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Source: Biochemical Pharmacology

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Total 204 results found since Jan 2013.

Selective anticancer effects of a synthetic flavagline on human Oct4-expressing cancer stem-like cells via a p38 MAPK-dependent caspase-3-dependent pathway.
This study also shows that FL3 selectively kills poorly differentiated and highly aggressive carcinomal cells, but has little effect on normal stem-like cells. Thus FL3 offers great promise for cancer treatment since it is able to target the carcinogenic process without affecting normal cells. PMID: 24607276 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - March 4, 2014 Category: Drugs & Pharmacology Authors: Emhemmed F, Azouaou SA, Thuaud F, Schini-Kerth V, Désaubry L, Muller CD, Fuhrmann G Tags: Biochem Pharmacol Source Type: research

p53 inactivation decreases dependence on estrogen/ERK signalling for proliferation but promotes EMT and susceptility to 3-bromopyruvate in ERα+ breast cancer MCF-7 cells.
Conclusions.- a) ERα(+) breast cancer cells dysfunctional for TP53 which proliferate irrespective of low estrogen and chemical MEK inhibition are likely to increase metabolic consumption becoming increasingly susceptible to 3-BrPA; b) targeting the pyruvate pathway may improve response to endocrine therapy in ERα(+) breast cancer with p53 dysfunction. PMID: 24486524 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - January 28, 2014 Category: Drugs & Pharmacology Authors: Rieber M, Strasberg-Rieber M Tags: Biochem Pharmacol Source Type: research

The novel pyrrolo-1,5-benzoxazepine, PBOX-6, synergistically enhances the apoptotic effects of carboplatin in drug sensitive and multidrug resistant neuroblastoma cells.
In conclusion, our findings indicate the potential of the PBOX compounds in enhancing chemosensitivity in neuroblastoma. PMID: 24406249 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - January 6, 2014 Category: Drugs & Pharmacology Authors: Lennon JC, Bright SA, Carroll E, Butini S, Campiani G, O'Meara A, Williams DC, Zisterer DM Tags: Biochem Pharmacol Source Type: research

Heat Shock Factor 1 Confers Resistance to Hsp90 Inhibitors through p62/SQSTM1 Expression and Promotion of Autophagic Flux.
We report a mechanism by which HSF1 activation diminishes the effect of Hsp90 inhibitors geldanamycin and 17-allylaminogeldanamycin (17-AAG, tanespimycin). Silencing HSF1 with siRNA or inhibiting HSF1 activity with KRIBB11 lowers the threshold for apoptosis in geldanamycin and 17-AAG-treated cancer cells. Autophagy also mitigates the actions of Hsp90 inhibitors. Blocking autophagy with 3-methyladenine (3-MA), bafilomycin A1, or beclin 1 siRNA also lower the threshold forapoptosis. Exploring a potential relationship between HSF1 and autophagy, we monitored autophagosome formation and autophagic flux in control and HSF1-sile...
Source: Biochemical Pharmacology - November 28, 2013 Category: Drugs & Pharmacology Authors: Samarasinghe B, Wales CT, Taylor FR, Jacobs AT Tags: Biochem Pharmacol Source Type: research

Bradykinin promotes vascular endothelial growth factor expression and increases angiogenesis in human prostate cancer cells.
Abstract Prostate cancer is the most commonly diagnosed malignancy in men and shows a tendency for metastasis to distant organs. Angiogenesis is required for metastasis. Bradykinin (BK) is an inflammatory mediator involved in tumor growth and metastasis, but its role in vascular endothelial growth factor (VEGF) expression and angiogenesis in human prostate cancer remains unknown. The aim of this study was to examine whether BK promotes prostate cancer angiogenesis via VEGF expression. We found that exogenous BK increased VEGF expression in prostate cancer cells and further promoted tube formation in endothelial pr...
Source: Biochemical Pharmacology - November 10, 2013 Category: Drugs & Pharmacology Authors: Yu HS, Wang SW, Chang AC, Tai HC, Yeh HI, Lin YM, Tang CH Tags: Biochem Pharmacol Source Type: research

Adenosine dialdehyde suppresses MMP-9-mediated invasion of cancer cells by blocking the Ras/Raf-1/ERK/AP-1 signaling pathway.
In this study, we aimed to determine the regulatory effect of AdOx on cancer invasion by using three different cell lines: MDA-MB-231, MCF-7, and U87. The invasive capacity of these cells in the presence (MCF-7) or absence (MDA-MB-231 and U87) of phorbal 12-myristate 13-actate (PMA) was strongly decreased by AdOx treatment. Furthermore, the expression, secretion, and activation of matrix metalloproteinase (MMP)-9, a critical enzyme regulating cell invasion, in these cells were diminished by AdOx treatment. AdOx strongly suppressed AP-1-mediated luciferase activity and, in parallel, reduced the translocation of c-Fos and c-...
Source: Biochemical Pharmacology - August 27, 2013 Category: Drugs & Pharmacology Authors: Kim JH, Kim JH, Kim SC, Yi YS, Yang WS, Yang Y, Kim HK, Lee JY, Kim KH, Yoo BC, Hong S, Cho JY Tags: Biochem Pharmacol Source Type: research

Salsalate and Adiponectin Ameliorate Hepatic Steatosis by Inhibition of the Hepatokine Feutin-A.
In conclusion, salsalate and fAd improved palmitate-induced steatosis and impairment of lipid metabolism in hepatocytes via fetuin-A inhibition through the AMPK-NFκB pathway. PMID: 23948064 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - August 12, 2013 Category: Drugs & Pharmacology Authors: Jung TW, Youn BS, Choi HY, Lee SY, Hong HC, Yang SJ, Yoo HJ, Kim BH, Baik SH, Choi KM Tags: Biochem Pharmacol Source Type: research

Gene Expression Profiling for Analysis Acquired Oxaliplatin Resistant Factors in Human Gastric Carcinoma TSGH-S3 Cells: the Role of IL-6 Signaling and Nrf2/AKR1C Axis Identification.
Abstract Oxaliplatin treatment is a mainstay of treatment for advanced gastrointestinal tract cancer, but the underlying mechanisms of acquired oxaliplatin resistance remain largely obscured. We previously demonstrated that increased DNA repair capacity and copper-transporting ATPase 1 (ATP7A) level contributed to oxaliplatin resistance in the human gastric carcinoma cell line TSGH-S3 (S3). In the present study, we applied gene array technology to identify additional resistance factors in S3 cells. We found that interleukin-6 (IL-6), aldo-keto reductase 1C1 (AKR1C1), and AKR1C3 are the top 3 upregulated genes in S...
Source: Biochemical Pharmacology - August 8, 2013 Category: Drugs & Pharmacology Authors: Chen CC, Chu CB, Liu KJ, Huang CY, Chang JY, Pan WY, Chen HH, Cheng YH, Lee KD, Chen MF, Kuo CC, Chen LT Tags: Biochem Pharmacol Source Type: research

Role of Hypoxia Inducible Factor-1α in the Regulation of the Cancer-Specific Variant of Organic Anion Transporting Polypeptide 1B3 (OATP1B3), in Colon and Pancreatic Cancer.
Abstract Organic anion transporting polypeptide 1B3 (OATP1B3) was initially considered to be a liver-specific transporter, mediating the uptake of a variety of endogenous and xenobiotic substances. Over the past decade, several investigations reported that OATP1B3 is also expressed across multiple types of cancers. Only recently, our laboratory and others demonstrated the identity of cancer-specific OATP1B3 variants (csOATP1B3) arising from the use of an alternative transcription initiation site, different from the wildtype (WT) OATP1B3 expressed in the normal liver. However, the mechanisms regulating the expressi...
Source: Biochemical Pharmacology - August 4, 2013 Category: Drugs & Pharmacology Authors: Han S, Kim K, Thakkar N, Kim D, Lee W Tags: Biochem Pharmacol Source Type: research

Transport of gabapentin by LAT1 (SLC7A5).
Abstract Gabapentin is used in the treatment of epilepsy and neuropathic pain. Gabapentin has high and saturable permeability across the BBB, but no mechanistic studies underpinning this process have been reported. The aim of the current study was to investigate the transport of gabapentin in a model of the BBB, identify the important drug transporter(s) and to use mathematical modelling to quantify the processes involved. A human brain endothelial cell line (hCMEC/D3) was utilised as an in-vitro model of the BBB. Uptake of radiolabeled gabapentin into cells in the presence of chemical inhibitors, siRNA or overexp...
Source: Biochemical Pharmacology - May 25, 2013 Category: Drugs & Pharmacology Authors: Dickens D, Webb SD, Antonyuk S, Giannoudis A, Owen A, Rädisch S, Hasnain SS, Pirmohamed M Tags: Biochem Pharmacol Source Type: research

Pregnane X receptor dependent up-regulation of CYP2C9 and CYP3A4 in tumor cells by antitumor acridine agents, C-1748 and C-1305, selectively diminished under hypoxia.
Abstract Induction of proteins involved in drug metabolism and in drug delivery has a significant impact on drug-drug interactions and on the final therapeutic effects. Two antitumor acridine derivatives selected for present studies, C-1748 (9-(2'-hydroxyethylamino)-4-methyl-1-nitroacridine) and C-1305 (5-dimethylaminopropylamino-8-hydroxy-triazoloacridinone), expressed high and low susceptibility to metabolic transformations with liver microsomes, respectively. In the current study, we examined the influence of these compounds on cytochrome P450 3A4 (CYP3A4) and 2C9 (CYP2C9) enzymatic activity and gene expression...
Source: Biochemical Pharmacology - May 17, 2013 Category: Drugs & Pharmacology Authors: Niemira M, Dastych J, Mazerska Z Tags: Biochem Pharmacol Source Type: research

Angiotensin II upregulates KCa3.1 channels and stimulates cell proliferation in rat cardiac fibroblasts.
Abstract The proliferation of cardiac fibroblasts is implicated in the pathogenesis of myocardial remodeling and fibrosis. Intermediate-conductance calcium-activated K(+) channels (KCa3.1 channels) have important roles in cell proliferation. However, it is unknown whether angiotensin II (Ang II), a potent profibrotic molecule, would regulate KCa3.1 channels in cardiac fibroblasts and participate in cell proliferation. In the present study, we investigated whether KCa3.1 channels were regulated by Ang II, and how the channel activity mediated cell proliferation in cultured adult rat cardiac fibroblasts using electr...
Source: Biochemical Pharmacology - May 15, 2013 Category: Drugs & Pharmacology Authors: Wang LP, Wang Y, Zhao LM, Li GR, Deng XL Tags: Biochem Pharmacol Source Type: research

Identification of upregulated phosphoinositide 3-kinase γ as a target to suppress breast cancer cell migration and invasion.
Abstract Metastasis is the major cause of breast cancer mortality. We recently reported that aberrant G-protein coupled receptor (GPCR) signaling promotes breast cancer metastasis by enhancing cancer cell migration and invasion. Phosphatidylinositol 3-kinase γ (PI3Kγ) is specifically activated by GPCRs. The goal of the present study was to determine the role of PI3Kγ in breast cancer cell migration and invasion. Immunohistochemical staining showed that the expression of PI3Kγ protein was significantly increased in invasive human breast carcinoma when compared to adjacent benign breast tissue or ductal carcinom...
Source: Biochemical Pharmacology - May 15, 2013 Category: Drugs & Pharmacology Authors: Xie Y, Abel PW, Kirui JK, Deng C, Sharma P, Wolff DW, Toews ML, Tu Y Tags: Biochem Pharmacol Source Type: research

Concurrent Regulation of the Transcription Factors Nrf2 and ATF4 Mediates the Enhancement of Glutathione Levels by the Flavonoid Fisetin.
Abstract Glutathione (GSH) and GSH-associated metabolism provide the major line of defense for the protection of cells from various forms of toxic stress. GSH also plays a key role in regulating the intracellular redox environment. Thus, maintenance of GSH levels is developing into an important therapeutic objective for the treatment of a variety of diseases. Among the transcription factors that play critical roles in GSH metabolism are NF-E2-related factor 2 (Nrf2) and activating transcription factor 4 (ATF4). Thus, compounds that can upregulate these transcription factors may be particularly useful as treatment ...
Source: Biochemical Pharmacology - April 22, 2013 Category: Drugs & Pharmacology Authors: Ehren JL, Maher P Tags: Biochem Pharmacol Source Type: research

Modulation of A-type K(+) channels by the short-chain cobrotoxin through the protein kinase C-delta isoform decreases membrane excitability in dorsal root ganglion neurons.
In this study, we identified the functional role of cobrotoxin, the short-chain α-neurotoxin isolated from Naja atra venom, which acts in the regulation of the transient A-type K(+) currents (I(A)) and membrane excitability in dorsal root ganglion (DRG) neurons via the activation of the muscarinic M3 receptor (M3R). Our results showed that cobrotoxin increased I(A) in a concentration-dependent manner, whereas the sustained delayed rectifier K(+) currents (I(DR)) were not affected. Cobrotoxin did not affect the activation of I(A) markedly, however, it shifted the inactivation curve significantly in the depolarizing directi...
Source: Biochemical Pharmacology - February 19, 2013 Category: Drugs & Pharmacology Authors: Guo Q, Jiang YJ, Jin H, Jiang XH, Gu B, Zhang YM, Wang JG, Qin ZH, Tao J Tags: Biochem Pharmacol Source Type: research