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

authors： Beerepoot P,Nazari R,Salahpour A

更新日期：2017-03-01 00:00:00

abstract：:The Ras-Raf-MEK-ERK (Map kinase) cellular pathway is a highly conserved eukaryotic signaling module that transduces extracellular signals from growth factors and cytokines into intracellular regulatory events that are involved in cell growth and proliferation or the contrary pathway of cell differentiation. Dysregulat...

journal_title：Pharmacological research

authors： Roskoski R Jr

更新日期：2017-03-01 00:00:00

abstract：:Indole-based compounds, such as the alkyl-indole (AI) compound WIN55212-2, activate the cannabinoid receptors, CB1 and CB2, two well-characterized G protein-coupled receptors (GPCR). Reports indicate that several indole-based cannabinoid agonists, including WIN55212-2, lack selectivity and interact with at least two a...

journal_title：Pharmacological research

authors： Fung S,Xu C,Hamel E,Wager-Miller JB,Woodruff G,Miller A,Sanford C,Mackie K,Stella N

更新日期：2017-01-01 00:00:00

abstract：:Mammalian cells are commonly employed in screening assays to identify active compounds that could potentially affect the progression of different human diseases including retinitis pigmentosa (RP), a class of inherited diseases causing retinal degeneration with compromised vision. Using transcriptome analysis, we comp...

journal_title：Pharmacological research

authors： Chen Y,Brooks MJ,Gieser L,Swaroop A,Palczewski K

更新日期：2017-01-01 00:00:00

abstract：:We previously demonstrated that the typical mitochondrial uncoupler carbonyl cyanide m-chlorophenylhydrazone (CCCP) inhibited artery constriction, but CCCP was used only as a pharmacological tool. Niclosamide is an anthelmintic drug approved by FDA. Niclosamide ethanolamine (NEN) is a salt form of niclosamide and has ...

journal_title：Pharmacological research

authors： Li SL,Yan J,Zhang YQ,Zhen CL,Liu MY,Jin J,Gao JL,Xiao XL,Shen X,Tai Y,Hu N,Zhang XZ,Sun ZJ,Dong DL

更新日期：2017-01-01 00:00:00

abstract：:Breast cancer is a leading cause of morbidity and mortality in women. Both Epidemiological and experimental studies indicate a positive correlation between alcohol consumption and the risk of breast cancer. While alcohol exposure may promote the carcinogenesis or onset of breast cancer, it may as well enhance the prog...

journal_title：Pharmacological research

authors： Wang Y,Xu M,Ke ZJ,Luo J

更新日期：2017-01-01 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

authors： Kenakin TP

更新日期：2016-12-01 00:00:00

abstract：:Inflammation plays a key role in tumor promotion and development. Indeed, cyclooxygenase-2 (COX-2) expression is strongly associated with different types of cancer. An emerging class of compounds with significant anti-inflammatory properties is the hydrogen sulfide-releasing non-steroidal anti-inflammatory drugs (H2S-...

journal_title：Pharmacological research

authors： De Cicco P,Panza E,Ercolano G,Armogida C,Sessa G,Pirozzi G,Cirino G,Wallace JL,Ianaro A

更新日期：2016-12-01 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

authors： Grañé-Boladeras N,Pérez-Torras S,Lozano JJ,Romero MR,Mazo A,Marín JJG,Pastor-Anglada M

更新日期：2016-11-01 00:00:00

abstract：:It has been suggested that hypertension results from a loss of immunological tolerance and the resulting autoimmunity may be an important underlying factor of its pathogenesis. This stems from the observations that many of the features involved in autoimmunity are also implicated in hypertension. Furthermore, the unde...

journal_title：Pharmacological research

authors： McCarthy CG,Wenceslau CF,Goulopoulou S,Ogbi S,Matsumoto T,Webb RC

更新日期：2016-11-01 00:00:00

abstract：:Mesial temporal lobe epilepsy (MTLE) is frequently associated with hippocampal sclerosis (Hs), possibly caused by a primary brain injury that occurs a long time before the appearance of neurological symptoms. MTLE-Hs is, however, a heterogeneous condition that evolves with time, involving both environmental and geneti...

journal_title：Pharmacological research

authors： Gambardella A,Labate A,Cifelli P,Ruffolo G,Mumoli L,Aronica E,Palma E

更新日期：2016-11-01 00:00:00

abstract：:Dementia with Lewy bodies (DLB) is a serious age-dependent human neurodegenerative disease, with multiple debilitating symptoms, including dementia, psychosis and significant motor deficits, but with little or no effective treatments. This comparative ligand autoradiographical study has quantified histamine H3 recepto...

journal_title：Pharmacological research

authors： Lethbridge NL,Chazot PL

更新日期：2016-11-01 00:00:00

abstract：:The cytokine thymic stromal lymphopoietin (TSLP) is involved in the development and the progression of allergic diseases. It is mainly released by epithelial cells at barriers such as skin and gut in response to danger signals. Overexpression of TSLP in keratinocytes (KC) can provoke the development of a type 2 inflam...

journal_title：Pharmacological research

authors： Schaper K,Rossbach K,Köther B,Stark H,Kietzmann M,Werfel T,Gutzmer R

更新日期：2016-11-01 00:00:00

abstract：:Sphingosine 1-phosphate (S1P) is an extracellular lipid signaling molecule that acts as a selective, high-affinity ligand for a family of five G protein-coupled receptors. This signaling system was first identified twenty years ago, and has since been shown to regulate a diverse range of physiological processes and di...

journal_title：Pharmacological research

authors： Chew WS,Wang W,Herr DR

更新日期：2016-11-01 00:00:00

abstract：:Exposure to ionizing radiation causes damage to living tissues; however, only a small number of agents have been approved for use in radiation injuries. Radioprotector is the primary countermeasure to radiation injury and none radioprotector has indeed reached the drug development stage. Repurposing the long list of a...

journal_title：Pharmacological research

authors： Ren L,Xie D,Li P,Qu X,Zhang X,Xing Y,Zhou P,Bo X,Zhou Z,Wang S

更新日期：2016-11-01 00:00:00

abstract：:The endogenous gasotransmitter hydrogen sulphide (H2S) is an important regulator of the cardiovascular system, particularly of myocardial function. Moreover, H2S exhibits cardioprotective activity against ischemia/reperfusion (I/R) or hypoxic injury, and is considered an important mediator of "ischemic preconditioning...

journal_title：Pharmacological research

authors： Testai L,Marino A,Piano I,Brancaleone V,Tomita K,Di Cesare Mannelli L,Martelli A,Citi V,Breschi MC,Levi R,Gargini C,Bucci M,Cirino G,Ghelardini C,Calderone V

更新日期：2016-11-01 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

authors： Villa V,Thellung S,Bajetto A,Gatta E,Robello M,Novelli F,Tasso B,Tonelli M,Florio T

更新日期：2016-11-01 00:00:00

abstract：:The Janus kinase (JAK) family of non-receptor protein-tyrosine kinases consists of JAK1, JAK2, JAK3, and TYK2 (tyrosine kinase-2). Each of these proteins contains a JAK homology pseudokinase (JH2) domain that regulates the adjacent protein kinase domain (JH1). JAK1/2 and TYK2 are ubiquitously expressed whereas JAK3 is...

journal_title：Pharmacological research

authors： Roskoski R Jr

更新日期：2016-09-01 00:00:00

abstract：:A major focus of contemporary drug screening strategies is the identification of novel anticancer compounds, which often results in underutilization of resources. Current drug evaluation involves in vivo tumor (xenograft) regression as proof-of-principle for cytotoxicity (POC). However, this end-point lacks any assess...

journal_title：Pharmacological research

authors： Naik RR,Luo T,Kohandel M,Bapat SA

更新日期：2016-09-01 00:00:00

abstract：:Extrasynaptically located γ-aminobutyric acid (GABA) receptors type A are often characterized by the presence of a δ subunit in the receptor complex. δ-Containing receptors respond to low ambient concentrations of GABA, or respond to spillover of GABA from the synapse, and give rise to tonic inhibitory currents. In ce...

journal_title：Pharmacological research

authors： Ahring PK,Bang LH,Jensen ML,Strøbæk D,Hartiadi LY,Chebib M,Absalom N

更新日期：2016-09-01 00:00:00

abstract：:Exogenous hydrogen sulfide (H2S) protects against myocardial ischemia/reperfusion injury but the mechanism of action is unclear. The present study investigated the effect of GYY4137, a slow-releasing H2S donor, on myocardial infarction given specifically at reperfusion and the signalling pathway involved. Thiobutabarb...

journal_title：Pharmacological research

authors： Karwi QG,Whiteman M,Wood ME,Torregrossa R,Baxter GF

更新日期：2016-09-01 00:00:00

abstract：:The first studies of histamine and diabetes date back to the 1950s. Since that time the involvement of histamine in diabetes was related to its well known vasoactive properties and permeability leakage effects. In particular, the first evidence for a correlation between histamine and diabetes arose in 1989 when an inc...

journal_title：Pharmacological research

authors： Pini A,Obara I,Battell E,Chazot PL,Rosa AC

更新日期：2016-09-01 00:00:00

abstract：:There is considerable evidence to support the role of anandamide (AEA), an endogenous ligand of cannabinoid receptors, in neuropathic pain modulation. AEA also produces effects mediated by other biological targets, of which the transient receptor potential vanilloid type 1 (TRPV1) has been the most investigated. Both,...

journal_title：Pharmacological research

authors： Malek N,Kostrzewa M,Makuch W,Pajak A,Kucharczyk M,Piscitelli F,Przewlocka B,Di Marzo V,Starowicz K

更新日期：2016-09-01 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

authors： Cho E,Park M

更新日期：2016-09-01 00:00:00

abstract：:Epidemiological studies support an inverse correlation between HDL-C and cardiovascular disease. However, low HDL-C levels do not always segregate with premature disease. These include, LCAT deficiency and the apolipoproteinA-IMilano (AIM) variant. AIM has a cysteine for arginine at position 173 in the otherwise cyste...

journal_title：Pharmacological research

authors： Bisgaier CL,Ackermann R,Rea T,Rodrigueza WV,Hartman D

更新日期：2016-09-01 00:00:00

abstract：:Pulmonary fibrosis is a chronic condition characterized by progressive scarring of lung parenchyma. The aim of this study was to examine the effects of an ultramicronized preparation of palmitoylethanolamide (PEA-um(®)), an endogenous fatty acid amide, in mice subjected to idiopathic pulmonary fibrosis. Idiopathic pul...

journal_title：Pharmacological research

authors： Di Paola R,Impellizzeri D,Fusco R,Cordaro M,Siracusa R,Crupi R,Esposito E,Cuzzocrea S

更新日期：2016-09-01 00:00:00

abstract：:Spinal muscular atrophy (SMA) is an autosomal recessive neurodegenerative disease characterized by motor neurons degeneration and muscular atrophy. There is no effective SMA treatment. Loganin is a botanical candidate with anti-inflammatory, anti-oxidant, glucose-lowering and anti-diabetic nephropathy activities. The ...

journal_title：Pharmacological research

authors： Tseng YT,Chen CS,Jong YJ,Chang FR,Lo YC

更新日期：2016-09-01 00:00:00

abstract：:The polyphenol resveratrol is considered to exert many beneficial actions, such as antioxidant, anti-inflammatory, insulin-sensitizer and anticancer effects. Its benefits in patients with type 2 diabetes mellitus (T2DM) are controversial. Our aims were to determine whether resveratrol supplementation at two different ...

journal_title：Pharmacological research

authors： Bo S,Ponzo V,Ciccone G,Evangelista A,Saba F,Goitre I,Procopio M,Pagano GF,Cassader M,Gambino R

更新日期：2016-09-01 00:00:00

abstract：:Segetoside I is a plant-derived bisdesmosidic saponin from Vaccaria segetalis (Neck) with reported anticancer activities. This development has raised an interest in the therapeutic potential of segetoside I. Here, we report the in vitro and in vivo antitumor activities of segetoside I against some selected cancer cell...

journal_title：Pharmacological research

authors： Firempong CK,Zhang HY,Wang Y,Chen J,Cao X,Deng W,Zhou J,Wang Q,Tong SS,Yu J,Xu X

更新日期：2016-08-01 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

authors： Pirro M,Mannarino MR,Bianconi V,Simental-Mendía LE,Bagaglia F,Mannarino E,Sahebkar A

更新日期：2016-08-01 00:00:00

abstract：:Cannabinoids have emerged as promising neuroprotective agents due to their capability to activate specific targets, which are involved in the control of neuronal homeostasis and survival. Specifically, those ligands that selectively target and activate the CB2 receptor may be useful for their anti-inflammatory and neu...

journal_title：Pharmacological research

authors： Gómez-Cañas M,Morales P,García-Toscano L,Navarrete C,Muñoz E,Jagerovic N,Fernández-Ruiz J,García-Arencibia M,Pazos MR

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

authors： Leishman E,Cornett B,Spork K,Straiker A,Mackie K,Bradshaw HB

更新日期：2016-08-01 00:00:00

abstract：:Thioredoxin is one of the most important cellular antioxidant systems known to date, and is responsible of maintaining the reduced state of the intracellular space. Trx-1 is a small cytosolic protein whose transcription is induced by stress. Therefore it is possible that this antioxidant plays a protective role agains...

journal_title：Pharmacological research

authors： D'Annunzio V,Perez V,Boveris A,Gelpi RJ,Poderoso JJ

更新日期：2016-07-01 00:00:00

abstract：:Osteopontin (OPN) is known as an active player in the progression of vascular remodeling diseases, however, the precise role in the proliferation of vascular smooth muscle cells (VSMC) is unclear. Thus, this study investigated the role of OPN in VSMC proliferation induced by 4-hydroxynonenal (HNE), and identified the ...

journal_title：Pharmacological research

authors： Lee SJ,Baek SE,Jang MA,Kim CD

更新日期：2016-06-01 00:00:00

abstract：:The Notch pathway represents a highly conserved signaling network with essential roles in regulation of key cellular processes and functions, many of which are critical for development. Accumulating evidence indicates that it is also essential for fibrosis and thus the pathogenesis of chronic fibroproliferative diseas...

journal_title：Pharmacological research

authors： Hu B,Phan SH

更新日期：2016-06-01 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

authors： Dinca M,Serban MC,Sahebkar A,Mikhailidis DP,Toth PP,Martin SS,Blaha MJ,Blüher M,Gurban C,Penson P,Michos ED,Hernandez AV,Jones SR,Banach M,for Lipid Blood Pressure Meta-analysis Collaboration LBPMC Group.

更新日期：2016-05-01 00:00:00

abstract：:The Renin Angiotensin System (RAS) is a pivotal physiological regulator of heart and kidney homeostasis, but also plays an important role in the pathophysiology of heart and kidney diseases. Recently, new components of the RAS have been discovered, including angiotensin converting enzyme 2 (ACE2), Angiotensin(Ang)-(1-...

journal_title：Pharmacological research

authors： Simões E Silva AC,Teixeira MM

更新日期：2016-05-01 00:00:00

abstract：:Aminoglycosides are very effective antibiotics for the treatment of severe infections, but they rank among the most frequent causes of drug-induced nephrotoxicity. Thus, prevention of aminoglycoside nephrotoxicity is an unmet therapeutic objective. Cardiotrophin-1 (CT-1), a member of the IL-6 family of cytokines, has ...

journal_title：Pharmacological research

authors： Quirós Y,Blanco-Gozalo V,Sanchez-Gallego JI,López-Hernandez FJ,Ruiz J,Perez de Obanos MP,López-Novoa JM

更新日期：2016-05-01 00:00:00

abstract：:The effects of Nigella sativa (NS) on plasma lipid concentrations are controversial. A systematic review and meta-analysis of randomized controlled trials (RCTs) was conducted to obtain a conclusive result in humans. PubMed-Medline, SCOPUS, Web of Science, and Google Scholar databases were searched (up to August 2015)...

journal_title：Pharmacological research

authors： Sahebkar A,Beccuti G,Simental-Mendía LE,Nobili V,Bo S

更新日期：2016-04-01 00:00:00

abstract：:Antioxidants have a great potential as adjuvant therapeutics in patients with Duchenne muscular dystrophy, although systematic comparisons at pre-clinical level are limited. The present study is a head-to-head assessment, in the exercised mdx mouse model of DMD, of natural compounds, resveratrol and apocynin, and of t...

journal_title：Pharmacological research

authors： Capogrosso RF,Cozzoli A,Mantuano P,Camerino GM,Massari AM,Sblendorio VT,De Bellis M,Tamma R,Giustino A,Nico B,Montagnani M,De Luca A

更新日期：2016-04-01 00:00:00