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Biochemical Pharmacology | Page 2

Lei Zhang, Peipei Xu, Yi Cheng, Peili Wang, Xinrun Ma, Mingyao Liu, Xin Wang, Feng Xu
Obesity increases the incidences of metabolic syndrome, including type 2 diabete, fatty liver, dyslipidemia, hyperglycemia, heart disease, hypertension and cancer. In particular, pharmacokinetics and pharmacodynamics of many drugs have changed in obese patients. However, little is known about the hepatic drug-metabolizing enzymes and transporters that are influenced by diet-induced obese. In this report, we established obesity and fatty liver models in male rats by high-fat diet. The expression profiles of drug-metabolizing enzymes and transporters were studied by quantitative real-timePCR and Western blotting analysis...
May 4, 2019: Biochemical Pharmacology
Matthew Campbell, Sarah L Doyle
Neovascularization is a hallmark pathology of numerous retinal diseases from diabetic retinopathy (DR) to age-related related macular degeneration (AMD). Over the past 2 decades, the rise of anti-VEGF based medications for neovascular eye conditions has revolutionized the treatment paradigm for patients and preserved the vision of millions. With any form of therapy however, there remain pitfalls and areas for improved interventions. Here, we succinctly present some current views on treatment options for patients with retinal and choroidal neovascularization...
April 27, 2019: Biochemical Pharmacology
Miguel Á González-Gay, Trinitario Pina, Diana Prieto-Peña, Mónica Calderon-Goercke, Oreste Gualillo, Santos Castañeda
Giant cell arteritis (GCA) is the most common form of vasculitis in adults. Cranial manifestations are typical clinical features of this vasculitis. Sometimes the presenting symptoms are nonspecific and, in some cases, large-vessel involvement may prevail. Polymyalgia rheumatica is a frequent manifestation that in some cases may be the presenting symptom of GCA. Visual complications, in particular the risk of blindness, constitute the most feared manifestations of GCA. Prompt recognition of this vasculitis is required to avoid irreversible complications...
April 26, 2019: Biochemical Pharmacology
Cong Liu, Yanshan Fang
Abnormal protein aggregation is a common pathological feature of neurodegenerative diseases such as Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease (HD) and amyotrophic lateral sclerosis (ALS). Protein posttranslational modifications (PTMs) play a crucial regulatory role in the formation of pathologic aggregation. Among the known PTMs involved in neurodegeneration, poly(ADP-ribosylation) (PARylation) has emerged with promising therapeutic potentials of the use of poly(ADP-ribose) (PAR) polymerase (PARP) inhibitors...
April 26, 2019: Biochemical Pharmacology
Isabella Faraoni, Manuela Giansanti, Maria Teresa Voso, Francesco Lo-Coco, Grazia Graziani
Acute myeloid leukaemia (AML) is a highly heterogeneous disease characterized by uncontrolled proliferation, block in myeloid differentiation and recurrent genetic abnormalities. In the search of new effective therapies, identification of synthetic lethal partners of AML genetic alterations might represent a suitable approach to tailor patient treatment. Genetic mutations directly affecting DNA repair genes are not commonly present in AML. Nevertheless, several studies indicate that AML cells show high levels of DNA lesions and genomic instability...
April 24, 2019: Biochemical Pharmacology
Jayant Dewangan, Sonal Srivastava, Sakshi Mishra, Aman Divakar, Sadan Kumar, Srikanta Kumar Rath
Cancer is a complex disease wherein cells begin to divideabnormally and spread into surrounding tissues. Angiogenesis plays a crucial role in tumor progression as it is required for sustained growth and metastasis, therefore targeting angiogenesis is a promising therapeutic approach for breast cancer management. Salinomycin (SAL) has been reported to exhibit anticancer response on various types of cancer. In the present study, we explored the antiangiogenic and anticancer efficacy of the polyether ionophore SAL in the breast cancer model...
April 24, 2019: Biochemical Pharmacology
Ai-Hua Jin, Ben Cristofori-Armstrong, Lachlan D Rash, Sergio Agustín Román González, Roberto Arreguín Espinosa, Richard J Lewis, Paul F Alewood, Irina Vetter
Conorfamides are a poorly studied family of cone snail venom peptides with broad biological activities, including inhibition of NMDA receptors, acid-sensing ion channels, voltage-gated potassium channels, and ligand-gated glutamate receptors. The aim of this study was to characterise the pharmacological activity of two novel linear conorfamides (conorfamide_As1a and conorfamide_As2a) and their non-amidated counterparts (conopeptide_As1b and conopeptide_As2b) that were isolated from the venom of the Mexican cone snail Conus austini...
April 24, 2019: Biochemical Pharmacology
Nadia Ciriaci, Romina Belén Andermatten, María Valeria Razori, Virginia Soledad Schuck, Gisel Sabrina Miszczuk, Anabela Carolina Medeot, Fernando Ariel Crocenzi, Marcelo Gabriel Roma, Ismael Ricardo Barosso, María Laura Ruiz, Enrique Juan Sánchez Pozzi
TNFα is a cytokine whose levels are increased in inflammatory pathologies that are associated with cholestasis. Endocytic internalization of Abcc2 (multidrug resistance-associated protein 2), a canalicular transporter of organic anions that is implicated in the clearance of clinically important drugs, is a phenomenon that occurs in inflammatory liver diseases, and it has been established that cytokines act as mediators. However, the intracellular mechanism involved in this effect remains unknown. The aim of the present work was to characterize the internalization of Abcc2 induced by TNFα and to study the role of ERK1/2 and reactive oxygen species as signaling mediators of transporter internalization...
April 23, 2019: Biochemical Pharmacology
Vernon J Ebegboni, Reham M Balahmar, John M Dickenson, Shiva D Sivasubramaniam
Adequate invasion and complete remodelling of the maternal spiral arteries by the invading extravillous trophoblasts are the major determinants of a successful pregnancy. Increase in oxidative stress during pregnancy has been linked to the reduction in trophoblast invasion and incomplete conversion of the maternal spiral arteries, resulting in pregnancy complications such as pre-eclampsia, intrauterine growth restriction, and spontaneous miscarriages resulting in foetal/maternal mortality. The use of antioxidant therapy (vitamin C and E) and other preventative treatments (such as low dose aspirin) have been ineffective in preventing pre-eclampsia...
April 22, 2019: Biochemical Pharmacology
Wenxiu Qi, Xiaohao Xu, Manying Wang, Li Xiangyan, Chaonan Wang, Liping Sun, Daqing Zhao, Liwei Sun
Resistance to standard induction therapy and relapse remain the primary challenges for improving therapeutic effects in acute myeloid leukemia (AML); thus, novel therapeutic strategies are urgently required. Ataxia telangiectasia and Rad3-related protein (ATR) is a key regulator of different types of DNA damage, which is crucial for the maintenance of genomic integrity. The ATR-selective inhibitor VE-822 has proper solubility, potency, and pharmacokinetic properties. In this study, we investigated the anti-leukemic effects of VE-822 alone or combined with Wee1-selective inhibitor AZD1775 in AML cells...
April 20, 2019: Biochemical Pharmacology
Joseph D Raffetto, Fiorella Calanni, Paolo Mattana, Raouf A Khalil
Sulodexide (SDX) is a highly purified glycosaminoglycan with antithrombotic and profibrinolytic properties and reported benefits in thrombotic and atherosclerotic vascular disorders. However, the effects of SDX on vascular function are unclear. We tested whether SDX affects vascular relaxation and examined the potential underlying mechanisms. Isolated segments of male rat abdominal aorta and mesenteric artery were suspended in a tissue bath, and the changes in arterial contraction/relaxation were measured. The α-adrenergic receptor agonist phenylephrine (Phe) (10-9 to 10-5 M) caused concentration-dependent aortic and mesenteric artery contraction that was reduced in tissues pretreated with SDX (1 mg/ml)...
April 20, 2019: Biochemical Pharmacology
Anna Zimdahl Kahlin, Sara Helander, Karin Skoglund, Peter Söderkvist, Lars-Göran Mårtensson, Malin Lindqvist Appell
Thiopurines are widely used in the treatment of leukemia and inflammatory bowel diseases. Thiopurine metabolism varies among individuals because of differences in the polymorphic enzyme thiopurine methyltransferase (TPMT, EC, and to avoid severe adverse reactions caused by incorrect dosing it is recommended that the patient's TPMT status be determined before the start of thiopurine treatment. This study describes the concordance between genotyping for common TPMT alleles and phenotyping in a Swedish cohort of 12,663 patients sampled before or during thiopurine treatment...
April 18, 2019: Biochemical Pharmacology
Taizhen Liang, Xuanxuan Zhang, Fangyuan Lai, Jian Lin, Chenliang Zhou, Xinfeng Xu, Xinghua Tan, Shuwen Liu, Lin Li
The persistence of latent human immunodeficiency virus type 1 (HIV-1) reservoirs remains a major hurdle for HIV-1 eradication. The "shock and kill" strategy relies on the drug-mediated reversion of HIV-1 latency and the subsequent death of HIV-producing cells. Unfortunately, none of the agents currently in use possess a sufficient potency to reactivate latent virus or eliminate the latent HIV-1 reservoir in vivo. Here, we demonstrated that a promising specific bromodomain and extraterminal domain inhibitor, CPI-203, could potently reactivate latent HIV-1 in different latently infected cell lines with minimal cytotoxicity by activating the positive transcription elongation factor b signaling pathway...
April 13, 2019: Biochemical Pharmacology
You-Cheng Hseu, Yi-Geng Ho, Dony Chacko Mathew, Hung-Rong Yen, Xuan-Zao Chen, Hsin-Ling Yang
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-melanogenic activity of CoQ10 (1-2 μM) in UVA (5 J/cm2 )-irradiated keratinocyte HaCaT cells and α-MSH stimulated B16-F10 cells. It was observed that CoQ10 suppressed p53/POMC, α-MSH production as well as inhibited ROS generation in UVA-irradiated keratinocyte HaCaT cells...
April 13, 2019: Biochemical Pharmacology
Harika Sabbineni, Arti Verma, Sandeep Artham, Daniel Anderson, Oge Amaka, Fang Liu, Subhadra P Narayanan, Payaningal R Somanath
Endothelial to mesenchymal transition (EndMT), where endothelial cells acquire mesenchymal characteristics has been implicated in several cardiopulmonary, vascular and fibrotic diseases. The most commonly studied molecular mechanisms involved in EndMT include TGFβ, Notch, interleukin, and interferon-γ signaling. As of today, the contributions of Akt1, an important mediator of TGFβ signaling and a key regulator of endothelial barrier function to EndMT remains unclear. By using the ShRNA based gene silencing approach and endothelial-specific inducible Akt1 knockdown (ECKOAkt1 ) mice, we studied the role of Akt1 in EndMT in vitro and pathological vascular remodeling in vivo...
April 13, 2019: Biochemical Pharmacology
Takao Hirai, Yuhei Mitani, Karen Kurumisawa, Kohei Nomura, Wei Wang, Ken-Ichi Nakashima, Makoto Inoue
Fibroblast growth factor 21 (FGF21), a member of the FGF subfamily that acts through the FGF receptor 1 with the co-receptor β-Klotho, functions as an important metabolic regulator of peripheral glucose tolerance and lipid homeostasis in an endocrine or autocrine and/or paracrine manner. Previous studies showed that FGF21 ameliorated and prevented the development of metabolic disorders, such as obesity and diabetes mellitus. In the present study, we demonstrated that berberine, a naturally occurring compound, stimulated FGF21 expression in brown adipose tissue (BAT)...
April 13, 2019: Biochemical Pharmacology
Chin-Hee Song, Nayoung Kim, Sun Min Lee, Ryoung Hee Nam, Soo In Choi, So Ra Kang, Eun Shin, Dong Ho Lee, Ha-Na Lee, Young-Joon Surh
Estrogen is known to have a protective effect in colorectal cancer (CRC) development. Previously, we reported the anti-inflammatory and antitumorigenic effects of 17β-estradiol (E2) in azoxymethane (AOM)/dextran sulfate sodium (DSS)-treated male mice. The aim of this study was to investigate whether ovariectomy in a female AOM/DSS mouse model increases colorectal tumorigenesis and whether tumorigenesis is reduced by estrogen supplementation after ovariectomy. Clinical symptoms and histological severity of colitis and the levels of inflammatory mediators were evaluated in the colon of AOM/DSS-treated ovariectomized (OVX) mice...
April 11, 2019: Biochemical Pharmacology
Pedro Buc Calderon, Raphaël Beck, Christophe Glorieux
A crucial process in biology is the conversion of the genetic information into functional proteins that carry out the genetic program. However, a supplementary step is required to obtain functional proteins: the folding of the newly translated polypeptides into well-defined, three-dimensional conformations. Proteins chaperones are crucial for this final step in the readout of genetic information, which results in the formation of functional proteins. In this review, a special attention will be given to the strategies targeting hsp90 family members in order to increase cancer cell death...
April 11, 2019: Biochemical Pharmacology
Olivier Malaise, Dominique de Seny
No abstract text is available yet for this article.
April 11, 2019: Biochemical Pharmacology
Daniel Villalobos-García, Rolando Hernández-Muñoz
Liver slices from starved rats and incubated without other substrates oxidized ethanol at a rate of 4.1 µmols • h-1 • g-1 . Addition of 10 mmols • L-1 lactate increased this rate 2-fold. 4-methylpyrazole (4-MP), an alcohol dehydrogenase (ADH) inhibitor, drastically decreased the rate of ethanol oxidation, but did not inhibit the stimulation due to lactate. In the same context, liver acetaldehyde production, as the main by-product of ethanol oxidation, appeared to be much less inhibited by 4-MP in the presence of lactate...
April 11, 2019: Biochemical Pharmacology
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