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Aromatase inhibitors

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https://www.readbyqxmd.com/read/28430630/estrogen-and-androgen-converting-enzymes-17%C3%AE-hydroxysteroid-dehydrogenase-and-their-involvement-in-cancer-with-a-special-focus-on-17%C3%AE-hydroxysteroid-dehydrogenase-type-1-2-and-breast-cancer
#1
REVIEW
Erik Hilborn, Olle Stål, Agneta Jansson
Sex steroid hormones such as estrogens and androgens are involved in the development and differentiation of the breast tissue. The activity and concentration of sex steroids is determined by the availability from the circulation, and on local conversion. This conversion is primarily mediated by aromatase, steroid sulfatase, and 17β-hydroxysteroid dehydrogenases. In postmenopausal women, this is the primary source of estrogens in the breast. Up to 70-80% of all breast cancers express the estrogen receptor-α, responsible for promoting the growth of the tissue...
February 20, 2017: Oncotarget
https://www.readbyqxmd.com/read/28429243/slco1b1-polymorphisms-and-plasma-estrone-conjugates-in-postmenopausal-women-with-er-%C3%A2-breast-cancer-genome-wide-association-studies-of-the-estrone-pathway
#2
Tanda M Dudenkov, James N Ingle, Aman U Buzdar, Mark E Robson, Michiaki Kubo, Irada Ibrahim-Zada, Anthony Batzler, Gregory D Jenkins, Tracy L Pietrzak, Erin E Carlson, Poulami Barman, Matthew P Goetz, Donald W Northfelt, Alvaro Moreno-Aspita, Clark V Williard, Krishna R Kalari, Yusuke Nakamura, Liewei Wang, Richard M Weinshilboum
BACKGROUND: Estrone (E1), the major circulating estrogen in postmenopausal women, promotes estrogen-receptor positive (ER+) breast tumor growth and proliferation. Two major reactions contribute to E1 plasma concentrations, aromatase (CYP19A1) catalyzed E1 synthesis from androstenedione and steroid sulfatase (STS) catalyzed hydrolysis of estrone conjugates (E1Cs). E1Cs have been associated with breast cancer risk and may contribute to tumor progression since STS is expressed in breast cancer where its activity exceeds that of aromatase...
April 20, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/28427518/controversies-in-clinicopathological-characteristics-and-treatment-strategies-of-male-breast-cancer-a-review-of-the-literature
#3
REVIEW
Agnese Losurdo, Selene Rota, Giuseppe Gullo, Giovanna Masci, Rosalba Torrisi, Giulia Bottai, Monica Zuradelli, Wolfgang Gatzemeier, Armando Santoro
Male breast cancer (MaBC) is a rare disease, accounting for less than 1% of malignancies in men. For this reason, literature data on its clinicopathological characteristics are very heterogeneous and treatment strategies have mostly been extrapolated from the female counterpart. However, immunohistochemical peculiarities of MaBC have recently emerged, defining it as a distinct entity from female breast cancer (FBC), thus requiring a tailored clinical approach. MaBC appears to be more often hormone receptor positive than FBC, while data on HER2 status still remain inconclusive, indicating a possible higher incidence of HER2 alterations...
May 2017: Critical Reviews in Oncology/hematology
https://www.readbyqxmd.com/read/28427017/aromatase-inhibitors-and-apoptotic-inducers-design-synthesis-anticancer-activity-and-molecular-modeling-studies-of-novel-phenothiazine-derivatives-carrying-sulfonamide-moiety-as-hybrid-molecules
#4
Mostafa M Ghorab, Mansour S Alsaid, Nermin Samir, Ghada A Abdel-Latif, Aiten M Soliman, Fatma A Ragab, Dalal A Abou El Ella
Hybrid molecules are used as anticancer agents to improve effectiveness and diminish drug resistance. So, the current study aimed to introduce twenty novel phenothiazine sulfonamide hybrids 5-22, 24 and 25 of promising anticancer activity. Compounds 11 and 13 revealed more potent anticancer properties (IC50 8.1 and 8.8 μM) than that of the reference drug (doxorubicin, IC50 = 9.8 μM) against human breast cancer cell line (T47D). To determine the mechanism of their anticancer activity, compounds 5, 6, 7, 11, 13, 14, 16, 17, 19 and 22 that showed promising activity on T47D, were evaluated for their aromatase inhibitory effect...
April 15, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28424084/durable-complete-remission-with-aromatase-inhibitor-therapy-in-a-patient-with-metastatic-uterine-carcinosarcoma-with-poor-performance-status-and-coagulation-disorders-a-case-report
#5
P Martin-Romano, M Jurado, M A Idoate, L Arbea, J L Hernandez-Lizoain, D Cano, J A Paramo, S Martin-Algarra
BACKGROUND: Chemotherapy is considered the most appropriate treatment for metastatic uterine sarcoma, despite its limited efficacy. No other treatment has been conclusively proved to be a real alternative, but some reports suggest that anti-hormonal therapy could be active in a small subset of patients. We report the case of a patient with metastatic uterine carcinosarcoma with positive hormonal receptors and a complete pathological response. CASE PRESENTATION: A 54-year-old white woman presented to our emergency room with hypovolemic shock and serious vaginal bleeding...
April 19, 2017: Journal of Medical Case Reports
https://www.readbyqxmd.com/read/28423398/treatment-restarting-after-discontinuation-of-adjuvant-hormone-therapy-in-breast-cancer-patients
#6
Wei He, Karin E Smedby, Fang Fang, Henrik Olsson, Sara Margolin, Per Hall, Kamila Czene
Background: Over half of breast cancer patients discontinue their adjuvant hormone therapy, permanently or temporarily. We aimed to identify predictors of treatment restarting after discontinuation of adjuvant hormone therapy and to test the hypothesis that treatment restarting is associated with better breast cancer outcomes. Methods: We conducted a population-based cohort study by linking data from the Stockholm-Gotland Breast Cancer Register, the Swedish Prescribed Drug Register, and a self-reported questionnaire...
October 1, 2017: Journal of the National Cancer Institute
https://www.readbyqxmd.com/read/28423275/single-or-multiple-access-channels-to-the-cyp450s-active-site-an-answer-from-free-energy-simulations-of-the-human-aromatase-enzyme
#7
Alessandra Magistrato, Jacopo Sgrignani, Rolf Krause, Andrea Cavalli
Cytochromes P450 (CYP450), in particular CYP19A1 and CYP17A1, are key clinical targets of breast and prostate anticancer therapies, critical players in drug metabolism and their overexpression in tumours is associated with drug resistance. In these enzymes ligands (substrates, drugs) metabolism occurs in deeply buried active sites accessible only via several gruelling channels, whose exact biological role remains unclear. Gaining direct insights on the mechanism by which ligands travel in and out, is becoming increasingly important given that channels are involved in the modulation of binding/dissociation kinetics and the specificity of ligands toward a CYP450...
April 19, 2017: Journal of Physical Chemistry Letters
https://www.readbyqxmd.com/read/28417244/ribociclib-first-global-approval
#8
Yahiya Y Syed
Ribociclib is an oral, small-molecule inhibitor of cyclin-dependent kinase (CDK) 4 and 6 that is under development by Novartis for the treatment of cancer. CDKs play an important role in cell cycle progression and cellular proliferation, and inhibition of these kinases with ribociclib results in G1 phase cell-cycle arrest. Ribociclib, in combination with an aromatase inhibitor, was recently approved in the USA for the first-line treatment of advanced breast cancer and has been submitted for approval in the EU for this indication...
April 17, 2017: Drugs
https://www.readbyqxmd.com/read/28416639/absent-progesterone-receptor-expression-in-the-lymph-node-metastases-of-er-positive-her2-negative-breast-cancer-is-associated-with-relapse-on-tamoxifen
#9
Cameron E Snell, Madeline Gough, Kathryn Middleton, Michael Hsieh, Lauren Furnas, Brenton Seidl, Kristen Gibbons, Christopher Pyke, Catherine Shannon, Natasha Woodward, Jane E Armes
AIMS: Progesterone receptor (PR) expression is prognostic in early stage breast cancer. There are several reports of discordant expression between primary tumour and axillary lymph node (ALN) metastasis expression of oestrogen receptor (ER) and PR. We sought to determine whether expression of these biomarkers in the synchronous ALN metastases of ER positive (+), HER2 negative (-) breast cancer could provide more accurate prognostic information. METHODS: The retrospective cohort included 229 patients from a single institution with ER+, HER2- breast cancer who had synchronous ALN metastatic disease (2005-2014)...
April 17, 2017: Journal of Clinical Pathology
https://www.readbyqxmd.com/read/28413771/management-of-aromatase-inhibitor-associated-bone-loss-aibl-in-postmenopausal-women-with-hormone-sensitive-breast-cancer-joint-position-statement-of-the-iof-cabs-ects-ieg-esceo-ims-and-siog
#10
REVIEW
Peyman Hadji, Matti S Aapro, Jean-Jacques Body, Michael Gnant, Maria Luisa Brandi, Jean Yves Reginster, M Carola Zillikens, Claus-C Glüer, Tobie de Villiers, Rod Baber, G David Roodman, Cyrus Cooper, Bente Langdahl, Santiago Palacios, John Kanis, Nasser Al-Daghri, Xavier Nogues, Erik Fink Eriksen, Andreas Kurth, Rene Rizzoli, Robert E Coleman
BACKGROUND: Several guidelines have been reported for bone-directed treatment in women with early breast cancer (EBC) for averting fractures, particularly during aromatase inhibitor (AI) therapy. Recently, a number of studies on additional fracture related risk factors, new treatment options as well as real world studies demonstrating a much higher fracture rate than suggested by randomized clinical controlled trials (RCTs). Therefore, this updated algorithm was developed to better assess fracture risk and direct treatment as a position statement of several interdisciplinary cancer and bone societies involved in the management of AI-associated bone loss (AIBL)...
June 2017: Journal of Bone Oncology
https://www.readbyqxmd.com/read/28412323/single-cpg-site-methylation-controls-estrogen-receptor-gene-transcription-and-correlates-with-hormone-therapy-resistance
#11
Kouki Tsuboi, Takamasa Nagatomo, Tatsuyuki Gohno, Toru Higuchi, Shunta Sasaki, Natsu Fujiki, Masafumi Kurosumi, Hiroyuki Takei, Yuri Yamaguchi, Toshifumi Niwa, Shin-Ichi Hayashi
Hormone therapy is the most effective treatment for patients with estrogen receptor α-positive breast cancers. However, although resistance occurs during treatment in some cases and often reflects changed estrogen receptor α status, the relationship between changes in estrogen receptor α expression and resistance to therapy are poorly understood. In this study, we identified a mechanism for altered estrogen receptor α expression during disease progression and acquired hormone therapy resistance in aromatase inhibitor-resistant breast cancer cell lines...
April 12, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28411130/ifitm1-suppression-blocks-proliferation-and-invasion-of-aromatase-inhibitor-resistant-breast-cancer-in%C3%A2-vivo-by-jak-stat-mediated-induction-of-p21
#12
Asona J Lui, Eric S Geanes, Joshua Ogony, Fariba Behbod, Jordan Marquess, Kelli Valdez, William Jewell, Ossama Tawfik, Joan Lewis-Wambi
Interferon induced transmembrane protein 1 (IFITM1) belongs to a family of interferon stimulated genes (ISGs) that is associated with tumor progression and DNA damage resistance, however, its role in endocrine resistance is not known. Here, we correlate IFITM1 expression with clinical stage and poor response to endocrine therapy in a tissue microarray consisting of 94 estrogen receptor (ER)-positive breast tumors. IFITM1 overexpression is confirmed in the AI-resistant MCF-7:5C cell line and not found in AI-sensitive MCF-7 cells...
April 12, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28407578/a-peek-into-the-drug-development-scenario-of-endometriosis-a-systematic-review
#13
REVIEW
Luxitaa Goenka, Melvin George, Maitrayee Sen
PURPOSE AND OBJECTIVE: Endometriosis is a gynaecological disease that is characterised by the presence of endometrium like tissue-epithelium and stroma that develops outside the uterine cavity, which is responsible for pelvic pain and infertility. Even though several medical therapies exist for the treatment of endometriosis, each of the drug class has its own limitations such as cost of treatment, side-effects and its short-term effect on the symptoms of endometriosis. In this review, we have attempted to summarize the current status and challenges of drug development for endometriosis...
April 10, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28404691/exemestane-and-its-active-metabolite-17-hydroexemestane-induce-udp-glucuronosyltransferase-ugt-2b17-expression-in-breast-cancer-cells
#14
Apichaya Chanawong, Peter Ian Mackenzie, Ross A McKinnon, Dong Gui Hu, Robyn Meech
Exemestane (EXE) is an aromatase inhibitor indicated for endocrine therapy of breast cancer in post-menopausal women. The primary active metabolite of EXE, 17-hydroexemestane (17-HE), is inactivated via glucuronidation, mainly by UGT2B17. UGT2B17 also has a primary role in inactivation of endogenous androgens testosterone and dihydrotestosterone (DHT) and may play an important role in regulation of breast and prostate tumour intracrinology. We recently reported that UGT2B17 could be induced by both estrogenic and androgenic ligands in breast cancer cells via binding of the estrogen receptor alpha (ERα) or the androgen receptor (AR) to a complex regulatory unit in the proximal UGT2B17 promoter...
April 12, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28403774/pharmacogenetics-of-aromatase-inhibitors-in-endocrine-responsive-breast-cancer-lessons-learnt-from-tamoxifen-and-cyp2d6-genotyping
#15
Karin Jeanne Baatjes, Magda Conradie, Justus Paul Apffelstaedt, Maritha Kotze
BACKGROUND: Genetics play a significant role in drug metabolism of endocrine therapy of breast cancer. These aspects have been studied extensively in patients on tamoxifen, but the pharmacogenetics of aromatase inhibitors are less established. In contrast to the protective effect of tamoxifen, aromatase inhibitors are linked with an increased risk for bone loss and fractures. OBJECTIVE: This review outlines key issues around implementation of pharmacogenetics of cytochrome P450 and tamoxifen as a model for optimal use of aromatase inhibitors in postmenopausal women with estrogen receptor positive breast cancer...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28400999/mtor-function-and-therapeutic-targeting-in-breast-cancer
#16
REVIEW
Stephen H Hare, Amanda J Harvey
The mTOR pathway was discovered in the late 1970s after the compound and natural inhibitor of mTOR, rapamycin was isolated from the bacterium Streptomyces hygroscopicus. mTOR is serine/threonine kinase belonging to the phosphoinositide 3-kinase related kinase (PIKK) family. It forms two distinct complexes; mTORC1 and mTORC2. mTORC1 has a key role in regulating protein synthesis and autophagy whilst mTORC2 is involved in regulating kinases of the AGC family. mTOR signaling is often over active in multiple cancer types including breast cancer...
2017: American Journal of Cancer Research
https://www.readbyqxmd.com/read/28398491/pregnancy-and-neonatal-outcomes-following-letrozole-use-in-frozen-thawed-single-embryo-transfer-cycles
#17
T Tatsumi, S C Jwa, A Kuwahara, M Irahara, T Kubota, H Saito
STUDY QUESTION: Are pregnancy and neonatal outcomes following letrozole use comparable with natural and HRT cycles in patients undergoing single frozen-thawed embryo transfer (FET)? SUMMARY ANSWER: Letrozole use was significantly associated with higher rates of clinical pregnancy, clinical pregnancy with fetal heart beat and live birth, and with a lower rate of miscarriage, compared with natural and HRT cycles. WHAT IS KNOWN ALREADY: Letrozole is the most commonly used aromatase inhibitor for mild ovarian stimulation in ART...
April 7, 2017: Human Reproduction
https://www.readbyqxmd.com/read/28396978/a-novel-strategy-to-co-target-estrogen-receptor-and-nuclear-factor-%C3%AE%C2%BAb-pathways-with-hybrid-drugs-for-breast-cancer-therapy
#18
Irida Kastrati, Marton I Siklos, Svitlana D Brovkovych, Gregory R J Thatcher, Jonna Frasor
Nearly 75% of breast tumors express estrogen receptor (ER), and will be treated with endocrine therapy, such as selective estrogen receptor modulator (SERM), tamoxifen, or aromatase inhibitors. Despite their proven success, as many as 40-50% of ER+ tumors fail to respond to endocrine therapy and eventually recur as aggressive, metastatic cancers. Therefore, preventing and/or overcoming endocrine resistance in ER+ tumors remains a major clinical challenge. Deregulation or activation of the nuclear factor κB (NFκB) pathway has been implicated in endocrine resistance and poor patient outcome in ER+ tumors...
April 10, 2017: Hormones & Cancer
https://www.readbyqxmd.com/read/28396197/anti-tumor-efficacy-of-new-7%C3%AE-substituted-androstanes-as-aromatase-inhibitors-in-hormone-sensitive-and-resistant-breast-cancer-cells
#19
Cristina Amaral, Carla L Varela, João Maurício, Ana Filipa Sobral, Saul C Costa, Fernanda M F Roleira, Elisiário J Tavares-da-Silva, Georgina Correia-da-Silva, Natércia Teixeira
The majority of breast cancer cases are estrogen receptor positive (ER(+)). Although, third-generation aromatase inhibitors (AIs) are used as first-line treatment in post-menopausal women, they cause endocrine resistance and bone loss, which limits their success. Therefore, there is a demand to discover new potent molecules, with less toxicity that can circumvent these drawbacks. Our group has previously demonstrated that new 7α-substituted steroidal molecules, 7α-(2ξ,3ξ-epoxypropyl)androsta-1,4-diene-3,17-dione (3), 7α-allylandrost-4-ene-3,17-dione (6), 7α-allylandrost-4-en-17-one (9), 7α-allyl-3-oxoandrosta-1,4-dien-17β-ol (10) and 7α-allylandrosta-1,4-diene-3,17-dione (12) are potent AIs in placental microsomes...
April 7, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28393092/hormonal-based-treatment-of-ovarian-anaplastic-ependymoma-with-anastrozole
#20
Justin Wayne Gorski, Jolyn Sharpe Taylor, Jing Zhang, Jinsong Liu, Amir Anthony Jazaeri
OBJECTIVE: Ovarian anaplastic ependymoma is a rare gynecologic malignancy that poses diagnostic and treatment challenges. Treatment of sub-optimally debulked disease usually portends poor prognosis. Molecular testing of tumor specimen can identify more specific targets for additional therapy such as estrogen and progesterone receptors (ER/PR). CASE: A 29-year-old woman presented with incidental finding of large bilateral adnexal masses and elevated CA 125. Biopsy proved anaplastic ovarian ependymoma with high ER/PR expression...
May 2017: Gynecologic Oncology Reports
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