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https://www.readbyqxmd.com/read/29779013/treatment-of-sec62-over-expressing-tumors-by-thapsigargin-and-trifluoperazine
#1
Christina Körbel, Maximilian Linxweiler, Florian Bochen, Silke Wemmert, Bernhard Schick, Markus Meyer, Hans Maurer, Michael D Menger, Richard Zimmermann, Markus Greiner
Treatment with analogues of the SERCA-inhibitor Thapsigargin is a promising new approach for a wide variety of cancer entities. However, our previous studies on various tumor cells suggested resistance of SEC62 over-expressing tumors to this treatment. Therefore, we proposed the novel concept that e.g. lung-, prostate-, and thyroid-cancer patients should be tested for SEC62 over-expression, and developed a novel therapeutic strategy for a combinatorial treatment of SEC62 over-expressing tumors. The latter was based on the observations that treatment of SEC62 over-expressing tumor cells with SEC62-targeting siRNAs showed less resistance to Thapsigargin as well as a reduction in migratory potential and that the siRNA effects can be mimicked by the Calmodulin antagonist Trifluoperazine...
May 19, 2018: Biomolecular Concepts
https://www.readbyqxmd.com/read/29769195/osteocyte-driven-downregulation-of-snail-restrains-effects-of-drd2-inhibitors-on-mammary-tumor-cells
#2
Shengzhi Liu, Yao Fan, Andy Chen, Aydin Jalali, Kazumasa Minami, Kazuhiko Ogawa, Harikrishna Nakshatri, Bai-Yan Li, Hiroki Yokota
While bone is a frequent target of breast cancer-associated metastasis, little is known about the effects of tumor-bone interactions on the efficacy of tumor-suppressing agents. Here we examined the effect of two FDA-approved dopamine modulators, Fluphenazine (FP) and Trifluoperazine (TFP), on mammary tumor cells, osteoclasts, osteoblasts, and osteocytes. These agents suppressed proliferation and migration of mammary tumor cells chiefly by antagonizing dopamine receptor D2 and reduced bone resorption by downregulating nuclear factor of activated T-cells, cytoplasmic 1 (Nfatc1)...
May 16, 2018: Cancer Research
https://www.readbyqxmd.com/read/29663486/calmodulin-antagonist-enhances-dr5-mediated-apoptotic-signaling-in-tra-8-resistant-triple-negative-breast-cancer-cells
#3
Romone M Fancy, Harrison Kim, Tiara Napier, Donald J Buchsbaum, Kurt R Zinn, Yuhua Song
Patients with triple negative breast cancer (TNBC) have no successful "targeted" treatment modality, which represents a priority for novel therapy strategies. Upregulated death receptor 5 (DR5) expression levels in breast cancer cells compared to normal cells enable TRA-8, a DR5 specific agonistic antibody, to specifically target malignant cells for apoptosis without inducing normal hepatocyte apoptosis. Drug resistance is a common obstacle in TRAIL-based therapy for TNBC. Calmodulin (CaM) is overexpressed in breast cancer...
April 16, 2018: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29644470/ruthenium-ii-n-alkyl-phenothiazine-complexes-as-potential-anticancer-agents
#4
Andreja Leskovac, Sandra Petrovic, Tamara Lazarevic-Pasti, Milena Krstic, Vesna Vasic
In recent years, the search for effective anticancer compounds based on transition metal complexes has been the focus of medical investigations. The synergy between the ruthenium(II) and N-alkylphenothiazine counter-ions (chlorpromazine hydrochloride, thioridazine hydrochloride and trifluoperazine dihydrochloride, respectively) through the formation of three different complexes (1-3) was investigated. We explored whether the selected counter-ions and complexes might affect redox homeostasis and genome integrity of normal human blood cells, and induce an inhibition of Na+ /K+ -ATPase and AChE at pharmacologically relevant doses...
April 11, 2018: Journal of Biological Inorganic Chemistry: JBIC
https://www.readbyqxmd.com/read/29614416/repositioning-of-the-antipsychotic-trifluoperazine-synthesis-biological-evaluation-and-in-silico-study-of-trifluoperazine-analogs-as-anti-glioblastoma-agents
#5
Seokmin Kang, Jung Moo Lee, Borami Jeon, Ahmed Elkamhawy, Sora Paik, Jinpyo Hong, Soo-Jin Oh, Sun Ha Paek, C Justin Lee, Ahmed H E Hassan, Sang Soo Kang, Eun Joo Roh
Repositioning of the antipsychotic drug trifluoperazine for treatment of glioblastoma, an aggressive brain tumor, has been previously suggested. However, trifluoperazine did not increase the survival time in mice models of glioblastoma. In attempt to identify an effective trifluoperazine analog, fourteen compounds have been synthesized and biologically in vitro and in vivo assessed. Using MTT assay, compounds 3dc and 3dd elicited 4-5 times more potent inhibitory activity than trifluoperazine with IC50  = 2...
March 23, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29580626/reprint-of-a-chemical-screen-identifies-trifluoperazine-as-an-inhibitor-of-glioblastoma-growth
#6
Tiago Pinheiro, Magdalena Otrocka, Brinton Seashore-Ludlow, Vilma Rraklli, Johan Holmberg, Karin Forsberg-Nilsson, András Simon, Matthew Kirkham
Glioblastoma (GBM) is regarded as the most common malignant brain tumor but treatment options are limited. Thus, there is an unmet clinical need for compounds and corresponding targets that could inhibit GBM growth. We screened a library of 80 dopaminergic ligands with the aim of identifying compounds capable of inhibiting GBM cell line proliferation and survival. Out of 45 active compounds, 8 were further validated. We found that the dopamine receptor D2 antagonist trifluoperazine 2HCl inhibits growth and proliferation of GBM cells in a dose dependent manner...
March 23, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29574355/early-prediction-of-olanzapine-induced-weight-gain-for-schizophrenia-patients
#7
Ching-Hua Lin, Shih-Chi Lin, Yu-Hui Huang, Fu-Chiang Wang, Chun-Jen Huang
The aim of this study was to determine whether weight changes at week 2 or other factors predicted weight gain at week 6 for schizophrenia patients receiving olanzapine. This study was the secondary analysis of a six-week trial for 94 patients receiving olanzapine (5 mg/d) plus trifluoperazine (5 mg/d), or olanzapine (10 mg/d) alone. Patients were included in analysis only if they had completed the 6-week trial (per protocol analysis). Weight gain was defined as a 7% or greater increase of the patient's baseline weight...
May 2018: Psychiatry Research
https://www.readbyqxmd.com/read/29568865/trifluoperazine-induces-apoptosis-through-the-upregulation-of-bax-bcl%C3%A2-2-and-downregulated-phosphorylation-of-akt-in-mesangial-cells-and-improves-renal-function-in-lupus-nephritis-mice
#8
Baodong Wang, Yankun Luo, Xiaoshuang Zhou, Rongshan Li
The inhibition of mesangial cell (MC) proliferation has become an important therapy in preventing glomerular proliferation diseases. Trifluoperazine (TFP) has been reported to inhibit the proliferation of several types of cancer cell, however, the effects of TFP in renal proliferation diseases remain to be fully elucidated. The present study examined the effects of TFP on the proliferation of MCs and quantified cell apoptosis progression in vivo and in vitro. The effects of various TFP concentrations and treatment durations on cell proliferation and cell apoptosis in vitro were analyzed using flow cytometry in conjunction with a Cell Counting kit‑8 assay...
March 13, 2018: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29555454/inhibitor-and-peptide-binding-to-calmodulin-characterized-by-high-pressure-fourier-transform-infrared-spectroscopy-and-f%C3%A3-rster-resonance-energy-transfer
#9
Süleyman Cinar, Claus Czeslik
We compare the binding of an inhibitor with that of a natural peptide to Ca2+ saturated calmodulin (holo-CaM). As inhibitor we have chosen trifluoperazine (TFP) that is inducing a huge conformational change of holo-CaM from the open dumbbell-shaped to the closed globular conformation upon binding. On the other hand, melittin is used as model peptide, which is a well-known natural binding partner of holo-CaM. The experiments are carried out as a function of pressure to reveal the contribution of volume or packing effects to the stability of the calmodulin-ligand complexes...
March 16, 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29536309/trifluoperazine-attenuates-store-dependent-ca-2-entry-in-macrophages
#10
Z I Krutetskaya, L S Milenina, A A Naumova, S N Butov, V G Antonov, A D Nozdrachev
Using Fura-2AM microfluorimetry, we have shown for the first time that preincubation of macrophages with the calsequestrin inhibitor neuroleptic trifluoperazine leads to a significant inhibition of the store-dependent Ca2+ entry induced by endoplasmic Ca2+ -ATPase inhibitors thapsigargin or cyclopiazonic acid in rat peritoneal macrophages. The results suggest calsequestrin involvement in the regulation of the store-dependent Ca2+ entry in macrophages.
January 2018: Doklady. Biochemistry and Biophysics
https://www.readbyqxmd.com/read/29536308/phospholipase-a-2-inhibitors-modulate-the-effect-of-trifluoperazine-on-the-intracellular-ca-2-concentration-in-macrophages
#11
Z I Krutetskaya, L S Milenina, A A Naumova, S N Butov, V G Antonov, A D Nozdrachev
Using Fura-2AM microfluorimetry, it was shown for the first time that phospholipase A2 inhibitors 4-bromophenacyl bromide and glucocorticosteroids prednisolone and dexamethasone attenuate Ca2+ responses induced by neuroleptic trifluoperazine in macrophages. The results suggest the involvement of phospholipase A2 and arachidonic acid metabolism cascade in the effect of trifluoperazine on intracellular Ca2+ concentration in macrophages.
January 2018: Doklady. Biochemistry and Biophysics
https://www.readbyqxmd.com/read/29530795/amphipathic-helical-peptides-hamper-protein-protein-interactions-of-the-intrinsically-disordered-chromatin-nuclear-protein-1-nupr1
#12
Patricia Santofimia-Castaño, Bruno Rizzuti, Olga Abián, Adrián Velázquez-Campoy, Juan L Iovanna, José L Neira
BACKGROUND: NUPR1 is a multifunctional intrinsically disordered protein (IDP) involved, among other functions, in chromatin remodelling, and development of pancreatic ductal adenocarcinoma (PDAC). It interacts with several biomolecules through hydrophobic patches around residues Ala33 and Thr68. The drug trifluoperazine (TFP), which hampers PDAC development in xenografted mice, also binds to those regions. Because of the large size of the hot-spot interface of NUPR1, small molecules could not be adequate to modulate its functions...
March 10, 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29453993/the-tegumental-allergen-like-proteins-of-schistosoma-mansoni-a-biochemical-study-of-smtal4-tal13
#13
Jack Carson, Charlotte M Thomas, Aaron McGinty, Gustavo Takata, David J Timson
Schistosoma mansoni, like other trematodes, expresses a number of unusual calcium binding proteins which consist of an EF-hand domain joined to a dynein light chain-like (DLC-like) domain by a flexible linker. These proteins have been implicated in host immune responses and drug binding. Three members of this protein family from S. mansoni (SmTAL1, SmTAL2 and SmTAL3) have been well characterised biochemically. Here we characterise the remaining family members from this species (SmTAL4-13). All of these proteins form homodimers and all except SmTAL5 bind to calcium and manganese ions...
April 2018: Molecular and Biochemical Parasitology
https://www.readbyqxmd.com/read/29390882/mitochondrial-impairment-as-a-key-factor-for-the-lack-of-attachment-after-cold-storage-of-hepatocyte-suspensions
#14
Gesine Pless-Petig, Björn Walter, Anja Bienholz, Ursula Rauen
Isolated primary hepatocytes, which are widely used for pharmacological and clinical purposes, usually undergo certain periods of cold storage in suspension during processing. While adherent hepatocytes were shown previously to suffer iron-dependent cell death during cold (4 °C) storage and early rewarming, we previously found little iron-dependent hepatocyte death in suspension but severely decreased attachment ability unless iron chelators were added. Here, we focus on the role of mitochondrial impairment in this nonattachment of hepatocyte suspensions...
December 2017: Cell Transplantation
https://www.readbyqxmd.com/read/29348654/low-concentration-trifluoperazine-promotes-proliferation-and-reduces-calcium-dependent-apoptosis-in-glioma-cells
#15
Yulin Wen, Yong Zhang, Jinbang Li, Feng Luo, Zhongxi Huang, Kunping Liu
Glioma patients constitute the greatest percentage of depressed neoplasm patients. These patients often require antidepressant treatment, but the effect of antidepressant drugs on glioma cells requires further evaluation. In the present study, we evaluated the effect of trifluoperazine (TFP) on the proliferation and apoptosis of glioma cells. Transcriptomic and bioinformatics analysis results suggested that antidepressant drugs, especially TFP, may upregulate the drug-resistant ability of glioma cells. A low concentration of TFP upregulated the viability of glioma cells...
January 18, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29336441/a-high-pressure-study-of-calmodulin-ligand-interactions-using-small-angle-x-ray-and-elastic-incoherent-neutron-scattering
#16
Süleyman Cinar, Samy Al-Ayoubi, Christian Sternemann, Judith Peters, Roland Winter, Claus Czeslik
Calmodulin (CaM) is a Ca2+ sensor and mediates Ca2+ signaling through binding of numerous target ligands. The binding of ligands by Ca2+ -saturated CaM (holo-CaM) is governed by attractive hydrophobic and electrostatic interactions that are weakened under high pressure in aqueous solutions. Moreover, the potential formation of void volumes upon ligand binding creates a further source of pressure sensitivity. Hence, high pressure is a suitable thermodynamic variable to probe protein-ligand interactions. In this study, we compare the binding of two different ligands to holo-CaM as a function of pressure by using X-ray and neutron scattering techniques...
January 31, 2018: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/29322188/management-of-morgellons-disease-with-low-dose-trifluoperazine
#17
Bernice Y Yan, Joseph L Jorizzo
No abstract text is available yet for this article.
February 1, 2018: JAMA Dermatology
https://www.readbyqxmd.com/read/29287071/uptake-of-polyphosphate-microparticles-in-vitro-saos-2-and-huvec-cells-followed-by-an-increase-of-the-intracellular-atp-pool-size
#18
Werner E G Müller, Shunfeng Wang, Matthias Wiens, Meik Neufurth, Maximilian Ackermann, Dinko Relkovic, Maria Kokkinopoulou, Qingling Feng, Heinz C Schröder, Xiaohong Wang
Recently two approaches were reported that addressed a vitally important problem in regenerative medicine, i. e. the successful treatment of wounds even under diabetic conditions. Accordingly, these studies with diabetic rabbits [Sarojini et al. PLoS One 2017, 12(4):e0174899] and diabetic mice [Müller et al. Polymers 2017, 9, 300] identified a novel (potential) target for the acceleration of wound healing in diabetes. Both studies propose a raise of the intracellular metabolic energy status via exogenous administration either of ATP, encapsulated into lipid vesicles, or of polyphosphate (polyP) micro-/nanoparticles...
2017: PloS One
https://www.readbyqxmd.com/read/29273456/the-antipsychotic-trifluoperazine-reduces-marble-burying-behavior-in-mice-via-d-2-and-5-ht-2a-receptors-implications-for-obsessive-compulsive-disorder
#19
Nobuaki Egashira, Naoki Kubota, Yu Goto, Takuya Watanabe, Kaori Kubota, Shutaro Katsurabayashi, Katsunori Iwasaki
Trifluoperazine, a typical antipsychotic drug, not only antagonizes dopamine D2 receptors but also enhances serotonin 5-HT2 receptor-mediated behavior. Moreover, trifluoperazine suppresses human purinergic receptor P2X7 responses and calmodulin. However, the effect of trifluoperazine on marble-burying behavior, which has been considered an animal model of obsessive-compulsive disorder (OCD), has not been studied. Here, we examined the effect of trifluoperazine on marble-burying behavior in mice. Oral administration of paroxetine, a selective serotonin reuptake inhibitor, significantly reduced marble-burying behavior without affecting total locomotor activity...
February 2018: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29227273/-poisoning-by-psychopharmacological-drugs-in-azerbaijan-the-results-of-8-year-prospective-observation
#20
I Afandiyev, V Azizov
Acute poisoning of chemical etiology is a significant global public health problem. The aim of this study was the analysis of the toxicoepidemiological structure of psychopharmacological drugs poisoning in Azerbaijan. We collected and analyzed the data on all cases of acute poisoning by psychopharmacological drugs (codes of categories T42/T43 ICD-10) undergoing inpatient treatment at the Center of Clinical Toxicology in Baku, Azerbaijan in 2009-2016. The total number of patients with acute intoxication by psychopharmacological drugs was 3,413, which was 48...
November 2017: Georgian Medical News
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