journal
MENU ▼
Read by QxMD icon Read
search

Biochemical Pharmacology

journal
https://www.readbyqxmd.com/read/28104437/pharmacological-intervention-for-dengue-virus-infection
#1
REVIEW
Jenn-Haung Lai, Yi-Ling Lin, Shie-Liang Hsieh
Dengue virus (DENV) infection has a considerable health impact in tropical and subtropical countries worldwide. Escalation of infection rates greatly increases morbidity and mortality, most commonly from deaths due to dengue hemorrhagic fever and dengue shock syndrome. Although the development of an effective, long-lasting vaccine has been a major aim for control and prevention of DENV infection, the currently licensed vaccine has limitations and is less than satisfactory. Thus, there remains an important need to identify effective and tolerable medications for treatment of DENV-infected patients both in the early phase, to prevent progression to fatal outcomes, and to minimize deaths after patients develop severe complications...
January 16, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28104436/capsaicin-synergizes-with-camptothecin-to-induce-increased-apoptosis-in-human-small-cell-lung-cancers-via-the-calpain-pathway
#2
Jamie R Friedman, Haley E Perry, Kathleen C Brown, Yin Gao, Ju Lin, Cathyrn D Stevenson, John D Hurley, Nicholas A Nolan, Austin T Akers, Yi Charlie Chen, Krista L Denning, Linda G Brown, Piyali Dasgupta
Small cell lung cancer (SCLC) is characterized by excellent initial response to chemotherapy and radiation therapy with a majority of the patients showing tumor shrinkage and even remission. However, the challenge with SCLC therapy is that patients inevitably relapse and subsequently do not respond to the first line treatment. Recent clinical studies have investigated the possibility of camptothecin-based combination therapy as first line treatment for SCLC patients. Conventionally, camptothecin is used for recurrent SCLC and has poor survival outcomes...
January 16, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28104435/inhibition-of-nrf2-enhances-the-anticancer-effect-of-6-o-angeloylenolin-in-lung-adenocarcinoma
#3
Yang Wang, Ru-Yuan Yu, Jing Zhang, Wei-Xia Zhang, Zhi-Hao Huang, Hui-Fang Hu, Yao-Lan Li, Bin Li, Qing-Yu He
6-O-Angeloylenolin (6-OA), a sesquiterpene lactone isolated from Centipeda minima (L.) A. Br. (Compositae), has been used to treat respiratory diseases for centuries. However, whether and how 6-OA exerts anticancer effects against lung cancer remains to be elucidated. In this study, we showed that 6-OA markedly suppressed the cell viability and colony formation of lung cancer cells H1299 and A549, with no significant toxic effect on non-cancer cells HBE. Annexin V/7-AAD assay revealed that 6-OA induced cell apoptosis in dose- and time-dependent manners, which was further confirmed by the increased expression of cleaved caspase-3...
January 16, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28087253/what-is-an-ideal-antibiotic-discovery-challenges-and-path-forward
#4
REVIEW
Sheo B Singh, Katherine Young, Lynn L Silver
An ideal antibiotic is an antibacterial agent that kills or inhibits the growth of all harmful bacteria in a host, regardless of site of infection without affecting beneficial gut microbes (gut flora) or causing undue toxicity to the host. Sadly, no such antibiotics exist. What exists are many effective Gram-positive antibacterial agents as well as broad-spectrum agents that provide treatment of certain Gram-negative bacteria but not holistic treatment of all bacteria. However effectiveness of all antibacterial agents is being rapidly eroded due to resistance...
January 10, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28065859/inhibition-of-human-udp-glucuronosyltransferase-enzymes-by-lapatinib-pazopanib-regorafenib-and-sorafenib-implications-for-hyperbilirubinemia
#5
John O Miners, Nuy Chau, Andrew Rowland, Kushari Burns, Ross A McKinnon, Peter I Mackenzie, Geoffrey T Tucker, Kathleen M Knights, Ganessan Kichenadasse
Kinase inhibitors (KIs) are a rapidly expanding class of drugs used primarily for the treatment of cancer. Data relating to the inhibition of UDP-glucuronosyltransferase (UGT) enzymes by KIs is sparse. However, lapatinib (LAP), pazopanib (PAZ), regorafenib (REG) and sorafenib (SOR) have been implicated in the development of hyperbilirubinemia in patients. This study aimed to characterise the role of UGT1A1 inhibition in hyperbilirubinemia and assess the broader potential of these drugs to perpetrate drug-drug interactions arising from UGT enzyme inhibition...
January 5, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28065858/role-of-transglutaminase-2-in-pac1-receptor-mediated-protection-against-hypoxia-induced-cell-death-and-neurite-outgrowth-in-differentiating-n2a-neuroblastoma-cells
#6
Alanood S Algarni, Alan J Hargreaves, John M Dickenson
The PAC1 receptor and tissue transglutaminase (TG2) play important roles in neurite outgrowth and modulation of neuronal cell survival. In this study, we investigated the regulation of TG2 activity by the PAC1 receptor in retinoic acid-induced differentiating N2a neuroblastoma cells. TG2 transamidase activity was determined using an amine incorporation and a peptide cross linking assay. In situ TG2 activity was assessed by visualising the incorporation of biotin-X-cadaverine using confocal microscopy. TG2 phosphorylation was monitored via immunoprecipitation and Western blotting...
January 5, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28043811/honokiol-induces-proteasomal-degradation-of-aml1-eto-oncoprotein-via-increasing-ubiquitin-conjugase-ubch8-expression-in-leukemia
#7
Bin Zhou, Haiying Li, Chongyun Xing, Haige Ye, Jianhua Feng, Jianbo Wu, Zhongqiu Lu, Jing Fang, Shenmeng Gao
AML1-ETO is the most common oncoprotein leading to acute myeloid leukemia (AML), in which 5-year survival rate is only about 30%. However, currently there are no specific therapies for AML patients with AML1-ETO. Here, we report that AML1-ETO protein is rapidly degraded by Honokiol (HNK), a natural phenolic compound isolated from the plant Magnolia officinalis. HNK induced the degradation of AML1-ETO in a concentration- and time-dependent manner in leukemic cell lines and primary AML blasts with t(8;21) translocation...
December 30, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28040476/asp73-dependent-and-independent-regulation-of-the-affinity-of-ligands-for-human-histamine-h1-receptors-by-na
#8
Shigeru Hishinuma, Kiyoe Kosaka, Chizuru Akatsu, Yoshihiro Uesawa, Hiroyuki Fukui, Masaru Shoji
The affinity of ligands for G-protein-coupled receptors (GPCR) is allosterically regulated by Na(+) via a highly conserved aspartate residue (Asp(2.50)) in the second transmembrane domain of GPCRs. In the present study, we examined the Na(+)-mediated regulation of the affinity of ligands for Gq/11-protein-coupled human histamine H1 receptors in Chinese hamster ovary cells. The affinities of 3 agonists and 20 antihistamines were evaluated by their displacement curves against the binding of [(3)H]-mepyramine to membrane preparations in the presence or absence of 100 mM NaCl...
December 28, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28027880/1-4-anhydro-4-seleno-d-talitol-setal-protects-endothelial-function-in-the-mouse-aorta-by-scavenging-superoxide-radicals-under-conditions-of-acute-oxidative-stress
#9
Hooi Hooi Ng, Chen Huei Leo, Kelly O'Sullivan, Stefanie-Ann Alexander, Michael J Davies, Carl H Schiesser, Laura J Parry
Hyperglycaemia increases the generation of reactive oxidants in blood vessels and is a major cause of endothelial dysfunction. A water-soluble selenium-containing sugar (1,4-Anhydro-4-seleno-D-talitol, SeTal) has potent antioxidant activity in vitro and is a promising treatment to accelerate wound healing in diabetic mice. One possible mechanism of SeTal action is a direct effect on blood vessels. Therefore, we tested the hypothesis that SeTal prevents endothelial dysfunction by scavenging reactive oxidants in isolated mouse aorta under conditions of acute oxidative stress induced by hyperglycaemia...
December 24, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28027879/a-novel-mode-of-operation-of-slc22a11-membrane-insertion-of-estrone-sulfate-versus-translocation-of-uric-acid-and-glutamate
#10
Peter Skwara, Edgar Schömig, Dirk Gründemann
Estrone sulfate alias estrone-3-sulfate (E3S) is considerably larger and much more hydrophobic than typical substrates of SLC22 transporters. It is puzzling that many otherwise unrelated transporters have been reported to transport E3S. The aim of this study was to scrutinize the mechanism of transport of E3S by SLC22A11, by direct comparison with uric acid (UA), an important physiological substrate. Heterologous expression of SLC22A11 in human 293 cells gave rise to a huge unidirectional efflux of glutamate (Glu) and aspartate, as determined by LC-MS/MS...
December 24, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28017773/antileishmanial-activity-of-verbascoside-selective-arginase-inhibition-of-intracellular-amastigotes-of-leishmania-leishmania-amazonensis-with-resistance-induced-by-lps-plus-ifn-%C3%AE
#11
Claudia do Carmo Maquiaveli, Arina Lázaro Rochetti, Heidge Fukumasu, Paulo Cezar Vieira, Edson Roberto da Silva
Verbascoside is the main component of the traditional medicinal plants that were used against protozoa parasites that cause malaria and leishmaniasis. Previously, we have described verbascoside inhibition of Leishmania amazonensis arginase as well as its antileishmanial action against extracellular promastigotes. In this study, we have assessed arginase parasite inhibition in intracellular amastigotes. In addition, we verified whether verbascoside can influence the host defense against the parasite by measuring gene expression of cytokines IL-1b, IL-10, IL-18, TNF-α and murine macrophage arginase as well as nitric oxide synthase enzymes...
December 23, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28017778/rhoa-s-nitrosylation-as-a-regulatory-mechanism-influencing-endothelial-barrier-function-in-response-to-g-bacterial-toxins
#12
F Chen, Y Wang, R Rafikov, S Haigh, W B Zhi, S Kumar, P T Doulias, O Rafikova, H Pillich, T Chakraborty, R Lucas, A V Verin, J D Catravas, J X She, S M Black, D J R Fulton
Disruption of the endothelial barrier in response to Gram positive (G(+)) bacterial toxins is a major complication of acute lung injury (ALI) and can be further aggravated by antibiotics which stimulate toxin release. The integrity of the pulmonary endothelial barrier is mediated by the balance of disruptive forces such as the small GTPase RhoA, and protective forces including endothelium-derived nitric oxide (NO). How NO protects against the barrier dysfunction is incompletely understood and our goal was to determine whether NO and S-nitrosylation can modulate RhoA activity and whether this mechanism is important for G(+) toxin-induced microvascular permeability...
December 22, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28017777/the-cardioprotective-effect-of-sildenafil-is-mediated-by-the-activation-of-malate-dehydrogenase-and-an-increase-in-the-malate-aspartate-shuttle-in-cardiomyocytes
#13
Gevi Federica, Campolo Federica, Naro Fabio, Zolla Lello
Recent evidence has shown showed the cardioprotective effect of PDE5 inhibition in myocardial ischemia/reperfusion injury, heart failure and cardiac hypertrophy. To investigate the biochemical changes that occur during PDE5 inhibition in cardiac cells, this study assessed the metabolic profile of the HL1 cell line, a murine atrial cell line with adult cardiomyocyte properties. After one hour of treatment with sildenafil, glycolysis was moderately but selectively stimulated, unlike the pentose phosphate pathway and the Krebs cycle...
December 22, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28017776/nobiletin-inhibits-oxidized-ldl-mediated-expression-of-tissue-factor-in-human-endothelial-cells-through-inhibition-of-nf-kb
#14
Plinio Cirillo, Stefano Conte, Giovanni Cimmino, Grazia Pellegrino, Francesca Ziviello, Giusi Barra, Ferdinando Carlo Sasso, Francesco Borgia, Raffaele De Palma, Bruno Trimarco
INTRODUCTION: Flavonoids are nutrients usually included in human diet with several significant biological activities. Nobiletin is a flavonoid that, besides having anti-inflammatory and anti-tumoral activity, seems to exert protective effects on cardiovascular system. Several studies investigated nobiletin as a natural drug to antagonize the atherosclerotic disease. On the contrary, literature about its potential role in modulating the main acute complication of atherosclerosis, thrombosis, is still scanty...
December 22, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28017775/the-network-of-immunosuppressive-pathways-in-glioblastoma
#15
REVIEW
Davide Mangani, Michael Weller, Patrick Roth
Glioblastoma remains a fatal tumor despite increased knowledge regarding the complex signalling pathways that drive this devastating disease. Recently, immunotherapeutic approaches have shown remarkable and durable responses in various cancers including metastatic melanoma and advanced non-small cell lung cancer. So far, it remains unclear whether these immunotherapeutics may also work against glioblastoma and other tumors residing in the central nervous system. It is well known that patients with glioblastoma suffer from profound local immunosuppression that represents the major hurdle to overcome in the context of immunotherapy...
December 22, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28017774/identification-of-esterase-involved-in-the-metabolism-of-two-corticosteroid-soft-drugs
#16
Ahmed Samir, Nicholas Bodor, Teruko Imai
The soft drug approach is successful in obtaining high local therapeutic efficacy without systemic adverse effects, because soft drugs are designed to be bioconverted to inactive form by hydrolytic enzymes in systemic circulation. However, there is little information about the exact nature of these metabolic enzymes. In this study, the human enzymes for biotransformation of soft drugs were investigated. Loteprednol etabonate (LE) and etiprednol dicloacetate (ED) were designed from Δ(1)-cortienic acid (Δ(1)-CA), the inactive metabolite of prednisolone, by introducing two labile ester bonds to restore the corticosteroidal activity...
December 22, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28017772/novel-%C3%AE-carboline-quinazolinone-hybrids-disrupt-leishmania-donovani-redox-homeostasis-and-show-promising-antileishmanial-activity
#17
Dandugudumula Ramu, Swati Garg, R Ayana, A K Keerthana, Vijeta Sharma, Subhabrata Sen, Soumya Pati, Shailja Singh
Visceral Leishmaniasis is a deadly parasitic disease caused by Leishmania donovani. Paucity exists in the discovery of novel chemotherapeutics against Leishmaniasis. In this study, we synthesized a natural product inspired Diversity Oriented Synthesis library of L. donovani Trypanothione reductase (LdTR) inhibitorμ β-carboline-quinazolinone hybrids, which are different in stereochemical architecture and diverse in the bioactive chemical space. It is noteworthy that chirality affects drug-to-protein binding affinity since proteins in any living system are present only in one of the chiral forms...
December 22, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28012959/non-coding-rnas-as-antibiotic-targets
#18
REVIEW
Savannah Colameco, Marie A Elliot
Antibiotics inhibit a wide range of essential processes in the bacterial cell, including replication, transcription, translation and cell wall synthesis. In many instances, these antibiotics exert their effects through association with non-coding RNAs. This review highlights many classical antibiotic targets (e.g. rRNAs and the ribosome), explores a number of emerging targets (e.g. tRNAs, RNase P, riboswitches and small RNAs), and discusses the future directions and challenges associated with non-coding RNAs as antibiotic targets...
December 22, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28012958/romidepsin-induces-g2-m-phase-arrest-via-erk-cdc25c-cdc2-cyclinb-pathway-and-apoptosis-induction-through-jnk-c-jun-caspase3-pathway-in-hepatocellular-carcinoma-cells
#19
Wei-Jian Sun, He Huang, Bin He, Dan-Hong Hu, Pi-Hong Li, Yao-Jun Yu, Xiao-Hu Zhou, Zhen Lv, Lei Zhou, Tian-Ye Hu, Zhi-Chao Yao, Ming-Dong Lu, Xian Shen, Zhi-Qiang Zheng
The aim of the study is to demonstrate the effect of Romidepsin in hepatocellular carcinoma (HCC) by inducing G2/M phase arrest via Erk/cdc25C/cdc2/cyclinB pathway and apoptosis through JNK/c-Jun/caspase3 pathway in vitro and in vivo. Human HCC cell lines were cultured with Romidepsin and DMSO (negative control) and 5-fluorouracil (positive control). Then the cells' viability and apoptosis were determined by cell proliferation assay and flow cytometry. Protein concentrations and expression changes were measured by Western blot...
December 22, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28012961/high-affinity-binding-of-the-peptide-agonist-tip-39-to-the-parathyroid-hormone-2-pth2-receptor-requires-the-hydroxyl-group-of-tyr-318-on-transmembrane-helix-5
#20
Richard E Weaver, Juan Carlos Mobarec, Mark J Wigglesworth, Christopher A Reynolds, Dan Donnelly
TIP39 ("tuberoinfundibular peptide of 39 residues") acts via the parathyroid hormone 2 receptor, PTH2, a Family B G protein-coupled receptor (GPCR). Despite the importance of GPCRs in human physiology and pharmacotherapy, little is known about the molecular details of the TIP39-PTH2 interaction. To address this, we utilised the different pharmacological profiles of TIP39 and PTH(1-34) at PTH2 and its related receptor PTH1: TIP39 being an agonist at the former but an antagonist at the latter, while PTH(1-34) activates both...
December 21, 2016: Biochemical Pharmacology
journal
journal
21606
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"