Cysteine Proteases: Modes of Activation and Future Prospects as Pharmacological Targets.

abstract：:G protein-coupled receptor kinase 2 (GRK2) is a ubiquitous member of the GRK family that restrains cellular activation by G protein-coupled receptor (GPCR) phosphorylation leading to receptor desensitization and internalization, but has been identified to regulate a variety of signaling molecules, among which may be a...

journal_title：Frontiers in pharmacology

authors： Palikhe S,Ohashi W,Sakamoto T,Hattori K,Kawakami M,Andoh T,Yamazaki H,Hattori Y

更新日期：2019-02-04 00:00:00

abstract：:Costunolide, a sesquiterpene isolated from Vladimiria souliei (Franch.) Ling, is known to exhibit anti-inflammatory, anti-viral, and anti-tumor activities. However, the effects of costunolide on liver injury are poorly understood. The current study aimed to investigate the hepatoprotective effects of costunolide again...

journal_title：Frontiers in pharmacology

authors： Mao J,Yi M,Wang R,Huang Y,Chen M

更新日期：2018-12-20 00:00:00

abstract：:Several aldo-keto reductase (AKR) enzymes from subfamilies 1B and 1C show retinaldehyde reductase activity, having low K(m) and k(cat) values. Only AKR1B10 and 1B12, with all-trans-retinaldehyde, and AKR1C3, with 9-cis-retinaldehyde, display high catalytic efficiency. Major structural determinants for retinaldehyde is...

journal_title：Frontiers in pharmacology

authors： Ruiz FX,Porté S,Parés X,Farrés J

更新日期：2012-04-17 00:00:00

abstract：:Metabolic syndrome is a disorder of energy use and storage, which is characterized by central obesity, dyslipidemia, and raised blood pressure and blood sugar levels. Maternal 25-hydroxyvitamin D deficiency is known to cause metabolic changes, chronic disease, and increased adiposity in adulthood. However, the underlyi...

journal_title：Frontiers in pharmacology

authors： Zheng J,Liu X,Zheng B,Zheng Z,Zhang H,Zheng J,Sun C,Chen H,Yang J,Wang Z,Lin M,Chen J,Zhou Q,Zheng Z,Xu X,Ying H

更新日期：2020-02-28 00:00:00

abstract：:Liver fibrosis, a chronic damage process related to further progression of hepatic cirrhosis, has yet no truly effective treatment. Isochlorogenic acid A (ICQA), isolated from a traditional Chinese herbal medicine named Laggera alata (DC.) Sch.Bip. ex Oliv. (Asteraceae), is proved to exhibit anti-inflammatory, hepatop...

journal_title：Frontiers in pharmacology

authors： Liu X,Huang K,Zhang RJ,Mei D,Zhang B

更新日期：2020-05-01 00:00:00

abstract：:Opioids are broad spectrum analgesics that are an integral part of the therapeutic armamentarium to combat pain in the clinical practice. Unfortunately, together with analgesia, a number of adverse effects can occur such as nausea, vomiting, constipation, gastrointestinal alterations and cognitive impairments. Naltrex...

journal_title：Frontiers in pharmacology

authors： Micheli L,Di Cesare Mannelli L,Lucarini E,Parisio C,Toti A,Fiorentino B,Rigamonti MA,Calosi L,Ghelardini C

更新日期：2020-09-18 00:00:00

abstract：:Background: Total flavonoids of Rhizoma Drynariae (TFRD), extracted from the kidney-tonifying traditional Chinese medicine Rhizoma Rrynariae, has been proved to be effective in treating osteoporosis, bone fractures and defects. However, pharmacological effects of TFRD on type H vessels, angiogenic-osteogenic coupling ...

journal_title：Frontiers in pharmacology

authors： Shen Z,Chen Z,Li Z,Zhang Y,Jiang T,Lin H,Huang M,Chen H,Feng J,Jiang Z

更新日期：2020-11-27 00:00:00

abstract：:Neurofibrillary pathology contributes to neuronal dysfunction and correlates with the clinical progression of Alzheimer's disease (AD). Tau phosphorylation is mainly regulated by a balance of glycogen synthase kinase-3β (GSK-3β) and protein phosphatase 2A (PP2A) activities. Cornel iridoid glycoside (CIG) is a main com...

journal_title：Frontiers in pharmacology

authors： Yang C,Li X,Gao W,Wang Q,Zhang L,Li Y,Li L,Zhang L

更新日期：2018-06-26 00:00:00

abstract：:Positive links have been found between periodontitis and numerous diseases in humans via persistent inflammation throughout the body. However, the main factors responsible for maintaining this pro-inflammatory condition are poorly understood. The spleen, the largest secondary immune organ, is a central hub regulating ...

journal_title：Frontiers in pharmacology

authors： Dekita M,Wu Z,Ni J,Zhang X,Liu Y,Yan X,Nakanishi H,Takahashi I

更新日期：2017-07-17 00:00:00

abstract：:Cucurbitacin C (CuC), a novel analogue of triterpenoids cucurbitacins, confers a bitter taste in cucumber. Genes and signaling pathways responsive for biosynthesis of CuC have been identified in the recent years. In the present study, we explored the anti-cancer effects of CuC against human cancers in vitro and in viv...

journal_title：Frontiers in pharmacology

authors： Wu D,Wang Z,Lin M,Shang Y,Wang F,Zhou J,Wang F,Zhang X,Luo X,Huang W

更新日期：2019-11-08 00:00:00

abstract：:Immune checkpoint inhibitors (ICIs) that target cytotoxic T lymphocyte antigen 4, programmed cell death-1, and PD-ligand 1 have revolutionized cancer treatment, achieving unprecedented efficacy in multiple malignancies. ICIs are increasingly being used in early cancer settings and in combination with various other typ...

journal_title：Frontiers in pharmacology

authors： Zhou YW,Zhu YJ,Wang MN,Xie Y,Chen CY,Zhang T,Xia F,Ding ZY,Liu JY

更新日期：2019-11-29 00:00:00

abstract：:ORY-1001, an inhibitor of covalent lysine (K)-specific demethylase 1A (KDM1A), has been used as a therapy for the treatment of acute leukemia. However, the underlying mechanisms of anticancer are still not fully elucidated. Here, we report that KDM1A is highly expressed in lung cancers, where it appears to drive aggre...

journal_title：Frontiers in pharmacology

authors： Lu Z,Guo Y,Zhang X,Li J,Li L,Zhang S,Shan C

更新日期：2018-12-04 00:00:00

abstract：:The vast majority of states have enacted full or partial medical marijuana (MMJ) programs, causing the number of patients seeking certification for MMJ use to increase dramatically in recent years. Despite increased use of MMJ across the nation, no studies thus far have examined the specific impact of MMJ on cognitive...

journal_title：Frontiers in pharmacology

authors： Gruber SA,Sagar KA,Dahlgren MK,Gonenc A,Smith RT,Lambros AM,Cabrera KB,Lukas SE

更新日期：2018-01-17 00:00:00

abstract：:Oncogenic activation of the KRAS gene via point mutations occurs in 20-30% of patients with non-small cell lung cancer (NSCLC). The RAS-RAF-ERK and RAS-PI3K-AKT pathways are the major hyper-activated downstream pathways in RAS mutation, which promotes the unlimited lifecycle of cancer cells and their metastasis in hum...

journal_title：Frontiers in pharmacology

authors： Lai H,Wang Y,Duan F,Li Y,Jiang Z,Luo L,Liu L,Leung ELH,Yao X

更新日期：2018-08-22 00:00:00

abstract：Objective:Drawing a growth curve of multidrug-resistant Pseudomonas aeruginosa (MDR-PA) provides a foundation for susceptibility testing. By observing in vitro antibacterial activity and ultrastructure cthanges on MDR-PA of the effective components in the drug-containing serum of rats after the administration of Fuzhen...

journal_title：Frontiers in pharmacology

authors： Xu H,Liu C,Li M,Wang C,Liu G,Wang H,Ma J,Li L,Chen M,Cheng M,Yao X,Lin Y,Zhao S,Wang Y,Wang M

更新日期：2020-02-12 00:00:00

abstract：:Most breast and prostate tumors are hormone-dependent, making it possible to use hormone therapy in patients with these tumors. The design of effective endocrine drugs that block the growth of tumors and have no severe side effects is a challenge. Thereupon, synthetic steroids are promising therapeutic drugs for the t...

journal_title：Frontiers in pharmacology

authors： Scherbakov AM,Komkov AV,Komendantova AS,Yastrebova MA,Andreeva OE,Shirinian VZ,Hajra A,Zavarzin IV,Volkova YA

更新日期：2018-01-10 00:00:00

abstract：:The hepatotoxicity induced by Polygoni Multiflori Radix Praeparata (PM) has aroused great concern throughout the world. Hence, it is worthwhile to perform studies on the detoxification with the combined use of medicinal herbs based on the compatibility theory of traditional Chinese medicine. In this work, the rat mode...

journal_title：Frontiers in pharmacology

authors： Gao D,Pang JY,Zhang CE,Li CY,Tu C,Zhang HZ,Niu M,Xiong Y,Xiao XH,Zhao KJ,Gao WW,Wang JB

更新日期：2016-10-18 00:00:00

abstract：:The objective of this study was to test the hypothesis that serotonin O-sulphate (5-HT-SO4) could be quantified in human plasma using modern liquid chromatography-mass spectrometry (LC-MS) method as well as develop and validate that method. First, a suitable LC-MS method for detection of 5-HT-SO4 in human plasma sampl...

journal_title：Frontiers in pharmacology

authors： Lozda R,Purviņš I

更新日期：2014-04-08 00:00:00

abstract：:The response to pazopanib in patients with metastatic renal cell carcinoma (mRCC) has been found to differ in Western and Eastern populations. Here, we analyzed the efficacy and side effects of pazopanib as first-line therapy in 31 consecutive patients with mRCC who were treated at a single Chinese center. Thirty-one ...

journal_title：Frontiers in pharmacology

authors： Wang B,Song JW,Chen HQ

更新日期：2020-10-29 00:00:00

abstract：:Background: From October 2018, adalimumab biosimilars could enter the European market. However, in some countries, such as Netherlands, high discounts reported for the originator product may have influenced biosimilar entry. Objectives: The aim of this paper is to provide a European overview of (list) prices of origin...

journal_title：Frontiers in pharmacology

authors： Moorkens E,Godman B,Huys I,Hoxha I,Malaj A,Keuerleber S,Stockinger S,Mörtenhuber S,Dimitrova M,Tachkov K,Vončina L,Palčevski VV,Achniotou G,Slabý J,Popelková L,Kohoutová K,Bartels D,Laius O,Martikainen JE,Selke GW,

更新日期：2021-01-08 00:00:00

abstract：:Fungal secondary metabolites serve as a rich resource for exploring lead compounds with medicinal importance. Diorcinol N (DN), a fungal secondary metabolite isolated from an endophytic fungus, Arthrinium arundinis, exhibits robust anticancer activity. However, the anticancer mechanism of DN remains unclear. In this s...

journal_title：Frontiers in pharmacology

authors： Yuan XL,Li XQ,Xu K,Hou XD,Zhang ZF,Xue L,Liu XM,Zhang P

更新日期：2020-10-15 00:00:00

abstract：:Deregulated activity of the Src tyrosine kinases leads to malignant transformation. Since the FDA approval of the tyrosine kinase inhibitor, imatinib, in 2001 for the treatment of chronic myeloid leukemia (CML), the number of these inhibitors together with Src tyrosine kinase inhibitors (STKIs) has increased notably d...

journal_title：Frontiers in pharmacology

authors： Rivera-Torres J,San José E

更新日期：2019-09-18 00:00:00

abstract：:Introduction: Over the past decades, early awareness and alert (EAA) activities and systems have gained importance and become a key early health technology assessment (HTA) tool. While a pioneer in HTA, Sweden had no national level EAA activities until 2010. We describe the evolution and current status of the Swedish ...

journal_title：Frontiers in pharmacology

authors： Eriksson I,Wettermark B,Persson M,Edström M,Godman B,Lindhé A,Malmström RE,Ramström H,von Euler M,Bergkvist Christensen A

更新日期：2017-10-05 00:00:00

abstract：:Lipopolysaccharide (LPS) can induce bone loss by stimulating bone resorption. Natural compounds have great potential for the treatment of osteolytic bone diseases. Magnesium lithospermate B (MLB) plays an important role in protecting against oxidative damage and also has potential anti-inflammatory pharmacological pro...

journal_title：Frontiers in pharmacology

authors： Wang J,Wu X,Duan Y

更新日期：2018-02-06 00:00:00

abstract：:Background and Objectives: Limited research focuses on the risk of ischemic cerebrovascular disease associated with use of dipeptidyl peptidase-4 inhibitors (DPP-4 inhibitors) in patients with type 2 diabetes mellitus in Taiwan. This study aimed to investigate the association between DPP-4 inhibitors use and the first...

journal_title：Frontiers in pharmacology

authors： Lai SW,Liao KF,Lin CL,Lin HF

更新日期：2017-11-22 00:00:00

abstract：:Background: No risk model for predicting thrombocytopenia associated with periprocedural tirofiban exposure is available. The purpose of this study was to develop a simple clinical pre-procedure risk model based on pre-procedural characteristics for early prediction of thrombocytopenia before patients were exposed to ...

journal_title：Frontiers in pharmacology

authors： Yi YH,Yin WJ,Gu ZC,Fang WJ,Li DY,Hu C,Liu K,Ma RR,Zhou LY

更新日期：2018-12-10 00:00:00

abstract：:The risk assessment of environmental chemicals and drugs is undergoing a paradigm shift in approach which seeks the full replacement of animal testing with high throughput, mechanistic, in vitro systems. This new approach will be reliant on the measurement in vitro, of concentration-dependent responses where prolonged...

journal_title：Frontiers in pharmacology

authors： McNally K,Loizou GD

更新日期：2015-10-12 00:00:00

abstract：:Random-pattern skin flap transplantation is frequently applied in plastic and reconstructive surgery. However, the distal part of the flap often suffers necrosis due to ischemia. In this study, the effects of salvianolic acid B (Sal B) on flap survival were evaluated, and the underlying mechanisms were investigated. S...

journal_title：Frontiers in pharmacology

authors： Lin J,Lin R,Li S,Wu H,Ding J,Xiang G,Li S,Wang Y,Lin D,Gao W,Kong J,Xu H,Zhou K

更新日期：2018-10-23 00:00:00

abstract：:One approach to experimental science involves creating hypotheses, then testing them by varying one or more independent variables, and assessing the effects of this variation on the processes of interest. We use this strategy to compare the intellectual status and available evidence for two models or views of mechanis...

journal_title：Frontiers in pharmacology

authors： Kell DB,Oliver SG

更新日期：2014-10-31 00:00:00

abstract：:Cholesterol is essential for development, growth, and maintenance of organisms. Mutations in cholesterol biosynthetic genes are embryonic lethal and few polymorphisms have been so far associated with pathologies in humans. Previous analyses show that lanosterol 14α-demethylase (CYP51A1) from the late part of cholester...

journal_title：Frontiers in pharmacology

authors： Režen T,Ogris I,Sever M,Merzel F,Golic Grdadolnik S,Rozman D

更新日期：2017-06-30 00:00:00