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Acadesine

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https://www.readbyqxmd.com/read/27847321/aicar-activates-er-stress-dependent-apoptosis-in-gallbladder-cancer-cells
#1
Jifeng Nie, Aidong Liu, Qunya Tan, Kai Zhao, Kui Hu, Yong Li, Bin Yan, Lin Zhou
AICAR (5-Aminoimidazole-4-carboxamide riboside or acadesine) is an AMP-activated protein kinase (AMPK) agonist, its activity in human gallbladder cancer cells was evaluated here. We show that AICAR provoked significant apoptosis in human gallbladder cancer cell lines (Mz-ChA-1, QBC939 and GBC-SD) and primary gallbladder cancer cells. AICAR-induced cytotoxicity in gallbladder cancer cells appears independent of AMPK activation. Inhibition of AMPK, via AMPKα shRNA knockdown or dominant negative mutation (T172A), failed to rescue GBC-SD cells from AICAR...
November 12, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27103440/aicar-induces-ampk-independent-programmed-necrosis-in-prostate-cancer-cells
#2
Feng Guo, Shuang-Qing Liu, Xing-Hua Gao, Long-Yang Zhang
AICAR (5-Aminoimidazole-4-carboxamide riboside or acadesine) is an AMP-activated protein kinase (AMPK) agonist, which induces cytotoxic effect to several cancer cells. Its potential activity in prostate cancer cells and the underlying signaling mechanisms have not been extensively studied. Here, we showed that AICAR primarily induced programmed necrosis, but not apoptosis, in prostate cancer cells (LNCaP, PC-3 and PC-82 lines). AICAR's cytotoxicity to prostate cancer cells was largely attenuated by the necrosis inhibitor necrostatin-1...
May 27, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/26987443/furanodiene-alters-mitochondrial-function-in-doxorubicin-resistant-mcf-7-human-breast-cancer-cells-in-an-ampk-dependent-manner
#3
Zhang-Feng Zhong, Wen Tan, William W Qiang, Virginia L Scofield, Ke Tian, Chun-Ming Wang, Wen-An Qiang, Yi-Tao Wang
Furanodiene is a bioactive sesquiterpene isolated from the spice-producing Curcuma wenyujin plant (Y. H. Chen and C. Ling) (C. wenyujin), which is a commonly prescribed herb used in clinical cancer therapy by modern practitioners of traditional Chinese medicine. Previously, we have shown that furanodiene inhibits breast cancer cell growth both in vitro and in vivo, however, the mechanism for this effect is not yet known. In this study, therefore, we asked (1) whether cultured breast cancer cells made resistant to the chemotherapeutic agent doxorubicin (DOX) via serial selection protocols are susceptible to furanodiene's anticancer effect, and (2) whether AMP-activated protein kinase (AMPK), which is a regulator of cellular energy homeostasis in eukaryotic cells, participates in this effect...
April 26, 2016: Molecular BioSystems
https://www.readbyqxmd.com/read/26913390/-acadesine-inhibits-the-proliferation-of-k562-cells-and-enhances-their-sensitivity-to-imatinib
#4
Jing-Jing Wu, Bin Wei, Yi-Han Ding, Zhi-Kui Deng, Yu-Ye Shi, Yu-Feng Li
OBJECTIVE: To investigate the effects of AMPK agonist Acadesine (AICAR) on growth inhibition of K562 cells and their sensitivity to imatinib (IM). METHODS: K562 cells were cultured with different concentrations of AICAR alone or its combination with IM for 48 hours, the CCK-8 assay was used to detect cell proliferation, the cell cycle distribution and apoptosis were analyzed by flow cytometry. The expression levels of Cyclin D1, Cyclin E1 and Caspase 3 protein were determined by Western blot...
February 2016: Zhongguo Shi Yan Xue Ye Xue za Zhi
https://www.readbyqxmd.com/read/26110568/bcl-2high-mantle-cell-lymphoma-cells-are-sensitized-to-acadesine-with-abt-199
#5
Arnau Montraveta, Sílvia Xargay-Torrent, Laia Rosich, Mònica López-Guerra, Jocabed Roldán, Vanina Rodríguez, Eriong Lee-Vergés, Mercè de Frías, Clara Campàs, Elias Campo, Gaël Roué, Dolors Colomer
Acadesine is a nucleoside analogue with known activity against B-cell malignancies. Herein, we showed that in mantle cell lymphoma (MCL) cells acadesine induced caspase-dependent apoptosis through turning on the mitochondrial apoptotic machinery. At the molecular level, the compound triggered the activation of the AMPK pathway, consequently modulating known downstream targets, such as mTOR and the cell motility-related vasodilator-stimulated phosphoprotein (VASP). VASP phosphorylation by acadesine was concomitant with a blockade of CXCL12-induced migration...
August 28, 2015: Oncotarget
https://www.readbyqxmd.com/read/25218533/predictors-of-contemporary-coronary-artery-bypass-grafting-outcomes
#6
RANDOMIZED CONTROLLED TRIAL
Richard D Weisel, Nancy Nussmeier, Mark F Newman, Ronald G Pearl, Andrew S Wechsler, Giuseppe Ambrosio, Bertram Pitt, Robert M Clare, Karen S Pieper, Linda Mongero, Tammy L Reece, Terrence M Yau, Stephen Fremes, Philippe Menasché, Armando Lira, Robert A Harrington, T Bruce Ferguson
OBJECTIVES: The study objective was to identify the predictors of outcomes in a contemporary cohort of patients from the Reduction in cardiovascular Events by acaDesine in patients undergoing CABG (RED-CABG) trial. Despite the increasing risk profile of patients who undergo coronary artery bypass grafting, morbidity and mortality have remained low, and identification of the current predictors of adverse outcomes may permit new treatments to further improve outcomes. METHODS: The RED-CABG trial was a multicenter, randomized, double-blind, placebo-controlled study that determined that acadesine did not reduce adverse events in moderately high-risk patients undergoing nonemergency coronary artery bypass grafting...
December 2014: Journal of Thoracic and Cardiovascular Surgery
https://www.readbyqxmd.com/read/25177017/synthesis-and-biological-evaluation-of-3-methyl-5-phenylthieno-2-3-d-pyrimidine-2-4-1h-3h-dione-derivatives-for-the-treatment-of-diet-induced-obesity
#7
Yun Sang, Heyin Pei, Liang Ma, Li Huang, Caifeng Xie, Jinying Chen, Xiaolin Liang, Yan Ran, Guangcheng Wang, Zhuang Yang, Dong Cao, Lin He, Yuzhe Wu, Linhong He, Jun Zhu, Jingbo Lan, Lijuan Chen
Triglycerides are the main part of fats and half of the lipids in hepatocytes, and play an important role in metabolism as energy sources and transporters of dietary fat. In this study, 33 derivatives based on 3-methyl-5-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione were synthesized and evaluated for their lipid-lowering activity. Among them, compound 1i was found to exhibit potent triglyceride-lowering potency in 3T3-L1 adipocytes which was comparable to that of the adenosine monophosphate-activated protein kinase (AMPK) agonist Acadesine (AIACR)...
2014: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/24519895/synergistic-anti-tumor-activity-of-acadesine-aicar-in-combination-with-the-anti-cd20-monoclonal-antibody-rituximab-in-in-vivo-and-in-vitro-models-of-mantle-cell-lymphoma
#8
Arnau Montraveta, Sílvia Xargay-Torrent, Mónica López-Guerra, Laia Rosich, Patricia Pérez-Galán, Itziar Salaverria, Silvia Beà, Susana G Kalko, Mercè de Frias, Clara Campàs, Gaël Roué, Dolors Colomer
Mantle cell lymphoma (MCL) is considered one of the most challenging lymphoma, with limited responses to current therapies. Acadesine, a nucleoside analogue has shown antitumoral effects in different preclinical cancer models as well as in a recent phase I/II clinical trial conducted in patients with chronic lymphocytic leukemia. Here we observed that acadesine exerted a selective antitumoral activity in the majority of MCL cell lines and primary MCL samples, independently of adverse cytogenetic factors. Moreover, acadesine was highly synergistic, both in vitro and in vivo, with the anti-CD20 monoclonal antibody rituximab, commonly used in combination therapy for MCL...
February 15, 2014: Oncotarget
https://www.readbyqxmd.com/read/24303202/acadesine-triggers-non-apoptotic-death-in-tumor-cells
#9
V A Glazunova, K V Lobanov, R S Shakulov, A S Mironov, A A Shtil
We studied the cytotoxicity of acadesine (5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside) for tumor and normal cells of various species and tissue origin. In tumor cells, acadesine triggered non-apoptotic death; the potency of the compound to normal cells was substantially lower. Acadesine was toxic for tumor cells with multidrug resistant phenotypes caused by the transmembrane transporter Р-glycoprotein or lack of proapoptotic p53. Activity of adenosine receptors was required for acadesine-induced cell death, whereas functioning of АМР-dependent protein kinase was not required...
July 2013: Acta Naturae
https://www.readbyqxmd.com/read/23924994/synthesis-of-new-acadesine-aica-riboside-analogues-having-acyclic-d-ribityl-or-4-hydroxybutyl-chains-in-place-of-the-ribose
#10
Stefano D'Errico, Giorgia Oliviero, Nicola Borbone, Jussara Amato, Vincenzo Piccialli, Michela Varra, Luciano Mayol, Gennaro Piccialli
The antiviral activity of certain acyclic nucleosides drew our attention to the fact that the replacement of the furanose ring by an alkyl group bearing hydroxyl(s) could be a useful structural modification to modulate the biological properties of those nucleosides. Herein, we report on the synthesis of some novel acadesine analogues, where the ribose moiety is mimicked by a D-ribityl or by a hydroxybutyl chain.
2013: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/23242185/extracellular-guanosine-regulates-extracellular-adenosine-levels
#11
Edwin K Jackson, Dongmei Cheng, Travis C Jackson, Jonathan D Verrier, Delbert G Gillespie
The aim of this investigation was to test the hypothesis that extracellular guanosine regulates extracellular adenosine levels. Rat preglomerular vascular smooth muscle cells were incubated with adenosine, guanosine, or both. Guanosine (30 μmol/l) per se had little effect on extracellular adenosine levels. Extracellular adenosine levels 1 h after addition of adenosine (3 μmol/l) were 0.125 ± 0.020 μmol/l, indicating rapid disposition of extracellular adenosine. Extracellular adenosine levels 1 h after addition of adenosine (3 μmol/l) plus guanosine (30 μmol/l) were 1...
March 1, 2013: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/23228986/acadesine-for-patients-with-relapsed-refractory-chronic-lymphocytic-leukemia-cll-a-multicenter-phase-i-ii-study
#12
MULTICENTER STUDY
Eric Van Den Neste, Bruno Cazin, Ann Janssens, Eva González-Barca, María José Terol, Vincent Levy, Jaime Pérez de Oteyza, Pierre Zachee, Andrew Saunders, Mercè de Frias, Clara Campàs
PURPOSE: Acadesine has shown in vitro to selectively induce apoptosis in B cells from chronic lymphocytic leukemia (CLL) patients. We conducted a phase I/II open-label clinical study, to determine the safety and tolerability of acadesine given intravenously as a 4-h infusion to CLL patients. METHODS: Patient population included CLL patients with relapsed/refractory disease who had received one or more prior lines of treatment including either a fludarabine or an alkylator-based regimen...
March 2013: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/22847168/surgery-no-benefit-of-acadesine-in-cabg
#13
COMMENT
Gregory B Lim
No abstract text is available yet for this article.
September 2012: Nature Reviews. Cardiology
https://www.readbyqxmd.com/read/22782417/effect-of-adenosine-regulating-agent-acadesine-on-morbidity-and-mortality-associated-with-coronary-artery-bypass-grafting-the-red-cabg-randomized-controlled-trial
#14
RANDOMIZED CONTROLLED TRIAL
Mark F Newman, T Bruce Ferguson, Jennifer A White, Giuseppe Ambrosio, Joerg Koglin, Nancy A Nussmeier, Ronald G Pearl, Bertram Pitt, Andrew S Wechsler, Richard D Weisel, Tammy L Reece, Armando Lira, Robert A Harrington
CONTEXT: Ischemia/reperfusion injury remains an important cause of morbidity and mortality after coronary artery bypass graft (CABG) surgery. In a meta-analysis of randomized controlled trials, perioperative and postoperative infusion of acadesine, a first-in-class adenosine-regulating agent, was associated with a reduction in early cardiac death, myocardial infarction, and combined adverse cardiac outcomes in participants undergoing on-pump CABG surgery. OBJECTIVE: To assess the efficacy and safety of acadesine administered in the perioperative period in reducing all-cause mortality, nonfatal stroke, and severe left ventricular dysfunction (SLVD) through 28 days...
July 11, 2012: JAMA: the Journal of the American Medical Association
https://www.readbyqxmd.com/read/21291368/novel-trends-in-the-treatment-of-cardiovascular-disorders-site-and-event-selective-adenosinergic-drugs
#15
REVIEW
A J Szentmiklósi, A Cseppento, G Harmati, P P Nánási
This review focuses on the potential role of site- and event-selective adenosinergic drugs in the treatment of cardiovascular diseases. Adenosine is released from the myocardium and vessels in response to various forms of stress and acts on four receptor subtypes (A1, A2A, A2B and A3). Adenosine is an important endogenous substance with important homeostatic activity in the regulation of cardiac function and circulation. Adenosine receptors are also involved in the modulation of various cellular events playing crucial role in physiological and pathological processes of the cardiovascular system...
2011: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/21244913/from-academic-vision-to-clinical-reality-a-case-study-of-acadesine
#16
K Mullane, D Bullough, D Shapiro
Acadesine is the prototype of a new class of therapeutic compounds termed adenosine-regulating agents (ARAs). The concept of adenosine regulation by acadesine and recognition of its potential therapeutic importance in myocardial ischemia was initiated in academia and led to the founding of a new biopharmaceutical company to develop acadesine and other ARAs. The historical background and preclinical studies that led to the discovery of acadesine and identification of its cardioprotective properties, culminating in international multicenter trials in patients undergoing cardiac surgery, are discussed...
November 1993: Trends in Cardiovascular Medicine
https://www.readbyqxmd.com/read/20664053/aicar-induces-apoptosis-independently-of-ampk-and-p53-through-up-regulation-of-the-bh3-only-proteins-bim-and-noxa-in-chronic-lymphocytic-leukemia-cells
#17
Antonio F Santidrián, Diana M González-Gironès, Daniel Iglesias-Serret, Llorenç Coll-Mulet, Ana M Cosialls, Mercè de Frias, Clara Campàs, Eva González-Barca, Esther Alonso, Verena Labi, Benoit Viollet, Adalberto Benito, Gabriel Pons, Andreas Villunger, Joan Gil
5-Aminoimidazole-4-carboxamide riboside or acadesine (AICAR) induces apoptosis in chronic lymphocytic leukemia (CLL) cells. A clinical study of AICAR is currently being performed in patients with this disease. Here, we have analyzed the mechanisms involved in AICAR-induced apoptosis in CLL cells in which it activates its only well-known molecular target, adenosine monophosphate-activated protein kinase (AMPK). However, AMPK activation with phenformin or A-769662 failed to induce apoptosis in CLL cells and AICAR also potently induced apoptosis in B lymphocytes from Ampkα1(-/-) mice, demonstrating an AMPK-independent mechanism of cell death...
October 21, 2010: Blood
https://www.readbyqxmd.com/read/20478949/avoiding-stroke-during-cardiac-surgery
#18
Kristine Kellermann, Bettina Jungwirth
The life saving benefits of cardiac surgery are frequently accompanied by negative side effects such as stroke, that occurs with an incidence of 2%-13% dependent to type of surgery. The etiology is most likely multifactorial with embolic events considered as main contributor. Although stroke presents a common complication, no guidelines for any routine use of pharmacological substances or non-pharmacological strategies exist to date. Non-pharmacological strategies include monitoring of brain oxygenation and perfusion with devices such as near infrared spectroscopy and Transcranial Doppler help...
June 2010: Seminars in Cardiothoracic and Vascular Anesthesia
https://www.readbyqxmd.com/read/20367195/aica-riboside-acadesine-an-activator-of-amp-activated-protein-kinase-with-potential-for-application-in-hematologic-malignancies
#19
REVIEW
Eric Van Den Neste, Georges Van den Berghe, Françoise Bontemps
IMPORTANCE OF THE FIELD: Despite considerable advances, B-cell chronic lymphocytic leukemia (CLL) is incurable with standard approaches. Thus, there remains a need for new therapies, particularly for patients who develop chemoresistance to DNA-targeting treatments. AICA-riboside (acadesine) is a nucleoside with a wide range of metabolic effects, including release of adenosine and activation of AMP-activated protein kinase (AMPK), which was initially developed as a cardioprotective agent...
April 2010: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/20185792/acadesine-inhibits-tissue-factor-induction-and-thrombus-formation-by-activating-the-phosphoinositide-3-kinase-akt-signaling-pathway
#20
Weiyu Zhang, Jianguo Wang, Huan Wang, Rong Tang, John D Belcher, Benoit Viollet, Jian-Guo Geng, Chunxiang Zhang, Chaodong Wu, Arne Slungaard, Chuhong Zhu, Yuqing Huo
OBJECTIVE: Acadesine, an adenosine-regulating agent and activator of AMP-activated protein kinase, has been shown to possess antiinflammatory activity. This study investigated whether and how acadesine inhibits tissue factor (TF) expression and thrombus formation. METHODS AND RESULTS: Human umbilical vein endothelial cells and human peripheral blood monocytes were stimulated with lipopolysaccharide to induce TF expression. Pretreatment with acadesine dramatically suppressed the clotting activity and expression of TF (protein and mRNA)...
May 2010: Arteriosclerosis, Thrombosis, and Vascular Biology
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