keyword
MENU ▼
Read by QxMD icon Read
search

Drug structure

keyword
https://www.readbyqxmd.com/read/29667820/identification-of-ingol-and-rhamnofolane-diterpenoids-from-euphorbia-resinifera-and-their-abilities-to-induce-lysosomal-biosynthesis
#1
Ning-Dong Zhao, Xiao Ding, Yu Song, Dong-Qiong Yang, Hai-Li Yu, Tiwalade Adegoke Adelakun, Wen-Dan Qian, Yu Zhang, Ying-Tong Di, Fang Gao, Xiao-Jiang Hao, Shun-Lin Li
The phytochemical study of Euphorbia resinifera afforded 18 structurally diverse diterpenoids, including 14 new ingol-type diterpenoids, euphorblins A-N (1-14), a new rhamnofolane diterpenoid, euphorblin O (15), and three known analogues (16-18). The structures of these compounds were deduced using 2D NMR spectroscopy and NOE experiments. The structure of compound 1 was confirmed by single-crystal X-ray crystallography. The abilities of the compounds to enhance lysosomal biosynthesis were evaluated through LysoTracker Red staining...
April 18, 2018: Journal of Natural Products
https://www.readbyqxmd.com/read/29667727/stimuli-responsive-peptide-gels-and-some-bio-applications
#2
Natashya Falcone, Heinz-Bernhard Kraatz
Supramolecular gels are a fascinating class of soft materials that have attracted significant attention in recent years. They are composed of small molecule gelators that assemble into supramolecular network structures. The resulting space is filled with solvent. Some gel materials are able to respond to various stimuli making them attractive drug delivery vehicles and as matrices for tissue regeneration. Peptide based gel materials are particularly attractive as they possess numerous advantages including biocompatibility and biodegradability...
April 18, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29667656/carbon-based-hybrid-nanogels-a-synergistic-nanoplatform-for-combined-biosensing-bioimaging-and-responsive-drug-delivery
#3
REVIEW
Hui Wang, Qianwang Chen, Shuiqin Zhou
Nanosized crosslinked polymer networks, named as nanogels, are playing an increasingly important role in a diverse range of applications by virtue of their porous structures, large surface area, good biocompatibility and responsiveness to internal and/or external chemico-physical stimuli. Recently, a variety of carbon nanomaterials, such as carbon quantum dots, graphene/graphene oxide nanosheets, fullerenes, carbon nanotubes, and nanodiamonds, have been embedded into responsive polymer nanogels, in order to integrate the unique electro-optical properties of carbon nanomaterials with the merits of nanogels into a single hybrid nanogel system for improvement of their applications in nanomedicine...
April 18, 2018: Chemical Society Reviews
https://www.readbyqxmd.com/read/29667556/ultrasound-promoted-green-synthesis-docking-study-of-indole-spliced-thiadiazole-%C3%AE-amino-phosphonates-as-anticancer-agents-and-anti-tyrosinase-agents
#4
Anna Pratima G Nikalje, Pramod Gawhane, Shailee Tiwari, Jaiprakash Sangshetti, Manoj Damale
In this work, a new series of diethyl ((1H-indole-3-yl)((5-phenyl-1,3,4-thiadiazole-2- yl)amino)methyl)phosphonate derivatives 6(a-j) were designed and synthesized in Ultrasound by green protocol using Kabachnik-Fields reaction. The structures of the synthesized compounds were confirmed by spectral analysis such as elemental analyses, IR, 1H NMR, 13C NMR, 31P NMR and mass spectra. The synthesized compounds 6(a-j) were appraised for their in vitro anticancer activity against human cancer cell lines such as SK-MEL-2 (melanoma), IMR-32 (Neuroblastoma), HT-29(Colon) and also on normal murine embryonic fibroblast NIH/3T3 by Sulforhodamine B (SRB) assay, using Adriamycin as a standard drug...
April 17, 2018: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29667549/dentification-and-quantification-of-quercetin-a-major-consitituent-of-artocarpus-altilis-by-targeting-related-genes-of-apoptosis-and-cell-cycle-in-vitro-cytotoxic-activity-against-human-lung-carcinoma-cell-lines-a549
#5
Silvana Russo, Walter Filgueira De Azevedo
BACKGROUND: Cannabinoid Receptor 1 (CB1) is a membrane protein prevalent in the central nervous system, whose crystallographic structure has recently been solved. Studies will be needed to investigate CB1 complexes with its ligands and its role in the development of new drugs. OBJECTIVE: Our goal here is to review the studies on CB1, starting with general aspects and focusing on the recent structural studies, with emphasis on the inverse agonists bound structures...
April 17, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29667437/transdermal-buprenorphine-for-moderate-chronic-noncancer-pain-syndromes
#6
Joseph V Pergolizzi, Flaminia Coluzzi, Robert Taylor
Chronic noncancer pain has remained a challenging clinical problem. Opioid analgesics are effective, but they are known to be associated with opioid use disorder and potentially treatment-limiting side effects. Buprenorphine is a Schedule III synthetic opioid in the USA with a chemical structure similar to that of morphine but with a longer duration of action, greater potency, and other unique pharmacological attributes. Its role in treatment of chronic noncancer pain may be broader than currently thought. Areas covered: The pharmacokinetics, pharmacodynamics, clinical efficacy, and safety profile of transdermal buprenorphine in moderate chronic noncancer pain syndromes patients will be discussed...
April 18, 2018: Expert Review of Neurotherapeutics
https://www.readbyqxmd.com/read/29667367/how-to-use-prior-knowledge-and-still-give-new-data-a-chance
#7
Kristina Weber, Rob Hemmings, Armin Koch
A common challenge for the development of drugs in rare diseases and special populations, eg, paediatrics, is the small numbers of patients that can be recruited into clinical trials. Extrapolation can be used to support development and licensing in paediatrics through the structured integration of available data in adults and prospectively generated data in paediatrics to derive conclusions that support licensing decisions in the target paediatric population. In this context, Bayesian analyses have been proposed to obtain formal proof of efficacy of a new drug or therapeutic principle by using additional information (data, opinion, or expectation), expressed through a prior distribution...
April 17, 2018: Pharmaceutical Statistics
https://www.readbyqxmd.com/read/29666839/the-structure-of-the-nucleus-in-normal-and-neoplastic-prostate-cells-untangling-the-role-of-type-2-dna-topoisomerases
#8
REVIEW
William G Nelson, Michael C Haffner, Srinivasan Yegnasubramanian
Donald S. Coffey, a pioneer in the study of the structural basis of mammalian genome organization, was fascinated by DNA topoisomerases, chemo-mechanical enzymes that could catalyze changes in DNA structure. Work initiated in his laboratory and carried on with his influence and inspiration has led to the elucidation of specific roles for each of the two type 2 topoisomerases in DNA replication, RNA transcription, and androgen action in prostate cells. TOP2A principally acts in DNA synthesis elongation to prevent tangling of daughter DNA molecules during genome replication and mitotic segregation; TOP2B is required for androgen-stimulation of target gene transcription...
2018: American Journal of Clinical and Experimental Urology
https://www.readbyqxmd.com/read/29666792/steady-state-linear-and-non-linear-optical-spectroscopy-of-organic-chromophores-and-bio-macromolecules
#9
REVIEW
Marco Marazzi, Hugo Gattuso, Antonio Monari, Xavier Assfeld
Bio-macromolecules as DNA, lipid membranes and (poly)peptides are essential compounds at the core of biological systems. The development of techniques and methodologies for their characterization is therefore necessary and of utmost interest, even though difficulties can be experienced due to their intrinsic complex nature. Among these methods, spectroscopies, relying on optical properties are especially important to determine their macromolecular structures and behaviors, as well as the possible interactions and reactivity with external dyes-often drugs or pollutants-that can (photo)sensitize the bio-macromolecule leading to eventual chemical modifications, thus damages...
2018: Frontiers in Chemistry
https://www.readbyqxmd.com/read/29666228/deep-learning-improves-prediction-of-drug-drug-and-drug-food-interactions
#10
Jae Yong Ryu, Hyun Uk Kim, Sang Yup Lee
Drug interactions, including drug-drug interactions (DDIs) and drug-food constituent interactions (DFIs), can trigger unexpected pharmacological effects, including adverse drug events (ADEs), with causal mechanisms often unknown. Several computational methods have been developed to better understand drug interactions, especially for DDIs. However, these methods do not provide sufficient details beyond the chance of DDI occurrence, or require detailed drug information often unavailable for DDI prediction. Here, we report development of a computational framework DeepDDI that uses names of drug-drug or drug-food constituent pairs and their structural information as inputs to accurately generate 86 important DDI types as outputs of human-readable sentences...
April 16, 2018: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/29666187/a-putative-g-quadruplex-structure-in-the-proximal-promoter-of-vegfr-2-has-implications-for-drug-design-to-inhibit-tumor-angiogenesis
#11
Yaping Liu, Wenxian Lan, Chunxi Wang, Chunyang Cao
Tumor angiogenesis is mainly regulated by vascular endothelial growth factor (VEGF), produced by cancer cells. It is active on the endothelium via VEGF receptor 2 (VEGFR-2). G-quadruplexes are DNA secondary structures formed by guanine-rich sequences, for example, within gene promoters where they may contribute to transcriptional activity. The proximal promoter of vegfr-2 contains a G-quadruplex, which has been suggested to interact with small molecules that inhibit VEGFR-2 expression and thereby tumor angiogenesis...
April 17, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29665849/an-innovative-immunotherapeutic-strategy-for-ovarian-cancer-clec10a-and-glycomimetic-peptides
#12
Laura L Eggink, Katherine F Roby, Robert Cote, J Kenneth Hoober
BACKGROUND: Receptors specific for the sugar N-acetylgalactosamine (GalNAc) include the human type II, C-type lectin receptor macrophage galactose-type lectin/C-type lectin receptor family member 10A (MGL/CLEC10A/CD301) that is expressed prominently by human peripheral immature dendritic cells, dendritic cells in the skin, alternatively-activated (M2a) macrophages, and to lesser extents by several other types of tissues. CLEC10A is an endocytic receptor on antigen-presenting cells and has been proposed to play an important role in maturation of dendritic cells and initiation of an immune response...
April 17, 2018: Journal for Immunotherapy of Cancer
https://www.readbyqxmd.com/read/29665557/negative-effects-of-artemisinin-on-phosphorus-solubilizing-bacteria-in-vitro
#13
Huiwen Zeng, Ling Yuan, Jianguo Huang
The anti-malarial drug artemisinin is extracted from the leaves of Artemisia annua L. Due to toxicity to some microorganisms, the release of artemisinin from this medicinal plant in commercial cultivation might produce a potential risk for phosphorus (P) solubilizing bacteria (PSB). Therefore, the growth, P mobilization, and proton and organic acid efflux by two PSB isolates, Bacillus subtilis and Pseudomonas fluorescens, obtained from the soil without growing A. annua L. in history in the region for growing A...
April 14, 2018: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29665554/inhibition-by-non-steroidal-anti-inflammatory-drugs-of-compound-action-potentials-in-frog-sciatic-nerve-fibers
#14
Rika Suzuki, Tsugumi Fujita, Kotaro Mizuta, Eiichi Kumamoto
AIMS: Although antinociception produced by non-steroidal anti-inflammatory drugs (NSAIDs) is partly attributed to nerve conduction inhibition, this has not been thoroughly examined yet. The aim of the present study was to reveal quantitatively how various types of NSAIDs affect compound action potentials (CAPs), a measure of nerve conduction. MAIN METHODS: CAPs were recorded from the frog sciatic nerve by using the air-gap method. KEY FINDINGS: Soaking the sciatic nerve with acetic acid-based NSAIDs (diclofenac and aceclofenac) reduced the peak amplitude of CAP in a concentration-dependent manner; their IC50 values were 0...
April 14, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29665527/discovery-of-1-8-acridinedione-derivatives-as-novel-gcn5-inhibitors-via-high-throughput-screening
#15
Huan Xiong, Jie Han, Jun Wang, Wenchao Lu, Chen Wang, Yu Chen, Fulin Lian, Naixia Zhang, Yu-Chih Liu, Chenhua Zhang, Hong Ding, Hualiang Jiang, Wencong Lu, Cheng Luo, Bing Zhou
The general control nonrepressed protein 5 (GCN5) plays a crucial role in many biological processes. Dysregulation of GCN5 has been closely related to various human diseases, especially cancers. Hence, the exploitation of small molecules targeting GCN5 is essential for drug design and academic research. Based on the amplified luminescent proximity homogeneous assay screen methodology, we performed high throughput screening and discovered a novel GCN5 inhibitor DC_G16 with 1,8-acridinedione scaffold. Structure optimization led to the identification of a highly potent inhibitor, namely DC_G16-11 with the half-maximal inhibitory concentration (IC50 ) value of 6...
February 14, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29665383/impact-of-aging-alzheimer-s-disease-and-parkinson-s-disease-on-the-blood-brain-barrier-transport-of-therapeutics
#16
Yijun Pan, Joseph A Nicolazzo
Older people are at greater risk of medicine-induced toxicities resulting from either increased drug sensitivity or age-related pharmacokinetic changes. The scenario is further complicated with the two most prevalent age-related neurodegenerative diseases, Alzheimer's disease (AD) and Parkinson's disease (PD). With aging, AD and PD, there is growing evidence of altered structure and function of the blood-brain barrier (BBB), including modifications to tight junctions and efflux transporters, such as P-glycoprotein...
April 14, 2018: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/29665064/tourism-labor-embodied-suffering-and-the-deportation-regime-in-the-dominican-republic
#17
Mark Padilla, José Félix Colón-Burgos, Nelson Varas-Díaz, Armando Matiz-Reyes, Caroline Mary Parker
In this article, we use syndemic theory to examine socio-structural factors that result in heightened vulnerability to HIV infection and drug addiction among Dominican deportees who survive post-deportation through informal tourism labor. Through an ongoing NIDA-funded ethnographic study of the syndemic of HIV and problematic drug use among men involved in tourism labor in the Dominican Republic, we argue that the legal and political-economic context of the global deportation regime contributes to structural vulnerabilities among deportees in the Dominican Republic, most of whom are men with histories of incarceration in the United States and/or Puerto Rico...
April 17, 2018: Medical Anthropology Quarterly
https://www.readbyqxmd.com/read/29664222/recent-developments-and-clinical-potential-on-decellularized-adipose-tissue
#18
REVIEW
Jia Dong, Mei Yu, Yan Zhang, Yin Yin, Weidong Tian
Natural and synthetic materials have been developed to provide a three-dimensional (3-D) scaffold that mimics the extracellular matrix properties for tissue regeneration and reconstruction. On account of the excellent biological and mechanical properties, diverse decellularized tissue materials have been developed as natural scaffolds. Among them, decellularized adipose tissue (DAT) has generated great interest in recent years due to the extensiveness of the source and the eximious potential to enhance the regeneration and repair of damaged tissues...
April 17, 2018: Journal of Biomedical Materials Research. Part A
https://www.readbyqxmd.com/read/29664104/self-assembled-nanodiamond-supraparticles-for-anticancer-chemotherapy
#19
Yue Yu, Masahiro Nishikawa, Ming Liu, Takahiro Tei, Sunil C Kaul, Renu Wadhawa, Minfang Zhang, Junko Takahashi, Eijiro Miyako
A nanodiamond (ND) is a promising material for drug delivery applications owing to its relatively low cost, amenability to large-scale synthesis, unique structure, and low toxicity. However, synthesizing drug-loaded ND conjugates with uniform and tunable sizes, high loading capacity, efficacy in drug delivery, and versatility in terms of surface functionalization has been challenging. Here, we show that perfluorooctanoic acid-functionalized NDs spontaneously transform into well-dispersed and biocompatible supraparticle (SP) nanoclusters...
April 17, 2018: Nanoscale
https://www.readbyqxmd.com/read/29663922/hyaluronan-based-tumor-targeting-and-ph-responsive-shell-cross-linkable-nanoparticles-for-the-controlled-release-of-doxorubicin
#20
Jianhong Liao, Haoran Zheng, Rui Hu, Jun Cao, Xuan Wei, Dan Li, Hua Zheng, Yihua Yin
In this study, a series of amphiphilic polymeric prodrugs (Azido-functionalized hyaluronan-triazole-imine-doxorubicin, HAimine-DOX) were designed and synthesized by the "Click" reaction with a remarkable grafting ratio of DOX. Nanoparticles with a core-shell structure can be obtained by self-assembling in aqueous media, which exhibited a particle size of 137-170 nm. Moreover, the HA-imine-DOX nanoparticles exhibited good stability in vitro, and the drug release was obviously mediated by the pH gradient...
March 1, 2018: Journal of Biomedical Nanotechnology
keyword
keyword
44759
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"