Abstract：
:Disruption of the circadian clock is associated with a variety of human pathologies, including cancer. Rather than being a mere consequence of a global changes associated with the cancer cell transcriptome, the aberrant clock gene expression observed in many tumors may serve for cancer cell survival. This scenario suggests the provocative hypothesis that pharmacological modulation of clock-related proteins may be suitable as an effective anticancer strategy. In this review, we focus on the functions of the druggable circadian nuclear receptors, REV-ERBα and REV-ERBβ, in cancer cell survival and describe the potential development of small molecule compounds that modulate REV-ERB activity as novel anticancer therapeutics. In addition, we debate the use of circadian rhythm-based synthetic lethal approaches to identify yet unexplored anticancer strategies.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Ercolani L,Ferrari A,De Mei C,Parodi C,Wade M,Grimaldi Bdoi
10.1016/j.phrs.2015.08.008subject
Has Abstractpub_date
2015-10-01 00:00:00pages
288-95eissn
1043-6618issn
1096-1186pii
S1043-6618(15)00176-0journal_volume
100pub_type
杂志文章,评审abstract：:Quiescent hepatic stellate cell (HSC) activation and subsequent conversion into myofibroblasts is the central event in hepatic fibrosis pathogenesis. Epithelial-mesenchymal transition (EMT), another vital participant in liver fibrosis, has the potential to initiate HSC activation, which promotes abundant myofibroblast...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2017.10.013
更新日期：2018-02-01 00:00:00
abstract：:Heparin-binding protein (HBP; CAP37/azurocidin) is secreted from neutrophil leukocytes early during inflammation and plays a central role in early capillary leakage and extravasation of neutrophils. Furthermore, HBP is chemotactic towards monocytes and lymphocytes and protects against stress-induced apoptosis, e.g. in...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2005.01.004
更新日期：2005-06-01 00:00:00
abstract：:This paper examines the effect of biphenylacetic acid on the antagonistic action of norfloxacin and enoxacin on the GABA(A)-mediated responses of the isolated guinea-pig ileum. GABA produced transient contractions followed by relaxation. The contractile effect of exogenously applied GABA was concentration-dependent wi...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.2001.0853
更新日期：2001-09-01 00:00:00
abstract：:Implantable cardioverter-defibrillators (ICDs) have revolutionized the primary and secondary prevention of patients with ventricular arrhythmias. However, the adverse effects of appropriate or inappropriate shocks may require the adjunctive use of anti-arrhythmic drugs (AADs). Beta blockers are the cornerstone of phar...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2019.03.020
更新日期：2019-05-01 00:00:00
abstract：:Autism-spectrum disorder (ASD) is a neurodevelopmental disorder characterized by persistent deficits in social communication and repetitive patterns of behavior. ASD is, however, often associated with medical comorbidities and gastrointestinal (GI) dysfunction is among the most common. Studies have demonstrated a corr...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2018.03.020
更新日期：2018-06-01 00:00:00
abstract：:Moderate wine consumption has been shown to reduce cardiovascular (CV) risk, due to alcohol and polyphenolic compounds, such as resveratrol. We investigated the associations between total urinary resveratrol metabolites (TRMs) as biomarkers of wine and resveratrol consumption and CV risk factors in a large cross-secti...
journal_title：Pharmacological research
pub_type： 杂志文章,多中心研究,随机对照试验
doi：10.1016/j.phrs.2012.03.009
更新日期：2012-06-01 00:00:00
abstract：:New quick-acting blood schizontocides are needed to contain the spread of multiple drug resistant strains of P. falciparum and for the treatment of the cerebral malaria cases. A multiple drug resistant strain of P. yoelii nigeriensis resistant to mefloquine (128 mg/kg x 6 days), quinine (300 mg/kg x 7 days) and chloro...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/1043-6618(89)90159-x
更新日期：1989-07-01 00:00:00
abstract：:The mitochondrial citrate carrier (CIC) is a nuclear-encoded protein located in the inner mitochondrial membrane. By mediating efflux of citrate from the mitochondria to the cytosol, CIC links mitochondrial central carbon metabolism and cytosolic lipogenesis together. Abnormal activity or expression of CIC was found i...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2020.105132
更新日期：2020-11-01 00:00:00
abstract：:A pharmacokinetic study of the metabolic profile of resveratrol has been performed in healthy men after moderate red wine (RW) consumption. The bioavailability of resveratrol is highly influenced by several factors such as the food matrix and, therefore, this study has been compared with a pilot study in which men ing...
journal_title：Pharmacological research
pub_type： 杂志文章,随机对照试验
doi：10.1016/j.phrs.2012.08.001
更新日期：2012-11-01 00:00:00
abstract：:The investigation was aimed at investigating whether the dopaminergic projection arriving at the nucleus septi lateralis (NSL) is involved in the facilitatory effect of vasopressin (AVP) on memory retrieval. The bilateral 6-OHDA lesions to the NSL were made in 20 male Wistar rats before testing the intracerebroventric...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1997.0280
更新日期：1998-02-01 00:00:00
abstract：:Memory T cells can be generated and remain long-term in different tissues following infection or immunization. Tissue-resident memory T (TRM) cells are a unique group of memory T cells that form and persist mainly in peripheral non-lymphoid organs. Unlike effector or central memory T (TEM or TCM) cells, TRM cells do n...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2020.104876
更新日期：2020-09-01 00:00:00
abstract：:Cytochrome P450-dependent arachidonic acid (AA) metabolism by medullary thick ascending limb of the loop of Henle (mTALH) cells, corneal epithelium and other transporting epithelia, such as those of the intestines, generate metabolites which affect Na(+)-K(+)-ATPase activity, vasomotion and, thereby, organ function. F...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/1043-6618(91)90046-z
更新日期：1991-05-01 00:00:00
abstract：:Asthma and COPD make up the majority of obstructive airways diseases (OADs), which affects ∼11 % of the population. The main drugs used to treat OADs have not changed in the past five decades, with advancements mainly comprising variations on existing treatments. The recent biologics are beneficial to only specific su...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.105029
更新日期：2020-09-01 00:00:00
abstract：:Ranolazine has characteristic properties of a selective inhibitor of the inward sodium current. It is primarily indicated as an anti-anginal agent in patients with coronary artery disease and chronic stable angina. Recently, ranolazine has been noted to possibly impart beneficial effects in various other cardiac condi...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2015.10.018
更新日期：2016-01-01 00:00:00
abstract：:Oxidative stress is an important contributor to the risk of chronic diseases. Dietary guidelines recommend increased consumption of fruits and vegetables to combat the incidence of human diseases such as cancer, cardiovascular disease, osteoporosis and diabetes. Fruits and vegetables are good sources of antioxidant ph...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2007.01.012
更新日期：2007-03-01 00:00:00
abstract：:The blood-brain barrier (BBB) keeps the central nervous system (CNS) safe from various brain diseases, while the BBB makes it difficult for effective drugs to enter the CNS. Mfsd2a is specifically expressed on the cell membrane of brain-microvascular endothelial cell (BMEC) and is implicated in the delivery of some su...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2015.12.024
更新日期：2016-02-01 00:00:00
abstract：:The effect of gentamicin on both glutamate synthesis and glutamate deamination was studied in kidney-cortex mitochondria and tubules isolated from both control and gentamicin-treated animals. In kidney-cortex mitochondria which were permeabilized in order to make a free access of substrates and antibiotic to the gluta...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/1043-6618(92)90235-4
更新日期：1992-12-01 00:00:00
abstract：:A substantial number of G-protein coupled receptors (GPCRs) genetic disorders are due to mutations that cause misfolding or dysfunction of the receptor product. Pharmacological chaperoning approaches can rescue such mutant receptors by stabilizing protein conformations that behave similar to the wild type protein. For...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2016.12.036
更新日期：2017-03-01 00:00:00
abstract：:Extensive studies have reported the significant roles of numerous cellular features and processes in properly maintaining neuronal morphology and function throughout the lifespan of an animal. Any alterations in their homeostasis appear to be strongly associated with neuronal aging and the pathogenesis of various neur...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2017.02.003
更新日期：2017-05-01 00:00:00
abstract：:Posttranslational modifications of proteins are important regulatory processes endowing the proteins functional complexity. Over the last decade, numerous studies have shed light on the roles of palmitoylation, one of the most common lipid modifications, in various aspects of neuronal functions. Major players regulati...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2016.06.008
更新日期：2016-09-01 00:00:00
abstract：:Purine release and prostaglandin (PG) outflow were simultaneously evaluated from untreated glial primary cultures of rat striatum, at rest and under field electrical stimulation. Purine release was also assayed from sister cultured cells in which a suitable pharmacological treatment with 1 x 10(-6) M dexamethasone or ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s1043-6618(89)80005-2
更新日期：1989-05-01 00:00:00
abstract：:QiShenYiQi Pills (QSYQ) is a compound Chinese medicine widely used in China for treatment of cardiovascular disease. However, limited data are available regarding the anti-fibrotic role of QSYQ after ischemia/reperfusion (I/R) injury. This study aimed to investigate the effect of post-treatment with QSYQ on myocardial...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2019.104272
更新日期：2019-08-01 00:00:00
abstract：:Diabetic nephropathy (DN) is a common and serious complication of diabetes and causes kidney failure. Ginsenoside Rg5 (Rg5) is an important monomer in the main protopanaxadiol component of black ginseng. Rg5 has exhibited some beneficial biological effects, such as anti-cancer, neuroprotection, and anti-depression, bu...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.104746
更新日期：2020-05-01 00:00:00
abstract：:Biochemical evaluations of the effects of the sulfhydryl-containing angiotensin-converting enzyme inhibitor (captopril) on the nephrotoxicity induced by doxorubicin in normal rats were carried out. A single dose of doxorubicin (15 mg kg-1) which caused nephrotoxicity was manifested biochemically by the elevation of se...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1998.0432
更新日期：1999-03-01 00:00:00
abstract：:A new class of methylfuroxans and methylfurazans arylthio, arylsulphinyl and arylsulphonyl substituted, characterized by vasodilating and antiaggregatory properties, is described. Vasodilating activity, tested on rabbit aortic rings percontracted with 1 microM noradrenaline, is enhanced by N-oxidation of the furazan r...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1993.1123
更新日期：1993-10-01 00:00:00
abstract：:This paper discusses the discovery of ligands for orphan receptors and the identification of the natural endogenous ligands for those receptors in physiology. The central thesis is that orphan seven transmembrane receptors (7TMRs) are allosteric conduits of chemical information exchange from extracellular ligands to i...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2016.01.022
更新日期：2016-12-01 00:00:00
abstract：:The presence of M(1)-M(4) receptors in guinea-pig gallbladder smooth muscle cells has been reported recently. The majority of these receptors are said to be of M(2) subtype. However, there are controversial reports about the functional muscarinic receptors that mediate contraction in this tissue. Similar to gallbladde...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1999.0536
更新日期：1999-11-01 00:00:00
abstract：:Several studies have demonstrated that any beneficial effects of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors (statins), of which simvastatin (Merck Sharp & Dohme) is an example, on coronary events are linked to their hypocholesterolemic properties. The in vivo effects of simvastatin treatment ...
journal_title：Pharmacological research
pub_type： 临床试验,杂志文章
doi：10.1006/phrs.2000.0787
更新日期：2001-04-01 00:00:00
abstract：:The gut microbiota and its short chain fatty acid (SCFA) metabolites have been established to play an important protective role against neurodegenerative diseases. Our previous study demonstrated that cerebral ischemic stroke triggers dysfunctional gut microbiota and increased intestinal permeability. In this study, w...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2019.104403
更新日期：2019-10-01 00:00:00
abstract：:Plasma lipid and lipoprotein levels were evaluated in 27 adults with essential hypertension at four different periods during a 12-month treatment with doxazosin. Mean plasma total cholesterol (TC), low-density lipoprotein-cholesterol (LDLC), triglyceride (TG), very low density lipoprotein-cholesterol (VLDLC) and the L...
journal_title：Pharmacological research
pub_type： 临床试验,杂志文章
doi：10.1016/1043-6618(94)80108-8
更新日期：1994-10-01 00:00:00
