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Paola Rogliani, Josuel Ora, Maria Gabriella Matera, Mario Cazzola, Luigino Calzetta
Introduction Long-acting β2 -adrenoceptor (β2 -AR) agonists (LABAs) plus long-acting muscarinic antagonists (LAMAs) is the cornerstone for treating chronic obstructive pulmonary disease (COPD). LABA/LAMA combinations elicit clinical and functional synergistic interaction, and such an interaction should permit to reduce the dose of each monocomponent in the drug mixture to minimize the risk of adverse events (AEs). Overall, currently available LABA/LAMA fixed-dose combinations (FDCs) combine the drugs at the same doses of formulations designed for a single drug...
May 1, 2018: Expert Opinion on Drug Safety
Keith Morrison, Franck Haag, Roland Ernst, Marc Iglarz, Martine Clozel
Selexipag is a selective non-prostanoid prostacyclin (PGI2 ) receptor (IP receptor) agonist that is approved for the treatment of pulmonary arterial hypertension (PAH). In contrast to selexipag, PGI2 analogs used in the clinic are non-selective agonists at prostanoid receptors and can also activate contractile EP3 receptors. Leg pain is a common side effect in patients receiving treatment with PGI2 analogs and peripheral vasoconstriction can be responsible for side effects related to muscular ischemia. This study tested the hypothesis that PGI2 analogs could cause paradoxical vasoconstriction of the femoral artery via EP3 receptor activation but that only vasorelaxation would be observed in response to selexipag and its active metabolite ACT-333679...
March 27, 2018: Journal of Pharmacology and Experimental Therapeutics
Barbara M A van Vugt-Lussenburg, Rosan B van der Lee, Hai-Yen Man, Irene Middelhof, Abraham Brouwer, Harrie Besselink, Bart van der Burg
Identification and monitoring of so-called endocrine-disrupting compounds has received ample attention; both the OECD and the United States Environmental Protection Agency (US EPA) have designed tiered testing approaches, involving in vitro bioassays to prioritize and partly replace traditional animal experiments. Since the estrogen (ER) and androgen (AR) receptor are frequent targets of endocrine disrupting chemicals, bioassays detecting interaction with these receptors have a high potential to be of use in risk assessment of endocrine active compounds...
January 2018: Reproductive Toxicology
Steven L Rains, Clarissa N Amaya, Brad A Bryan
Based largely on retrospective analyses and a handful of prospective case reports, pharmacological inhibition of the beta adrenergic receptors using beta blockers has shown clinical anti-cancer efficacy in reproductive cancers, as well as angiosarcoma and multiple myeloma. Because of the potential promise of beta blockers as an adjunct to standard anti-cancer therapy, it is imperative to identify other tumor types expressing beta adrenergic (β-AR) receptors so future preclinical and clinical studies can be directed at the most promising tumor targets...
July 2017: Oncoscience
Mariana Di Lorenzo, Maurizio Forte, Salvatore Valiante, Vincenza Laforgia, Maria De Falco
Dibutylphthalate (DBP) is an environmental pollutant widely used as plasticizer in a variety of industrial applications worldwide. This agent can be found in personal-care products, children's toy, pharmaceuticals, food products. Exposure to DBP can occur via ingestion and inhalation as well as intravenous or skin contact. DBP belongs to the family of endocrine disrupting chemicals (EDCs) and its effects on reproductive system were demonstrated both in vivo and in vitro. In the present study we evaluated the effects of DBP on human prostate adenocarcinoma epithelial cells (LNCaP) in order to highlight xenoestrogens influence on human prostate...
January 2018: Ecotoxicology and Environmental Safety
Willemijne A M E Schrijver, Karianne Schuurman, Annelot van Rossum, Ton Peeters, Natalie Ter Hoeve, Wilbert Zwart, Paul J van Diest, Cathy B Moelans
Discordance in estrogen receptor alpha (ERα), progesterone receptor (PR), androgen receptor (AR) and human epidermal growth factor receptor 2 (HER2) status between primary breast cancers and solid distant metastases ("conversion") has been reported previously. Even though metastatic spread to the peritoneal and pleural cavities occurs frequently and is associated with high mortality, the rate of receptor conversion and the prognostic implications thereof remain elusive. We therefore determined receptor conversion in 91 effusion metastases (78 pleural, 13 peritoneal effusions) of 69 patients by immunohistochemistry (IHC) and in situ hybridization...
August 15, 2017: Oncotarget
Andrea M Steely, Jamin A Willoughby, Shyam N Sundar, Vasiliki I Aivaliotis, Gary L Firestone
Androgen receptor (AR) expression and activity is highly linked to the development and progression of prostate cancer and is a target of therapeutic strategies for this disease. We investigated whether the antimalarial drug artemisinin, which is a sesquiterpene lactone isolated from the sweet wormwood plant Artemisia annua, could alter AR expression and responsiveness in cultured human prostate cancer cell lines. Artemisinin treatment induced the 26S proteasome-mediated degradation of the receptor protein, without altering AR transcript levels, in androgen-responsive LNCaP prostate cancer cells or PC-3 prostate cancer cells expressing exogenous wild-type AR...
October 2017: Anti-cancer Drugs
Kamil Zaręba, Iwona Sidorkiewicz
In this brief review we present an outline of the current state of research on examples of hyperandrogenism that can be strongly associated with diverse modifications in the androgen signaling pathway. We discuss the most prominent clinical features of androgen excess and correlate them with studies on androgen receptor (AR) alterations. For the first time we summarize the confirmed localizations of all known AR receptors in women. The knowledge of ARs may be the basis for AR-targeted therapies of androgenic disorders in women, including malignancy, as it has recently been demonstrated for triple-negative breast cancer...
2017: Developmental Period Medicine
Maciej Równiak
The generation of emotional responses by the amygdala is determined largely by the balance of excitatory and inhibitory inputs to its principal neurons. These responses are often sex-specific, and any imbalance in excitatory and/or inhibitory tones leads to serious psychiatric disorders which occur with different rates in men versus women. To investigate the neural basis of sex-specific processing in the amygdala, relationships between the neurons expressing calbindin (CB), parvalbumin (PV) and calretinin (CR), which form in the amygdala main subsets of γ-aminobutyric acid (GABA)-ergic inhibitory system, and neurons endowed with oestrogen alpha (ERα), oestrogen beta (ERβ) or androgen (AR) receptors were analysed using double immunohistochemistry in male and female guinea pig subjects...
November 2017: Brain Structure & Function
Susanne Grässel, Dominique Muschter
The importance of the nociceptive nervous system for maintaining tissue homeostasis has been known for some time, and it has also been suggested that organogenesis and tissue repair are under neuronal control. Changes in peripheral joint innervation are supposed to be partly responsible for degenerative alterations in joint tissues which contribute to development of osteoarthritis. Various resident cell types of the musculoskeletal system express receptors for sensory and sympathetic neurotransmitters, allowing response to peripheral neuronal stimuli...
April 28, 2017: International Journal of Molecular Sciences
Willemijne A M E Schrijver, Karianne Schuurman, Annelot van Rossum, Ton Peeters, Natalie Ter Hoeve, Wilbert Zwart, Paul J van Diest, Cathy B Moelans
Discordance in estrogen receptor alpha (ERα), progesterone receptor (PR), androgen receptor (AR) and human epidermal growth factor receptor 2 (HER2) status between primary breast cancers and solid distant metastases ("conversion") has been reported previously. Even though metastatic spread to the peritoneal and pleural cavities occurs frequently and is associated with high mortality, the rate of receptor conversion and the prognostic implications thereof remain elusive.We therefore determined receptor conversion in 91 effusion metastases (78 pleural, 13 peritoneal effusions) of 69 patients by immunohistochemistry (IHC) and in situ hybridization...
February 20, 2017: Oncotarget
Kyu-Pyo Kim, Robert A Parise, Julianne L Holleran, Lionel D Lewis, Leonard Appleman, Nielka van Erp, Michael J Morris, Jan H Beumer
Inhibiting the androgen receptor (AR) pathway is an important clinical strategy in metastatic prostate cancer. Novel agents including abiraterone acetate and enzalutamide have been shown to prolong life in men with metastatic, castration-resistant prostate cancer (mCRPC). To evaluate the pharmacokinetics of AR-targeted agents, we developed and validated an LC-MS/MS assay for the quantitation of enzalutamide, N-desmethyl enzalutamide, abiraterone and bicalutamide in 0.05mL human plasma. After protein precipitation, chromatographic separation was achieved with a Phenomenex Synergi Polar-RP column and a linear gradient of 0...
May 10, 2017: Journal of Pharmaceutical and Biomedical Analysis
Ozge Berrak, Elif Damla Arisan, Pinar Obakan-Yerlikaya, Ajda Coker-Gürkan, Narçin Palavan-Unsal
Purvalanol and roscovitine are cyclin dependent kinase (CDK) inhibitors that induce cell cycle arrest and apoptosis in various cancer cells. We further hypothesized that co-treatment of CDK inhibitors with rapamycin, an mTOR inhibitor, would be an effective combinatory strategy for the inhibition of prostate cancer regard to androgen receptor (AR) status due to inhibition of proliferative pathway, PI3K/AKT/mTOR, and induction of cell death mechanisms. Androgen responsive (AR+), PTEN(-/-) LNCaP and androgen independent (AR-), PTEN(+/-) DU145 prostate cancer cells were exposed to purvalanol (20 µM) and roscovitine (30 µM) with or without rapamycin for 24 h...
October 2016: Apoptosis: An International Journal on Programmed Cell Death
L Ekenros, Z Papoutsi, C Fridén, K Dahlman Wright, A Lindén Hirschberg
AIM: Variations in sex hormone levels during the menstrual cycle may affect neuromuscular performance and the risk of sustaining musculoskeletal injury in women. The aim of this study was to investigate mRNA and protein levels for sex steroid hormone receptors in skeletal muscle in three distinct phases of the menstrual cycle. METHODS: Fifteen, healthy women with regular menstrual cycles participated in the study. Muscle biopsies from the vastus lateralis were obtained in three hormonally verified phases of the menstrual cycle for each individual, that is the follicular phase, the ovulatory phase and the luteal phase...
February 2017: Acta Physiologica
M Paola Castelli, Saturnino Spiga, Andrea Perra, Camilla Madeddu, Giovanna Mulas, M Grazia Ennas, Gian Luigi Gessa
α2 adrenoreceptors (α2-ARs) play a key role in the control of noradrenaline and dopamine release in the medial prefrontal cortex (mPFC). Here, using UV-laser microdissection-based quantitative mRNA expression in individual neurons we show that in hTH-GFP rats, a transgenic line exhibiting intense and specific fluorescence in dopaminergic (DA) neurons, α2A adrenoreceptor (α2A-AR) mRNA is expressed at high and low levels in DA cells in the ventral tegmental area (VTA) and substantia nigra compacta (SNc), respectively...
September 22, 2016: Neuroscience
He-Sheng Jiang, Xia-Ying Kuang, Wei-Li Sun, Yan Xu, Yi-Zi Zheng, Yi-Rong Liu, Guan-Tian Lang, Feng Qiao, Xin Hu, Zhi-Ming Shao
In this study we sought to correlate androgen receptor (AR) expression with tumor progression and disease-free survival (DFS) in breast cancer patients. We investigated AR expression in 450 breast cancer patients. We found that breast cancers expressing the estrogen receptor (ER) are more likely to co-express AR compared to ER-negative cancers (56.0% versus 28.1%, P < 0.001). In addition, we found that AR expression is correlated with increased DFS in patients with luminal breast cancer (P < 0.001), and decreased DFS in TNBC (triple negative breast cancer, P = 0...
July 5, 2016: Oncotarget
Miguel Henriques Abreu, Noémia Afonso, Pedro Henriques Abreu, Francisco Menezes, Paula Lopes, Rui Henrique, Deolinda Pereira, Carlos Lopes
PURPOSE: Male Breast Cancer (MBC) remains a poor understood disease. Prognostic factors are not well established and specific prognostic subgroups are warranted. PATIENTS/METHODS: Retrospectively revision of 111 cases treated in the same Cancer Center. Blinded-central pathological revision with immunohistochemical (IHQ) analysis for estrogen (ER), progesterone (PR) and androgen (AR) receptors, HER2, ki67 and p53 was done. Cox regression model was used for uni/multivariate survival analysis...
April 2016: Breast: Official Journal of the European Society of Mastology
Katsuhiko Yoshizawa, Michiko Yuki, Yuichi Kinoshita, Yuko Emoto, Takashi Yuri, Nobuaki Shikata, Susan A Elmore, Airo Tsubura
The frequency of breast cancer in men is extremely rare, reported to be less than 1% and there is currently no available animal model for male mammary tumors. We compared the characteristics of various immunohistochemical markers in N-methyl-N-nitrosourea (MNU)-induced mammary adenocarcinomas in male and female Crj:CD(SD)IGS rats including: estrogen receptor α (ER), progesterone receptor (PgR), androgen receptor (AR), receptor tyrosine-protein kinase erbB-2 (HER2), GATA binding protein 3 (GATA3), and proliferating cell nuclear antigen (PCNA)...
May 2016: Experimental and Toxicologic Pathology: Official Journal of the Gesellschaft Für Toxikologische Pathologie
Jenny-Maria Jönsson, Nicolai Skovbjerg Arildsen, Susanne Malander, Anna Måsbäck, Linda Hartman, Mef Nilbert, Ingrid Hedenfalk
BACKGROUND AND AIMS: Although most ovarian cancers express estrogen (ER), progesterone (PR), and androgen (AR) receptors, they are currently not applied in clinical decision making. We explored the prognostic impact of sex steroid hormone receptor protein and mRNA expression on survival in epithelial ovarian cancer. METHODS: Immunohistochemical stainings for ERα, ERβ, PR, and AR were assessed in relation to survival in 118 serous and endometrioid ovarian cancers...
October 2015: Translational Oncology
Justyna Barć, Ewa Lucja Gregoraszczuk
Polychlorinated naphthalenes (PCNs) are thought to interact with the aryl hydrocarbon receptor (AHR) and to have enzyme-inducing properties comparable to polychlorinated dibenzo-p-dioxins, therefore activation of steroid hormone receptors in endocrine tissues is also possible. The aim of the present study was to examine the effects of PCNs mixture, Halowax 1051 on gene and protein expression of receptors: estradiol (ERα/β), androgen (AR) and AHRGene expression was evaluated by real-time PCR after 6 h of exposition and protein expression by Western blot after 24 h...
February 2016: Chemosphere
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