liang, Wen Shi, Quansheng Zhang, Peiqing Sun, Rong Xiang, Yue Wang, Shuang Yang
Antiestrogen resistance is a major obstacle to endocrine therapy for breast cancers. Although reduced estrogen receptor-α (ER-α) expression is a known contributing factor to antiestrogen resistance, the mechanisms of ER-α downregulation in antiestrogen resistance are not fully understood. Here, we report that ectopic zinc-finger E-box binding homeobox 1 (ZEB1) is associated with ER-α deficiency in breast cancer cells and thus confers antiestrogen resistance. Mechanistically, ZEB1 represses ER-α transcription by forming a ZEB1/DNA methyltransferase (DNMT)3B/histone deacetylase (HDAC)1 complex on the ER-α promoter, leading to DNA hypermethylation and the silencing of ER-α...
April 6, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28377489/preclinical-activity-of-the-novel-anti-prolactin-receptor-prlr-antibody-drug-conjugate-regn2878-dm1-in-prlr-positive-breast-cancers
#5
Marcus P Kelly, Carlos Hickey, Sosina Makonnen, Sandra Coetzee, Sumreen Jalal, Yu Wang, Frank Delfino, Jing Shan, Terra B Potocky, Ishita Chatterjee, Julian Andreev, Arthur Kunz, Christopher D'Souza, Jason T Giurleo, Thomas Nittoli, Pamela A Trail, Gavin Thurston, Jessica R Kirshner
The Prolactin Receptor (PRLR) is a type 1 cytokine receptor that is expressed in a subset of breast cancers and may contribute to its pathogenesis. It is relatively over-expressed in ~25% of human breast tumors while expressed at low levels in some normal human tissues including the mammary gland. We developed an anti-PRLR antibody-drug conjugate (ADC), to target PRLR positive breast cancer. REGN2878-DM1 is comprised of a fully human high affinity function-blocking anti-PRLR IgG1 antibody (REGN2878) conjugated via a non-cleavable SMCC linker to the cytotoxic maytansine derivative DM1...
April 4, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28376210/estrogen-receptor-%C3%AE-as-a-therapeutic-target-in-breast-cancer-stem-cells
#6
Ran Ma, Govindasamy-Muralidharan Karthik, John Lövrot, Felix Haglund, Gustaf Rosin, Anne Katchy, Xiaonan Zhang, Lisa Viberg, Jan Frisell, Cecilia Williams, Stig Linder, Irma Fredriksson, Johan Hartman
Background: Breast cancer cells with tumor-initiating capabilities (BSCs) are considered to maintain tumor growth and govern metastasis. Hence, targeting BSCs will be crucial to achieve successful treatment of breast cancer. Methods: We characterized mammospheres derived from more than 40 cancer patients and two breast cancer cell lines for the expression of estrogen receptors (ERs) and stem cell markers. Mammosphere formation and proliferation assays were performed on cells from 19 cancer patients and five healthy individuals after incubation with ER-subtype selective ligands...
March 1, 2017: Journal of the National Cancer Institute
https://www.readbyqxmd.com/read/28376201/re-final-overall-survival-fulvestrant-500%C3%A2-mg-vs-250%C3%A2-mg-in-the-randomized-confirm-trial
#7
Miguel Martin, John Boyer, Mary Stuart, Angelo di Leo
No abstract text is available yet for this article.
March 1, 2017: Journal of the National Cancer Institute
https://www.readbyqxmd.com/read/28374222/the-evolving-role-of-the-estrogen-receptor-mutations-in-endocrine-therapy-resistant-breast-cancer
#8
REVIEW
Rinath Jeselsohn, Carmine De Angelis, Myles Brown, Rachel Schiff
Recurrent ligand-binding domain ESR1 mutations have recently been detected in a substantial number of patients with metastatic ER+ breast cancer and evolve under the selective pressure of endocrine treatments. In this review, we evaluate the current understanding of the biological and clinical significance of these mutations. The preclinical studies revealed that these mutations lead to constitutive ligand-independent activity, indicating resistance to aromatase inhibitors and decreased sensitivity to tamoxifen and fulvestrant...
May 2017: Current Oncology Reports
https://www.readbyqxmd.com/read/28363954/estrogen-deficiency-attenuates-fluid-flow-induced-ca-2-i-oscillations-and-mechanoresponsiveness-of-mlo-y4-osteocytes
#9
Vishwa Deepak, Pushpalata Kayastha, Laoise M McNamara
It has been proposed that estrogen regulates the mechanosensitivity of osteocytes; however, the effects of estrogen deficiency that arises during postmenopausal osteoporosis on mechanical stimulation-induced calcium signaling in osteocytes remains elusive. Here, we pretreated MLO-Y4 osteocytes with 10 nM E2 for 2, 3 and 5 d, then simulated postmenopausal conditions either by withdrawing estrogen (EW) from culture medium, or by inhibiting the estrogen receptor by using fulvestrant and estrogen (FE; ICI 182,780) in vitro We investigated [Ca(2+)]i oscillations and mechanobiologic responses of osteocytes (EW and FE) that were exposed to oscillatory fluid flow (OFF; 1 Pa, 0...
March 31, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28344099/mechanisms-of-resistance-to-selective-estrogen-receptor-down-regulator-in-metastatic-breast-cancer
#10
REVIEW
Doudou Huang, Fang Yang, Yucai Wang, Xiaoxiang Guan
Based on the prominent role estrogen receptor (ER) plays in breast cancer, endocrine therapy has been developed to block the ER pathway and has shown great effectiveness. Fulvestrant, the first selective ER down-regulator (SERD), was demonstrated to completely suppress ERα and notably efficient. However, resistance to fulvestrant occurs, either intrinsic or acquired during the treatment. Several potential mechanisms inducing fulvestrant resistance have been proposed, composed of activated ERα-independent compensatory growth factor signaling, stimulated downstream kinases, altered cell cycle mediators, etcetera...
March 23, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28337663/outcomes-of-fulvestrant-therapy-among-japanese-women-with-advanced-breast-cancer-a-retrospective-multicenter-cohort-study-jbcrg-c06-safari
#11
H Kawaguchi, N Masuda, T Nakayama, K Aogi, K Anan, Y Ito, S Ohtani, N Sato, S Saji, E Tokunaga, S Nakamura, Y Hasegawa, M Hattori, T Fujisawa, S Morita, M Yamaguchi, T Yamashita, Y Yamamoto, S Ohno, M Toi
PURPOSE: This retrospective study evaluated the effect of clinical background and treatment line on time to treatment failure (TTF) in advanced/metastatic breast cancer (AMBC) patients receiving F500 in Japan (UMIN 000015168). METHODS: Patients who commenced F500 treatment were registered at 16 sites in Japan. Correlations between baseline clinicopathological factors, treatment line, and TTF were investigated by Kaplan-Meier analysis. TTF data were analyzed using univariate analysis and multivariate analysis with a Cox proportional hazards model...
March 23, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/28326039/estrone-sulfate-transport-and-steroid-sulfatase-activity-in-colorectal-cancer-implications-for-hormone-replacement-therapy
#12
Lorna C Gilligan, Ali Gondal, Vivien Tang, Maryam T Hussain, Anastasia Arvaniti, Anne-Marie Hewitt, Paul A Foster
Hormone replacement therapy (HRT) affects the incidence and potential progression of colorectal cancer (CRC). As HRT primarily consists of estrone sulfate (E1S), understanding whether this conjugated estrogen is transported and metabolized in CRC will define its potential effect in this malignancy. Here, we show that a panel of CRC cell lines (Colo205, Caco2, HCT116, HT-29) have steroid sulfatase (STS) activity, and thus can hydrolyze E1S. STS activity is significantly higher in CRC cell lysate, suggesting the importance of E1S transport in intracellular STS substrate availability...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28325261/cdk4-6-inhibitors-in-her2-positive-breast-cancer
#13
REVIEW
Silvia Paola Corona, Andrea Ravelli, Daniele Cretella, Maria Rosa Cappelletti, Laura Zanotti, Martina Dester, Angela Gobbi, Pier Giorgio Petronini, Daniele Generali
Notwithstanding the continuous progress made in cancer treatment in the last 20 years, and the availability of new targeted therapies, metastatic Breast Cancer (BC) is still incurable. Targeting the cell cycle machinery has emerged as an attractive strategy to tackle cancer progression, showing very promising results in the preclinical and clinical settings. The first selective inhibitors of CDK4/6 received breakthrough status and FDA approval in combination with letrozole (February 2015) and fulvestrant (February 2016) as first-line therapy in ER-positive advanced and metastatic BC...
April 2017: Critical Reviews in Oncology/hematology
https://www.readbyqxmd.com/read/28324247/fulvestrant-plus-targeted-agents-versus-fulvestrant-alone-for-treatment-of-hormone-receptor-positive-advanced-breast-cancer-progressed-on-previous-endocrine-therapy-a-meta-analysis-of-randomized-controlled-trials
#14
REVIEW
Wen-Zhao Lin, Qi-Ni Xu, Hong-Biao Wang, Xu-Yuan Li
To compare the addition of targeted agents to fulvestrant with fulvestrant alone in hormone-receptor positive advanced breast cancer progressed on previous endocrine therapy; a meta-analysis of all relevant randomized controlled trials was performed. The PubMed, Embase databases and the Cochrane Central Register of Controlled Trials were searched for relevant publications reporting randomized controlled trials between January 2000 and June 2016. Progression-free survival (PFS), objective response rate (ORR), disease control rate (DCR), and toxicity were assessed...
March 21, 2017: Breast Cancer: the Journal of the Japanese Breast Cancer Society
https://www.readbyqxmd.com/read/28319364/a-new-spin-on-antibody-drug-conjugates-trastuzumab-fulvestrant-colloidal-drug-aggregates-target-her2-positive-cells
#15
Ahil N Ganesh, Christopher K McLaughlin, Da Duan, Brian K Shoichet, Molly S Shoichet
While the formation of colloidal aggregates leads to artifacts in early drug discovery, their composition makes them attractive as nanoparticle formulations for targeted drug delivery as the entire nanoparticle is composed of drug. The typical transient stability of colloidal aggregates has inhibited exploiting this property. To overcome this limitation, we investigated a series of proteins to stabilize colloidal aggregates of the chemotherapeutic, fulvestrant, including the following: bovine serum albumin, a generic human immunoglobulin G, and trastuzumab, a therapeutic human epidermal growth factor receptor 2 antibody...
April 12, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28319069/the-branched-chain-amino-acid-transaminase-1-sustains-growth-of-antiestrogen-resistant-and-er%C3%AE-negative-breast-cancer
#16
V Thewes, R Simon, M Hlevnjak, M Schlotter, P Schroeter, K Schmidt, Y Wu, T Anzeneder, W Wang, P Windisch, M Kirchgäßner, N Melling, N Kneisel, R Büttner, U Deuschle, H P Sinn, A Schneeweiss, S Heck, S Kaulfuss, H Hess-Stumpp, J G Okun, G Sauter, A E Lykkesfeldt, M Zapatka, B Radlwimmer, P Lichter, M Tönjes
Antiestrogen-resistant and triple-negative breast tumors pose a serious clinical challenge because of limited treatment options. We assessed global gene expression changes in antiestrogen-sensitive compared with antiestrogen-resistant (two tamoxifen resistant and two fulvestrant resistant) MCF-7 breast cancer cell lines. The branched-chain amino acid transaminase 1 (BCAT1), which catalyzes the first step in the breakdown of branched-chain amino acids, was among the most upregulated transcripts in antiestrogen-resistant cells...
March 20, 2017: Oncogene
https://www.readbyqxmd.com/read/28314478/osteoinductive-effects-of-glyceollins-on-adult-mesenchymal-stromal-stem-cells-from-adipose-tissue-and-bone-marrow
#17
Marjorie E Bateman, Amy L Strong, Ryan S Hunter, Melyssa R Bratton, Rajesh Komati, Jayalakshmi Sridhar, Kevin E Riley, Guangdi Wang, Daniel J Hayes, Stephen M Boue, Matthew E Burow, Bruce A Bunnell
BACKGROUND: While current therapies for osteoporosis focus on reducing bone resorption, the development of therapies to regenerate bone may also be beneficial. Promising anabolic therapy candidates include phytoestrogens, such as daidzein, which effectively induce osteogenesis of adipose-derived stromal cells (ASCs) and bone marrow stromal cells (BMSCs). PURPOSE: To investigate the effects of glyceollins, structural derivatives of daidzein, on osteogenesis of ASCs and BMSCs...
April 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28301080/hsp90-inhibitor-auy922-can-reverse-fulvestrant-induced-feedback-reaction-in-human-breast-cancer-cells
#18
Jingchao Bai, Guanglin Zhou, Yufan Qiu, Yunhui Hu, Jingjing Liu, Jing Zhao, Sheng Zhang, Jin Zhang
Hormone therapy has become one of the main strategy for breast cancer, however, many estrogen receptor(ER) positive patients ends in tumor collapse due to initial or acquired resistance to hormone treatment, which includes Fulvestrant. Here we report that ErbB Receptors and downstream PI3K/AKT and ERK pathway have been reactivated after treatment of Fulvestrant in ER positive MCF-7 and T47D cells, which are related to Fulvestrant resistance. HSP90 is a universally expressed chaperone protein and plays a vital role in both normal and cancer cells, HSP90 inhibitor AUY922 can reverse this feedback reactivation effect of Fulvestrant by targeting multiple proteins related in ErbB Receptors, PI3K/AKT and ERK pathway, which is much better than single targeting inhibitors...
March 16, 2017: Cancer Science
https://www.readbyqxmd.com/read/28281842/opportunities-and-challenges-of-long-term-anti-estrogenic-adjuvant-therapy-treatment-forever-or-intermittently
#19
Poulomi Bhattacharya, Balkees Abderrahman, V Craig Jordan
Extended adjuvant (5-10 years) therapy targeted to the estrogen receptor (ER) has significantly decreased mortality from breast cancer (BC). Areas covered: Translational research advanced clinical testing of extended adjuvant therapy with tamoxifen or aromatase inhibitors (AIs). Short term therapy or non-compliance increase recurrence, but surprisingly recurrence and death does not increase dramatically after 5 years of adjuvant therapy stops. Expert commentary: Compliance ensures optimal benefit from extended antihormone adjuvant therapy...
April 2017: Expert Review of Anticancer Therapy
https://www.readbyqxmd.com/read/28280092/a-phase-i-ib-study-of-enzalutamide-alone-and-in-combination-with-endocrine-therapies-in-women-with-advanced-breast-cancer
#20
Lee S Schwartzberg, Denise Yardley, Anthony Elias, Manish Patel, Patricia M LoRusso, Howard A Burris, Ayca Gucalp, Amy Peterson, Martha Blaney, Joyce Steinberg, Jacqueline Gibbons, Tiffany A Traina
PURPOSE: Several lines of evidence support targeting the androgen signaling pathway in breast cancer. Enzalutamide is a potent inhibitor of androgen receptor signaling. Preclinical data in estrogen-expressing breast cancer models demonstrated activity of enzalutamide monotherapy and enhanced activity when combined with various endocrine therapies (ETs). Enzalutamide is a strong cytochrome P450 3A4 (CYP3A4) inducer, and ETs are commonly metabolized by CYP3A4. The pharmacokinetic (PK) interactions, safety, and tolerability of enzalutamide monotherapy and in combination with ETs were assessed in this phase I/Ib study...
March 9, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
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