Abstract:
:Most solid tumor cells adapt to their heterogeneous microenvironment by depending largely on aerobic glycolysis for energy production, a phenomenon called the Warburg effect, which is a hallmark of cancer. The altered energy metabolism not only provides cancer cell with ATP for cellular energy, but also generate essential metabolic intermediates that play a pivotal role in the biosynthesis of macromolecules, to support cell proliferation, invasiveness, and chemoresistance. The cellular metabolic reprogramming in cancer is regulated by several oncogenic proteins and tumor suppressors such as hypoxia-inducible factor (HIF-1), Myc, p53, and PI3K/Akt/mTOR pathway. A better understanding of the mechanisms involved in the regulation of aerobic glycolysis can help in developing glycolytic inhibitors as anticancer agents. These metabolic antiglycolytic agents could be more effective if used in drug combinations to combat cancer. Several preclinical and early clinical studies have shown the effectiveness of targeting the glycolytic pathway as a therapeutic approach to suppress cancer progression. This review aimed to present the most recent data on the emerging drug candidate targeting enzymes and intermediates involved in glucose metabolism to provide therapeutic opportunities and challenges for antiglycolytic cancer therapy.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Abdel-Wahab AF,Mahmoud W,Al-Harizy RMdoi
10.1016/j.phrs.2019.104511subject
Has Abstractpub_date
2019-12-01 00:00:00pages
104511eissn
1043-6618issn
1096-1186pii
S1043-6618(19)31673-1journal_volume
150pub_type
杂志文章,评审abstract::Mast cells take part of armamentarium immunologic for host defense against parasitic and bacterial infections. They are derived from bone marrow progenitors and can be activated by immunological and chemical stimuli in order to get its degranulation. The activation of mast cells generates a signalling cascade leaded t...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2009.11.014
更新日期:2010-09-01 00:00:00
abstract::Augmented vasoconstriction is a hallmark of hypertension and is mediated partly by hyper-stimulation of G protein couple receptors (GPCRs) and downstream signaling components. Although GPCR blockade is a key component of current anti-hypertensive strategies, whether hypertension is better managed by directly targeting...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2019.01.012
更新日期:2019-03-01 00:00:00
abstract::Heart rate recovery at 1min (HRR1) is a strong predictor of all-cause mortality. The effects of statins on the autonomic nervous system may account for their beneficial effects in survival. Our aim was to determine if statin therapy improves heart rate recovery in hypercholesterolemic patients with type 2 diabetes mel...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2006.09.002
更新日期:2006-12-01 00:00:00
abstract::Serotonin (5-HT) is present in high concentration in enterochromaffin cells throughout the gastrointestinal tract, where it plays a very important role, being involved, e.g., in peristaltic and secretory reflexes in response to chemical or mechanical stimuli of the gut. Intestinal 5-HT is inactivated by metabolic degr...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2006.04.005
更新日期:2006-08-01 00:00:00
abstract::Idiopathic pulmonary fibrosis (IPF) is a debilitating condition where excess collagen deposition occurs in the extracellular matrix. At first sight, it is expected that the level of different kinds of matrix metalloproteinases might be downregulated in IPF as it is a matrix degrading collagenase. However, the role of ...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2019.104591
更新日期:2020-02-01 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::We studied here the effect of a wide range of adenosine concentration and time of preincubation, on the histamine release induced in the guinea pig mast cells by different stimulus. Adenosine (10(-5)-10(-3)m) potentiated the histamine release induced by antigen in the guinea pig heart (isolated and dispersed tissue) a...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1999.0589
更新日期:2000-03-01 00:00:00
abstract::Alcoholic liver disease (ALD) is a major cause of chronic liver disease worldwide that afflicts human health. With the in-depth study of the disease, its pathogenesis has gradually become clear. Although great breakthroughs have been made in the research of ALD, the research and development of drugs related to ALD has...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2019.104501
更新日期:2019-12-01 00:00:00
abstract::The formation of reactive oxygen species (ROS) appears to play a significant role in many pathological states including cystic fibrosis and asthma. Although stimulated inflammatory cells represent a major source of oxygen metabolites and these cells are able to generate the potent oxidant hypochlorous acid (HOCl) effe...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1999.0628
更新日期:2000-05-01 00:00:00
abstract::We aimed to elucidate the role of vitamin D supplementation on adipokines through a systematic review and a meta-analysis of randomized placebo-controlled trials (RCTs). The search included PUBMED, Scopus, Web of Science and Google Scholar through July 1st, 2015. Finally we identified 9 RCTs and 484 participants. Meta...
journal_title:Pharmacological research
pub_type: 杂志文章,meta分析,评审
doi:10.1016/j.phrs.2016.03.035
更新日期:2016-05-01 00:00:00
abstract::In this study, we have addressed the pharmacogenomic basis of the response of gastrointestinal tumors to six anticancer drugs using a panel of fifteen cell lines derived from pancreatic, stomach and biliary tract cancers. We determined the constitutive expression levels of 96 genes, whose encoded proteins contribute t...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.09.007
更新日期:2016-11-01 00:00:00
abstract::The objective of this study was to investigate the effects of 3-aminobenzamide (3-AB) on tissue damage in lung after hind limb ischemia-reperfusion (I/R), by assessing blood biochemical assay and histopathological analysis. Thirty-five adult Wistar rats were divided into five groups. After application of anaesthesia b...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2004.11.007
更新日期:2005-05-01 00:00:00
abstract::Advanced glycation end-products (AGE) and the receptor for AGE (RAGE) have been linked to numerous diabetic vascular complications. RAGE activation promotes a self-sustaining state of chronic inflammation and has been shown to induce apoptosis in various cell types. Although previous studies in vascular smooth muscle ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2015.12.015
更新日期:2016-02-01 00:00:00
abstract::In incubated blood mononuclear cells from normal subjects bezafibrate inhibited the incorporation of 14C-acetate into squalene, methylsterols and cholesterol. Similarly, the drug produced a sharp decrease of the incorporation of labelled 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) into non-saponifiable lipids, whi...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(89)80002-7
更新日期:1989-05-01 00:00:00
abstract::Adaptive responses to stress are critical to enhance physical and mental well-being, but excessive or prolonged stress may cause inadaptability and increase the risks of psychiatric disorders, such as depression. GABABR signaling is fundamental to brain function and has been identified in neuropsychiatric disorders. K...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.105355
更新日期:2021-01-01 00:00:00
abstract::Pre-eclampsia (PE) is a complication of pregnancy that is associated with mortality and morbidity in mothers and fetuses worldwide. Oxygen dysregulation in the placenta, abnormal remodeling of the spiral artery, defective placentation, oxidative stress at the fetal-maternal border, inflammation and angiogenic impairme...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2020.104692
更新日期:2020-05-01 00:00:00
abstract::Changes in vascular responsiveness are the basis for some of the cardiovascular complications in cholestasis. Since the duration of cholestasis is important in determining the degree of the complications, we investigated the time-course dependent evolution of vascular relaxation responsiveness in the aortic rings of c...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.2001.0892
更新日期:2001-12-01 00:00:00
abstract::Cysteamine, a potent somatostatin depletor, was used in the present study to investigate the role of endogenous somatostatin in acute peripheral inflammation. The acute inflammation was induced by intraplantar injection of carrageenan (1%), histamine (5 micromol), or formalin (2.5%) in the rat hind paw. The induced in...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.2002.0955
更新日期:2002-04-01 00:00:00
abstract::The metabolism of arachidonic acid by cytochrome P450 (CYP) epoxygenases generates epoxyeicosatrienoic acids (EETs) which affect numerous cellular process including Ca(2+) signaling and the activity of Ca(2+)-dependent K(+) channels. The expression of the CYP epoxygenase(s) that generate EETs in endothelial cells is n...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2003.11.016
更新日期:2004-06-01 00:00:00
abstract:AIM:To evaluate canrenone effects compared to other therapies on cardiovascular mortality in patients with chronic heart failure (CHF) and preserved systolic function after 10 years of evaluation. METHODS:We enrolled 532 patients with CHF and preserved systolic function. Patients were followed with a mean follow-up of...
journal_title:Pharmacological research
pub_type: 杂志文章,多中心研究
doi:10.1016/j.phrs.2018.11.037
更新日期:2019-03-01 00:00:00
abstract::The lack of availability of appropriate medicines for children is an extensive and well known problem. As a consequence off label or unlicensed administration of medicinal products in every day paediatric practice is frequent. A variety of obstacles hinder the development of paediatric indications for drugs primarily ...
journal_title:Pharmacological research
pub_type: 社论,评审
doi:10.1016/j.phrs.2011.01.016
更新日期:2011-09-01 00:00:00
abstract::Epidemiological, clinical and animal studies revealed that sex differences exist in the manifestation and outcome of cardiovascular disease (CVD). The underlying molecular mechanisms implicated in these sex differences are not fully understood. The reasons for sex differences in CVD are definitely multifactorial, but ...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2017.01.019
更新日期:2017-05-01 00:00:00
abstract::Receptor concentrations for adrenaline, steroid hormones, PGF2alpha, LH and FSH were measured in the hypophysis and ovary of dairy cows with ovarian cysts and the results were compared with those of healthy animals. Significant modifications were found in all receptor concentrations, either between follicular and lute...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1998.0442
更新日期:1999-04-01 00:00:00
abstract::Dyslipidemia and hyperglycemia are associated with an increased risk of ischemic cardiovascular disease. Positive effects of a nutraceutical combination comprising red yeast rice, berberine, policosanol, astaxanthin, coenzyme Q10 and folic acid (NComb) on plasma lipid and glucose levels have been reported in some but ...
journal_title:Pharmacological research
pub_type: 杂志文章,meta分析,评审
doi:10.1016/j.phrs.2016.04.021
更新日期:2016-08-01 00:00:00
abstract:BACKGROUND AND PURPOSE:The enzymes fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) hydrolyze endogenous cannabinoids (eCBs), N-arachidonoyl ethanolamine (AEA) and 2-arachidonoyl glycerol (2-AG), respectively. These enzymes also metabolize eCB analogs such as lipoamines and 2-acyl glycerols, most of...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.04.020
更新日期:2016-08-01 00:00:00
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::In this study, we evaluated anti-hyperglycemic effect and body weight reduction activity of Gymnema yunnanense extract in obese ob/ob and diabetic db/db mice. Animals received daily intraperitoneal injections of the extract 100 mg/kg for 12 days. On Day 5, the extract-treated ob/ob mice had significantly lower fasting...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(02)00322-5
更新日期:2003-04-01 00:00:00
abstract::Derivatization of phenothiazine (PTZ, 1) has been a commonly used method to develop drugs with various pharmacological properties. In the present study, a series of PTZ derivatives 1-11 were investigated on the inhibition of the cloned α7 subunit of the human nicotinic acetylcholine receptor (α7-nAChR) expressed in Xe...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2012.05.008
更新日期:2012-09-01 00:00:00
abstract::Hepatitis E virus (HEV) is the most common cause of viral hepatitis worldwide. Genotypes 1 and 2 (GT1 and GT2) are mainly present in developing countries, while GT3 and GT4 are prevalent in developed and high-income countries. In the majority of cases, HEV causes a self-limiting hepatitis. GT3 and GT4 can be responsib...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2018.02.030
更新日期:2018-04-01 00:00:00
abstract::We tested the efficacy of novel cyclooxygenase 2 (COX-2) inhibitors in counteracting glia-driven neuroinflammation induced by the amyloidogenic prion protein fragment PrP90-231 or lipopolysaccharide (LPS). In search for molecules with higher efficacy than celecoxib, we focused our study on its 2,3-diaryl-1,3-thiazolid...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.09.010
更新日期:2016-11-01 00:00:00