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Source: Biochemical Pharmacology

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Total 204 results found since Jan 2013.

Involvement of Src and the actin cytoskeleton in the antitumorigenic action of adenosine dialdehyde.
In this study, we examined the effects of transmethylation on tumorigenic responses and its regulatory mechanism using an upregulation strategy of adenosylhomocysteine (SAH) acting as a negative feedback inhibitor. Treatment with adenosine dialdehyde (AdOx), an inhibitor of transmethylation-suppressive adenosylhomocysteine (SAH) hydrolase (SAHH), enhanced the level of SAH and effectively blocked the proliferation, migration, and invasion of cancer cells; the treatment also induced the differentiation of C6 glioma cells and suppressed the neovascular genesis of eggs in a dose-dependent manner. Through immunoblotting analysi...
Source: Biochemical Pharmacology - January 24, 2013 Category: Drugs & Pharmacology Authors: Kim JH, Lee YG, Yoo S, Oh J, Jeong D, Song WK, Yoo BC, Rhee MH, Park J, Cha SH, Hong S, Cho JY Tags: Biochem Pharmacol Source Type: research

c-Src-dependent MAPKs/AP-1 activation is involved in TNF-α-induced matrix metalloproteinase-9 expression in rat heart-derived H9c2 cells.
Abstract TNF-α plays a critical mediator in the pathogenesis of chronic heart failure contributing to cardiac remodeling and peripheral vascular disturbances. The implication of TNF-α in inflammatory responses has been shown to be mediated through up-regulation of inflammatory genes, including matrix metalloproteinase-9 (MMP-9). However, the detailed mechanisms of TNF-α-induced MMP-9 expression are largely unclear in the heart cells. Here, we demonstrated that in rat embryonic-heart derived H9c2 cells, TNF-α could induce MMP-9 mRNA expression associated with an increase in the secretion of MMP-9, determined by...
Source: Biochemical Pharmacology - January 24, 2013 Category: Drugs & Pharmacology Authors: Yang CM, Lee IT, Lin CC, Wang CH, Cherng WJ, Hsiao LD Tags: Biochem Pharmacol Source Type: research

Saxifragifolin D induces the interplay between apoptosis and autophagy in breast cancer cells through ROS-dependent endoplasmic reticulum stress.
In conclusion, SD inhibits breast cancer cell growth and induces interplay between apoptosis and autophagy through ROS-mediated endoplasmic reticulum stress. It will provide molecular bases for developing SD into a drug candidate for the treatment of breast cancer. PMID: 23348250 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - January 21, 2013 Category: Drugs & Pharmacology Authors: Shi JM, Bai LL, Zhang DM, Yiu A, Yin ZQ, Han WL, Liu JS, Li Y, Fu DY, Ye WC Tags: Biochem Pharmacol Source Type: research

AMP-Activated Protein Kinase as Regulator of P2Y6 Receptor-Induced Insulin Secretion in Mouse Pancreatic β-Cells.
Abstract 5'-AMP-activated protein kinase (AMPK) and its pharmacological modulators have been targeted for treating type 2 diabetes. Extracellular uridine 5'-diphosphate (UDP) activates P2Y(6) receptors (P2Y(6)Rs) in pancreatic β-cells to release insulin and reduce apoptosis, which would benefit diabetes. Here, we studied the role of P2Y(6)R in activation of AMPK in MIN6 mouse pancreatic β-cells and insulin secretion. Treatment with a potent P2Y(6)R dinucleotide agonist MRS2957 (500nM) activated AMPK, which was blocked by P2Y(6)R-selective antagonist MRS2578. Also, MRS2957 induced phosphorylation of acetyl-coenzy...
Source: Biochemical Pharmacology - January 17, 2013 Category: Drugs & Pharmacology Authors: Balasubramanian R, Maruoka H, Jayasekara MP, Gao ZG, Jacobson KA Tags: Biochem Pharmacol Source Type: research

Inhibition of T-type calcium channels disrupts Akt signaling and promotes apoptosis in glioblastoma cells.
In this study, we found that inhibition of T-type Ca(2+) channels in GBM cells significantly reduced their survival and resistance to therapy. Moreover, either T-type selective antagonists, such as mibefradil, or siRNA-mediated knockdown of the T-type channel alpha subunits not only reduced cell viability and clonogenic potential, but also induced apoptosis. In response to channel blockade or ablation, we observed reduced phosphorylation of Akt and Rictor, suggesting inhibition of the mTORC2/Akt pathway. This was followed by reduction in phosphorylation of anti-apoptotic Bad and caspases activation. The apoptotic response ...
Source: Biochemical Pharmacology - December 31, 2012 Category: Drugs & Pharmacology Authors: Valerie NC, Dziegielewska B, Hosing AS, Augustin E, Gray LS, Brautigan DL, Larner JM, Dziegielewski J Tags: Biochem Pharmacol Source Type: research

Metformin-mediated downregulation of p38 mitogen-activated protein kinase-dependent excision repair cross-complementing 1 decreases DNA repair capacity and sensitizes human lung cancer cells to paclitaxel.
Abstract Metformin, an extensively used and well-tolerated drug for treating individuals with type 2 diabetes, has recently gained significant attention as an anticancer drug. On the other hand, paclitaxel (Taxol) is a new antineoplastic drug that has shown promise in the treatment of non-small cell lung cancer (NSCLC). High expression levels of excision repair cross-complementary 1 (ERCC1) in cancers have been positively associated with the DNA repair capacity and a poor prognosis in NSCLC patients treated with platinum-containing chemotherapy. In this current study, paclitaxel was found to increase phosphorylati...
Source: Biochemical Pharmacology - December 7, 2012 Category: Drugs & Pharmacology Authors: Tseng SC, Huang YC, Chen HJ, Chiu HC, Huang YJ, Wo TY, Weng SH, Lin YW Tags: Biochem Pharmacol Source Type: research

Interleukin-6 induces vascular endothelial growth factor expression and promotes angiogenesis through apoptosis signal-regulating kinase 1 in human osteosarcoma.
Abstract Osteosarcoma is characterized by a high malignant and metastatic potential. Angiogenesis is essential for the caner metastasis. Interleukin-6 (IL-6) is a multifunctional cytokine that is associated with the disease status and outcomes of cancers. However, the relationship between IL-6 and vascular endothelial growth factor (VEGF) expression in human osteosarcoma is mostly unknown. Here we found that the IL-6 and VEGF expression was correlated with tumor stage and significantly higher than that in normal bone. Incubation of osteosarcoma cells with IL-6 increased VEGF mRNA and protein expression. Pretreatme...
Source: Biochemical Pharmacology - December 5, 2012 Category: Drugs & Pharmacology Authors: Tzeng HE, Tsai CH, Chang ZL, Su CM, Wang SW, Hwang WL, Tang CH Tags: Biochem Pharmacol Source Type: research

Folic acid inhibits endothelial cell migration through inhibiting the RhoA activity mediated by activating the folic acid receptor/cSrc/p190RhoGAP-signaling pathway.
Abstract Previously, our in vivo studies demonstrated that folic acid (FA) could inhibit angiogenesis and in vitro studies showed that FA reduced vascular endothelial cell proliferation through activating the cSrc/ERK-2/NFκB/p53 pathway mediated by FA receptor (FR). Here, we further examined the effect of FA on endothelial cell migration. Our results showed that FA (10μM) inhibited the formation of lamellipodia, migration and capillary-like tube formation of human umbilical venous endothelial cells (HUVEC). These inhibition effects induced by FA treatment were not due to reduction of cell survival and cell adhes...
Source: Biochemical Pharmacology - November 23, 2012 Category: Drugs & Pharmacology Authors: Hou TC, Lin JJ, Wen HC, Chen LC, Hsu SP, Lee WS Tags: Biochem Pharmacol Source Type: research

Inhibition of CIP2A determines erlotinib-induced apoptosis in hepatocellular carcinoma.
In conclusion, inhibition of CIP2A determines the effects of erlotinib on apoptosis in HCC. CIP2A may be useful as a therapeutic biomarker for predicting clinical response to erlotinib in HCC treatment. PMID: 23178652 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - November 23, 2012 Category: Drugs & Pharmacology Authors: Yu HC, Chen HJ, Chang YL, Liu CY, Shiau CW, Cheng AL, Chen KF Tags: Biochem Pharmacol Source Type: research