abstract：:Pain is a classical sign of inflammation, and sensitization of primary sensory neurons (PSN) is the most important mediating mechanism. This mechanism involves direct action of inflammatory mediators such as prostaglandins and sympathetic amines. Pharmacologic control of inflammatory pain is based on two principal str...

journal_title：Biochemical pharmacology

authors： Gomes FIF,Cunha FQ,Cunha TM

更新日期：2020-06-01 00:00:00

abstract：:Nitric oxide (NO) and hydrogen sulfide (H2S) are two gasotransmitters that are produced in the human body and have a key role in many of the physiological activities of the various organ systems. Decreased NO bioavailability and deficiency of H2S are involved in the pathophysiology of type 2 diabetes and its complicat...

journal_title：Biochemical pharmacology

authors： Gheibi S,Samsonov AP,Gheibi S,Vazquez AB,Kashfi K

更新日期：2020-06-01 00:00:00

abstract：:Dihydromyricetin (DMY) is the most abundant flavonoid in Ampelopsis grossedentata possessing many pharmacological activities. But less is known about its protective effect against nonalcoholic steatohepatitis (NASH) in the context of metabolic syndrome. The present study is aimed to evaluate the pharmacological effect...

journal_title：Biochemical pharmacology

authors： Zeng Y,Hua YQ,Wang W,Zhang H,Xu XL

更新日期：2020-05-01 00:00:00

abstract：:The increasing incidence of severe liver diseases worldwide has resulted in a high demand for curative liver transplantation. Unfortunately, the need for transplants by far eclipses the availability of suitable grafts leaving many waitlisted patients to face liver failure and often death. Routine use of smaller grafts...

journal_title：Biochemical pharmacology

authors： Greenbaum LE,Ukomadu C,Tchorz JS

更新日期：2020-05-01 00:00:00

abstract：:Hepcidin peptide is crucial in the regulation of systemic iron availability controlling its uptake from the diet and its release from the body storage tissues. Hepcidin dysregulation causes different human disorders ranging from iron overload (e.g. hemochromatosis) to iron deficiency (e.g. anemia). Hepcidin excess is ...

journal_title：Biochemical pharmacology

authors： Asperti M,Denardo A,Gryzik M,Castagna A,Girelli D,Naggi A,Arosio P,Poli M

更新日期：2020-05-01 00:00:00

abstract：:Cardiorenal syndrome type-3 (CRS-3) is characterized by acute cardiac injury induced by acute kidney injury. Here, we investigated the causes of CRS-3 by analyzing cardiac function after renal ischemia-reperfusion injury (IRI) using echocardiography and evaluation of pro-inflammatory markers, calcium balance, mitochon...

journal_title：Biochemical pharmacology

authors： Wang J,Toan S,Li R,Zhou H

更新日期：2020-04-01 00:00:00

abstract：:Nuclear factor-E2-related factor 2 (Nrf2) is a master transcription factor in antioxidant response, protecting against oxidative damage and various diseases. Previous studies suggest that Nrf2 is suppressed in fibrotic skin and Nrf2 agonists represent a therapeutic strategy, which is mainly attributed to Nrf2 function...

journal_title：Biochemical pharmacology

authors： Wu R,Zhang H,Zhao M,Li J,Hu Y,Fu J,Pi J,Wang H,Xu Y

更新日期：2020-04-01 00:00:00

abstract：:α6β2-Containing nicotinic acetylcholine receptors (α6β2* nAChRs) are predominantly expressed in midbrain dopaminergic neurons, including substantia nigra pars compacta (SNc) neurons and their projections to striatal regions, where they regulate dopamine release and nigrostriatal activity. It is well established that n...

journal_title：Biochemical pharmacology

authors： van Hout M,Klein J,Ahring PK,Brown DT,Thaneshwaran S,Dos Santos AB,Jensen AA,Kohlmeier KA,Christophersen P,Dyhring T

更新日期：2020-04-01 00:00:00

abstract：:Atopic diseases (atopic dermatitis, asthma and allergic rhinitis) affects a huge number of people around the world and their incidence rate is on rise. Atopic dermatitis (AD) is more prevalent in paediatric population which sensitizes an individual to develop allergic rhinitis and asthma later in life. The complex pat...

journal_title：Biochemical pharmacology

authors： Sharma S,Naura AS

更新日期：2020-03-01 00:00:00

abstract：:Glucuronidation, catalyzed by UDP-glucuronosyltransferases (UGTs), is a crucial substance metabolism and elimination process that mostly occurs in the liver to protect the body from toxic substances and maintain homeostasis. The reaction functions well in a uridine diphosphate glucuronic acid (UDPGA) -dependent manner...

journal_title：Biochemical pharmacology

authors： Zhang L,Zhu L,Qu W,Wu F,Hu M,Xie W,Liu Z,Wang C

更新日期：2020-02-01 00:00:00

abstract：:The aim of this review is to summarize current available information about the role of PI3K/AKT/mTOR signaling in head and neck cancer as a potential target for new therapy options. 90% of all head and neck cancers are squamous cell carcinomas (HNSCC). The most common genetic alteration is inactivation of p16 gene whi...

journal_title：Biochemical pharmacology

authors： Marquard FE,Jücker M

更新日期：2020-02-01 00:00:00

abstract：:UDP-glucuronosyltransferases (UGTs) are essential drug-conjugation enzymes that metabolize a variety of endobiotic and xenobiotic substrates. The molecular characteristics of UGTs have been extensively investigated in humans, but remain to be investigated in common marmosets, a nonhuman primate species widely used in ...

journal_title：Biochemical pharmacology

authors： Uno Y,Uehara S,Inoue T,Kawamura S,Murayama N,Nishikawa M,Ikushiro S,Sasaki E,Yamazaki H

更新日期：2020-02-01 00:00:00

abstract：:Increasing evidence supports NLRP3 inflammasome as a new target to control inflammation. Dysregulation of NLRP3 inflammasome has been reported to be involved in the pathogenesis of several human inflammatory diseases. However, no NLRP3 inflammasome inhibitors are available in clinic. Terpenoids are natural products wi...

journal_title：Biochemical pharmacology

authors： Hortelano S,González-Cofrade L,Cuadrado I,de Las Heras B

更新日期：2020-02-01 00:00:00

abstract：:Human butyrylcholinesterase (E.C. 3.1.1.8) purified from blood plasma has previously been shown to provide protection against up to five and a half times the median lethal dose of an organophosphorus nerve agent in several animal models. In this study the stoichiometric nature of the protection afforded by human butyr...

journal_title：Biochemical pharmacology

authors： Cerasoli DM,Armstrong SJ,Reeves TE,Hodgins SM,Kasten SA,Lee-Stubbs RB,Cadieux CL,Otto TC,Capacio BR,Lenz DE

更新日期：2020-01-01 00:00:00

abstract：:Taxol-based chemotherapy is widely used as the first-line treatment for non-small cell lung cancer (NSCLC), however, the subsequent development of taxol-resistance is a major concern and challenge, resulting in tumor relapse and poor prognosis. Given the complex nature of taxol-resistance, we further delved into its m...

journal_title：Biochemical pharmacology

authors： Lin H,Hu B,He X,Mao J,Wang Y,Wang J,Zhang T,Zheng J,Peng Y,Zhang F

更新日期：2020-01-01 00:00:00

abstract：OBJECTIVE:The evolution of the "cholinergic anti-inflammatory pathway" and the fact that the α 7 subunit of the nicotinic acetylcholine receptor (α7nAChR) is present in the spleen, joint and on the surface of lymphocytes, opened up the prospective in this study of targeting the α7nAChR by the anticholinesterase and cho...

journal_title：Biochemical pharmacology

authors： Gowayed MA,Rothe K,Rossol M,Attia AS,Wagner U,Baerwald C,El-Abhar HS,Refaat R

更新日期：2019-12-01 00:00:00

abstract：:Chronic pain is a debilitating condition that often emerges as a clinical symptom of inflammatory diseases. It has therefore been widely accepted that the immune system critically contributes to the pathology of chronic pain. Microglia, a type of immune cell in the central nervous system, has attracted researchers' at...

journal_title：Biochemical pharmacology

authors： Tozaki-Saitoh H,Tsuda M

更新日期：2019-11-01 00:00:00

abstract：:DNA-dependent protein kinase (DNA-PK) plays a key role in repair of radiation-induced DNA double strand breaks (DSB) by non-homologous end-joining. DNA-PK inhibitors (DNA-PKi) are therefore efficient radiosensitisers, but normal tissue radiosensitisation represents a risk for their use in radiation oncology. Here we d...

journal_title：Biochemical pharmacology

authors： Wong WW,Jackson RK,Liew LP,Dickson BD,Cheng GJ,Lipert B,Gu Y,Hunter FW,Wilson WR,Hay MP

更新日期：2019-11-01 00:00:00

abstract：BACKGROUND:Flavonoids form a diverse class of naturally occurring polyphenols ascribed various biological activities, including inhibition of amyloid β (Aβ) fibrillisation and neurotoxicity of relevance to Alzheimer's disease. Cannabis contains a unique subset of prenylated flavonoids, the cannflavins. While selected c...

journal_title：Biochemical pharmacology

authors： Eggers C,Fujitani M,Kato R,Smid S

更新日期：2019-11-01 00:00:00

abstract：:Parkin (PRKN) is a ubiquitin E3 ligase that catalyzes the ubiquitination of several proteins. Mutations in the human Parkin gene, PRKN, leads to degeneration of dopaminergic (DA) neurons, resulting in autosomal recessive early-onset parkinsonism and the loss of PRKN function is linked to sporadic Parkinson's disease (...

journal_title：Biochemical pharmacology

authors： González-Barbosa E,García-Aguilar R,Vega L,Cabañas-Cortés MA,Gonzalez FJ,Segovia J,Morales-Lázaro SL,Cisneros B,Elizondo G

更新日期：2019-10-01 00:00:00

abstract：:Diabetic retinopathy (DR) is a secondary complication of diabetes. DR can cause irreversible blindness, and its pathogenesis is considered multifactorial. DR can progress from non-proliferative DR to proliferative DR, characterized by retinal neovascularization. The main cause of vision loss in diabetic patients is di...

journal_title：Biochemical pharmacology

authors： Lazzara F,Fidilio A,Platania CBM,Giurdanella G,Salomone S,Leggio GM,Tarallo V,Cicatiello V,De Falco S,Eandi CM,Drago F,Bucolo C

更新日期：2019-10-01 00:00:00

abstract：:Mineralocorticoid receptor (MR) overactivation promotes cardiac fibrosis. We studied the ability of the non-steroidal MR antagonist finerenone to prevent fibrotic remodeling. In neonatal rat cardiac fibroblasts, finerenone prevented aldosterone-induced nuclear MR translocation. Treatment with finerenone decreased the ...

journal_title：Biochemical pharmacology

authors： Lavall D,Jacobs N,Mahfoud F,Kolkhof P,Böhm M,Laufs U

更新日期：2019-10-01 00:00:00

abstract：:Mitochondrial biogenesis is a key feature of energy expenditure and organismal energy balance. Genetic deletion of PARP1 or PARP2 was shown to induce mitochondrial biogenesis and energy expenditure. In line with that, PARP inhibitors were shown to induce energy expenditure in skeletal muscle. We aimed to investigate w...

journal_title：Biochemical pharmacology

authors： Nagy L,Rauch B,Balla N,Ujlaki G,Kis G,Abdul-Rahman O,Kristóf E,Sipos A,Antal M,Tóth A,Debreceni T,Horváth A,Maros T,Csizmadia P,Szerafin T,Bai P

更新日期：2019-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Beraprost is a prostacyclin analogue and IP receptor agonist which is approved to treat pulmonary arterial hypertension (PAH) in Asia. The beraprost-314d isomer (esuberaprost) is one of four stereoisomers contained within the racemic mixture of beraprost. The pharmacological profile of esuberapro...

journal_title：Biochemical pharmacology

authors： Shen L,Patel JA,Norel X,Moledina S,Whittle BJ,von Kessler K,Sista P,Clapp LH

更新日期：2019-08-01 00:00:00

abstract：:Inflammatory events are tightly associated with the death caused by Herpes simplex virus 1 (HSV-1) infection of the brain. Heat shock protein 90 (Hsp90) is a molecular chaperone that is stimulated in response to many stressful conditions (e.g., inflammation and hypoxia) and Hsp90 inhibitors are suggested to be potent ...

journal_title：Biochemical pharmacology

authors： Li F,Song X,Su G,Wang Y,Wang Z,Qing S,Jia J,Wang Y,Huang L,Zheng K,Wang Y

更新日期：2019-08-01 00:00:00

abstract：:Despite the steadily increased numbers of formyl peptide receptor (FPR) ligands identified over the years, few have been characterized in studies using animal disease models and even less have entered clinical trials in human subjects. A small-molecule compound, Act-389949, was however recently tested in a phase I cli...

journal_title：Biochemical pharmacology

authors： Lind S,Sundqvist M,Holmdahl R,Dahlgren C,Forsman H,Olofsson P

更新日期：2019-08-01 00:00:00

abstract：:Duration of gene silencing due to the short-term silencing effects induced by exogenous siRNA have limited the therapeutic applications of RNAi and the development of RNAi-based therapeutics. We here generated Eg5 shRNA-expressing plasmids using the inverted terminal repeats (ITRs) sequences to produce Eg5 hairpin RNA...

journal_title：Biochemical pharmacology

authors： Seraj S,Lee J,Ahn HJ

更新日期：2019-08-01 00:00:00

abstract：:Pancreatic cancer is a major cause of cancer-related mortality around the world. Currently, options for diagnosis and treatment are extremely limited, which culminates in a very high mortality rate. Intensive research spanning more than four decades has met several roadblocks in terms of improvement in overall surviva...

journal_title：Biochemical pharmacology

authors： Guha Majumdar A,Subramanian M

更新日期：2019-08-01 00:00:00

abstract：:Osteoarthritis is the most prevalent musculoskeletal disorder and one for which there is no disease modifying therapy available at present. Our current understanding of the disease mechanism of osteoarthritis is limited owing to a lacuna of knowledge about the development and maintenance of articular cartilage that is...

journal_title：Biochemical pharmacology

authors： Jaswal AP,Bandyopadhyay A

更新日期：2019-07-01 00:00:00

abstract：:Matrix metalloproteinases (MMPs), A Disintegrin and Metalloproteinase (ADAM) and A Disintegrin and Metalloproteinase with Thrombospondin Motif (ADAMTS) are zinc-dependent endopeptidases that play a critical role in the destruction of extracellular matrix proteins and, the shedding of membrane-bound receptor molecules ...

journal_title：Biochemical pharmacology

authors： Malemud CJ

更新日期：2019-07-01 00:00:00

abstract：:Coenzyme CoQ10 (CoQ10), a ubiquinone compound, has been reported to inhibit tyrosinase activity and melanin production in melanoma B16F10 cells. However, the molecular mechanism underlying this inhibitory effect is poorly understood. In this paper we aimed to investigate the molecular mechanisms involved in the anti-m...

journal_title：Biochemical pharmacology

authors： Hseu YC,Ho YG,Mathew DC,Yen HR,Chen XZ,Yang HL

更新日期：2019-06-01 00:00:00

abstract：:Metamizole is an analgesic and antipyretic, but can cause neutropenia and agranulocytosis. We investigated the toxicity of the metabolites N-methyl-4-aminoantipyrine (MAA), 4-aminoantipyrine (AA), N-formyl-4-aminoantipyrine (FAA) and N-acetyl-4-aminoantipyrine (AAA) on neutrophil granulocytes and on HL60 cells (granul...

journal_title：Biochemical pharmacology

authors： Rudin D,Lanzilotto A,Bachmann F,Housecroft CE,Constable EC,Drewe J,Haschke M,Krähenbühl S

更新日期：2019-05-01 00:00:00

abstract：:Methotrexate (MTX) is a chemotherapy agent linked to cognitive deficits in cancer patients received chemotherapy treatment. MTX decreases cell proliferation in the hippocampus, which is concomitant with cognitive deficits in animal models. The present study aimed to investigate the disadvantages of MTX on cognition as...

journal_title：Biochemical pharmacology

authors： Sirichoat A,Krutsri S,Suwannakot K,Aranarochana A,Chaisawang P,Pannangrong W,Wigmore P,Welbat JU

更新日期：2019-05-01 00:00:00

abstract：:The therapeutic efficacy of immunosuppressive agents has been intensively studied for colitis management. We synthesized a series of andrographolide derivatives and reported their structure-activity-relationship and anti-inflammatory activity in our previous studies. Among these derivatives, compound 3b exhibited the ...

journal_title：Biochemical pharmacology

authors： Guo BJ,Liu Z,Ding MY,Li F,Jing M,Xu LP,Wang YQ,Zhang ZJ,Wang Y,Wang D,Zhou GC,Wang Y

更新日期：2019-05-01 00:00:00

abstract：:Ca2+/calmodulin-dependent protein kinase II (CaMKII) plays an important role in the cardiovascular system. However, the potential protective role of inhibitor 1 of protein phosphatase 1 (I1PP1), which is able to regulate CaMKII, in high glucose-induced cardiomyocytes injury remains unknown. In the present study, cardi...

journal_title：Biochemical pharmacology

authors： Sun L,Chen Y,Luo H,Xu M,Meng G,Zhang W

更新日期：2019-05-01 00:00:00

abstract：:The development of neuroprotective agents is necessary for the treatment of neurodegenerative diseases. Here, we report PQA-11, a prenylated quinolinecarboxylic acid (PQA) derivative, as a potent neuroprotectant. PQA-11 inhibits glutamate-induced cell death and caspase-3 activation in hippocampal cultures, as well as ...

journal_title：Biochemical pharmacology

authors： Ogura M,Kikuchi H,Shakespear N,Suzuki T,Yamaki J,Homma MK,Oshima Y,Homma Y

更新日期：2019-04-01 00:00:00

abstract：:H460 non-small cell lung, HCT116 colon and 4T1 breast tumor cell lines induced into senescence by exposure to either etoposide or doxorubicin were able to recover proliferative capacity both in mass culture and when enriched for the senescence-like phenotype by flow cytometry (based on β-galactosidase staining and cel...

journal_title：Biochemical pharmacology

authors： Saleh T,Tyutyunyk-Massey L,Murray GF,Alotaibi MR,Kawale AS,Elsayed Z,Henderson SC,Yakovlev V,Elmore LW,Toor A,Harada H,Reed J,Landry JW,Gewirtz DA

更新日期：2019-04-01 00:00:00

abstract：:SARM is the fifth and most conserved member of the Toll/Il-1 Receptor (TIR) adaptor family. However, unlike the other TIR adaptors, MyD88, Mal, TRIF and TRAM, SARM does not participate in transducing signals downstream of TLRs. By contrast SARM inhibits TLR signalling by interacting with the adaptors TRIF and MyD88. I...

journal_title：Biochemical pharmacology

authors： Carty M,Bowie AG

更新日期：2019-03-01 00:00:00

abstract：:Alcoholic ketoacidosis and diabetic ketoacidosis are life-threatening complications that share the characteristic features of high anion gap metabolic acidosis. Ketoacidosis is attributed in part to the massive release of ketone bodies (e.g., β-hydroxybutyrate; βOHB) from the liver into the systemic circulation. To da...

journal_title：Biochemical pharmacology

authors： Srinivasan MP,Shawky NM,Kaphalia BS,Thangaraju M,Segar L

更新日期：2019-02-01 00:00:00

abstract：:Augmented endothelium-dependent contractions (EDC) contributes to endothelial dysfunction and vascular disease progression. An early signal in EDC is cytosolic [Ca2+]i rise in endothelial cells, which stimulates the production of contractile prostanoids, leading to vascular contraction. In this study, the molecular id...

journal_title：Biochemical pharmacology

authors： Liang C,Zhang Y,Zhuo D,Lo CY,Yu L,Lau CW,Kwan YW,Tse G,Huang Y,Yao X

更新日期：2019-01-01 00:00:00