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Biochemical Pharmacology

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https://www.readbyqxmd.com/read/28551099/wnt-%C3%AE-catenin-signaling-plays-an-essential-role-in-%C3%AE-7-nicotinic-receptor-mediated-neuroprotection-of-dopaminergic-neurons-in-a-mouse-parkinson-s-disease-model
#1
Yuan Liu, Shuai Hao, Beibei Yang, Yi Fan, Xiaodong Qin, Yun Chen, Jun Hu
Parkinson's disease (PD) is a neurodegenerative disorder with an incidence second only to Alzheimer's disease. The main pathological feature of PD is the death of dopaminergic neurons in the substantia nigra pars compacta. Nicotinic receptor agonists are neuroprotective in several PD models and there is considerable evidence that α7 nicotinic acetylcholine receptors (α7-nAChRs) are important therapeutic targets for neurodegenerative diseases. However, the involvement of α7-nAChRs and underlying signaling mechanisms in PD pathogenesis are unclear...
May 24, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28539264/op16-a-novel-ent-kaurene-diterpenoid-potentiates-the-antitumor-effect-of-rapamycin-by-inhibiting-rapamycin-induced-feedback-activation-of-akt-signaling-in-esophageal-squamous-cell-carcinoma
#2
Ke-Zheng Peng, Yu Ke, Qi Zhao, Fei Tian, Hong-Min Liu, Guiqin Hou, Zhaoming Lu
Hyperactivation of mTOR signaling pathway has been viewed as a significant molecular pathogenesis of cancer. However, inhibition of mTOR by rapamycin and its analogs could induce numerous negative feedback loops to attenuate their therapeutic efficacy. As a traditional Chinese herbal medicine, Rabdosia rubescens has been used to treat esophageal squamous cell carcinoma (ESCC) for hundreds of years, and its major effective component is oridonin. Here we reported that OP16, a novel analog of oridonin, showed potent inhibition of cell proliferation and Akt phosphorylation in ESCC cells...
May 21, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28539263/nutrients-neurogenesis-and-brain-ageing-from-disease-mechanisms-to-therapeutic-opportunities
#3
REVIEW
Marco Fidaleo, Virve Cavallucci, Giovambattista Pani
Appreciation of the physiological relevance of mammalian adult neurogenesis has in recent years rapidly expanded from a phenomenon of homeostatic cell replacement and brain repair to the current view of a complex process involved in high order cognitive functions. In parallel, an array of endogenous or exogenous triggers of neurogenesis have also been identified, among which metabolic and nutritional cues have drawn significant attention. Converging evidence from animal and in vitro studies point to nutrient sensing and energy metabolism as major physiological determinants of neural stem cell fate, and modulators of the whole neurogenic process...
May 21, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28539262/synthetic-anti-endotoxin-peptides-inhibit-cytoplasmic-lps-mediated-responses
#4
Anja Pfalzgraff, Lena Heinbockel, Qi Su, Klaus Brandenburg, Günther Weindl
Toll-like receptor (TLR) 4-independent recognition of lipopolysaccharide (LPS) in the cytosol by inflammatory caspases leads to non-canonical inflammasome activation and induction of IL-1 secretion and pyroptosis. The discovery of this novel mechanism has potential implications for the development of effective drugs to treat sepsis since LPS-mediated hyperactivation of caspases is critically involved in endotoxic shock. Previously, we demonstrated that Pep19-2.5, a synthetic anti-endotoxin peptide, efficiently neutralises pathogenicity factors of Gram-negative and Gram-positive bacteria and protects against sepsis in vivo...
May 21, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28535906/the-effects-of-curcumin-on-proliferation-apoptosis-invasion-and-nedd4-expression-in-pancreatic-cancer
#5
Jingna Su, Xiuxia Zhou, Xuyuan Yin, Lixia Wang, Zhe Zhao, Yingying Hou, Nana Zheng, Jun Xia, Zhiwei Wang
Pancreatic cancer (PC) is one of the most fatal cancers worldwide. The incidence and death rates are still increasing for PC. Curcumin is the biologically active diarylheptanoid constituent of the spice turmeric, which exerts its anticancer properties in various human cancers including PC. In particular, accumulating evidence has proved that curcumin targets numerous therapeutically important proteins in cell signaling pathways. The neural precursor cell expressed developmentally down-regulated protein 4 (NEDD4) is an E3 HECT ubiquitin ligase and is frequently over-expressed in various cancers...
May 20, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28532626/single-nucleotide-polymorphisms-of-abcc2-modulate-renal-secretion-of-endogenous-organic-anions
#6
Kienana Muhrez, Bérenger Largeau, Patrick Emond, Montigny Frédéric, Jean-Michel Halimi, Patrick Trouillas, Chantal Barin-LE Guellec
The ATP-binding cassette family transporter MRP2 (multidrug resistance-associated protein 2), encoded by the ABCC2 gene, is involved in the renal excretion of numerous xenobiotics and it is likely that it also transports many endogenous molecules arising from not only normal essential metabolic processes but also from environmental toxins or food intake. We used a targeted gas chromatography-mass spectrometry metabolomics analysis to study whether endogenous organic anions are differentially excreted in urines of healthy volunteers according to their genotype for three functional single nucleotide polymorphisms (SNPs) in ABCC2...
May 19, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28528695/protein-phosphatase-5-promotes-hepatocarcinogenesis-through-interaction-with-amp-activated-protein-kinase
#7
Yao-Li Chen, Man-Hsin Hung, Pei-Yi Chu, Tzu-I Chao, Ming-Hsien Tsai, Li-Ju Chen, Yung-Jen Hsiao, Chih-Ting Shih, Feng-Shu Hsieh, Kuen-Feng Chen
The serine-threonine protein phosphatase family members are known as critical regulators of various cellular functions, such as survival and transformation. Growing evidence suggests that pharmacological manipulation of phosphatase activity exhibits therapeutic benefits. Ser/Thr protein phosphatase 5 (PP5) is known to participate in glucocorticoid receptor (GR) and stress-induced signaling cascades that regulate cell growth and apoptosis, and has been shown to be overexpressed in various human malignant diseases...
May 18, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28527616/catalase-increases-ethanol-oxidation-through-the-purine-catabolism-in-rat-liver
#8
Daniel Villalobos-García, Rolando Hernández-Muñoz
Hepatic ethanol oxidation increases according to its concentration and is raised to near-saturation levels of alcohol dehydrogenase (ADH); therefore, re-oxidation of NADH becomes rate limiting in ethanol metabolism by the liver. Adenosine is able to increase liver ethanol oxidation in both in vivo and in vitro conditions; the enhancement being related with the capacity of the nucleoside to accelerate the transport of cytoplasmic reducing equivalents to mitochondria, by modifying the subcellular distribution of the malate-aspartate shuttle components...
May 18, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28522408/multipotency-and-therapeutic-potential-of-ng2-cells
#9
REVIEW
Martin Valny, Pavel Honsa, Jan Kriska, Miroslava Anderova
NG2 cells represent one of the most proliferative glial cell populations in the intact mammalian central nervous system (CNS). They are well-known for their ability to renew themselves or to generate new oligodendrocytes during development as well as in adulthood, therefore also being termed oligodendrocyte progenitor cells. Following CNS injuries, such as demyelination, trauma or ischemia, the proliferative capacity of NG2 cells rapidly increases and moreover, their differentiation potential broadens, as documented by numerous reports also describing their differentiation into astrocytes or even neurons...
May 15, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28522407/high-throughput-screening-and-bioinformatic-analysis-to-ascertain-compounds-that-prevent-saturated-fatty-acid-induced-%C3%AE-cell-apoptosis
#10
Seung-Hee Lee, Daniel Cunha, Carlo Piermarocchi, Giovanni Paternostro, Anthony Pinkerton, Laurence Ladriere, Piero Marchetti, Decio L Eizirik, Miriam Cnop, Fred Levine
Pancreatic β-cell lipotoxicity is a central feature of the pathogenesis of type 2 diabetes. To study the mechanism by which fatty acids cause β-cell death and develop novel approaches to prevent it, a high-throughput screen on the β-cell line INS1 was carried out. The cells were exposed to palmitate to induce cell death and compounds that reversed palmitate-induced cytotoxicity were ascertained. Hits from the screen were analyzed by an increasingly more stringent testing funnel, ending with studies on primary human islets treated with palmitate...
May 15, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28522406/therapeutic-effect-of-cryptotanshinone-on-experimental-rheumatoid-arthritis-through-downregulating-p300-mediated-stat3-acetylation
#11
Ying Wang, Chun Zhou, Hui Gao, Cuixian Li, Dong Li, Peiqing Liu, Min Huang, Xiaoyan Shen, Liang Liu
BACKGROUND AND PURPOSE: The balance between T helper 17 (Th17) cells and regulatory T (Treg) cells, plays a critical role in rheumatoid arthritis (RA). The differentiation of Th17 cells requires the activation of STAT3, which determines the balance of Th17/Treg. Here, we investigated the therapeutic effect of Cryptotanshinone (CTS) on collagen induced mouse arthritis and explored the underlying mechanisms. EXPERIMENTAL APPROACH: Arthritis was induced in DBA/1 mice with bovine collagen type II and complete Freund's adjuvant...
May 15, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28522405/challenges-and-opportunities-for-the-development-of-new-antipsychotic-drugs
#12
REVIEW
Carlos Forray, Raimund Buller
In spite of the significant impact that the serendipitous discovery of drugs with antipsychotic properties had on the care of patients with psychotic disorders, there are significant challenges when aiming at therapeutic goals such as remission, recovery, improved health-related quality of life and functioning. The efficacy and effectiveness of existing antipsychotic drugs fail to address the full spectrum of symptoms and functional deficits that currently prevent patients with psychotic disorders from achieving fulfilling lives...
May 15, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28506758/decreased-homodimerization-and-increased-timp-1-complexation-of-uteroplacental-and-uterine-arterial-matrix-metalloproteinase-9-during-hypertension-in-pregnancy
#13
Juanjuan Chen, Zongli Ren, Minglin Zhu, Raouf A Khalil
Preeclampsia is a complication of pregnancy manifested as hypertension-in-pregnancy (HTN-Preg) and often intrauterine growth restriction (IUGR). Placental ischemia could be an initiating event, but the molecular mechanisms are unclear. To test the hypothesis that dimerization of matrix metalloproteinases (MMPs) plays a role in HTN-Preg and IUGR, the levels/activity of MMP-9, tissue inhibitor of metalloproteinase (TIMP-1), and their dimerization forms were measured in the placenta, uterus, and uterine artery of normal pregnant (Preg) rats and a rat model of reduced uteroplacental perfusion pressure (RUPP)...
May 12, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28501501/anti-tumor-effects-of-differentiation-inducing-factor-1-in-malignant-melanoma-gsk-3-mediated-inhibition-of-cell-proliferation-and-gsk-3-independent-suppression-of-cell-migration-and-invasion
#14
Masaki Arioka, Fumi Takahashi-Yanaga, Momoko Kubo, Kazunobu Igawa, Katsuhiko Tomooka, Toshiyuki Sasaguri
Differentiation-inducing factor-1 (DIF-1) isolated from Dictyostelium discoideum strongly inhibits the proliferation of various mammalian cells through the activation of glycogen synthase kinase-3 (GSK-3). To evaluate DIF-1 as a novel anti-cancer agent for malignant melanoma, we examined whether DIF-1 has anti-proliferative, anti-migratory, and anti-invasive effects on melanoma cells using in vitro and in vivo systems. DIF-1 reduced the expression levels of cyclin D1 and c-Myc by facilitating their degradation via GSK-3 in mouse (B16BL6) and human (A2058) malignant melanoma cells, and thereby strongly inhibited their proliferation...
May 10, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28483461/the-gut-microbiota-a-key-factor-in-the-therapeutic-effects-of-poly-phenols
#15
REVIEW
Juan Carlos Espín, Antonio González-Sarrías, Francisco A Tomás-Barberán
(Poly)phenols (PPs) constitute a large family of phytochemicals with high chemical diversity that are known to be active principles of plant-derived nutraceuticals and herbal medicinal products. Their pharmacological activity, however, is difficult to demonstrate due to their mild physiological effects, and to the large inter-individual variability observed. Many PPs have little bioavailability and reach the colon almost unaltered. There they encounter the gut microbes resulting in a two-way interaction in which PPs modulate the gut microbiota composition, and the intestinal microbes catabolize the ingested PPs to release metabolites that are often more active and better absorbed than the native phenolic compounds...
May 6, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28483462/the-impact-of-cocaine-on-adult-hippocampal-neurogenesis-potential-neurobiological-mechanisms-and-contributions-to-maladaptive-cognition-in-cocaine-addiction-disorder
#16
REVIEW
Estela Castilla-Ortega, David Ladrón de Guevara-Miranda, Antonia Serrano, Francisco J Pavón, Juan Suárez, Fernando Rodríguez de Fonseca, Luis J Santín
After discovering that addictive drugs alter adult neurogenesis, the potential role of adult-born hippocampal neurons in drug addiction has become a promising research field, in which cocaine is the most frequently investigated drug. Although a substantial amount of pre-clinical evidence has accumulated, additional studies are required to reveal the mechanisms by which cocaine modulates adult hippocampal neurogenesis (AHN) and determine whether these adult-born neurons have a role in cocaine-related behaviors, such as cocaine-mediated cognitive symptoms...
May 5, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28483460/voacamine-alters-leishmania-ultrastructure-and-kills-parasite-by-poisoning-unusual-bi-subunit-topoisomerase-ib
#17
Somenath Roy Chowdhury, Ashish Kumar, Joseane Lima Prado Godinho, Sara Teixeira De Macedo Silva, Aline Araujo Zuma, Sourav Saha, Neha Kumari, Juliany Cola Fernandez Rodrigues, Shyam Sundar, Jean-Claude Dujardin, Syamal Roy, Wanderley De Souza, Sibabrata Mukhopadhyay, Hemanta K Majumder
Indole alkaloids possess a large spectrum of biological activities including anti-protozoal action. Here we report for the first time that voacamine, isolated from the plant Tabernaemontana coronaria, is an antiprotozoal agent effective against a large array of trypanosomatid parasites including Indian strain of Leishmania donovani and Brazilian strains of Leishmania amazonensis and Trypanosoma cruzi. It inhibits the relaxation activity of topoisomerase IB of L. donovani (LdTop1B) and stabilizes the cleavable complex...
May 5, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28479300/p2x7-receptor-antagonism-implications-in-diabetic-retinopathy
#18
Chiara Bianca Maria Platania, Giovanni Giurdanella, Luisa Di Paola, Gian Marco Leggio, Filippo Drago, Salvatore Salomone, Claudio Bucolo
Diabetic retinopathy (DR) is the most frequent complication of diabetes and one of leading causes of blindness worldwide. Early phases of DR are characterized by retinal pericyte loss mainly related to concurrent inflammatory process. Recently, an important link between P2X7 receptor (P2X7R) and inflammation has been demonstrated indicating this receptor as potential pharmacological target in DR. Here we first carried out an in silico molecular modeling study in order to characterize the allosteric pocket in P2X7R, and identify a suitable P2X7R antagonist through molecular docking...
May 4, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28476332/in-vivo-%C3%AE-hydroxylation-of-a-2-alkylindole-antagonist-of-the-oxe-receptor-for-the-eosinophil-chemoattractant-5-oxo-6-8-11-14-eicosatetraenoic-acid-in-monkeys
#19
Shishir Chourey, Qiuji Ye, Chintam Nagendra Reddy, Chantal Cossette, Sylvie Gravel, Matthias Zeller, Irina Slobodchikova, Dajana Vuckovic, Joshua Rokach, William S Powell
We have developed a selective indole antagonist (230) targeting the OXE receptor for the potent eosinophil chemoattractant 5-oxo-ETE (5-oxo-6,8,11,14-eicosatetraenoic acid), that may be useful for the treatment of eosinophilic diseases such as asthma. In previous studies we identified ω2-oxidation of the hexyl side chain of racemic 230 as a major metabolic route in monkeys, but also obtained evidence for another pathway that appeared to involve hydroxylation of the hexyl side chain close to the indole. The present study was designed to investigate the metabolism of the active S-enantiomer of 230 (S230) and to identify the novel hydroxy metabolite and its chirality...
May 3, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28476333/identification-of-4-arylidene-curcumin-analogues-as-novel-proteasome-inhibitors-for-potential-anticancer-agents-targeting-19s-regulatory-particle-associated-deubiquitinase
#20
Xin Yue, Yinglin Zuo, Hongpeng Ke, Jiaming Luo, Lanlan Lou, Wenjing Qin, Youqiao Wang, Ziyi Liu, Daoyuan Chen, Haixia Sun, Weichao Zheng, Cuige Zhu, Ruimin Wang, Gesi Wen, Jun Du, Binhua Zhou, Xianzhang Bu
The proteasomal 19S regulatory particle (RP) associated deubiquitinases (DUBs) have attracted much attention owing to its potential as a therapeutic target for cancer therapy. Identification of new entities against 19S RP associated DUBs and illustration of the underlying mechanisms is crucial for discovery of novel proteasome blockers. In this study, a series of 4-arylidene curcumin analogues were identified as potent proteasome inhibitor by preferentially blocking deubiquitinase function of proteasomal 19S RP with moderate 20S CP inhibition...
May 2, 2017: Biochemical Pharmacology
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