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https://www.readbyqxmd.com/read/29050342/role-of-the-cyp3a4-mediated-11-12-epoxyeicosatrienoic-acid-pathway-in-the-development-of-tamoxifen-resistant-breast-cancer
#1
Nguyen Thi Thuy Phuong, Ji Won Kim, Jung-Ae Kim, Jang Su Jeon, Ji-Yoon Lee, Wen Jun Xu, Jin Won Yang, Sang Kyum Kim, Keon Wook Kang
Epoxyeicosatrienoic acid (EET) production via cytochrome P450 (CYP) epoxygenases closely correlates with the progression of breast cancer. However, its role in the development of chemoresistant breast cancers has yet to be elucidated. Here, we found that CYP3A4 expression and its epoxy-product, 11,12-epoxyeicosatrienoic acid (11,12-EET) was enhanced in tamoxifen (TAM)-resistant MCF-7 (TAMR-MCF-7) breast cancer cells compared to control MCF-7 cells. Treatment of TAMR-MCF-7 cells with ketoconazole and azamulin (selective CYP3A4 inhibitors) or 14,15-epoxyeicosa-5(Z)-enoic acid (14,15-EEZE, an EET antagonist) inhibited cellular proliferation and recovered the sensitivity to 4-hydroxytamoxifen...
September 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29050316/pharmacokinetics-and-drug-drug-interaction-between-enalapril-enalaprilat-and-felodipine-extended-release-er-in-healthy-subjects
#2
Dai Li, Sumei Xu, Yulu Wang, Dan Li, Xiaomin Li, Jing Pan, Pingsheng Xu
Since angiotensin-converting enzyme (ACE) inhibitors and calcium antagonists have complimentary mechanisms of action, enalapril, an ACE inhibitor, is used in combination with felodipine, a vascular selective dihydropyridine calcium antagonist, for the treatment of hypertension. The present study was designed to investigate the possible drug-drug interaction between these two agents in Chinese healthy subjects. A randomized, open-label, multiple-dose, 3-treatment, 3-period, 6-sequence cross-over study enrolling 12 healthy subjects (six male and six female subjects) was performed...
September 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29050241/combination-treatment-with-rucaparib-rubraca-and-mdm2-inhibitors-nutlin-3-and-rg7388-has-synergistic-and-dose-reduction-potential-in-ovarian-cancer
#3
Maryam Zanjirband, Nicola Curtin, Richard J Edmondson, John Lunec
Ovarian cancer is the seventh most common cancer worldwide for females and the most lethal of all gynecological malignancies. The treatment of ovarian cancer remains a challenge in spite of advances in debulking surgery and changes in both chemotherapy schedules and routes of administration. Cancer treatment has recently been improving with the introduction of targeted therapies to achieve greater specificity and less cytotoxicity. Both PARP inhibitors and MDM2-p53 binding antagonists are targeted therapeutic agents entered into clinical trials...
September 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29050210/astaxanthin-acts-via-lrp-1-to-inhibit-inflammation-and-reverse-lipopolysaccharide-induced-m1-m2-polarization-of-microglial-cells
#4
Xiaojun Wen, Lijiao Xiao, Zhuoyan Zhong, Limin Wang, Ze Li, Xiaoping Pan, Zhonglin Liu
Microglia become activated during neuroinflammation and produce neurotoxic and neurotrophic factors, depending on whether they acquire M1 proinflammatory or M2 anti-inflammatory phenotypes. Astaxanthin (ATX), a natural carotenoid, has anti-inflammatory and neuroprotective effects. We investigated whether ATX could reverse M1/M2 polarization and suppress neuroinflammation via low-density lipoprotein receptor-related protein-1 (LRP-1). We observed increased expression of M1 (TNF-α, IL-1β, and CD86) and decreased expression of M2 (Arg-1, IL-10, and CD206) markers in BV2 microglial cells stimulated with lipopolysaccharide (LPS)...
September 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29050146/-metabolism-genes-and-pharmacogenetics-of-non-vitamin-k-antagonist-oral-anticoagulants
#5
W Y Pang, X W Chen, Z G Zhai
No abstract text is available yet for this article.
September 26, 2017: Zhonghua Yi Xue za Zhi [Chinese medical journal]
https://www.readbyqxmd.com/read/29049988/magnolia-officinalis-bark-extract-induces-depolarization-of-pacemaker-potentials-through-m2-and-m3-muscarinic-receptors-in-cultured-murine-small-intestine-interstitial-cells-of-cajal
#6
Hyun Jung Kim, Taewon Han, Yun Tai Kim, Insuk So, Byung Joo Kim
BACKGROUND: Magnolia officinalis Rehder and EH Wilson (M. officinalis) are traditional Chinese medicines widely used for gastrointestinal (GI) tract motility disorder in Asian countries. We investigated the effects of an ethanol extract of M. officinalis (MOE) on the pacemaker potentials of cultured interstitial cells of Cajal (ICCs) in vitro and its effects on GI motor functions in vivo. METHODS: We isolated ICCs from small intestines, and the whole-cell patch-clamp configuration was used to record the pacemaker potentials in cultured ICCs in vitro...
October 19, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29049960/lethal-effects-of-cr-iii-alone-and-in-combination-with-propiconazole-and-clothianidin-in-honey-bees
#7
Fabio Sgolastra, Sonia Blasioli, Teresa Renzi, Simone Tosi, Piotr Medrzycki, Roberto Molowny-Horas, Claudio Porrini, Ilaria Braschi
Several anthropogenic contaminants, including pesticides and heavy metals, can affect honey bee health. The effects of mixtures of heavy metals and pesticides are rarely studied in bees, even though bees are likely to be exposed to these contaminants in both agricultural and urban environments. In this study, the lethal toxicity of Cr alone and in combination with the neonicotinoid insecticide clothianidin and the ergosterol-biosynthesis-inhibiting fungicide propiconazole was assessed in Apis mellifera adults...
October 12, 2017: Chemosphere
https://www.readbyqxmd.com/read/29049782/rotational-speed-modulation-used-with-continuous-flow-left-ventricular-assist-device-provides-good-pulsatility
#8
Noritsugu Naito, Takashi Nishimura, Kei Iizuka, Yoshiaki Takewa, Akihide Umeki, Masahiko Ando, Minoru Ono, Eisuke Tatsumi
OBJECTIVES: Continuous-flow left ventricular assist devices (CF-LVADs) are widely used to treat patients with end-stage heart failure. Although continuous flow is different from physiological flow, patients show improved outcomes after CF-LVAD implantation. A novel rotational speed (RS) modulation system used with CF-LVAD (EVAHEART) has been developed, which can change RS in synchronization with the native cardiac cycle. We conducted the present study to investigate the influence of the system on pulsatility in peripheral perfusion...
August 10, 2017: Interactive Cardiovascular and Thoracic Surgery
https://www.readbyqxmd.com/read/29049722/a-ppar-gamma-agonist-rosiglitazone-suppresses-fibrotic-response-in-human-pterygium-fibroblasts-by-modulating-the-p38-mapk-pathway
#9
Selikem Abla Nuwormegbe, Joon Hyung Sohn, Sun Woong Kim
Purpose: Fibroblast activation may play an important role in pterygium progression. Synthetic peroxisome proliferator-activated receptor γ (PPAR-γ) ligands have been shown to be effective antifibrotic agents against transforming growth factor β1 (TGF-β1) induced fibrosis in several tissues. We aimed to investigate the antifibrotic effects of the PPAR-γ ligand rosiglitazone in pterygium fibroblasts and the underlying mechanisms. Methods: Profibrotic activation was induced by TGF-β1 in primary cultured human pterygium fibroblasts and the effect of rosiglitazone treatment on α-smooth muscle actin (α-SMA), and extra cellular matrix proteins synthesis was detected by western blotting, real-time PCR, immunostaining, and flow cytometry...
October 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/29049492/association-of-hsd3b1-genotype-with-response-to-androgen-deprivation-therapy-for-biochemical-recurrence-after-radiotherapy-for-localized-prostate-cancer
#10
Jason W D Hearn, Wanling Xie, Mari Nakabayashi, Nima Almassi, Chad A Reichard, Mark Pomerantz, Philip W Kantoff, Nima Sharifi
Importance: The variant HSD3B1 (1245C) allele enhances dihydrotestosterone synthesis and predicts resistance to androgen-deprivation therapy (ADT) for biochemically recurrent prostate cancer after prostatectomy and for metastatic disease. Whether this is true after radiotherapy is unknown. Objective: To determine whether the HSD3B1 (1245C) allele predicts worse clinical outcomes from ADT for biochemical recurrence after radiotherapy. Design, Setting, and Participants: The Prostate Clinical Research Information System at Dana-Farber Cancer Institute was used to identify the study cohort, which included men treated with ADT for biochemical recurrence after primary radiotherapy between 1996 and 2013...
October 12, 2017: JAMA Oncology
https://www.readbyqxmd.com/read/29049325/effect-of-therapeutic-interchange-on-medication-reconciliation-during-hospitalization-and-upon-discharge-in-a-geriatric-population
#11
Jessica S Wang, Robert L Fogerty, Leora I Horwitz
BACKGROUND: Therapeutic interchange of a same class medication for an outpatient medication is a widespread practice during hospitalization in response to limited hospital formularies. However, therapeutic interchange may increase risk of medication errors. The objective was to characterize the prevalence and safety of therapeutic interchange. METHODS AND FINDINGS: Secondary analysis of a transitions of care study. We included patients over age 64 admitted to a tertiary care hospital between 2009-2010 with heart failure, pneumonia, or acute coronary syndrome who were taking a medication in any of six commonly-interchanged classes on admission: proton pump inhibitors (PPIs), histamine H2-receptor antagonists (H2 blockers), hydroxymethylglutaryl CoA reductase inhibitors (statins), angiotensin-converting enzyme (ACE) inhibitors, angiotensin receptor blockers (ARBs), and inhaled corticosteroids (ICS)...
2017: PloS One
https://www.readbyqxmd.com/read/29049116/basic-translational-development-of-forthcoming-opioid-and-nonopioid-targeted-pain-therapeutics
#12
Nebojsa Nick Knezevic, Ajay Yekkirala, Tony L Yaksh
Opioids represent an efficacious therapeutic modality for some, but not all pain states. Singular reliance on opioid therapy for pain management has limitations, and abuse potential has deleterious consequences for patient and society. Our understanding of pain biology has yielded insights and opportunities for alternatives to conventional opioid agonists. The aim is to have efficacious therapies, with acceptable side effect profiles and minimal abuse potential, which is to say an absence of reinforcing activity in the absence of a pain state...
November 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29048920/different-role-of-ca1-5ht3-serotonin-receptors-on-memory-acquisition-deficit-induced-by-total-tsd-and-rem-sleep-deprivation-rsd
#13
Zainab Eydipour, Gholamhassan Vaezi, Mohammad Nasehi, Seyed-Ali Haeri-Rouhani, Mohammad-Reza Zarrindast
BACKGROUND: Serotonin receptors such as 5-HT3 plays critical role in regulation of sleep, wake cycle and cognitive process. Thus, we investigated the role of CA1 5HT3 serotonin receptors in memory acquisition deficit induced by total sleep deprivation (TSD; for 24 hour) and REM sleep deprivation (RSD; for 24 hour). Pain perception and locomotor activity were also assessed as factors that may affect the memory process. METHODS: Modified water box and multi-platform apparatus were used to induce TSD or RSD, respectively...
September 2017: Archives of Iranian Medicine
https://www.readbyqxmd.com/read/29048889/lipoyl-homotaurine-derivative-adm_12-reverts-oxaliplatin-induced-neuropathy-and-reduces-cancer-cells-malignancy-by-inhibiting-carbonic-anhydrase-ix-caix
#14
Marco Fragai, Giuseppina Comito, Lorenzo Di Cesare Mannelli, Roberta Gualdani, Vito Calderone, Alexandra Louka, Barbara Richichi, Oscar Francesconi, Andrea Angeli, Alessio Nocentini, Paola Gratteri, Paola Chiarugi, Carla Ghelardini, Francesco Tadini-Buoninsegni, Claudiu T Supuran, Cristina Nativi
Oxaliplatin (OXA) is a valuable and largely used cancer drug, which induces a serious and intractable neuropathy. The lipoyl-homotaurine derivative, ADM_12, reverts in vivo OXA-induced neuropathy and it is an effective antagonist of the nociceptive sensor channel TRPA1. Unprecedentedly, this safe analgesic showed a synergy with OXA in vitro and proved to inhibit CA IX, a relevant therapeutic target, clearly interfering with pancreatic cancer cells aggressiveness.
October 19, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29048607/the-arabidopsis-chromatin-remodeling-factor-chr5-regulates-plant-immune-responses-and-nucleosome-occupancy
#15
Baohong Zou, Qi Sun, Wenli Zhang, Yuan Ding, Dong-Lei Yang, Jian Hua
ATP-dependent chromatin remodeling factors use the energy of ATP hydrolysis to alter the structure of chromatin and are important regulators of eukaryotic gene expression. One such factor CHR5 (Chromatin Remodeling Factor 5) in Arabidopsis (Arabidopsis thaliana) was previously found to be involved in growth and development regulation. Here we show that CHR5 is required for the upregulation of the intracellular immune receptor gene SNC1 (SUPPRESSOR OF npr1-1, CONSTITUTIVE1) and consequently the autoimmunity induced by SNC1 upregulation...
October 17, 2017: Plant & Cell Physiology
https://www.readbyqxmd.com/read/29048484/adiponectin-suppression-of-late-inflammatory-mediator-hmgb1-induced-cytokine-expression-in-raw-264-macrophage-cells
#16
Mohamed Elfeky, Takeshi Yoneshiro, Yuko Okamatsu-Ogura, Kazuhiro Kimura
High mobility group protein B1 (HMGB1) is a late inflammatory mediator released from inflammatory cells when stimulated, resulting in exaggerating septic symptoms. We recently demonstrated that full-length adiponectin, a potent anti-inflammatory adipokine, inhibits lipopolysaccharide-induced HMGB1 release. However, the effects of adiponectin on HMGB1-induced exaggerating signals currently remain unknown. This study aimed to investigate the effects of adiponectin on the pro-inflammatory function of HMGB1 in RAW264 macrophage cells...
October 18, 2017: Journal of Biochemistry
https://www.readbyqxmd.com/read/29048423/identification-of-cross-talk-between-sumoylation-and-ubiquitylation-using-a-sequential-peptide-immunopurification-approach
#17
Francis P McManus, Frédéric Lamoliatte, Pierre Thibault
Ubiquitin and ubiquitin-like modifiers (UBLs) such as small ubiquitin-like modifier (SUMO) can act as antagonists to one another by competing to occupy similar residues in the proteome. In addition, SUMO and ubiquitin can be coupled to each other at key lysine residues to form highly branched protein networks. The interplay between these modifications governs important biological processes such as double-strand break repair and meiotic recombination. We recently developed an approach that permits the identification of proteins that are modified by both SUMOylation and ubiquitylation...
November 2017: Nature Protocols
https://www.readbyqxmd.com/read/29048353/p2x-receptor-antagonists-inhibit-the-interaction-of-s-aureus-hemolysin-a-with-membranes
#18
Markus Schwiering, Matthias Husmann, Nadja Hellmann
The pore forming hemolysin A, Hla, is a major virulence factor of Staphylococcus aureus. Apparently, 1-2 pore(s) per cell suffice(s) to cause cell death. Accumulated experimental evidence points towards a major role of ATP-gated purinergic receptors (P2XR) for hemolysis caused by Hla, complement and other pore forming proteins, presumably by increasing membrane permeability. Indeed, in experiments employing rabbit erythrocytes, inhibitory concentrations of frequently employed P2XR-antagonists were in a similar range as previously reported for erythrocytes of other species and other toxins...
October 19, 2017: Toxins
https://www.readbyqxmd.com/read/29047460/computational-insights-into-the-subtype-selectivity-and-message-address-efficacy-mechanisms-of-opioid-receptors-through-jdtic-binding-and-unbinding
#19
Jian-Xin Cheng, Tao Cheng, Wei-Hua Li, Gui-Xia Liu, Wei-Liang Zhu, Yun Tang
In drug design and discovery, binding affinity and selectivity are two basic properties of a drug candidate. Opioid receptors (ORs) are the main targets of strong analgesics. Like some other class A members of G-protein-coupled receptors (GPCRs), ORs exhibit complex selectivity on their ligands. The diversity of binding activity and selectivity among opioids has deeply attracted researchers for a long time. To investigate the subtype selectivity of μ, δ and κ ORs in detail, using the κ-selective antagonist JDTic as a probe, we performed a series of computational simulations, including molecular dynamics and metadynamics, on JDTic-μ/δ/κ-OR complexes...
October 19, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29047348/effectiveness-and-safety-of-vitamin-k-antagonists-and-new-anticoagulants-in-the-prevention-of-thromboembolism-in-atrial-fibrillation-in-older-adults-a-systematic-review-of-reviews-and-the-development-of-recommendations-to-reduce-inappropriate-prescribing
#20
REVIEW
Christina Sommerauer, Lisa Schlender, Mark Krause, Sabine Weißbach, Anja Rieckert, Yolanda V Martinez, David Reeves, Anna Renom-Guiteras, Ilkka Kunnamo, Andreas Sönnichsen
No abstract text is available yet for this article.
October 16, 2017: BMC Geriatrics
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