Whey Protein in Cancer Therapy: A Narrative Review
Publication date: Available online 18 April 2019Source: Pharmacological ResearchAuthor(s): Filipe J. Teixeira, Heitor O. Santos, Scott L. Howell, Gustavo D. PimentelAbstractCancer remains a public health challenge in the identification and development of ideal pharmacological therapies and dietary strategies. The use of whey protein as a dietary strategy is widespread in the field of oncology. The two types of whey protein, sweet or acid, result from several processing techniques and possess distinct protein subfraction compositions. Mechanistically, whey protein subfractions have specific anti-cancer effects. Alpha-lactal...
Source: Pharmacological Research - April 20, 2019 Category: Drugs & Pharmacology Source Type: research

Interprofessional and interdisciplinary collaboration for early phase oncological clinical trials in academia – myo-Inositoltrispyrophophate as model
Publication date: Available online 19 April 2019Source: Pharmacological ResearchAuthor(s): Regina Grossmann, Marcel Andre Schneider, Michael Linecker, Jean-Marie Lehn, Claude Nicolau, Martin Traber, Fabian Tay, Diego Vicente, Alexander Jetter, Annette Mollet, Thomas Szucs, Rolf Graf, Pierre-Alain Clavien, Perparim Limani (Source: Pharmacological Research)
Source: Pharmacological Research - April 20, 2019 Category: Drugs & Pharmacology Source Type: research

Drugs and hepatic transporters: A review
Publication date: Available online 17 April 2019Source: Pharmacological ResearchAuthor(s): Alexander Jetter, Gerd A. Kullak-UblickAbstractThe liver is the primary organ for the metabolic degradation of xenobiotics. Transmembrane transport proteins from the ABC and the SLC families mediate the uptake of endogenous compounds and xenobiotics into the hepatocyte as well as their elimination from the cells. Multiple processes are involved. The uptake of xenobiotics in hepatocytes is mediated by organic anion transporting polypeptides (OATPs) and by organic anion and cation transporters (OATs and OCTs). The elimination of drugs ...
Source: Pharmacological Research - April 18, 2019 Category: Drugs & Pharmacology Source Type: research

Endothelial Progenitor Cells: potential novel therapeutics for ischaemic stroke
Publication date: Available online 17 April 2019Source: Pharmacological ResearchAuthor(s): Ulvi BayraktutanABSTRACTStroke is classified into two main groups depending on its aetiology; ischaemic stroke and haemorrhagic stroke which successively develop from the occlusion or rupture of an artery leading to the brain. Despite being the leading cause of human cerebral damage, there is currently no medical therapy for haemorrhagic stroke and thrombolysis with recombinant tissue plasminogen activator remains the only approved pharmacotherapy for ischaemic stroke. However, due to its short therapeutic window (first 4.5 h ...
Source: Pharmacological Research - April 18, 2019 Category: Drugs & Pharmacology Source Type: research

Honokiol for cancer therapeutics: A traditional medicine that can modulate multiple oncogenic targets
Publication date: Available online 17 April 2019Source: Pharmacological ResearchAuthor(s): Kishore Banik, Abhishek Manoj Ranaware, Vishwas Deshpande, Savita Pravin Nalawade, Ganesan Padmavathi, Devivasha Bordoloi, Bethsebie Lalduhsaki Sailo, Muthu K. Shanmugam, Lu Fan, Frank Arfuso, Gautam Sethi, Ajaikumar B. KunnumakkaraAbstractIn spite of billions of dollars expended on cancer research every year, the incidence rate and the mortality rate due to this widespread disease has increased drastically over the last few decades. Recent reports from the World Health Organization advocate that overall global cancer burden and deat...
Source: Pharmacological Research - April 17, 2019 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: May 2019Source: Pharmacological Research, Volume 143Author(s): (Source: Pharmacological Research)
Source: Pharmacological Research - April 17, 2019 Category: Drugs & Pharmacology Source Type: research

Improvements of Symptoms of Alzheimer`s Disease by Inhibition of the Angiotensin System
Publication date: Available online 13 April 2019Source: Pharmacological ResearchAuthor(s): Ursula Quitterer, Said AbdAllaAbstractWith ageing of the global society, the frequency of ageing-related neurodegenerative diseases such as Alzheimer`s disease (AD) is on the rise worldwide. Currently, there is no cure for AD, and the four drugs approved for AD only have very small effects on AD symptoms. Consequently, there are enormous efforts worldwide to identify new targets for treatment of AD. Approaches that interfere with classical neuropathologic features of AD, such as extracellular senile plaques formed of aggregated amylo...
Source: Pharmacological Research - April 14, 2019 Category: Drugs & Pharmacology Source Type: research

Network Pharmacology Based investigation into the Effect and mechanism of Modified Sijunzi Decoction against the subtypes of Chronic Atrophic Gastritis
In this study, immune repertoire sequencing techniques combined with symptom scores, electronic gastroscopy as well as pathologic changes were used to evaluate the effect and the underlying mechanism of Modified Sijunzi Decoction (MSD) in treating CAG. The results showed that MSD could relieve CAG symptoms, improve pathologic changes in CAG with fatigue and tiredness symptom, but with no help in CAG with reversal heat symptom. Moreover, MSD could regulate immune disorders in CAG with fatigue and tiredness symptom, and 7 TCR biomarkers were explored in CAG patients with immune disorders. All these results indicated that MSD...
Source: Pharmacological Research - April 14, 2019 Category: Drugs & Pharmacology Source Type: research

LongShengZhi Capsule reduces carrageenan-induced thrombosis by reducing activation of platelets and endothelial cells
Publication date: Available online 12 April 2019Source: Pharmacological ResearchAuthor(s): Qi Li, Yi Chen, Dan Zhao, Shu Yang, Shuang Zhang, Zhuo Wei, Yong Wang, Ke Qian, Buchang Zhao, Yan Zhu, Yuanli Chen, Yajun Duan, Jihong Han, Xiaoxiao YangAbstractFormation of thrombosis is associated with activation of platelets and endothelial cells. The effect of LongShengZhi Capsule (LSZ), a traditional Chinese medicine used for treatment of vascular diseases, on thrombosis was investigated in this study. BALB/c mice were induced thrombosis by injection of carrageenan while receiving pre or simultaneous LSZ treatment. We also compa...
Source: Pharmacological Research - April 14, 2019 Category: Drugs & Pharmacology Source Type: research

Publisher's note
Publication date: Available online 8 April 2019Source: Pharmacological ResearchAuthor(s): (Source: Pharmacological Research)
Source: Pharmacological Research - April 9, 2019 Category: Drugs & Pharmacology Source Type: research

Cordycepin Inhibits Drug-resistance Non-small Cell Lung Cancer Progression by Activating AMPK Signaling Pathway
Publication date: Available online 8 April 2019Source: Pharmacological ResearchAuthor(s): Chunli Wei, Xiaojun Yao, Zebo Jiang, Yuwei Wang, Dianzheng Zhang, Xi Chen, Xingxing Fan, Chun Xie, Jingliang Cheng, Junjiang Fu, Elaine Lai-Han LeungAbstractLung cancer is the most commonly diagnosed cancer worldwide and it is also the most leading cause of cancer-related deaths. Although multiple generations of targeted therapeutic drugs such as gefitinib and afatinib specifically targeting the epidermal growth factor receptor (EGFR) pathway are currently available for lung cancer treatment, none of them can escape their eventual dru...
Source: Pharmacological Research - April 9, 2019 Category: Drugs & Pharmacology Source Type: research

Molecular targets of fenofibrate in the cardiovascular-renal axis: a unifying perspective of its pleiotropic benefits
Publication date: Available online 7 April 2019Source: Pharmacological ResearchAuthor(s): Pitchai Balakumar, Ramanathan Sambathkumar, Nanjaian Mahadevan, Abdullatif Bin Muhsinah, Abdulrhman Alsayari, Nallasamy Venkateswaramurthy, Sokkalingam A DhanarajAbstractThe activation of peroxisome proliferator-activated receptor α (PPARα) is a key pharmacological drug target for dyslipidemic management. Dyslipidemia is associated with abnormal serum lipid profiles viz. elevated total cholesterol, high triglyceride, elevated low-density lipoprotein cholesterol, and reduced high-density lipoprotein cholesterol levels. Feno...
Source: Pharmacological Research - April 7, 2019 Category: Drugs & Pharmacology Source Type: research

Hydrogen sulfide stabilizes atherosclerotic plaques in apolipoprotein E knockout mice
In conclusion, H2S exerts protective effects against atherogenesis at least partly by stabilizing atherosclerotic plaque.Graphical abstract (Source: Pharmacological Research)
Source: Pharmacological Research - April 6, 2019 Category: Drugs & Pharmacology Source Type: research

Saponins regulate intestinal inflammation in colon cancer and IBD
Publication date: Available online 5 April 2019Source: Pharmacological ResearchAuthor(s): Jianyi Dong, Wei Liang, Tianxiao Wang, Jingru Sui, Jingyu Wang, Zhaobin Deng, Dapeng ChenAbstractThe saponins are natural surface-active glycosides which are the principal components of many popular herbal medicinal plants such as ginseng, astragalus, and bupleurum. Recent studies have suggested that saponins can exert strong anti-inflammatory effects and induce immune homeostasis in many diseases. Intestinal-inflammation-related digestive diseases include inflammatory bowel disease (IBD), irritable bowel syndrome, intestinal ischemia...
Source: Pharmacological Research - April 6, 2019 Category: Drugs & Pharmacology Source Type: research

Important roles of Protein Tyrosine Phosphatase PTPN12 in Tumor Progression
Publication date: Available online 5 April 2019Source: Pharmacological ResearchAuthor(s): Chaelin Lee, Inmoo RheeAbstractProtein tyrosine phosphatases (PTPs), which are ubiquitously expressed in hematopoietic and non-hematopoietic cells, are critical for regulating cell proliferation as well as differentiation in the physiology of multicellular organisms. PTPs regulate the intracellular signaling mechanism of immune cells via dephosphorylation of multiple targets and are associated with the onset of various autoimmune diseases through genomic alterations. PTPs also affect disease through their role in innate and/or acquire...
Source: Pharmacological Research - April 6, 2019 Category: Drugs & Pharmacology Source Type: research

Mitochondrial dna: a new driver for sex differences in spontaneous hypertension
This study contributes to the understanding of a need for more personalized therapeutic strategies for men and women with hypertension. Keywords: Sex differences, Arterial hypertension, Mitochondrial DNA, Toll-Like receptor 9.Graphical abstract (Source: Pharmacological Research)
Source: Pharmacological Research - April 6, 2019 Category: Drugs & Pharmacology Source Type: research

Serelaxin (recombinant human relaxin-2) treatment affects the endogenous synthesis of long chain poly-unsaturated fatty acids and induces substantial alterations of lipidome and metabolome profiles in rat cardiac tissue
Conclusion and Implications: Serelaxin (human recombinant relaxin-2) treatment induces significant changes in cardiac major components of the membrane lipid bilayer such as glycerophospholipids and sphingolipids, known to have structural roles but also very relevant regulatory effects in cardiac function. Serelaxin induced also modifications in several aminoacids of high influence in cardiac energy metabolism regulation. Our results highlight the need to further understand the role of relaxin-2 in the regulation of cardiac energy metabolism, in the context of the therapeutic strategies for the treatment of cardiometabolic ...
Source: Pharmacological Research - April 6, 2019 Category: Drugs & Pharmacology Source Type: research

Complex regulation of ecto-5′-nucleotidase/CD73 and A2AR-MEdiated adenosine signaling at neurovascular unit: A link between acute and chronic neuroinflammation
Publication date: Available online 5 April 2019Source: Pharmacological ResearchAuthor(s): Nadezda NedeljkovicAbstractThe review summarizes available data regarding the complex regulation of CD73 at the neurovascular unit (NVU) during neuroinflammation. Based on available data we propose the biphasic pattern of CD73 regulation at NVU, with an early attenuation and a postponed up-regulation of CD73 activity. Transient attenuation of CD73 activity on leukocyte/vascular endothelium and leukocyte/astrocyte surface, required for the initiation of a neuroinflammatory response, may be effectuated either by catalytic inhibition of ...
Source: Pharmacological Research - April 6, 2019 Category: Drugs & Pharmacology Source Type: research

Lipid-regulating properties of butyric acid and 4-phenylbutyric acid: Molecular mechanisms and therapeutic applications
Publication date: Available online 5 April 2019Source: Pharmacological ResearchAuthor(s): Bo He, Régis MoreauAbstractIn the past two decades, significant advances have been made in the etiology of lipid disorders. Concomitantly, the discovery of new liporegulatory functions of certain short-chain fatty acids has generated interest in their clinical applications. In particular, butyric acid (BA) and its derivative, 4-phenylbutyric acid (PBA), afford health benefits against lipid disorders while being generally well tolerated by animals and humans. This review examines the evidence from cell, animal and human studies ...
Source: Pharmacological Research - April 6, 2019 Category: Drugs & Pharmacology Source Type: research

Carbon nanomaterials and amyloid-beta interactions: potentials for the detection and treatment of Alzheimer's disease?
Publication date: May 2019Source: Pharmacological Research, Volume 143Author(s): Mohammad Mohajeri, Behzad Behnam, George E. Barreto, Amirhossein SahebkarAbstractCarbon-based nanomaterials have unique physicochemical properties relevant to the diagnosis and treatment of various diseases. There have been many reports indicating that carbon nanomaterials (CNMs) can interact and perturb biomolecules such as proteins and amyloid structures. This review is an attempt to reflect the role of CNMs in the treatment and detection of Alzheimer's disease (AD). The potential of CNMs in the field of neuroscience has also been reviewed. ...
Source: Pharmacological Research - April 6, 2019 Category: Drugs & Pharmacology Source Type: research

The Problem of Poly-pharmacotherapy in Patients on a Mephedrone Binge
Publication date: Available online 2 April 2019Source: Pharmacological ResearchAuthor(s): M. Ordak, T. Nasierowski, E. Muszynska (Source: Pharmacological Research)
Source: Pharmacological Research - April 3, 2019 Category: Drugs & Pharmacology Source Type: research

Corrigendum to “Targeting ERK1/2 protein-serine/threonine kinases in human cancers” [Pharmcol. Res. 142 (2019) 151–168]
Publication date: Available online 3 April 2019Source: Pharmacological ResearchAuthor(s): Robert Roskoski (Source: Pharmacological Research)
Source: Pharmacological Research - April 3, 2019 Category: Drugs & Pharmacology Source Type: research

Plant lectins in cancer therapeutics: Targeting apoptosis and autophagy-dependent cell death
Publication date: Available online 3 April 2019Source: Pharmacological ResearchAuthor(s): Sujit K Bhutia, Prashanta K Panda, Niharika Sinha, Prakash P Praharaj, Chandra S Bhol, Debasna P Panigrahi, Kewal K Mahapatra, Sarbari Saha, Srimanta Patra, Soumya R Mishra, Bishnu P Behera, Shankargouda Patil, Tapas K MaitiAbstractPlant lectins are non-immunoglobin in nature and bind to the carbohydrate moiety of the glycoconjugates without altering any of the recognized glycosyl ligands. Plant lectins have found applications as cancer biomarkers for recognizing the malignant tumor cells for the diagnosis and prognosis of cancer. Int...
Source: Pharmacological Research - April 3, 2019 Category: Drugs & Pharmacology Source Type: research

Dysregulated Autophagy in COPD: A Pathogenic Process to Be Deciphered
Publication date: Available online 3 April 2019Source: Pharmacological ResearchAuthor(s): W.S. Daniel Tan, Han-Ming Shen, W.S. Fred WongAbstractAutophagy is an evolutionary conserved process that is responsible for maintaining cellular homeostasis through lysosome-dependent degradation of damaged proteins, lipid and organelles. When autophagy is dysregulated by factors such as cigarette smoking, environmental insults and ageing, it can lead to formation of aggresome-bodies and enhanced production of reactive oxygen species (ROS), of which contribute to the pathogenesis of chronic obstructive pulmonary disease (COPD). This ...
Source: Pharmacological Research - April 3, 2019 Category: Drugs & Pharmacology Source Type: research

Carbon nanomaterials and amyloid beta interactions: Possible potentials in the detection and treatment of Alzheimer's disease
Publication date: Available online 31 March 2019Source: Pharmacological ResearchAuthor(s): Mohammad Mohajeri, Behzad Behnam, George E. Barreto, Amirhossein SahebkarAbstractCarbon-based nanomaterials have unique physicochemical properties relevant to the diagnosis and treatment of various diseases. There have been many reports indicating that carbon nanomaterials (CNMs) can interact and perturb biomolecules such as proteins and amyloid structures. This review is an attempt to reflect the role of CNMs in the treatment and detection of Alzheimer's disease (AD). The potential of CNMs in the field of neuroscience has also been ...
Source: Pharmacological Research - April 1, 2019 Category: Drugs & Pharmacology Source Type: research

Protective or deleterious role of Wnt/beta-catenin signaling in diabetic nephropathy: An unresolved issue
Publication date: Available online 29 March 2019Source: Pharmacological ResearchAuthor(s): Qiaoyan Guo, Wei Zhong, Aosong Duan, Guanggong Sun, Wenpeng Cui, Xiaohua Zhuang, Lihua LiuAbstractIn recent years, the Wnt/β-catenin signaling has gained tremendous attention due to its ability to modulate a number of diseases including diabetic nephropathy. Studies have shown that there is decrease in the secretion of Wnt proteins including Wnt4, 5a and Wnt 6 during high glucose concentration or diabetic conditions, which leads to decreased translocation of β-catenin to nucleus. The down-regulation of Wnt/β-catenin si...
Source: Pharmacological Research - March 31, 2019 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: April 2019Source: Pharmacological Research, Volume 142Author(s): (Source: Pharmacological Research)
Source: Pharmacological Research - March 29, 2019 Category: Drugs & Pharmacology Source Type: research

Cardiovascular events with pcsk9 inhibitors: an updated meta-analysis of randomised controlled trials
Publication date: Available online 26 March 2019Source: Pharmacological ResearchAuthor(s): Manuela Casula, Elena Olmastroni, Mezio T. Boccalari, Elena Tragni, Angela Pirillo, Alberico L. CatapanoAbstractThe therapy with proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors efficiently reduces plasma cholesterol levels, which has been recently associated with improvement in cardiovascular outcomes. This meta-analysis aimed at investigating the safety and efficacy of treatment with the clinically available anti-PCSK9 monoclonal antibodies (mAbs) in all published randomized clinical trials (RCTs), updating the avai...
Source: Pharmacological Research - March 28, 2019 Category: Drugs & Pharmacology Source Type: research

Anti-Arrhythmic Drug Therapy in Implantable Cardioverter-Defibrillator Recipients
Publication date: Available online 23 March 2019Source: Pharmacological ResearchAuthor(s): Ahmed AlTurki, Riccardo Proietti, Vincenzo Russo, Tarvinder Dhanjal, Prithwish Banerjee, Vidal EssebagAbstractImplantable 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 pharmacological primary and secondary prevention of ventricular arrhythmias. In addition to their established effi...
Source: Pharmacological Research - March 25, 2019 Category: Drugs & Pharmacology Source Type: research

Dysregulation of the hippo pathway signaling in aging and cancer
Publication date: Available online 22 March 2019Source: Pharmacological ResearchAuthor(s): Yiu To Yeung, Angelica Guerrero-Castilla, Mercedes Cano, Mario F. Muñoz, Antonio Ayala, Sandro ArgüellesAbstractHuman beings are facing emerging degenerative and cancer diseases, in large part, as a consequence of increased life expectancy. In the near future, researchers will have to put even more effort into fighting these new challenges, one of which will be prevention of cancer while continuing to improve the aging process through this increased life expectancy. In the last few decades, relevance of the Hippo pathway ...
Source: Pharmacological Research - March 23, 2019 Category: Drugs & Pharmacology Source Type: research

A review of gene- and cell-based therapies for familial hypercholesterolemia
Publication date: Available online 22 March 2019Source: Pharmacological ResearchAuthor(s): Saeideh Hajighasemi, Armita Mahdavi Gorabi, Vanessa Bianconi, Matteo Pirro, Maciej Banach, Hossein Ahmadi tafti, Željko Reiner, Amirhossein SahebkarAbstractFamilial hypercholesterolemia (FH) is a genetic autosomal dominant disorder caused by an impaired receptor-mediated low-density lipoprotein (LDL) removal from the circulation, mainly due to disruptive autosomal co-dominant mutations in the LDL receptor (LDLr) gene, but also less frequently in the apolipoprotein B100 (APOB) and proprotein convertase subtilisin/kexin type 9 (PCSK9)...
Source: Pharmacological Research - March 23, 2019 Category: Drugs & Pharmacology Source Type: research

Anticoagulant Selection for Patients with VTE—Evidence from A Systematic Literature Review of Network Meta-analyses
Publication date: Available online 21 March 2019Source: Pharmacological ResearchAuthor(s): Alexander T. Cohen, Samantha E. Berger, Dušan Milenković, Nathan R. Hill, Steven ListerAbstractThe aim of this study was to systematically review published network meta-analyses (NMAs) that compare venous thromboembolism (VTE) treatments.A systematic literature search (in MEDLINE, Embase, and Cochrane Database of Systematic Reviews through September 2017) was conducted to identify NMAs that compared the safety and efficacy of direct oral anticoagulants (DOACs) for the treatment of VTE in the acute and extended treatment setti...
Source: Pharmacological Research - March 23, 2019 Category: Drugs & Pharmacology Source Type: research

Adenylyl cyclase 7 and neuropsychiatric disorders: A new target for depression?
Publication date: Available online 20 March 2019Source: Pharmacological ResearchAuthor(s): Tatum Price, Tarsis F. BrustAbstractAdenylyl cyclases (ACs) are enzymes that catalyze the production of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP). Humans express nine isoforms of membranous ACs and a soluble AC. Studies with genetic knockout or overexpression rodent models have indicated that AC isoforms may be targeted to achieve specific therapeutic outcomes. AC1, for instance, has been suggested and pursued as a target for relieving pain. Notably, previous studies examining genetically modified mice a...
Source: Pharmacological Research - March 22, 2019 Category: Drugs & Pharmacology Source Type: research

Expanding spectrum of anticancer drug, imatinib, in the disorders affecting brain and spinal cord
Publication date: Available online 19 March 2019Source: Pharmacological ResearchAuthor(s): Manish Kumar, Ritu Kulshrestha, Nirmal Singh, Amteshwar Singh JaggiAbstractImatinib is a tyrosine kinase inhibitor and is used as a first line drug in the treatment of Philadelphia-chromosome-positive chronic myeloid leukaemia and gastrointestinal stromal tumors. Being tyrosine kinase inhibitor, imatinib modulates the activities of Abelson gene (c-Abl), Abelson related gene (ARG), platelet-derived growth factor receptor (PDGFR), FMS-like tyrosine kinase 3 (FLT3), lymphocyte-specific protein (Lck), mitogen activated protein kinase (MA...
Source: Pharmacological Research - March 20, 2019 Category: Drugs & Pharmacology Source Type: research

Cholinergic System in Sleep Regulation of Emotion and Motivation
Publication date: Available online 17 March 2019Source: Pharmacological ResearchAuthor(s): Ping Mu, Yanhua H. HuangAbstractSleep profoundly regulates our emotional and motivational state of mind. Human brain imaging and animal model studies are providing initial insights on the underlying neural mechanisms. Here, we focus on the brain cholinergic system, including cholinergic neurons in the basal forebrain, ventral striatum, habenula, and brain stem. Although much is learned about cholinergic regulations of emotion and motivation, less is known on their interactions with sleep. Specifically, we present an anatomical framew...
Source: Pharmacological Research - March 19, 2019 Category: Drugs & Pharmacology Source Type: research

Mechanisms of statin-associated skeletal muscle-associated symptoms
Publication date: Available online 12 March 2019Source: Pharmacological ResearchAuthor(s): Jamal Bouitbir, Gerda M. Sanvee, Miljenko V. Panajatovic, François Singh, Stephan KrähenbühlAbstractStatins lower the serum low-density lipoprotein cholesterol and prevent cardiovascular events by inhibiting 3-hydroxy-3-methyl-glutaryl-CoA reductase. Although the safety of statins is documented, many patients ingesting statins may suffer from skeletal muscle-associated symptoms (SAMS). Importantly, SAMS are a common reason for stopping the treatment with statins. Statin-associated muscular symptoms include fatigue, w...
Source: Pharmacological Research - March 14, 2019 Category: Drugs & Pharmacology Source Type: research

Properties of FDA-approved small molecule protein kinase inhibitors
Publication date: Available online 13 March 2019Source: Pharmacological ResearchAuthor(s): Robert RoskoskiAbstractBecause mutations, overexpression, and dysregulation of protein kinases play essential roles in the pathogenesis of many illnesses, this enzyme family has become one of the most important drug targets in the past 20 years. The US FDA has approved 48 small molecule protein kinase inhibitors, nearly all of which are orally effective with the exceptions of netarsudil (which is given as an eye drop) and temsirolimus (which is given intravenously). Of the 48 approved drugs, the majority (25) target receptor protein-...
Source: Pharmacological Research - March 14, 2019 Category: Drugs & Pharmacology Source Type: research

Novel urokinase-plasminogen activator inhibitor SPINK13 inhibits growth and metastasis of hepatocellular carcinoma in vivo
Publication date: Available online 9 March 2019Source: Pharmacological ResearchAuthor(s): Ling Wei, Yongzhi Lun, Xiaoping Zhou, Shang He, Lijuan Gao, Yan Liu, Zheng He, Baoming Li, Chengbin WangAbstractAdvanced hepatocellular carcinoma (HCC) is a highly aggressive malignancy that is a serious threat to the public health system of China. Urokinase-plasminogen activator (uPA) can promote the invasive growth and metastasis of HCC cells by activating matrix metalloproteinases (MMPs), leading to the breakage of the extra-cellular matrix. uPA is a promising target for advanced HCC treatment. In this stuy the expression of uPA wa...
Source: Pharmacological Research - March 10, 2019 Category: Drugs & Pharmacology Source Type: research

Cortisol-induced srsf3 expression promotes gr splicing, rack1 expression and breast cancer cells migration
Publication date: Available online 9 March 2019Source: Pharmacological ResearchAuthor(s): Erica Buoso, Melania Ronfani, Marilisa Galasso, Denise Ventura, Emanuela Corsini, Marco RacchiAbstractRecent data have demonstrated that triple negative breast cancer (TNBC) with high glucocorticoid receptor (GR) expression are associated to therapy resistance and increased mortality. Given that GR alternative splicing generates mainly GRα, responsible of glucocorticoids action, we investigated its role in the regulation of RACK1 (Receptor for Activated C Kinase 1), a scaffolding protein with a GRE (Glucocorticoid Response Eleme...
Source: Pharmacological Research - March 10, 2019 Category: Drugs & Pharmacology Source Type: research

Drugs targeting SIRT1, a new generation of therapeutics for osteoporosis and other bone related disorders?
Publication date: Available online 9 March 2019Source: Pharmacological ResearchAuthor(s): Kayvan ZainabadiAbstractWith an aging population and limited treatment options, osteoporosis currently represents a significant public health challenge. Recent animal studies indicate that longevity-associated SIRT1 may serve as an attractive pharmacological target for the treatment of osteoporosis and other bone related disorders. Pre-clinical studies demonstrate that mice treated with SIRT1 agonists show protection against age-related, post-menopausal, and disuse models of osteoporosis. Conversely, SIRT1 knockout models display low ...
Source: Pharmacological Research - March 10, 2019 Category: Drugs & Pharmacology Source Type: research

Hydroxytyrosol protects from aging process via ampk and autophagy; a review of its effects on cancer, metabolic syndrome, osteoporosis, immune-mediated and neurodegenerative diseases
Publication date: Available online 7 March 2019Source: Pharmacological ResearchAuthor(s): Rocío M. de Pablos, Ana María Espinosa-Oliva, Ruth Hornedo-Ortega, Mercedes Cano, Sandro ArguellesAbstractAging is a complex process. It is considered a risk factor for several diseases such as cancer, neurodegenerative diseases, cardiovascular diseases, and diabetes, most of which have an oxidative and inflammatory base. Given that life expectancy is increasing, there is a present interest in the search for anti-aging strategies that allow a healthy aging. Interestingly, in Spain, where the Mediterranean Diet (MD) is th...
Source: Pharmacological Research - March 9, 2019 Category: Drugs & Pharmacology Source Type: research

Corrigendum to “The role of STAG2 in bladder cancer” [Pharmacol. Res. 131 (2018) 143–149]
Publication date: Available online 8 March 2019Source: Pharmacological ResearchAuthor(s): Lanni Aquila, Joyce Ohm, Anna Woloszynska-Read (Source: Pharmacological Research)
Source: Pharmacological Research - March 9, 2019 Category: Drugs & Pharmacology Source Type: research

Novel function of VEGF-B as an antioxidant and therapeutic implications
Publication date: Available online 6 March 2019Source: Pharmacological ResearchAuthor(s): Rongyuan Chen, Chunsik Lee, Xianchai Lin, Chen Zhao, Xuri LiAbstractOxidative stress, due to insufficiency of antioxidants or over-production of oxidants, can lead to severe cell and tissue damage. Oxidative stress occurs constantly and has been shown to be involved in innumerable diseases, such as degenerative, cardiovascular, neurological, and metabolic disorders, cancer, and aging, thus highlighting the vital need of antioxidant defense mechanisms. Vascular endothelial growth factor B (VEGF-B) was discovered a long time ago, and is...
Source: Pharmacological Research - March 7, 2019 Category: Drugs & Pharmacology Source Type: research

Safety of red yeast rice supplementation: a systematic review and meta-analysis of randomized controlled trials
Publication date: Available online 4 March 2019Source: Pharmacological ResearchAuthor(s): Federica Fogacci, Maciej Banach, Dimitri P. Mikhailidis, Eric Bruckert, Peter P. Toth, Gerald F. Watts, Željko Reiner, John Mancini, Manfredi Rizzo, Olena Mitchenko, Daniel Pella, Zlatko Fras, Amirhossein Sahebkar, Michal Vrablik, Arrigo F.G. Cicero, on behalf of the Lipid and Blood Pressure Meta-analysis Collaboration (LBPMC) Group the International Lipid Expert Panel (ILEP)AbstractRecently, concerns regarding the safety of red yeast rice (RYR) have been raised after the publication of some case reports claiming toxicity. Since the ...
Source: Pharmacological Research - March 5, 2019 Category: Drugs & Pharmacology Source Type: research

Biased signaling agonist of Dopamine D3 receptor induces receptor internalization independent of β-Arrestin recruitment
In this study, using radioligand binding assay, immunoblot or immunocytochemistry methods, we observed that SK608 induced internalization of human D3R stably expressed in CHO, HEK and SH-SY5Y cells which are derived from neuroblastoma cells, suggesting that it is not a cell-type specific event. Further, we have evaluated the potential mechanism of D3R internalization induced by these biased signaling agonists. SK608-induced D3R internalization was time- and concentration-dependent. In comparison, dopamine induced D3R upregulation and pharmacological sequestration in the same assays. GRK2 and clathrin/dynamin I/II are the k...
Source: Pharmacological Research - March 5, 2019 Category: Drugs & Pharmacology Source Type: research

Anti-arrhythmic therapy in patients with non-ischemic cardiomyopathy
Publication date: Available online 4 March 2019Source: Pharmacological ResearchAuthor(s): Riccardo Proietti, Vincenzo Russo, Ahmed AlTurkiAbstractImplantable cardiac defibrillators (ICD) are the foundation of therapy for the prevention of sudden cardiac death. While ICDs prevent SCD, they do not prevent the occurrence of ventricular arrhythmias which are usually symptomatic. Though catheter ablation has been successful in substrate modification of ventricular tachycardia in patients with ischemic cardiomyopathy, there is much less evidence to support its use in non-ischemic cardiomyopathy. Therefore, anti-arrhythmic drugs ...
Source: Pharmacological Research - March 5, 2019 Category: Drugs & Pharmacology Source Type: research

Role of endocannabinoid system in dopamine signalling within the reward circuits affected by chronic pain
Publication date: Available online 1 March 2019Source: Pharmacological ResearchAuthor(s): Jakub Mlost, Agnieszka Wąsik, Katarzyna StarowiczAbstractThe association between chronic pain, depression and anxiety has gained particular attention due to high rates of comorbidity. Recent data demonstrated that the mesolimbic reward circuitry is involved in the pathology of chronic pain. Interestingly, the mesolimbic reward circuit participates both in pain perception and in pain relief. The endocannabinoid system (ECS) has emerged as a highly relevant player involved in both pain perception and reward processing. Targeting ECS co...
Source: Pharmacological Research - March 4, 2019 Category: Drugs & Pharmacology Source Type: research

Harnessing the immune system to fight cancer with Toll-like receptor and RIG-I-like receptor agonists
Publication date: Available online 2 March 2019Source: Pharmacological ResearchAuthor(s): Carole Bourquin, Aurélien Pommier, Christian HotzAbstractCancer immunotherapy has come of age with the advent of immune checkpoint inhibitors. In this article we review how agonists for receptors of the innate immune system, the Toll-like receptors and the RIG-I-like receptors, impact anticancer immune responses. Treatment with these agonists enhances the activity of anticancer effector cells, such as cytotoxic T cells and NK cells, and at the same time blocks the activity of immunosuppressive cell types such as regulatory T ce...
Source: Pharmacological Research - March 4, 2019 Category: Drugs & Pharmacology Source Type: research

Pharmacological targeting of age-related changes in skeletal muscle tissue
Publication date: Available online 4 March 2019Source: Pharmacological ResearchAuthor(s): Aurel B. Leuchtmann, Christoph HandschinAbstractSarcopenia, the age-related loss of skeletal muscle mass and function, increases the risk of developing chronic diseases in older individuals and is a strong predictor of disability and death. Because of the ongoing demographic transition, age-related muscle weakness is responsible for an alarming and increasing contribution to health care costs in Western countries. Exercise-based interventions are most successful in preventing the decline in skeletal muscle mass and in preserving or am...
Source: Pharmacological Research - March 4, 2019 Category: Drugs & Pharmacology Source Type: research

Autophagy Inhibition Plays a Protective Role against 3, 4-Methylenedioxymethamphetamine (MDMA)-induced Loss of Serotonin Transporters and Depressive-like Behaviors in Rats
Publication date: Available online 28 February 2019Source: Pharmacological ResearchAuthor(s): Jui-Hu Shih, Chuang-Hsin Chiu, Kuo-Hsing Ma, Yuahn-Sieh Huang, Chyng-Yann Shiue, Ting-Yin Yeh, Li-Ting Kao, Yang-Yi Lin, I-Hsun LiAbstractThe 3,4-methylenedioxymethamphetamine (MDMA) is a popular recreational drug, which ultimately leads to serotonergic (5-HT) neurotoxicity and psychiatric disorders. Previous in vitro studies have consistently demonstrated that MDMA provokes autophagic activation, as well as damage of 5-HT axons and nerve fibers. So far, whether autophagy, a well-conserved cellular process that is critical for cel...
Source: Pharmacological Research - March 1, 2019 Category: Drugs & Pharmacology Source Type: research