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https://www.readbyqxmd.com/read/27923139/plga-peg-plga-triblock-copolymeric-micelles-as-oral-drug-delivery-system-in-vitro-drug-release-and-in-vivo-pharmacokinetics-assessment
#1
Xiufen Chen, Jianzhong Chen, Bowen Li, Xiang Yang, Rongjie Zeng, Yajun Liu, Tao Li, Rodney J Y Ho, Jingwei Shao
Poly (d,l-lactide-co-glycolide)-poly (ethylene glycol)-poly (d,l-lactide-co-glycolide) triblock copolymers (PLGA-PEG-PLGA) has been proven to be desirable for anti-cancer drug delivery by intravenous administration. But till now there is no report of developing this micelle as a sustained oral formulation for cancer therapy. 3β-acetoxy-urs-12-en-28-oic acid hexamethylenediamine (US597), a derivative of natural product ursolic acid has been developed as a novel cancer metastasis chemopreventive agent by us...
November 26, 2016: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/27922821/identification-of-salvia-haenkei-as-gerosuppressant-agent-by-using-an-integrated-senescence-screening-assay
#2
Ivana Matic, Ajinkya Revandkar, Jingjing Chen, Angela Bisio, Stefano Dall'Acqua, Veronica Cocetta, Paola Brun, Giorgio Mancino, Martina Milanese, Maurizio Mattei, Monica Montopoli, Andrea Alimonti
Cellular senescence is a stable cell cycle arrest that is the causative process of aging. The PI3K/AKT/mTOR pathway is implicated in the control of cellular senescence and inhibitors of this pathway have been successfully used for life span prolongation experiments in mammals. PTEN is the major regulator of the PI3K/AKT/mTOR pathway and loss of PTEN promotes a senescence response termed PICS. Here we report a novel-screening assay, for the identification of compounds that block different types of senescence response...
December 1, 2016: Aging
https://www.readbyqxmd.com/read/27922739/tyrosine-kinase-aurora-kinase-and-leucine-aminopeptidase-as-attractive-drug-targets-in-anticancer-therapy-characterisation-of-their-inhibitors
#3
Joanna Ziemska, Jolanta Solecka
Cancers are the leading cause of deaths all over the world. Available anticancer agents used in clinics exhibit low therapeutic index and usually high toxicity. Wide spreading drug resistance of cancer cells induce a demanding need to search for new drug targets. Currently, many on-going studies on novel compounds with potent anticancer activity, high selectivity as well as new modes of action are conducted. In this work, we describe in details three enzyme groups, which are at present of extensive interest to medical researchers and pharmaceutical companies...
2016: Roczniki Państwowego Zakładu Higieny
https://www.readbyqxmd.com/read/27922189/optimal-arac-cytotoxicity-to-aml-cells-requires-erk5-activity
#4
Ruifang Zheng, George P Studzinski
Cytarabine (AraC) has been the primary treatment agent for Acute Myeloid Leukemia (AML) in the past 30 years, but the precise mechanism of its action is not completely known. Here we assessed the role of ERK5 in AraC-induced cell death in AML cell lines HL60 and U937 using ERK5 inhibitors BIX02189 and XMD8-92. We report that inhibition of MEK5/ERK5 activity reduces AraC-induced cell death, DNA damage, the upregulated DNA damage biomarkers, and produced G2 phase cell cycle arrest. In addition, the pro-survival protein P-Bcl2 Ser70 was found to be associated with decreased AraC-induced cell death following XMD8-92 treatment, suggesting a regulatory role of ERK5 on Bcl2 phosphorylation...
December 6, 2016: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/27922182/retinoid-derivative-tp80-exhibits-anti-hepatitis-c-virus-activity-through-restoration-of-gi-gpx-expression
#5
Nguyen Bao Ngoc, Yukiko Okuno, Masahiko Ajiro, Kei Iida, Masatsugu Denawa, Makoto Yamamoto, Naoya Sakamoto, Hiroyuki Kagechika, Masatoshi Hagiwara
Hepatitis C virus (HCV) is a positive-sense single-stranded RNA virus with an estimated infection in ∼180 million people worldwide, and its chronic infection leads to development of cirrhosis and hepatocellular carcinoma. Although recent development of direct acting antiviral (DAA) compounds improved anti-HCV regimens, alternative therapeutic compounds are still demanded due to an expected emergence of escape mutants for those DAAs. In order to identify novel anti-HCV agents, we conducted chemical library screening for 2,086 compounds using HCV Rep-Feo reporter replicon in Huh7 hepatoma cells...
December 6, 2016: Journal of Medical Virology
https://www.readbyqxmd.com/read/27922044/from-tumour-heterogeneity-to-advances-in-precision-treatment-of-colorectal-cancer
#6
REVIEW
Cornelis J A Punt, Miriam Koopman, Louis Vermeulen
In recent years, the high heterogeneity of colorectal cancer (CRC) has become evident. Hence, biomarkers need to be developed that enable the stratification of patients with CRC into different prognostic subgroups and in relation to response to therapies, according to the distinctive tumour biology. Currently, only RAS-mutation status is used routinely as a negative predictive marker to avoid treatment with anti-EGFR agents in patients with metastatic CRC, and mismatch-repair status can guide the use of adjuvant chemotherapy in patients with early stage colon cancer...
December 6, 2016: Nature Reviews. Clinical Oncology
https://www.readbyqxmd.com/read/27921359/modulation-of-vegf-signaling-in-a-mouse-model-of-diabetes-by-xanthohumol-and-8-prenylnaringenin-unveiling-the-angiogenic-paradox-and-metabolism-interplay
#7
Raquel Costa, Ilda Rodrigues, Luísa Guardão, Joana Quelhas Lima, Emília Sousa, Raquel Soares, Rita Negrão
SCOPE: Imbalance in kidney and heart neovascularization is common in type2 Diabetes (T2DM) patients. Nevertheless, the mechanisms governing this angiogenic paradox have not been elucidated. Xanthohumol (XN) and 8-prenylnaringenin (8PN) beer polyphenols modulate angiogenesis, being thus targets for T2DM-related complications. Our work examined whether polyphenols consumption affects angiogenic paradox and metabolism in a T2DM mouse model. METHODS AND RESULTS: An increase in kidney and a reduction in left ventricle (LV) microvessels of diabetic C57Bl/6 mice were observed...
December 6, 2016: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/27921260/development-of-oral-flexible-tablet-oft-formulation-for-pediatric-and-geriatric-patients-a-novel-age-appropriate-formulation-platform
#8
Prabagaran Chandrasekaran, Ruckmani Kandasamy
Development of palatable formulations for pediatric and geriatric patients involves various challenges. However, an innovative development with beneficial characteristics of marketed formulations in a single formulation platform was attempted. The goal of this research was to develop solid oral flexible tablets (OFTs) as a platform for pediatrics and geriatrics as oral delivery is the most convenient and widely used mode of drug administration. For this purpose, a flexible tablet formulation using cetirizine hydrochloride as model stability labile class 1 and 3 drug as per the Biopharmaceutical Classification System was developed...
December 5, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27921177/feasibility-of-adjuvant-chemotherapy-with-s-1-plus-carboplatin-followed-by-single-agent-maintenance-therapy-with-s-1-for-completely-resected-non-small-cell-lung-cancer-results-of-the-setouchi-lung-cancer-group-study-1001
#9
Norihito Okumura, Makoto Sonobe, Kazunori Okabe, Hiroshige Nakamura, Masafumi Kataoka, Motohiro Yamashita, Masao Nakata, Kazuhiko Kataoka, Yoshinori Yamashita, Junichi Soh, Hiroshige Yoshioka, Katsuyuki Hotta, Keitaro Matsuo, Junichi Sakamoto, Shinichi Toyooka, Hiroshi Date
BACKGROUND: This multicenter study evaluated the feasibility of novel adjuvant chemotherapy with S-1 plus carboplatin followed by single-agent, long-term maintenance with S-1 in patients with completely resected stage II-IIIA non-small-cell lung cancer (NSCLC). METHODS: Patients received four cycles of S-1 (80 mg/m(2)/day for 2 weeks, followed by 2 weeks rest) plus carboplatin (area under the curve 5, day 1) followed by S-1 (80 mg/m(2)/day for 2 weeks, followed by a 1-week rest)...
December 5, 2016: International Journal of Clinical Oncology
https://www.readbyqxmd.com/read/27920772/streptococcus-thermophilus-apc151-strain-is-suitable-for-the-manufacture-of-naturally-gaba-enriched-bioactive-yogurt
#10
Daniel M Linares, Tom F O'Callaghan, Paula M O'Connor, R P Ross, Catherine Stanton
Consumer interest in health-promoting food products is a major driving force for the increasing global demand of functional (probiotic) dairy foods. Yogurt is considered the ideal medium for delivery of beneficial functional ingredients. Gamma-amino-butyric acid has potential as a bioactive ingredient in functional foods due to its health-promoting properties as an anti-stress, anti-hypertensive, and anti-diabetic agent. Here, we report the use of a novel Streptococcus thermophilus strain, isolated from the digestive tract of fish, for production of yogurt naturally enriched with 2 mg/ml of gamma-amino-butyric acid (200 mg in a standard yogurt volume of 100 ml), a dose in the same range as that provided by some commercially available gamma-amino-butyric acid supplements...
2016: Frontiers in Microbiology
https://www.readbyqxmd.com/read/27920443/polymer-matrix-nanocomposites-for-automotive-structural-components
#11
Amit K Naskar, Jong K Keum, Raymond G Boeman
Over the past several decades, the automotive industry has expended significant effort to develop lightweight parts from new easy-to-process polymeric nanocomposites. These materials have been particularly attractive because they can increase fuel efficiency and reduce greenhouse gas emissions. However, attempts to reinforce soft matrices by nanoscale reinforcing agents at commercially deployable scales have been only sporadically successful to date. This situation is due primarily to the lack of fundamental understanding of how multiscale interfacial interactions and the resultant structures affect the properties of polymer nanocomposites...
December 6, 2016: Nature Nanotechnology
https://www.readbyqxmd.com/read/27920432/discovery-of-an-enzyme-and-substrate-selective-inhibitor-of-adam10-using-an-exosite-binding-glycosylated-substrate
#12
Franck Madoux, Daniela Dreymuller, Jean-Phillipe Pettiloud, Radleigh Santos, Christoph Becker-Pauly, Andreas Ludwig, Gregg B Fields, Thomas Bannister, Timothy P Spicer, Mare Cudic, Louis D Scampavia, Dmitriy Minond
ADAM10 and ADAM17 have been shown to contribute to the acquired drug resistance of HER2-positive breast cancer in response to trastuzumab. The majority of ADAM10 and ADAM17 inhibitor development has been focused on the discovery of compounds that bind the active site zinc, however, in recent years, there has been a shift from active site to secondary substrate binding site (exosite) inhibitor discovery in order to identify non-zinc-binding molecules. In the present work a glycosylated, exosite-binding substrate of ADAM10 and ADAM17 was utilized to screen 370,276 compounds from the MLPCN collection...
December 2016: Scientific Reports
https://www.readbyqxmd.com/read/27920129/chronic-inhibition-of-renal-outer-medullary-potassium-channel-not-only-prevented-but-also-reversed-development-of-hypertension-and-end-organ-damage-in-dahl-salt-sensitive-rats
#13
Xiaoyan Zhou, Michael J Forrest, Wanda Sharif-Rodriguez, Gail Forrest, Daphne Szeto, Olga Urosevic-Price, Yonghua Zhu, Andra S Stevenson, Yuchen Zhou, Sloan Stribling, Maya Dajee, Shawn P Walsh, Alexander Pasternak, Kathleen A Sullivan
The renal outer medullary potassium (ROMK) channel mediates potassium recycling and facilitates sodium reabsorption through the Na(+)/K(+)/2Cl(-) cotransporter in the loop of Henle and potassium secretion at the cortical collecting duct. Evidence from the phenotype of humans and rodents with functional ROMK deficiency supports the contention that selective ROMK inhibitors (ROMKi) will represent a novel diuretic with potential of therapeutic benefit for hypertension. ROMKi have recently been synthesized by Merck & Co, Inc...
December 5, 2016: Hypertension
https://www.readbyqxmd.com/read/27919959/dynamin-2-inhibitors-as-novel-therapeutic-agents-against-cervical-cancer-cells
#14
Yoo-Young Lee, Hye-Kyung Jeon, Jungeun Lee, Ji Eun Hong, In-Gu DO, Chel Hun Choi, Tae-Joong Kim, Byoung-Gie Kim, Duk-Soo Bae, Yong-Chul Kim, Jeong-Won Lee
AIM: We investigated the feasibility of dynamin 2 as a potential treatment target in cervical cancer cells. MATERIALS AND METHODS: We performed tissue microarray for dynamin 2 expression in 208 patients with early cervical cancer and in vitro in HeLa cells with dynamin 2 inhibitors MiTMAB, OcTMAB, Dynasore, and DD-6. RESULTS: Tumor size greater than 2 cm or tumor invasion of more than half of the entire cervix was associated with expression of dynamin 2 compared to no expression (p=0...
December 2016: Anticancer Research
https://www.readbyqxmd.com/read/27919659/synthesis-and-sar-study-of-novel-sarsasapogenin-derivatives-as-potent-neuroprotective-agents-and-no-production-inhibitors
#15
Hui Pan, Pham Van Khang, Dong Dong, Rui Wang, Lei Ma
Sarsasapogenin, isolated from rhizomes of Anemarrhena asphodeloides, was found to be able to enhance memory. On the basis of the structure of Sarsasapogenin, a series of derivatives were synthesized and evaluated for their neuroprotective activity in PC12 cells and NO production inhibitory activity in RAW264.7 cell lines. The preliminary structure-activity relationship of them indicated that introduction of carbamate groups at the 3-hydroxyl position of sarsasapogenin might improve neuroprotective activity...
November 24, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27919655/novel-carbazole-sulfonamide-derivatives-of-antitumor-agent-synthesis-antiproliferative-activity-and-aqueous-solubility
#16
Lianqi Sun, Yanbin Wu, Yonghua Liu, Xiaofang Chen, Laixing Hu
The current optimization of IG-105 (3) on the carbazole-ring provided a series of new carbazole sulfonamides derivatives 13a-13m. All of the compounds have been evaluated against HepG2 cells (hepatoma cancer) for antiproliferative activity. Compounds that showed activity better or comparable to that of 3 versus HepG2 were evaluated against MCF-7 (breast cancer), MIA PaCa-2 (pancreatic cancer), and Bel-7402 (hepatoma/liver cancer) for antiproliferative activity. Of the seven compounds selected for further study five (13b, 13g, 13j, 13k and 13l) were found to give IC50 values against the four cell lines comparable to those for 3...
November 25, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27919216/topoisomerase-ii-inhibitors-and-poisons-and-the-influence-of-cell-cycle-checkpoints
#17
Nicholas D Arcy, Brian Gabrielli
Interactions between the decatenation checkpoint and Topoisomerase II (TopoII) are vital for maintaining integrity of the genome. Agents that target this enzyme have been in clinical use in cancer therapy for over 30 years with great success. The types of compounds that have been developed to target TopoII are broadly divided into poisons and catalytic inhibitors. The TopoII poisons are in clinical use as anti-cancer therapies, although in common to most chemotherapeutic agents, they display considerable normal tissue toxicity...
December 5, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27918995/phenylthiazole-antibiotics-a-metabolism-guided-approach-to-overcome-short-duration-of-action
#18
Eman Yahia, Haroon Mohammad, Tamer M Abdelghany, Eman Fayed, Mohamed N Seleem, Abdelrahman S Mayhoub
Antibacterial resistance is a pressing global health challenge that necessitates the development of new therapeutic agents. Phenylthiazole antibacterial agents have been extensively studied, by our group, as a potential novel class of antibiotics to circumvent the scourge of antibacterial resistance. Previously, the phenylthiazole lead compound 1 was shown to possess potent activity against clinical isolates of methicillin- and vancomycin-resistant Staphylococcus aureus (MRSA and VRSA). The promising activity of this novel class of antibiotics is hampered by their short half-life due to rapid hepatic metabolism...
November 22, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27918946/toxicity-of-ar-curcumene-and-epi-%C3%AE-bisabolol-from-hedychium-larsenii-zingiberaceae-essential-oil-on-malaria-chikungunya-and-japanese-encephalitis-mosquito-vectors
#19
Mashael Marzouq AlShebly, Fatma Saeed AlQahtani, Marimuthu Govindarajan, Kasi Gopinath, Periasamy Vijayan, Giovanni Benelli
Mosquitoes act as vectors of key pathogens and parasites. Plant essential oils have been recognized as important sources of biopesticides, which do not induce resistance and have limited toxic effects on human health and non-target organisms. In this research, we evaluated the larvicidal and oviposition deterrence activity of Hedychium larsenii essential oil (EO) and its major compounds ar-curcumene and epi-β-bisabolol. Both molecules showed high toxicity against early third instars of Anopheles stephensi (LC50=10...
December 2, 2016: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/27918490/activity-of-eribulin-in-a-primary-culture-of-well-differentiated-dedifferentiated-adipocytic-sarcoma
#20
Alessandro De Vita, Giacomo Miserocchi, Federica Recine, Laura Mercatali, Federica Pieri, Laura Medri, Alberto Bongiovanni, Davide Cavaliere, Chiara Liverani, Chiara Spadazzi, Dino Amadori, Toni Ibrahim
Eribulin mesylate is a novel, non-taxane, synthetic microtubule inhibitor showing antitumor activity in a wide range of tumors including soft tissue sarcomas (STS). Eribulin has been recently approved for the treatment of metastatic liposarcoma (LPS) patients previously treated with anthracyclines. This work investigated the mechanism of action of this innovative antitubulin agent in well-differentiated/dedifferentiated LPS (ALT/DDLPS) which represents one of the most common adipocytic sarcoma histotypes. A primary culture of ALT/DDLPS from a 54-year-old patient was established...
December 3, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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