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https://www.readbyqxmd.com/read/29164917/efficacy-and-safety-of-palbociclib-in-heavily-pretreated-patients-with-hr-her2-%C3%A2-metastatic-breast-cancer
#1
Marija Ban, Branka Petrić Miše, Ana Majić, Ivanka Dražić, Eduard Vrdoljak
AIM: CDK4/6 inhibitors in the first and second treatment line in patients with HR+/HER2- metastatic breast cancer (mBC) in combination with hormonal therapy improve progression free survival. Role of CDK4/6 inhibitors in further treatment lines remains unclear. METHODS: Retrospective analysis of 24 HR+/HER2- heavily pretreated mBC patients is presented. RESULTS: A total of 58.3% patients achieved stable disease. No objective response was observed...
November 22, 2017: Future Oncology
https://www.readbyqxmd.com/read/29164377/systemic-and-local-effects-of-vaginal-dehydroepiandrosterone-dhea-ncctg-n10c1-alliance
#2
Debra L Barton, Lynne T Shuster, Travis Dockter, Pamela J Atherton, Jacqueline Thielen, Stephen N Birrell, Richa Sood, Patricia Griffin, Shelby A Terstriep, Bassam Mattar, Jacqueline M Lafky, Charles L Loprinzi
BACKGROUND: Dehydroepiandrosterone (DHEA) is helpful for treating vaginal symptoms. This secondary analysis evaluated the impact of vaginal DHEA on hormone concentrations, bone turnover, and vaginal cytology in women with a cancer history. METHODS: Postmenopausal women, diagnosed with breast or gynecologic cancer, were eligible if they reported at least moderate vaginal symptoms. Participants could be on tamoxifen or aromatase inhibitors (AIs). Women were randomized to 3...
November 21, 2017: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/29163055/study-of-sex-differences-in-duloxetine-efficacy-for-depression-in-transgenic-mouse-models
#3
Yong Xu, Lei Ma, Wei Jiang, Yuhong Li, Gang Wang, Rena Li
Clinical evidences show sex differences in risk of developing depressive disorders as well as effect of antidepressants in depression treatment. However, whether such a sex-dependent risk of depression and efficacy of antidepressants is dependent on endogenous estrogen level remain elusive. The aim of this study is to explore the molecular mechanisms of sex differences in antidepressant duloxetine. In the present study, we used genetic knockout or overexpression estrogen-synthesizing enzyme aromatase (Ar) gene as models for endogenous estrogen deficiency and elevation endogenous estrogen, respectively, to examine the anti-depressive efficacy of duloxetine in males and females by force swimming test (FST)...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/29160820/ergostane-type-sterols-from-king-trumpet-mushroom-pleurotus-eryngii-and-their-inhibitory-effects-on-aromatase
#4
Takashi Kikuchi, Naoki Motoyashiki, Takeshi Yamada, Kanae Shibatani, Kiyofumi Ninomiya, Toshio Morikawa, Reiko Tanaka
Two new ergostane-type sterols; (22E)-5α,6α-epoxyergosta-8,14,22-triene-3β,7β-diol (1) and 5α,6α-epoxyergost-8(14)-ene-3β,7α-diol (2) were isolated from the fruiting bodies of king trumpet mushroom (Pleurotus eryngii), along with eight known compounds (3-10). All isolated compounds were evaluated for their inhibitory effects on aromatase. Among them, 4 and 6 exhibited comparable aromatase inhibitory activities to aminoglutethimide.
November 21, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29158011/extended-adjuvant-intermittent-letrozole-versus-continuous-letrozole-in-postmenopausal-women-with-breast-cancer-sole-a-multicentre-open-label-randomised-phase-3-trial
#5
Marco Colleoni, Weixiu Luo, Per Karlsson, Jacquie Chirgwin, Stefan Aebi, Guy Jerusalem, Patrick Neven, Erika Hitre, Marie-Pascale Graas, Edda Simoncini, Claus Kamby, Alastair Thompson, Sibylle Loibl, Joaquín Gavilá, Katsumasa Kuroi, Christian Marth, Bettina Müller, Seamus O'Reilly, Vincenzo Di Lauro, Andrea Gombos, Thomas Ruhstaller, Harold Burstein, Karin Ribi, Jürg Bernhard, Giuseppe Viale, Rudolf Maibach, Manuela Rabaglio-Poretti, Richard D Gelber, Alan S Coates, Angelo Di Leo, Meredith M Regan, Aron Goldhirsch
BACKGROUND: In animal models of breast cancer, resistance to continuous use of letrozole can be reversed by withdrawal and reintroduction of letrozole. We therefore hypothesised that extended intermittent use of adjuvant letrozole would improve breast cancer outcome compared with continuous use of letrozole in postmenopausal women. METHODS: We did the multicentre, open-label, randomised, parallel, phase 3 SOLE trial in 240 centres (academic, primary, secondary, and tertiary care centres) in 22 countries...
November 17, 2017: Lancet Oncology
https://www.readbyqxmd.com/read/29157627/letrozole-may-be-a-valuable-maintenance-treatment-in-high-grade-serous-ovarian-cancer-patients
#6
V Heinzelmann-Schwarz, A Knipprath Mészaros, S Stadlmann, F Jacob, A Schoetzau, K Russell, M Friedlander, G Singer, M Vetter
OBJECTIVES: Endocrine therapy is used as maintenance in estrogen receptor (ER) positive breast cancers and has been proposed in low-grade serous ovarian cancers (LGSOC). Here we examine a rationale for its use as maintenance in high-grade serous ovarian cancers (HGSOC). METHODS: We accessed the TCGA PANCAN dataset to evaluate the expression of ESR1. ESR1 expression data on all cancers (n=8901) and HGSOC (n=527) were followed by investigation of ER expression via immunohistochemistry (IHC) (n=4071)...
November 17, 2017: Gynecologic Oncology
https://www.readbyqxmd.com/read/29155450/risk-of-ovarian-function-recovery-should-be-considered-when-switching-from-treatment-with-adjuvant-tamoxifen-to-aromatase-inhibitor-therapy-in-women-with-chemotherapy-induced-amenorrhea
#7
https://www.readbyqxmd.com/read/29154779/letrozole-pre-treatment-prior-to-medical-termination-of-pregnancy-a-systematic-review
#8
Christopher M Nash, Lauren Philp, Prakesh Shah, Kellie E Murphy
OBJECTIVE(S): The purpose of this systematic review was to evaluate the efficacy of pretreatment with letrozole prior to either a first or second trimester medical termination of pregnancy. STUDY DESIGN: We searched letrozole, femara, aromatase inhibitors, abortifacient agents, termination of pregnancy, and labour induction in MEDLINE, EMBASE, Cochrane Database, Google Scholar, and PubMed from inception of each database until September 2015 with no language limitation...
November 14, 2017: Contraception
https://www.readbyqxmd.com/read/29153737/structure-activity-relationships-and-docking-studies-of-synthetic-2-arylindole-derivatives-determined-with-aromatase-and-quinone-reductase-1
#9
Allan M Prior, Xufen Yu, Eun-Jung Park, Tamara P Kondratyuk, Yan Lin, John M Pezzuto, Dianqing Sun
In our ongoing effort of discovering anticancer and chemopreventive agents, a series of 2-arylindole derivatives were synthesized and evaluated toward aromatase and quinone reductase 1 (QR1). Biological evaluation revealed that several compounds (e.g., 2d, IC50 = 1.61 μM; 21, IC50 = 3.05 μM; and 27, IC50 = 3.34 μM) showed aromatase inhibitory activity with half maximal inhibitory concentration (IC50) values in the low micromolar concentrations. With regard to the QR1 induction activity, 11 exhibited the highest QR1 induction ratio (IR) with a low concentration to double activity (CD) value (IR = 8...
November 6, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29151792/fluoxetine-modulates-sex-steroid-levels-in-vitro
#10
Diana Lupu, Marcus O D Sjödin, Mukesh Varshney, Johan Lindberg, Felicia Loghin, Joëlle Rüegg
Background and aims: Selective serotonin reuptake inhibitors (SSRIs) are antidepressants increasingly prescribed against depression during and after pregnancy. However, these compounds cross the placenta and are found in breast milk, thus reaching, and possibly affecting, the fetus and infant during critical developmental stages. Fluoxetine (FLX), a widely used SSRI, can interfere with estrogen signaling, which is important for the development of female sex organs and certain brain areas, among others...
2017: Clujul Medical (1957)
https://www.readbyqxmd.com/read/29148520/an-in-vitro-prototype-of-a-porcine-biomimetic-testis-like-cell-culture-system-a-novel-tool-for-the-study-of-reassembled-sertoli-and-leydig-cells
#11
Iva Arato, Giovanni Luca, Francesca Mancuso, Catia Bellucci, Cinzia Lilli, Mario Calvitti, Barbara C Hansen, Domenico Milardi, Giuseppe Grande, Riccardo Calafiore
At present, there is no reliable in vitro assembled prepubertal testis-like biomimetic organ culture system designed to assess the functional effects of human gonadotropins on Sertoli and Leydig cells. Spermatogenesis is regulated by endocrine, paracrine, and juxtacrine factors (testicular cross-talk), mainly orchestrated by gonadotropins such as luteinizing hormone (LH) and follicle-stimulating hormone (FSH) that play a pivotal role by stimulating Leydig and Sertoli cells, respectively. The aim of our study was to set up an in vitro prepubertal porcine bioengineered construct as a new model for experimental studies on reassembled Sertoli and Leydig cells...
November 10, 2017: Asian Journal of Andrology
https://www.readbyqxmd.com/read/29144249/effect-of-antiandrogen-aromatase-inhibitor-and-gonadotropin-releasing-hormone-analog-on-adult-height-in-familial-male-precocious-puberty
#12
Ellen Werber Leschek, Armando C Flor, Joy C Bryant, Janet V Jones, Kevin M Barnes, Gordon B Cutler
OBJECTIVE: Antiandrogen, aromatase inhibitor, and gonadotropin-releasing hormone analog (GnRHa) treatment normalizes growth rate and bone maturation and increases predicted adult height (AH) in boys with familial male-limited precocious puberty (FMPP). To evaluate the effect of long-term antiandrogen, aromatase inhibitor, and GnRHa on AH, boys with FMPP who were treated were followed to AH. STUDY DESIGN: Twenty-eight boys with FMPP, referred to the National Institutes of Health, were started on antiandrogen and aromatase inhibitor at 4...
November 2017: Journal of Pediatrics
https://www.readbyqxmd.com/read/29141657/local-estrogen-axis-in-the-human-bone-microenvironment-regulates-estrogen%C3%A2-receptor-positive%C3%A2-breast-cancer-cells
#13
Derek F Amanatullah, John S Tamaresis, Pauline Chu, Michael H Bachmann, Nhat M Hoang, Deborah Collyar, Aaron T Mayer, Robert B West, William J Maloney, Christopher H Contag, Bonnie L King
BACKGROUND: Approximately 70% of all breast cancers express the estrogen receptor, and are regulated by estrogen. While the ovaries are the primary source of estrogen in premenopausal women, most breast cancer is diagnosed following menopause, when systemic levels of this hormone decline. Estrogen production from androgen precursors is catalyzed by the aromatase enzyme. Although aromatase expression and local estrogen production in breast adipose tissue have been implicated in the development of primary breast cancer, the source of estrogen involved in the regulation of estrogen receptor-positive (ER+) metastatic breast cancer progression is less clear...
November 15, 2017: Breast Cancer Research: BCR
https://www.readbyqxmd.com/read/29137864/synthesis-molecular-docking-and-qsar-study-of-sulfonamide-based-indoles-as-aromatase-inhibitors
#14
Ratchanok Pingaew, Prasit Mandi, Veda Prachayasittikul, Supaluk Prachayasittikul, Somsak Ruchirawat, Virapong Prachayasittikul
Thirty four of indoles bearing sulfonamides (11-44) were synthesized and evaluated for their anti-aromatase activities. Interestingly, all indole derivatives inhibited the aromatase with IC50 range of 0.7-15.3 μM. Indoles (27-36) exerted higher aromatase inhibitory activity than that of ketoconazole. The phenoxy analogs 28 and 34 with methoxy group were shown to be the most potent compounds with sub-micromolar IC50 values (i.e., 0.7 and 0.8 μM, respectively) without affecting to the normal cell line. Molecular docking demonstrated that the indoles 28, 30 and 34 could occupy the same binding site on the aromatase pocket and share several binding residues with those of the natural substrate (androstenedione), which suggested the competitive binding could be the mode of inhibition of the compounds...
October 20, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29137842/comparison-of-pharmacokinetics-of-newly-discovered-aromatase-inhibitors-by-a-cassette-microdosing-approach-in-healthy-japanese-subjects
#15
Hiroyuki Kusuhara, Tadayuki Takashima, Hisako Fujii, Tsutomu Takashima, Masaaki Tanaka, Akira Ishii, Shusaku Tazawa, Kazuhiro Takahashi, Kayo Takahashi, Hidekichi Tokai, Tsuneo Yano, Makoto Kataoka, Akihiro Inano, Suguru Yoshida, Takamitsu Hosoya, Yuichi Sugiyama, Shinji Yamashita, Taisuke Hojo, Yasuyoshi Watanabe
The aim of the present study is to investigate the pharmacokinetics of our newly developed aromatase inhibitors (cetrozole and TMD-322) in healthy subjects by a cassette microdose strategy. A cocktail of cetrozole and TMD-322 was administered intravenously or orally (1.98 μg for each drug) to six healthy volunteers in a crossover fashion. Anastrozole (1.98 μg) was also included in the oral cocktail. Total body clearance and bioavailability were 12.1 ± 7.1 mL/min/kg and 34.9 ± 32.3% for cetrozole, and 16...
September 21, 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29137418/a-randomized-phase-ii-study-of-aromatase-inhibitors-plus-metformin-in-pre-treated-postmenopausal-patients-with-hormone-receptor-positive-metastatic-breast-cancer
#16
Yannan Zhao, Chengcheng Gong, Zhonghua Wang, Jian Zhang, Leiping Wang, Sheng Zhang, Jun Cao, Zhonghua Tao, Ting Li, Biyun Wang, Xichun Hu
Background: Everolimus significantly improves progression-free survival (PFS) and has been approved to use in aromatase inhibitor pretreated patients with hormone receptor positive advanced breast cancer. Metformin has been shown to inhibit mTOR pathway, with more favorable safety profile, leading to this hypothesis-generating trial to assess whether metformin enhances the efficacy of aromatase inhibitors. Methods: 60 postmenopausal women with hormone receptor positive locally advanced or metastatic breast cancer were randomly assigned 1:1 to aromatase inhibitor (exemestane 25mg/d or letrozole 2...
October 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/29136387/randomized-multicenter-placebo-controlled-clinical-trial-of-duloxetine-versus-placebo-for-aromatase-inhibitor-associated-arthralgias-in-early-stage-breast-cancer-swog-s1202
#17
N Lynn Henry, Joseph M Unger, Anne F Schott, Louis Fehrenbacher, Patrick J Flynn, Debra M Prow, Carl W Sharer, Gary V Burton, Charles S Kuzma, Anna Moseley, Danika L Lew, Michael J Fisch, Carol M Moinpour, Dawn L Hershman, James L Wade
Purpose Adherence to aromatase inhibitor (AI) therapy for early-stage breast cancer is limited by AI-associated musculoskeletal symptoms (AIMSS). Duloxetine is US Food and Drug Administration approved for treatment of multiple chronic pain disorders. We hypothesized that treatment of AIMSS with duloxetine would improve average joint pain compared with placebo. Methods This randomized, double-blind, phase III trial included AI-treated postmenopausal women with early-stage breast cancer and who had average joint pain score of ≥ 4 out of 10 that developed or worsened since AI therapy initiation...
November 14, 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/29135127/is-switching-to-tamoxifen-the-only-choice-of-treatment-for-improving-aromatase-inhibitor-toxicity
#18
Kadri Altundag
No abstract text is available yet for this article.
September 2017: Journal of B.U.ON.: Official Journal of the Balkan Union of Oncology
https://www.readbyqxmd.com/read/29134635/ribociclib-bioavailability-is-not-affected-by-gastric-ph-changes-or-food-intake-in-silico-and-clinical-evaluations
#19
Tanay S Samant, Shyeilla Dhuria, Yasong Lu, Marc Laisney, Shu Yang, Arnaud Grandeury, Martin Mueller-Zsigmondy, Kenichi Umehara, Felix Huth, Michelle Miller, Caroline Germa, Mohamed Elmeliegy
Ribociclib (KISQALI®), a cyclin-dependent kinase 4/6 inhibitor approved for the first-line treatment of HR+/HER2- advanced breast cancer with an aromatase inhibitor, is administered with no restrictions on concomitant gastric pH-elevating agents or food intake. The influence of proton pump inhibitors (PPIs) on ribociclib bioavailability was assessed using (1) biorelevant media solubility, (2) physiologically based pharmacokinetic (PBPK) modeling, (3) non-compartmental analysis (NCA) of clinical trial data, and (4) population PK (PopPK) analysis...
November 14, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29132837/prepubertal-chrysin-exposure-upregulates-either-ar-in-male-ventral-prostate-or-ar-and-er%C3%AE-in-skene-s-paraurethral-gland-of-pubertal-and-adult-gerbils
#20
Naiara C S Ribeiro, Mônica S Campos, Mariana B Santos, Gabriela M Ayusso, Patrícia S L Vilamaior, Luis O Regasini, Sebastião R Taboga, Manoel F Biancardi, Ana P S Perez, Fernanda C A Santos
Chrysin is a plant-derived polyphenol that has the potential to increase endogenous testosterone levels both by inhibiting the aromatase enzyme and by stimulating testicular steroidogenesis. The effects of chrysin on the prostate are unknown, especially during its development and functional maturation. Thus, the aim of this study was to evaluate the effects of chrysin prepubertal exposure on the male and female prostates of both pubertal and adult gerbils. To evaluate the possible androgenic responses of chrysin, gerbils were also exposed to testosterone...
November 10, 2017: Fitoterapia
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