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https://www.readbyqxmd.com/read/28445970/acid-ceramidase-is-a-novel-drug-target-for-pediatric-brain-tumors
#1
Ninh B Doan, Ha S Nguyen, Andrew Montoure, Mona M Al-Gizawiy, Wade M Mueller, Shekar Kurpad, Scott D Rand, Jennifer M Connelly, Christopher R Chitambar, Kathleen M Schmainda, Shama P Mirza
Pediatric brain tumors are the most common solid tumors in children and are also a leading culprit of cancer-related fatalities in children. Pediatric brain tumors remain hard to treat. In this study, we demonstrated that medulloblastoma, pediatric glioblastoma, and atypical teratoid rhabdoid tumors express significant levels of acid ceramidase, where levels are highest in the radioresistant tumors, suggesting that acid ceramidase may confer radioresistance. More importantly, we also showed that acid ceramidase inhibitors are highly effective at targeting these pediatric brain tumors with low IC50 values (4...
April 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28445958/repressing-cd147-is-a-novel-therapeutic-strategy-for-malignant-melanoma
#2
REVIEW
Xing Hu, Juan Su, Youyou Zhou, Xiaoyun Xie, Cong Peng, Zhimin Yuan, Xiang Chen
CD147/basigin, a transmembrane protein, is a member of the immunoglobulin super family. Accumulating evidence has revealed the role of CD147 in the development and progression of various cancers, including malignant melanoma (MM). MM is a malignancy of pigment-producing cells that causes the greatest number of skin cancer-related deaths worldwide. CD147 is overexpressed in MM and plays an important role in cell viability, apoptosis, proliferation, invasion, and metastasis, probably by mediating vascular endothelial growth factor (VEGF) production, glycolysis, and multi-drug resistance (MDR)...
April 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28445950/the-discovery-of-a-novel-compound-with-potent-antitumor-activity-virtual-screening-synthesis-biological-evaluation-and-preliminary-mechanism-study
#3
Yuanyuan Jin, Linhu Li, Zhaoyong Yang, Mingliang Liu, Huiyuan Guo, Weiyi Shen
Farnesyltransferase has been regarded as a promising drug target against cancer as it is critical for membrane association of several signal transduction proteins. In this study, a novel farnesyltransferase inhibitor (IMB-1406) was identified through virtual screening. It exhibits stronger potency (IC50s: 6.92-8.99 μM) than Sunitinib against all of the tested cancer cell lines. Preliminary studies on mechanism reveal that IMB-1406 induces apoptosis in HepG2 cells by arresting the cell cycle at the S phase, altering anti- and pro-apoptotic proteins leading to mitochondrial dysfunction and activation of caspase-3...
April 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28445934/jarid2-is-essential-for-the-maintenance-of-tumor-initiating-cells-in-bladder-cancer
#4
Xin-Xing Zhu, Ya-Wei Yan, Chun-Zhi Ai, Shan Jiang, Shan-Shan Xu, Min Niu, Xiang-Zhen Wang, Gen-Shen Zhong, Xi-Feng Lu, Yu Xue, Shaoqi Tian, Guangyao Li, Shaojun Tang, Yi-Zhou Jiang
Bladder cancer is the most common urologic malignancy in China, with an increase of the incidence and mortality rates over past decades. Recent studies suggest that bladder tumors are maintained by a rare fraction of cells with stem cell proprieties. Targeting these bladder tumor initiating cell (TICs) population can overcome the drug-resistance of bladder cancer. However, the molecular and genetic mechanisms regulating TICs in bladder cancer remain poorly defined. Jarid2 is implicated in signaling pathways regulating cancer cell epithelial-mesenchymal transition, and stem cell maintenance...
April 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28445844/upregulation-of-mir-142-3p-improves-drug-sensitivity-of-acute-myelogenous-leukemia-through-reducing-p-glycoprotein-and-repressing-autophagy-by-targeting-hmgb1
#5
Yuan Zhang, Yufeng Liu, Xueju Xu
miR-142-3p was reported to be downregulated in acute myelogenous leukemia (AML) and acted as a novel diagnostic marker. However, the regulatory effect of miR-142-3p on drug resistance of AML cells and its underlying mechanism have not been elucidated. Here, we found that miR-142-3p was significantly downregulated and high mobility group box 1 (HMGB1) was dramatically upregulated in AML samples and cells, as well as drug-resistant AML cells. P-gp level and autophagy were markedly enhanced in HL-60/ADR and HL-60/ATRA cells...
April 23, 2017: Translational Oncology
https://www.readbyqxmd.com/read/28445625/the-use-of-an-occlusion-perfusion-catheter-to-deliver-paclitaxel-to-the-arterial-wall
#6
Marzieh K Atigh, Emily Turner, Uwe Christians, Saami K Yazdani
AIM: Non-stent drug delivery platforms have recently emerged as an alternative treatment of peripheral arterial disease. Perfusion catheters have the potential to directly deliver anti-proliferative agents to the medial arterial layer to prevent restenosis. The purpose of this study was to therefore determine the effectiveness of a perfusion catheter to deliver paclitaxel, a proven anti-proliferative agent, to combat restenosis. METHODS: A bench-top model was utilized to determine the varying parameters of a novel occlusion perfusion catheter to maximize paclitaxel delivery using pharmacokinetic evaluation and fluorescent microscopy...
April 26, 2017: Cardiovascular Therapeutics
https://www.readbyqxmd.com/read/28445605/high-throughput-cell-mechanical-phenotyping-for-label-free-titration-assays-of-cytoskeletal-modifications
#7
Stefan Golfier, Philipp Rosendahl, Alexander Mietke, Maik Herbig, Jochen Guck, Oliver Otto
The mechanical fingerprint of cells is inherently linked to the structure of the cytoskeleton and can serve as a label free marker for cell homeostasis or pathologic states. How cytoskeletal composition affects the physical response of cells to external loads has been intensively studied with a spectrum of techniques, yet quantitative and statistically powerful investigations in the form of titration assays are hampered by the low throughput of most available methods. In this study, we employ real-time deformability cytometry (RT-DC), a novel microfluidic tool to examine the effects of biochemically modified F-actin and microtubule stability and nuclear chromatin structure on cell deformation in a human leukemia cell line (HL60)...
April 26, 2017: Cytoskeleton
https://www.readbyqxmd.com/read/28445553/a-novel-rat-head-gaze-determination-system-based-on-optomotor-responses
#8
Mengbo You, Toshiyuki Yamane, Hiroshi Tomita, Eriko Sugano, Takuya Akashi
The optomotor response of animals is commonly used to measure their visual performance, e.g., rats of different genetically altered strains or various drug tests. With the presentation of stimuli using computer screens or projectors, the common idea focuses on measuring the eye movement or head and/or body movement to characterize changes of the head gaze. However, traditional methods rely on either the invasive fixation of animals, or the judgment of a human observer who reports the stimulus-tracking movements...
2017: PloS One
https://www.readbyqxmd.com/read/28445429/exploring-the-behavioral-and-metabolic-phenotype-generated-by-re-introduction-of-the-ghrelin-receptor-in-the-ventral-tegmental-area
#9
Louise J Skov, Morten Jensen, Søren H Christiansen, Cecilia Ratner, David P D Woldbye, Birgitte Holst
Ghrelin receptor (Ghr-R) signaling in neurons of the ventral tegmental area (VTA) can modulate dopaminergic function and the reward-related effects of both palatable foods and drugs of abuse. In this study, we re-introduced the Ghr-R in VTA neurons in Ghr-R knockout mice (Ghr-R(VTA) mice) to specifically study the importance of the constitutively active Ghr-R for VTA neuronal signaling. Our results showed that re-introduction of the Ghr-R in the VTA had no impact on body weight or food intake under basal conditions...
April 26, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28445233/preclinical-models-for-translational-sarcoma-research
#10
Rainer Hamacher, Sebastian Bauer
PURPOSE OF REVIEW: Sarcoma is a basket term for mesenchymal tumors for which more than 75 genetically and histologically distinct subtypes are recognized. Therapeutic progress has largely been achieved with classical chemotherapeutic drugs that were tested in empirical clinical trials. However, outcome in metastatic patients remains poor and with few exceptions numerous trials have failed or only provided limited improvement in recent years. RECENT FINDINGS: Given the genomic heterogeneity, preclinical model systems will be indispensable to identify new molecular targets and to prioritize drugs and drug combinations...
April 25, 2017: Current Opinion in Oncology
https://www.readbyqxmd.com/read/28445176/novel-lipid-modifying-drugs-to-lower-ldl-cholesterol
#11
Arjen J Cupido, Laurens F Reeskamp, John J P Kastelein
PURPOSE OF REVIEW: Statins have long been the cornerstone for the prevention of cardiovascular disease (CVD). However, because of perceived adverse effects and insufficient efficacy in certain groups of patients, considerable interest exists in the search for alternatives to lower LDL-cholesterol (LDL-C), and the recent approvals of proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors underlines the success of this quest. Here, we give an updated overview on the most recent developments in the area of LDL-C lowering agents...
April 25, 2017: Current Opinion in Lipidology
https://www.readbyqxmd.com/read/28445124/a-novel-triazolonaphthalimide-induces-apoptosis-and-inhibits-tumor-growth-by-targeting-dna-and-dna-associated-processes
#12
Liyan Ji, Simin Yang, Shasha Li, Shan Liu, Shunan Tang, Zhongqiu Liu, Xiangbao Meng, Siwang Yu
DNA and DNA-associated processes have been classes of the most important targets of chemotherapeutic drugs. As classic DNA intercalators and topoisomerase inhibitors, naphthalimides have been extensively investigated as potential anti-cancer drugs. We recently synthesized a novel series of triazolonaphthalimides with excellent anti-cancer activities. In the present study, one of the most potent triazolonaphthalimides, LSS-11, was investigated. LSS-11 bound to DNA in vitro and in cell mainly by minor groove binding and significantly increased the stability of DNA, which could be fundamental for the biological activities of LSS-11...
April 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/28445005/proteomic-based-investigations-on-the-mode-of-action-of-the-marine-anticancer-compound-rhizochalinin
#13
Sergey A Dyshlovoy, Katharina Otte, Simone Venz, Jessica Hauschild, Heike Junker, Tatyana N Makarieva, Stefan Balabanov, Winfried H Alsdorf, Ramin Madanchi, Friedemann Honecker, Carsten Bokemeyer, Valentin A Stonik, Gunhild von Amsberg
Rhizochalinin (Rhiz) is a novel marine natural sphingolipid-like compound which shows promising in vitro and in vivo activity in human castration-resistant prostate cancer (CRPC). In the present study, a global proteome screening approach was applied to investigate molecular targets and biological processes affected by Rhiz in CRPC. Bioinformatical analysis of the data predicted an anti-migratory effect of Rhiz on cancer cells. Validation of proteins involved in the cancer-associated processes, including cell migration and invasion, revealed down-regulation of specific isoforms of stathmin and LASP1, as well as up-regulation of Grp75, keratin 81, and precursor IL-1β by Rhiz...
April 26, 2017: Proteomics
https://www.readbyqxmd.com/read/28445001/inhibition-properties-of-some-flavonoids-on-carbonic-anhydrase-i-and-ii-isoenzymes-purified-from-human-erythrocytes
#14
Zübeyir Huyut, Şükrü Beydemir, İlhami Gülçin
Carbonic anhydrases (CAs, E.C.4.2.1.1) play a critical role in many important physiological events and treatment of some diseases. Flavonoids or phenolic compounds have been discovered as novel CAs inhibitors instead of the traditional sulfonamides, with different binding to CAs, pro-drug activities, and new inhibition mechanisms. Here, we investigated the inhibition effects of some flavonoids including malvin, callistephin, oenin, pelargonin, silychristin, and 1-(4-methoxyphenyl)-2-methyl-3-nitro-1-H-indol-6-ol (ID-8) against hCA I and II, which purified from human erythrocytes by affinity column chromatography...
April 26, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/28444771/oestrone-targeted-liposomes-for-mitoxantrone-delivery-via-oestrogen-receptor-synthesis-physicochemical-characterization-and-in-vitro-evaluation
#15
Qiang Hao, Guoxing Xu, Yue Yang, Yuxin Sun, Dengli Cong, Hongrui Li, Xin Liu, Zeng Wang, Zheng Zhang, Jinglin Chen, Yao Li, Xue Luan, Lin Wang, Lin Tian, Kun Liu, Yan Li, Qianru Jiao, Jin Pei
OBJECTIVES: Targeted delivery of mitoxantrone (MTO, an anthraquinone drug with high antitumour effect) may be achieved using a novel nanoparticulate delivery system via binding the oestrogen receptor (ER, highly expressed in a variety of human tumours). METHODS: A novel liposomal nanoparticle (NP) was developed using a conjugate derived from 1, 2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino (polyethylene glycol)-2000] (DSPE-PEG2000 -NH2 ) and oestrone (ES, is known to bind the ER) to produce an ES-targeted PEGylated liposome (ES-SSL)...
April 26, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28444716/the-relative-bioavailability-of-ibuprofen-after-administration-with-a-novel-soft-chewable-drug-formulation
#16
Magnus N Hattrem, Morten J Dille, Tore Seternes, Thorfinn Ege, Kurt I Draget
The first aim of the present study was to evaluate the bioavailability of ibuprofen dispersed in a novel soft chewable formulation compared with a traditional ibuprofen tablet; its second was to map the quality of taste masking and patient product satisfaction. In a phase 1, single-center, open-label, randomized, crossover study, healthy subjects received a soft-chew formulation or a hard tablet (reference), both containing 100 mg ibuprofen. Serial blood samples were collected over 24 hours to assess ibuprofen bioavailability...
April 25, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28444555/evaluating-the-effectiveness-of-a-novel-atomized-liquid-needle-free-transdermal-delivery-system
#17
Yi-Huei Huang, Chieh-Shen Hu, Yi-Jhen Ke, Chiao-Hsi Chiang, Po-Da Hong, Ming-Kung Yeh
Needle-free jet injections constitute a crucial method for drug delivery. A novel liquid drug delivery system has been proposed recently, in which pressure atomizes liquid before delivering that atomized liquid to the patient's body; however, the mechanism and efficiency of the system are unclear. This study explored the shot delivery pressure, penetration depth, and cumulative amount of permeation of this system. This system was used to deliver 0.5% (w/v) methylene blue to agarose phantoms at various shot delivery pressures...
April 25, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28444310/arl3-and-rp2-regulate-the-trafficking-of-ciliary-tip-kinesins
#18
Nele Schwarz, Amelia Lane, Katarina Jovanovich, David A Parfitt, Monica Aguila, Clare L Thompson, Lyndon da Cruz, Peter J Coffey, J Paul Chapple, Alison J Hardcastle, Michael E Cheetham
Ciliary trafficking defects are the underlying cause of many ciliopathies, including Retinitis Pigmentosa (RP). Anterograde intraflagellar transport (IFT) is mediated by kinesin motor proteins; however, the function of the homodimeric Kif17 motor in cilia is poorly understood, whereas Kif7 is known to play an important role in stabilising cilia tips. Here we identified the ciliary tip kinesins Kif7 and Kif17 as novel interaction partners of the small GTPase Arl3 and its regulatory GTPase activating protein (GAP) Retinitis Pigmentosa 2 (RP2)...
April 21, 2017: Human Molecular Genetics
https://www.readbyqxmd.com/read/28443923/use-of-alcl3-in-friedel-crafts-arylation-type-reactions-and-beyond-an-overview-on-the-development-of-unique-methodologies-leading-to-n-heteroarenes
#19
REVIEW
Rajnikanth Sunke, Suresh Babu Nallapati, Jetta Sandeep Kumar, K Shiva Kumar, Manojit Pal
As a privileged class of heterocyclic compounds N-heteroarenes have found enormous applications in many areas including medicinal/pharmaceutical chemistry and drug discovery. Consequently, a wide variety of methods have been reported for their synthesis. While not free from their own limitations the AlCl3 mediated methods appeared to have some particular advantages in preparing a number of useful N-heteroarenes. Besides the famous Friedel-Crafts (FC) alkylation/acylation reactions one such example is AlCl3-induced heteroarylation of arenes and heteroarenes (FC arylation type reactions) that can be used to prepare a certain class of N-heteroarenes in an operationally simple, efficient and cost effective manner...
April 26, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28443514/compound-libraries-recent-advances-and-their-applications-in-drug-discovery
#20
Zhen Gong, Guoping Hu, Qiang Li, Zhiguo Liu, Fei Wang, Xuejin Zhang, Jian Xiong, Peng Li, Yan Xu, Rujian Ma, Shuhui Chen, Jian Li
Hit identification is the starting point of small-molecule drug discovery and is therefore very important to the pharmaceutical industry. One of the most important approaches to identify a new hit is to screen a compound library using an in vitro assay. High-throughput screening has made great contributions to drug discovery since the 1990s but requires expensive equipment and facilities, and its success depends on the size of the compound library. Recent progress in the development of compound libraries has provided more efficient ways to identify new hits for novel drug targets, thereby helping to promote the development of the pharmaceutical industry, especially for first-in-class drugs...
April 25, 2017: Current Drug Discovery Technologies
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