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Biochemical Pharmacology

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https://www.readbyqxmd.com/read/28431939/modulation-of-hat-activity-by-the-brca2n372hvariation-is-a-novel-mechanism-of-paclitaxel-resistance-in-breast-cancer-cell-lines
#1
Woo Sun Kwon, Sun Young Rha, Hei-Cheul Jeung, Tae Soo Kim, Hyun Cheol Chung
Paclitaxel stabilizes microtubule polymerization, enhances microtubule assembly, andG2/M arrests, leading to cell death. Paclitaxel resistance has been attributed to a variety of mechanisms. In the present study, we define a new resistance mechanism to paclitaxel based onBRCA2variation. Chemo-sensitivity to paclitaxel based on the variations was compared. Restoration of paclitaxel sensitivity was induced indirectly with combined treatment of paclitaxel and HDAC inhibitor. Variant and wild type of BRCA2 clones were obtained from wild and variant cells, respectively...
April 18, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28431938/selective-inhibition-of-ezh2-by-a-small-molecule-inhibitor-regulates-microglial-gene-expression-essential-for-inflammation
#2
Sarder Arifuzzaman, Amitabh Das, Sun Hwa Kim, Taeho Yoon, Young Seek Lee, Kyoung Hwa Jung, Young Gyu Chai
Multiple studies have documented that Enhancer of zeste homolog 2 (EZH2) could play a role in inflammation and a wide range of malignancies; however, the underlying mechanisms remain largely unaddressed. Microglial activation is a key process in the production and release of numerous pro-inflammatory mediators that play important roles in inflammation and neurodegeneration in the central nervous system (CNS). Therefore, our aim was to investigate whether inhibition of EZH2 with the selective small molecule inhibitor EPZ-6438 protects against neonatal microglial activation...
April 18, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28414139/ligand-dependent-and-independent-regulation-of-human-hepatic-sphingomyelin-phosphodiesterase-acid-like-3a-expression-by-pregnane-x-receptor-and-crosstalk-with-liver-x-receptor
#3
Judith Jeske, Andreas Bitter, Wolfgang E Thasler, Thomas S Weiss, Matthias Schwab, Oliver Burk
Pregnane X receptor (PXR) mainly regulates xenobiotic metabolism and detoxification. Additionally, it exerts pleiotropic effects on liver physiology, which in large parts depend on transrepression of other liver-enriched transcription factors. Based on the hypothesis that lower expression levels of PXR may reduce the extent of this inhibition, an exploratory genome-wide transcriptomic profiling was performed using HepG2 cell clones with different expression levels of PXR. This screen and confirmatory real-time RT-PCR identified sphingomyelin phosphodiesterase acid-like (SMPDL) 3A, a novel nucleotide phosphodiesterase and phosphoramidase, as being up-regulated by PXR-deficiency...
April 13, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28414138/apigenin-a-modulator-of-ppar%C3%AE-attenuates-hfd-induced-nafld-by-regulating-hepatocyte-lipid-metabolism-and-oxidative-stress-via-nrf2-activation
#4
Xiujing Feng, Wen Yu, Xinda Li, Feifei Zhou, Wenlong Zhang, Qi Shen, Jianxin Li, Can Zhang, Pingping Shen
Lipid metabolic disorders and oxidative stress in the liver are key steps in the progression of nonalcoholic fatty liver disease (NAFLD), which is a major risk factor for the development of metabolic syndrome. To date, no pharmacological treatment for this condition has been approved. Our previous study has found that the food-derived compound apigenin (Api) significantly attenuates obesity-induced metabolic syndrome by acting as a peroxisome proliferator-activated receptor gamma modulator (PPARM). Herein, a high fat diet (HFD) induced NAFLD model was used to dig out whether Api had the effect on NAFLD...
April 13, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28411115/sponging-off-nature-for-new-drug-leads
#5
REVIEW
Raymond Andersen
Marine sponges have consistently been the richest source of new marine natural products with unprecedented chemical scaffolds and potent biological activities that have been reported in the chemical literature since the early 1970s. During the last 40 years, chemists in the Andersen laboratory at UBC, in collaboration with biologists, have discovered many novel bioactive sponge natural products. Four experimental drug candidates for treatment of inflammation and cancer, that were inspired by members of this sponge natural product collection, have progressed to phase I/II/III clinical trials...
April 11, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28408345/icariin-protects-against-glucocorticoid-induced-osteoporosis-increases-the-expression-of-the-bone-enhancer-dec1-and-modulates-the-pi3k-akt-gsk3%C3%AE-%C3%AE-catenin-integrated-signaling-pathway
#6
Hu Jinhua, Mao Zhao, He Shuangcheng, Zhan Yuanran, Ning Rui, Liu Wei, Yan Bingfang, Yang Jian
Osteoporosis is a serious public health concern worldwide. Herba epimedii has been used for centuries and even thousands of years to treat osteoporotic conditions. Icariin, a flavonol glycoside, is one of the major active ingredients. In this study, we have shown that icariin protected against glucocorticoid-induced osteoporotic changes in SaoS-2 cells and mice. We have also shown that dexamethasone (a glucocorticoid) suppressed and icariin induced DEC1, a structurally distinct helix-loop-helix protein. DEC1 overexpression promoted whereas DEC1 knockdown decreased osteogenic activity...
April 10, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28408344/repurposing-bacterial-toxins-for-intracellular-delivery-of-therapeutic-proteins
#7
REVIEW
Greg L Beilhartz, Seiji N Sugiman-Marangos, Roman A Melnyk
Despite enormous efforts, achieving efficacious levels of proteins inside mammalian cells remains one of the greatest challenges in biologics-based drug discovery and development. The inability of proteins to readily cross biological membranes precludes access to the wealth of intracellular targets and applications that lie within mammalian cells. Existing methods of delivery commonly suffer from an inability to target specific cells and tissues, poor endosomal escape, and limited in vivo efficacy. The aim of the present commentary is to highlight the potential of certain classes of bacterial toxins, which naturally deliver a large protein into the cytosolic compartment of target cells after binding a host cell-surface receptor with high affinity, as robust protein delivery platforms...
April 10, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28408343/the-impact-of-cellular-senescence-in-skin-ageing-a-notion-of-mosaic-and-therapeutic-strategies
#8
REVIEW
Marie Toutfaire, Emilie Bauwens, Florence Debacq-Chainiaux
Cellular senescence is now recognized as one of the nine hallmarks of ageing. Recent data show the involvement of senescent cells in tissue ageing and some age-related diseases. Skin represents an ideal model for the study of ageing. Indeed, skin ageing varies between individuals depending on their chronological age but also on their exposure to various exogenous factors (mainly ultraviolet rays). If senescence traits can be detected with ageing in the skin, the senescent phenotype varies among the various skin cell types...
April 10, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28404378/axl-molecular-targeting-counteracts-aggressiveness-but-not-platinum-resistance-of-ovarian-carcinoma-cells
#9
Cristina Corno, Laura Gatti, Noemi Arrighetti, Nives Carenini, Nadia Zaffaroni, Cinzia Lanzi, Paola Perego
Ovarian carcinoma, the most common gynecological cancer, is characterized by high lethality mainly due to late diagnosis and treatment failure. The efficacy of platinum drug-based therapy in the disease is limited by the occurrence of drug resistance, a phenomenon often associated with increased metastatic potential. Because the Tyr-kinase receptor Axl can be deregulated in ovarian carcinoma and plays a pro-metastatic/anti-apoptotic role, the aim of this study was to examine if Axl inhibition modulates drug resistance and aggressive features of ovarian carcinoma cells, using various pairs of cisplatin-sensitive and -resistant cell lines...
April 9, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28404377/h2s-induced-s-sulfhydration-of-lactate-dehydrogenase-a-ldha-stimulates-cellular-bioenergetics-in-hct116-colon-cancer-cells
#10
Ashley A Untereiner, Gabor Oláh, Katalin Módis, Mark R Hellmich, Csaba Szabo
Cystathionine-β-synthase (CBS) is upregulated and hydrogen sulfide (H2S) production is increased in colon cancer cells. The functional consequence of this response is stimulation of cellular bioenergetics and tumor growth and proliferation. Lactate dehydrogenase A (LDHA) is also upregulated in various colon cancer cells and has been previously implicated in tumor cell bioenergetics and proliferation. In the present study, we sought to determine the potential interaction between the H2S pathway and LDH activity in the control of bioenergetics and proliferation of colon cancer, using the colon cancer line HCT116...
April 9, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28396196/enhancing-reproducibility-failures-from-reproducibility-initiatives-underline-core-challenges
#11
REVIEW
Kevin Mullane, Michael Williams
Efforts to address reproducibility concerns in biomedical research include: initiatives to improve journal publication standards and peer review; increased attention to publishing methodological details that enable experiments to be reconstructed; guidelines on standards for study design, implementation, analysis and execution; meta-analyses of multiple studies within a field to synthesize a common conclusion and; the formation of consortia to adopt uniform protocols and internally reproduce data. Another approach to addressing reproducibility are Reproducibility Initiatives (RIs), well-intended, high-profile, systematically peer-vetted initiatives that are intended to replace the traditional process of scientific self-correction...
April 7, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28396195/treatment-with-salvianolic-acid-b-restores-endothelial-function-in-angiotensin-ii-induced-hypertensive-mice
#12
Wei Chih Ling, Jian Liu, Chi Wai Lau, Dharmani Devi Murugan, Mohd Rais Mustafa, Yu Huang
Salvianolic acid B (Sal B) is one of the most abundant phenolic acids derived from the root of Danshen with potent anti-oxidative properties. The present study examined the vasoprotective effect of Sal B in hypertensive mice induced by angiotensin II (Ang II). Sal B (25mg/kg/day) was administered via oral gavage for 11days to Ang II (1.2mg/kg/day)-infused C57BL/6J mice (8-10weeks old). The vascular reactivity (both endothelium-dependent relaxations and contractions) in mouse arteries was examined by wire myography...
April 7, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28392095/real-time-analysis-of-the-binding-of-fluorescent-vegf165a-to-vegfr2-in-living-cells-effect-of-receptor-tyrosine-kinase-inhibitors-and-fate-of-internalized-agonist-receptor-complexes
#13
Laura E Kilpatrick, Rachel Friedman-Ohana, Diana C Alcobia, Kristin Riching, Chloe J Peach, Amanda J Wheal, Stephen J Briddon, Matthew B Robers, Kris Zimmerman, Thomas Machleidt, Keith V Wood, Jeanette Woolard, Stephen J Hill
Vascular endothelial growth factor (VEGF) is an important mediator of angiogenesis. Here we have used a novel stoichiometric protein-labeling method to generate a fluorescent variant of VEGF (VEGF165a-TMR) labeled on a single cysteine within each protomer of the antiparallel VEGF homodimer. VEGF165a-TMR has then been used in conjunction with full length VEGFR2, tagged with the bioluminescent protein NanoLuc, to undertake a real time quantitative evaluation of VEGFR2 binding characteristics in living cells using bioluminescence energy transfer (BRET)...
April 6, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28390939/guanine-%C3%AE-carboxy-nucleoside-phosphonate-g-%C3%AE-cnp-shows-a-different-inhibitory-kinetic-profile-against-the-dna-polymerases-of-human-immunodeficiency-virus-hiv-and-herpes-viruses
#14
Jan Balzarini, Michael Menni, Kalyan Das, Lizette van Berckelaer, Alan Ford, Nuala M Maguire, Sandra Liekens, Paul E Boehmer, Eddy Arnold, Matthias Götte, Anita R Maguire
α-Carboxy nucleoside phosphonates (α-CNPs) are modified nucleotides that represent a novel class of nucleotide-competing reverse transcriptase (RT) inhibitors (NcRTIs). They were designed to act directly against HIV-1 RT without the need for prior activation (phosphorylation). In this respect, they differ from the nucleoside or nucleotide RTIs [N(t)RTIs] that require conversion to their triphosphate forms before being inhibitory to HIV-1 RT. The guanine derivative (G-α-CNP) has now been synthesized and investigated for the first time...
April 5, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28390938/natural-product-based-amyloid-inhibitors
#15
REVIEW
Paul Velander, Ling Wu, Frances Henderson, Shijun Zhang, David R Bevan, Bin Xu
Many chronic human diseases, including multiple neurodegenerative diseases, are associated with deleterious protein aggregates, also called protein amyloids. One common therapeutic strategy is to develop protein aggregation inhibitors that can slow down, prevent, or remodel toxic amyloids. Natural products are a major class of amyloid inhibitors, and several dozens of natural product-based amyloid inhibitors have been identified and characterized in recent years. These plant- or microorganism-extracted compounds have shown significant therapeutic potential from in vitro studies as well as in vivo animal tests...
April 5, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28390937/steroid-receptor-coactivators-present-a-unique-opportunity-for-drug-development-in-hormone-dependent-cancers
#16
REVIEW
Aarti D Rohira, David M Lonard
Steroid receptor coactivators (SRCs) are essential regulators of nuclear hormone receptor function. SRCs coactivate transcription mediated by hormone stimulation of nuclear receptors and other transcription factors and have essential functions in human physiology and health. The SRCs are over expressed in a number of cancers such as breast, prostate, endometrial and pancreatic cancers where they promote tumor growth, invasion, metastasis and chemo-resistance. With their multiple roles in cancer, the SRCs are promising targets for the development of small molecule agents that can interfere with their function...
April 5, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28389227/restore-the-brake-on-tumor-progression
#17
REVIEW
Renata E Gordon, Li Zhang, Zeng-Jie Yang
Sonic hedgehog (Shh) signaling plays a key role in regulating normal development. The negative feedback mechanism mediated by the transcriptional factor, Gli3, acts to finely tune Shh signaling, providing tight control of normal developmental processes. Hyperactivation of Shh signaling often leads to many human malignancies, including basal cell carcinoma and medulloblastoma (MB). However, how tumor cells sustain the aberrant activation of Shh signaling is still not completely understood. We recently revealed that during MB formation, tumor cells express Nestin, a type VI intermediate filament protein, which maintains uncontrolled Shh signaling by abolishing negative feedback by Gli3...
April 4, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28377279/inositol-1-4-5-trisphosphate-3-kinase-a-itpka-is-frequently-over-expressed-and-functions-as-an-oncogene-in-several-tumor-types
#18
REVIEW
Sabine Windhorst, Kai Song, Adi F Gazdar
At present targeted tumor therapy is based on inhibition of proteins or protein mutants that are up-regulated in tumor but not in corresponding normal cells. The actin bundling Inositol-trisphosphate 3-kinase A (ITPKA) belongs to such molecular targets. ITPKA is expressed in a broad range of tumor types but shows limited expression in normal cells. In lung and breast cancer expression of ITPKA is stimulated by gene body methylation which increases with increasing malignancy of these tumors but is not detectable in the corresponding normal tissues...
April 2, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28377278/factors-modulating-bioavailability-of-quercetin-related-flavonoids-and-the-consequences-of-their-vascular-function
#19
REVIEW
Junji Terao
Nowadays dietary flavonoids attract much attention in the prevention of chronic diseases. Epidemiological and intervention studies strongly suggest that flavonoid intake has beneficial effects on vascular health. It is unlikely that flavonoids act as direct antioxidants, although oxidative stress profoundly contributes to vascular impairment leading to cardiovascular diseases. Instead, flavonoids may exert their function by tuning the cellular redox state to an adaptive response or tolerable stress. However, the optimum intake of flavonoids from supplements or diet has not been clarified yet, because a number of exogenous and endogenous factors modulating their bioavailability affect their vascular function...
April 2, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28377280/is-there-a-future-for-andrographolide-to-be-an-anti-inflammatory-drug-deciphering-its-major-mechanisms-of-action
#20
REVIEW
W S Daniel Tan, Wupeng Liao, Shuo Zhou, W S Fred Wong
Andrographis paniculata has long been part of the traditional herbal medicine system in Asia and in Scandinavia. Andrographolide was isolated as a major bioactive constituent of A. paniculata in 1951, and since 1984, andrographolide and its analogs have been scrutinized with modern drug discovery approach for anti-inflammatory properties. With this accumulated wealth of pre-clinical data, it is imperative to review and consolidate different sources of information, to decipher the major anti-inflammatory mechanisms of action in inflammatory diseases, and to provide direction for future studies...
April 1, 2017: Biochemical Pharmacology
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