keyword
MENU ▼
Read by QxMD icon Read
search

Designer drugs

keyword
https://www.readbyqxmd.com/read/29220793/design-synthesis-and-biological-evaluation-of-novel-highly-selective-polo-like-kinase-2-inhibitors-based-on-the-tetrahydropteridin-chemical-scaffold
#1
Mei-Miao Zhan, Yang Yang, Jinfeng Luo, Xing-Xing Zhang, Xuan Xiao, Shiyu Li, Kai Cheng, Zhouling Xie, Zhengchao Tu, Chenzhong Liao
Polo-like kinase 2 (Plk2) is a potential target for the treatment of cancer, which displays an important role in tumor cell proliferation and survival. In this report, according to the analysis of critical amino acid residue differences among Plk1, Plk2 and Plk3, and structure-based drug design strategies, two novel series of selective Plk2 inhibitors based on tetrahydropteridin chemical scaffold were designed and synthesized to target two specific residues, Lys86 and Tyr161 of Plk2. All compounds were evaluated for their inhibitory activity against Plk1-Plk3 and the cellular inhibition activity on six different human cancer cell lines...
November 23, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29220792/4-quinolone-derivatives-and-their-activities-against-gram-positive-pathogens
#2
Gui-Fu Zhang, Shu Zhang, Baofeng Pan, Xiaofeng Liu, Lian-Shun Feng
Gram-positive bacteria are responsible for a broad range of infectious diseases, and the emergency and wide spread of drug-resistant Gram-positive pathogens including MRSA and MRSE has caused great concern throughout the world. 4-Quinolones which are exemplified by fluoroquinolones are mainstays of chemotherapy against various bacterial infections including Gram-positive pathogen infections, and their value and role in the treatment of bacterial infections continues to expand. However, the resistance of Gram-positive organisms to 4-quinolones develops rapidly and spreads widely, making them more and more ineffective...
November 29, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29220642/substance-use-patterns-associated-with-recent-exposure-to-fentanyl-among-people-who-inject-drugs-in-vancouver-canada-a-cross-sectional-urine-toxicology-screening-study
#3
Kanna Hayashi, M-J Milloy, Mark Lysyshyn, Kora DeBeck, Ekaterina Nosova, Evan Wood, Thomas Kerr
INTRODUCTION: Vancouver, Canada is experiencing an opioid overdose crisis where fentanyl, a potent, synthetic opioid contaminating the illicit drug supply, has been detected in the majority of fatal overdose cases. Despite its growing presence throughout North America, few studies have characterized exposure to fentanyl among people who use illicit drugs (PWUD). We sought to identify the prevalence and correlates of fentanyl exposure among PWUD in Vancouver. METHODS: Data were derived from cohort studies of PWUD in Vancouver...
December 5, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29220610/predictors-of-alcohol-use-during-pregnancy-among-women-attending-midwife-obstetric-units-in-the-cape-metropole-south-africa
#4
Petal Petersen-Williams, Catherine Mathews, Esmé Jordaan, Charles D H Parry
INTRODUCTION: Little is known about the nature and extent of substance use among pregnant women in Cape Town (South Africa) despite the very high levels of substance use and related consequences such as FASD in this part of the country. The aim of the study was to determine predictors of alcohol use among pregnant women. METHODS: A cross-sectional survey was conducted among pregnant women attending 11 Midwife Obstetric Units (MOUs) in greater Cape Town. A two-stage cluster survey design was used...
December 8, 2017: Substance Use & Misuse
https://www.readbyqxmd.com/read/29220568/aniline-based-inhibitors-of-influenza-h1n1-virus-acting-on-hemagglutinin-mediated-fusion
#5
Rosana Leiva, Marta Barniol-Xicota, Sandra Codony, Tiziana Ginex, Evelien Vanderlinden, Marta Montes, Michael Caffrey, F Javier Luque, Lieve Naesens, Santiago Vazquez
Two series of easily accessible anilines were identified as inhibitors of influenza A virus subtype H1N1, and extensive chemical synthesis and analysis of the structure-activity relationship were performed. The compounds were shown to interfere with low pH-induced membrane fusion mediated by the H1 and H5 (group 1) hemagglutinin (HA) subtypes. A combination of virus resistance, HA interaction and molecular dynamics simulation studies elucidated the binding site of these aniline-based influenza fusion inhibitors, which significantly overlaps with the pocket occupied by some H3 HA-specific inhibitors, indicating the high relevance of this cavity for drug design...
December 8, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29218635/long-range-paramagnetic-nmr-data-can-provide-a-closer-look-on-metal-coordination-in-metalloproteins
#6
Linda Cerofolini, Tommaso Staderini, Stefano Giuntini, Enrico Ravera, Marco Fragai, Giacomo Parigi, Roberta Pierattelli, Claudio Luchinat
Paramagnetic NMR data can be profitably incorporated in structural refinement protocols of metalloproteins or metal-substituted proteins, mostly as distance or angle restraints. However, they could in principle provide much more information, because the magnetic susceptibility of a paramagnetic metal ion is largely determined by its coordination sphere. This information can in turn be used to evaluate changes occurring in the coordination sphere of the metal when ligands (e.g.: inhibitors) are bound to the protein...
December 7, 2017: Journal of Biological Inorganic Chemistry: JBIC
https://www.readbyqxmd.com/read/29218520/design-synthesis-and-evaluation-of-glut-inhibitors
#7
Carlotta Granchi, Tiziano Tuccinardi, Filippo Minutolo
The Warburg effect describes how most cancer cells exhibit higher-than-normal glucose consumption, not only under hypoxic conditions, but also when normal oxygen levels are present. Although glucose transporter 1 (GLUT1) has been found to play a key role in the cellular uptake of glucose, especially in cancer cells, where it is generally overexpressed, it has not been given consideration as a suitable target for the development of anticancer drugs. In this chapter, an example of molecular design and realization of novel GLUT1 inhibitors, including in silico modeling, chemical synthesis, and biological characterization, is provided...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/29218506/in-silico-discovery-of-novel-ligands-for-antimicrobial-lipopeptides-for-computer-aided-drug-design
#8
REVIEW
Satya Eswari Jujjavarapu, Swasti Dhagat
The increase in antibiotic-resistant strains of pathogens has created havoc worldwide. These antibiotic-resistant pathogens require potent drugs for their inhibition. Lipopeptides, which are produced as secondary metabolites by many microorganisms, have the ability to act as potent safe drugs. Lipopeptides are amphiphilic molecules containing a lipid chain bound to the peptide. They exhibit broad-spectrum activities against both bacteria and fungi. Other than their antimicrobial properties, they have displayed anti-cancer properties as well, but their mechanism of action is not understood...
December 7, 2017: Probiotics and Antimicrobial Proteins
https://www.readbyqxmd.com/read/29218501/evaluating-safety-reporting-in-paediatric-antibiotic-trials-2000-2016-a-systematic-review-and-meta-analysis
#9
REVIEW
Paola Pansa, Yingfen Hsia, Julia Bielicki, Irja Lutsar, A Sarah Walker, Mike Sharland, Laura Folgori
BACKGROUND: There are very few options to treat multidrug-resistant bacterial infections in children. A major barrier is the duration and complexity of regulatory trials of new antibiotics. Extrapolation of safety data from adult trials could facilitate drug development for children. OBJECTIVE: We performed a systematic review on the safety of antibiotic clinical trials (CTs) in children (0-18 years) to evaluate the overall quality of safety trials conducted in children and to determine if age-specific adverse events (AEs) could be identified for specific antibiotic classes...
December 7, 2017: Drugs
https://www.readbyqxmd.com/read/29218003/eye-drops-for-activation-of-dreadds
#10
William T Keenan, Diego C Fernandez, Lukas J Shumway, Haiqing Zhao, Samer Hattar
Designer Receptors Exclusively Activated by Designer Drugs (DREADDs) are an important tool for modulating and understanding neural circuits. Depending on the DREADD system used, DREADD-targeted neurons can be activated or repressed in vivo following a dose of the DREADD agonist clozapine-N-oxide (CNO). Because DREADD experiments often involve behavioral assays, the method of CNO delivery is important. Currently, the most common delivery method is intraperitoneal (IP) injection. IP injection is both a fast and reliable technique, but it is painful and stressful particularly when many injections are required...
2017: Frontiers in Neural Circuits
https://www.readbyqxmd.com/read/29217952/control-of-hypertension-among-diabetic-patients-in-a-referral-hospital-in-tanzania-a-cross-sectional-study
#11
Semvua B Kilonzo, Daniel W Gunda, Fatma A Bakshi, Fredrick Kalokola, Henry A Mayala, Hollo Dadi
Background: Hypertension is common among diabetic patients. The co-existence of two conditions carries an excessive risk of severe complications and mortalities. Limited information exists on the determinants of poor hypertension control among these patients. We aimed at determining the prevalence and factors associated with poor hypertension control in these patients. Methods: Data of diabetic patients who were also hypertensive attending an outpatient clinic from 1 August 2015 to 31 December 2015 at Bugando Medical Centre were retrospectively analyzed...
September 2017: Ethiopian Journal of Health Sciences
https://www.readbyqxmd.com/read/29217936/utilization-of-primary-health-care-services-in-jaba-local-government-area-of-kaduna-state-nigeria
#12
Agofure Otovwe, Sarki Elizabeth
Background: Primary health care was designed to provide accessible health care for all. However, most primary health care facilities are in various states of disrepair, catering for less than 20% of potential patients in the population. This study was designed to investigate the utilisation of primary health care services in Jaba Local Government Area of Kaduna State Nigeria. Methods: The study employed a cross-sectional study design conducted among 383 respondents utilising simple random sampling techniques...
July 2017: Ethiopian Journal of Health Sciences
https://www.readbyqxmd.com/read/29217475/in-vitro-drug-release-and-in-vivo-safety-of-vitamin-e-and-cysteamine-loaded-contact-lenses
#13
Phillip Dixon, Richard C Fentzke, Arnab Bhattacharya, Aditya Konar, Sarbani Hazra, Anuj Chauhan
Cystinosis is an orphan disease caused by a genetic mutation that leads to deposition of cystine crystals in many organs including cornea. Ophthalmic manifestation of the disease can be treated with hourly instillation of cysteamine eye drops. The hourly eye drop instillation is tedious to the patients leading to poor compliance and additionally, significant degradation of the drug occurs within one week of opening the bottle, which further complicates this delivery approach. This paper focuses on designing a contact lens to treat the disease with improved efficacy compared to eye drops, and also exploring safety of the drug eluding contact lens in an animal model...
December 4, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29217457/focusing-on-claudin-5-a-promising-candidate-in-the-regulation-of-bbb-to-treat-ischemic-stroke
#14
REVIEW
Jianjun Lv, Wei Hu, Zhi Yang, Tian Li, Shuai Jiang, Zhiqiang Ma, Fulin Chen, Yang Yang
Claudin-5 is a tight junction (TJ) protein in the blood-brain barrier (BBB) that has recently attracted increased attention. Numerous studies have demonstrated that claudin-5 regulates the integrity and permeability of the BBB. Increased claudin-5 expression plays a neuroprotective role in neurological diseases, particularly in cerebral ischemic stroke. Moreover, claudin-5 might be a potential marker for early hemorrhagic transformation detection in ischemic stroke. In light of the distinctive effects of claudin-5 on the nervous system, we present the elaborate network of roles that claudin-5 plays in ischemic stroke...
December 4, 2017: Progress in Neurobiology
https://www.readbyqxmd.com/read/29216878/adaptive-phenotype-drives-resistance-to-androgen-deprivation-therapy-in-prostate-cancer
#15
Nicoletta Ferrari, Ilaria Granata, Matteo Capaia, Marina Piccirillo, Mario Rosario Guarracino, Roberta Venè, Antonella Brizzolara, Andrea Petretto, Elvira Inglese, Martina Morini, Simonetta Astigiano, Adriana Agnese Amaro, Francesco Boccardo, Cecilia Balbi, Paola Barboro
BACKGROUND: Prostate cancer (PCa), the second most common cancer affecting men worldwide, shows a broad spectrum of biological and clinical behaviour representing the epiphenomenon of an extreme heterogeneity. Androgen deprivation therapy is the mainstay of treatment for advanced forms but after few years the majority of patients progress to castration-resistant prostate cancer (CRPC), a lethal form that poses considerable therapeutic challenges. METHODS: Western blotting, immunocytochemistry, invasion and reporter assays, and in vivo studies were performed to characterize androgen resistant sublines phenotype in comparison to the parental cell line LNCaP...
December 8, 2017: Cell Communication and Signaling: CCS
https://www.readbyqxmd.com/read/29216803/neutrophil-mediated-delivery-of-nanotherapeutics-across-blood-vessel-barrier
#16
Xinyue Dong, Dafeng Chu, Zhenjia Wang
Nanotherapeutics, nanoparticles (NPs) loaded with drugs, show the ability of tissue targeting, long circulation and low toxicity compared with free drugs. Endothelium lying the lumen of a blood vessel is a barrier to restrain tissue deposition of nanotherapeutics. Neutrophils, a type of white blood cells, migrate across endothelium during inflammation. There is an emerging concept that in situ targeting of neutrophils allows delivery of nanotherapeutics into deep tissues at disease sites. Here we summarize the recent advances in delivery of nanotherapeutics to inflammatory tissues or tumor microenvironments via neutrophil infiltration...
January 2018: Therapeutic Delivery
https://www.readbyqxmd.com/read/29216759/pharmaceutical-potential-of-quantum-dots
#17
Swati Jha, Prateek Mathur, Suman Ramteke, Narendra Kumar Jain
Quantum dots (QDs) or fluorescent nanocrystals are designed nanoparticles that are promising for several biological and bio-medical applications as well as drug delivery and simultaneous cellular imaging. QD's have exhibited promising potential primarily in receptor based targeting as a result of their distinctive physicochemical properties. Functionalized QDs (f-QDs) have been developed as effective, safe, nano-sized smart systems to deliver a wide range of bio-actives. Surface modified fluorescent carbon QDs with surface modification have attracted attention as targeting ligand to accomplish cellular targeting with enhanced specificity...
December 7, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/29216714/fabrication-of-hyperbranched-block-statistical-copolymer-based-prodrug-with-dual-sensitivities-for-controlled-release
#18
Luping Zheng, Yunfei Wang, Xianshuo Zhang, Liwei Ma, Baoyan Wang, Xiangling Ji, Hua Wei
Dendrimer with hyperbranched structure and multivalent surface is regarded as one of the most promising candidates close to the ideal drug delivery systems, but the clinical translation and scale-up production of dendrimer has been hampered significantly by the synthetic difficulties. Therefore there is considerable scope for the development of novel hyperbranched polymer that can not only address the drawbacks of dendrimer but maintain its advantages. The reversible addition-fragmentation chain transfer self-condensing vinyl polymerization (RAFT-SCVP) technique has enabled facile preparation of segmented hyperbranched polymer (SHP) by using chain transfer monomer (CTM)-based double-head agent during the past decade...
December 7, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29216713/poly-2-oxazoline-pterostilbene-block-copolymer-nanoparticles-for-dual-anticancer-drug-delivery
#19
Matteo Romio, Giulia Morgese, Lucca Trachsel, Samuel Babity, Cristina Paradisi, Davide Brambilla, Edmondo Maria Benetti
Functional block-copolymers based on poly(2-oxazoline)s are versatile building blocks for the fabrication of dual-drug delivery nanoparticles (NPs) that show promising properties for the development of a anticancer chemotherapy. Core-shell NPs are fabricated from diblock-copolymers featuring a long and hydrophilic poly(2-methyl-2-oxazoline) (PMOXA) block, coupled to a relatively short and functionalizable poly(2-methylsuccinate-2-oxazoline) (PMestOXA) segment. The PMOXA block stabilizes the NP dispersions, whereas the PMestOXA segment is used to conjugate pterostilbene (PTS), a natural bioactive phenolic compound that is used as lipophilic model-drug and constitutes the hydrophobic core of the designed NPs...
December 7, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/29216682/simultaneous-determination-and-validation-of-emtricitabine-rilpivirine-and-tenofovir-from-biological-samples-using-lc-and-ce-methods
#20
Mehmet Gumustas, Mehmet Gokhan Caglayan, Feyyaz Onur, Sibel A Ozkan
A combination of antiretroviral agents is frequently used in effective treatment of the Human Immunodeficiency Virus infection. In this study, two different separation methods are presented for the simultaneous determination of emtricitabine, rilpivirine, and tenofovir from raw materials and urine samples. Developed liquid chromatography and capillary electrophoresis methods were thoroughly optimized for high analytical performances. Optimization of multiple variables at the same time by performing a minimum number of experiments was achieved by the Box-Behnken design, which is an experimental design in Response Surface Methodology, in capillary electrophoresis...
December 7, 2017: Biomedical Chromatography: BMC
keyword
keyword
27693
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"