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https://www.readbyqxmd.com/read/29454290/ligand-based-computer-aided-drug-design-reveals-new-tropomycin-receptor-kinase-a-trka-inhibitors
#1
Rand Shahin, Iman Mansi, Lubna Swellmeen, Tahani Alwidyan, Nabil Al-Hashimi, Yaser Al-Qarar'h, Omar Shaheen
Targeting tropomycin kinase A (TrkA) by small molecule inhibitors is considered as a promising strategy for treating several human cancers. To achieve this goal, a ligand based QSAR model was applied using the Discovery studio 4.5 (DS 4.5). Hence, a total list of 161 TrkA inhibitors was investigated. The TrkA inhibitors were extensively explored to detect their optimal physicochemical properties and pharmacophoric binding modes, which were converted into numeric descriptors and allowed to compete within the context of the Genetic Function Algorithm (GFA) approximations to find the subset of terms that correlates best with the activity...
January 13, 2018: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/29454159/an-aligned-porous-electrospun-fibrous-membrane-with-controlled-drug-delivery-an-efficient-strategy-to-accelerate-diabetic-wound-healing-with-improved-angiogenesis
#2
Xiaozhi Ren, Yiming Han, Jie Wang, Yuqi Jiang, Zhengfang Yi, He Xu, Qinfei Ke
A chronic wound in diabetic patients is usually characterized by poor angiogenesis and delayed wound closure. The exploration of efficient strategy to significantly improve angiogenesis in the diabetic wound bed and thereby accelerate wound healing is still a significant challenge. Herein, we reported a kind of aligned porous poly (L-lactic acid) (PLLA) electrospun fibrous membranes containing dimethyloxalylglycine (DMOG)-loaded mesoporous silica nanoparticles (DS) for diabetic wound healing. The PLLA electrospun fibers aligned in a single direction and there were ellipse-shaped nano-pores in situ generated onto the surface of fibers, while the DS were well distributed in the fibers and the DMOG as well as Si ion could be controlled released from the nanopores on the fibers...
February 14, 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29454157/nanofibrous-plga-electrospun-scaffolds-modified-with-type-i-collagen-influence-hepatocyte-function-and-support-viability-in-vitro
#3
Jessica H Brown, Prativa Das, Michael D DiVito, David Ivancic, Lay Poh Tan, Jason A Wertheim
A major challenge of maintaining primary hepatocytes in vitro is progressive loss of hepatocyte-specific functions, such as protein synthesis and cytochrome P450 (CYP450) catalytic activity. We developed a three-dimensional (3D) nanofibrous scaffold made from poly(L-lactide-co-glycolide) (PLGA) polymer using a newlyoptimizedwet electrospinning techniquethat resulted in a highly porous structure that accommodated inclusion of primary human hepatocytes. Extracellular matrix (ECM) proteins (type I collagen or fibronectin) at varying concentrations were chemically linked to electrospun PLGA using amine coupling to develop an in vitro culture system containing the minimal essential ECM components of the liver micro-environment that preserve hepatocyte function in vitro...
February 14, 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29453908/effective-anti-adhesives-of-uropathogenic-escherichia-coli
#4
Rosana Ribić, Tomislav Meštrović, Marijana Neuberg, Goran Kozina
Urinary tract infections (UTIs) caused by uropathogenic Escherichia coli (UPEC) are among the most common infectious diseases in humans. Due to their frequent occurrence in the community and nosocomial settings, as well as the development of resistance to the commonly prescribed antimicrobial agents, an enormous financial burden is placed on healthcare systems around the world. Therefore, novel approaches to the prevention and treatment of UTIs are needed. Although UPEC may harbour a plethora of virulence factors, type I fimbriae and P pili are two of the most studied adhesive organelles, since the attachment to host cells in the urinary tract is a crucial step towards infection...
March 1, 2018: Acta Pharmaceutica
https://www.readbyqxmd.com/read/29453806/cq-sensitizes-human-pancreatic-cancer-cells-to-gemcitabine-through-the-lysosomal-apoptotic-pathway-via-reactive-oxygen-species
#5
Zhiping Fu, Cheng Xi, Jie Kuang, Haoran Feng, Lingxie Chen, Juyong Liang, Xiaonan Shen, Stanley Yuen, Peng Chenghong, Shen Baiyong, Jin Zhijian, Weihua Qiu
As an established anti-cancer drug, gemcitabine (GEM) is an effective systemic treatment for advanced pancreatic cancer (PC). However, little is known about the potential effectors that may modify tumour cell sensitivity towards GEM. Autophagy, as a physiological cellular mechanism, is involved in both cell survival and cell death. In this study, we found that exposure to GEM induced a significant increase in autophagy in a dose-dependent manner in PANC-1 and BxPC-3 cells. Inhibition of autophagy by chloroquine (CQ) and ATG7 siRNA increased GEM-induced cytotoxicity, and CQ was more effective than ATG7 siRNA...
February 17, 2018: Molecular Oncology
https://www.readbyqxmd.com/read/29453754/pacap38-in-human-models-of-primary-headaches
#6
Håkan Ashina, Song Guo, Anne L H Vollesen, Messoud Ashina
BACKGROUND: To review the role of PACAP38 in human models of primary headaches, discuss possible mechanisms of PACAP38-induced migraine, and outline future directions. DISCUSSION: Experimental studies have established PACAP38 as a potent pharmacological "trigger" molecule of migraine-like attacks. These studies have also revealed a heterogeneous PACAP38 migraine response in migraine without aura patients. In addition, findings from brain imaging studies have demonstrated neuronal and vascular changes in migraine patients both ictally and interictally after PACAP38 infusion...
November 23, 2017: Journal of Headache and Pain
https://www.readbyqxmd.com/read/29453670/incidence-and-drug-resistance-of-zoonotic-mycobacterium-bovis-infection-in-peshawar-pakistan
#7
Irfan Khattak, Muhammad Hassan Mushtaq, Sultan Ayaz, Sajid Ali, Anwar Sheed, Javed Muhammad, Muhammad Luqman Sohail, Haq Amanullah, Irshad Ahmad, Sadeeq Ur Rahman
Prevalence of zoonotic Mycobacterium bovis (bTB) disease in human population is underreported from the North of Pakistan. Here, we report on the proportion of human bTB disease among the overall TB patients, drug resistance pattern of bTB isolates, and knowledge, attitude, and practices (KAP)-based analysis of bTB disease. For this purpose, sputum samples from a total of 300 clinically diagnosed TB patients and 100 randomly selected school children suspected of pulmonary TB were processed by culture as well as polymerase chain reaction (PCR) for isolation, identification, and confirmation of Mycobacterium tuberculosis (mTB) and bTB species...
February 17, 2018: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/29453628/safety-tolerability-and-preliminary-activity-of-imgn529-a-cd37-targeted-antibody-drug-conjugate-in-patients-with-relapsed-or-refractory-b-cell-non-hodgkin-lymphoma-a-dose-escalation-phase-i-study
#8
Anastasios Stathis, Ian W Flinn, Sumit Madan, Kami Maddocks, Arnold Freedman, Steven Weitman, Emanuele Zucca, Mihaela C Munteanu, M Lia Palomba
Background CD37 is expressed on B-cell lymphoid malignancies, thus making it an attractive candidate for targeted therapy in non-Hodgkin lymphoma (NHL). IMGN529 is an antibody-drug conjugate comprising a CD37-binding antibody linked to the maytansinoid DM1, a potent anti-mitotic agent. Methods This first-in-human, phase 1 trial recruited adult patients with relapsed or refractory B-cell NHL. The primary objective was to determine the maximum tolerated dose (MTD) and recommended phase 2 dose. Secondary objectives were to evaluate safety, pharmacokinetics, and preliminary clinical activity...
February 17, 2018: Investigational New Drugs
https://www.readbyqxmd.com/read/29453607/semaphorin-7a-in-circulating-regulatory-t-cells-is-increased-in-autosomal-dominant-polycystic-kidney-disease-and-decreases-with-tolvaptan-treatment
#9
Yashang Lee, Katrina Lehmann Blount, Feng Dai, Siobhan Thompson, Jonathan Kaufman Scher, Sherrie Bitterman, Madeline Droher, Erica L Herzog, Gilbert Moeckel, Anil Karihaloo, Neera K Dahl
BACKGROUND: Semaphorin 7A (SEMA7A) is an immunomodulating protein implicated in lung and liver fibrosis. In autosomal-dominant polycystic kidney disease (ADPKD), the progressive expansion of renal cysts, inflammation, and subsequent renal fibrosis leads to end-stage renal disease (ESRD). SEMA7A may play a role in renal fibrosis and in ADPKD. METHODS: We evaluated Sema7a in a mouse model of renal fibrosis and determined the expression of SEMA7A in human ADPKD kidney...
February 16, 2018: Clinical and Experimental Nephrology
https://www.readbyqxmd.com/read/29453600/argininosuccinate-synthetase-1-ass1-loss-in-high-grade-neuroendocrine-carcinomas-of-the-urinary-bladder-implications-for-targeted-therapy-with-adi-peg-20
#10
Sounak Gupta, Divya Sahu, John S Bomalaski, Igor Frank, Stephen A Boorjian, Prabin Thapa, John C Cheville, Donna E Hansel
High-grade neuroendocrine carcinomas (HGNECs) of the urinary bladder encompass small cell (SCNEC) and large cell neuroendocrine carcinomas (LCNEC). Currently, recommended initial management is with systemic chemotherapy, followed by consolidative therapy with either radical cystectomy or radiotherapy in patients with localized disease. Nevertheless, survival in this setting remains poor. We therefore evaluated the potential to modify arginine metabolism as an alternative, targeted therapy approach in these carcinomas...
February 16, 2018: Endocrine Pathology
https://www.readbyqxmd.com/read/29453596/effectiveness-of-the-sesquiterpene-%C3%AE-bisabolol-in-dogs-with-naturally-acquired-canine-leishmaniosis-an-exploratory-clinical-trial
#11
V Corpas-López, G Merino-Espinosa, C Acedo-Sánchez, V Díaz-Sáez, M C Navarro-Moll, F Morillas-Márquez, J Martín-Sánchez
The use of natural products is a promising approach for treating visceral leishmaniosis. (-)-α-Bisabolol is a sesquiterpene that have been proved active in vivo on Leishmania infantum-infected mice without showing toxicity. A single-centre, parallel-group, randomized, exploratory study was designed to assess its efficacy in a canine leishmaniosis model involving naturally infected dogs. In this clinical trial, 12 dogs were allocated into two groups and were treated with either meglumine antimoniate (100 mg/kg) through subcutaneous route or (-)-α-bisabolol (30 mg/kg) through oral route for two treatment series of 30 days, separated by a 30-day interval...
February 16, 2018: Veterinary Research Communications
https://www.readbyqxmd.com/read/29453543/toxic-and-beneficial-potential-of-silver-nanoparticles-the-two-sides-of-the-same-coin
#12
Lilian Rodrigues Rosa Souza, Veronica Santana da Silva, Leonardo Pereira Franchi, Tiago Alves Jorge de Souza
Nanotechnology has allowed great changes in chemical, biological and physical properties of metals when compared to their bulk counterparts. Within this context, silver nanoparticles (AgNPs) play a major role due to their unique properties, being widely used in daily products such as fabrics, washing machines, water filters, food and medicine. However, AgNPs can enter cells inducing a "Trojan-horse" type mechanism which potentially leads to cellular autophagy, apoptosis or necrosis. On the other hand, this cytotoxicity mechanism can be optimized to develop drug nanocarriers and anticancer therapies...
2018: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/29453540/cellular-and-molecular-toxicity-of-iron-oxide-nanoparticles
#13
Blanca Laffon, Natalia Fernández-Bertólez, Carla Costa, Fátima Brandão, João Paulo Teixeira, Eduardo Pásaro, Vanessa Valdiglesias
Iron oxide nanoparticles (ION) have attracted much attention because of their particular physico-chemical properties, including superparamagnetism. These features make them suitable for many purposes and several interesting biomedical applications, such as to increase contrast in magnetic resonance imaging (MRI), as drug delivery systems and as hyperthermia agents. However, they have also shown to be easily accumulated in diverse tissues and induce toxicity at different levels. This chapter reviews the different cellular and molecular effects induced by ION reported from in vitro studies with human and non-human cell lines...
2018: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/29453250/retinal-chitosan-conjugates-effectively-deliver-active-chromophores-to-retinal-photoreceptor-cells-in-blind-mice-and-dogs
#14
Songqi Gao, Shirin Kahremany, Jianye Zhang, Beata Jastrzebska, Janice Querubin, Simon M Petersen-Jones, Krzysztof Palczewski
The retinoid (visual) cycle consists of a series of biochemical reactions needed to regenerate the visual chromophore, 11-cis-retinal and sustain vision. Genetic or environmental factors affecting chromophore production can lead to blindness. Using animal models that mimic human retinal diseases, we previously demonstrated that mechanism-based pharmacological interventions can maintain vision in otherwise incurable genetic diseases of the retina. Here, we report that after 9-cis-retinal administration to lecithin:retinol acyltransferase-deficient (Lrat-/-) mice, the drug was rapidly absorbed and then cleared within 1-2 h...
February 16, 2018: Molecular Pharmacology
https://www.readbyqxmd.com/read/29453199/simultaneous-assessment-of-clearance-metabolism-induction-and-drug-drug-interaction-potential-using-a-long-term-in-vitro-liver-model-for-a-novel-hepatitis-b-virus-inhibitor
#15
Nicole A Kratochwil, Miriam Triyatni, Martina B Mueller, Florian Klammers, Brian Leonard, Dan Turley, Josephine Schmaler, Aynur Ekiciler, Birgit Molitor, Isabelle Walter, Pierre-Alexis Gonsard, Charles A Tournillac, Alexandre Durrwell, Michaela Marschmann, Russell Jones, Mohammed Ullah, Franziska Boess, Giorgio Ottaviani, Yuyan Yin, Neil J Parrott, Stephen Fowler
Long-term in vitro liver models are now widely explored for human hepatic metabolic clearance prediction, enzyme phenotyping, cross species metabolism, comparison of low clearance drugs as well as induction studies. Here, we present studies using a long-term liver model which show how metabolism and active transport, drug-drug interactions and enzyme induction in healthy and diseased states, e.g. hepatitis B virus (HBV) infection, may be assessed in a single test system to enable effective data integration for PBPK modeling...
February 16, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29453043/understanding-of-human-atp-binding-cassette-superfamily-and-novel-multidrug-resistance-modulators-to-overcome-mdr
#16
REVIEW
Imran Shair Mohammad, Wei He, Lifang Yin
Indeed, multi-drug resistance (MDR) is a significant obstacle to effective chemotherapy. The overexpression of ATP-binding cassette (ABC) membrane transporters is a principal cause of enhanced cytotoxic drug efflux and treatment failure in various types of cancers. At cellular level, the pumps of ABC family regulate the transportation of numerous substances including drugs in and out of the cells. In past, the overexpression of ABC pumps suggested a well-known mechanism of drug resistance in cancers as well as infectious diseases...
February 13, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29452809/test-of-neural-inertia-in-humans-during-general-anaesthesia
#17
M H Kuizenga, P J Colin, K M E M Reyntjens, D J Touw, H Nalbat, F H Knotnerus, H E M Vereecke, M M R F Struys
BACKGROUND: Neural inertia is defined as the tendency of the central nervous system to resist transitions between arousal states. This phenomenon has been observed in mice and Drosophila anaesthetized with volatile anaesthetics: the effect-site concentration required to induce anaesthesia in 50% of the population (C 50 ) was significantly higher than the effect-site concentration for 50% of the population to recover from anaesthesia. We evaluated this phenomenon in humans using propofol or sevoflurane (both with or without remifentanil) as anaesthetic agents...
March 2018: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/29452108/effect-of-brimonidine-an-%C3%AE-2-adrenergic-agonist-on-human-meibomian-gland-epithelial-cells
#18
Xi Han, Yang Liu, Wendy R Kam, David A Sullivan
We recently discovered that the anti-glaucoma pharmaceuticals timolol, a β adrenergic antagonist, and pilocarpine, a cholinergic compound, negatively influence the morphology, proliferative capacity and survival of human meibomian gland epithelial cells (HMGECs). We hypothesize that another class of anti-glaucoma drugs, the α2 adrenergic agonists, also acts directly on HMGECs to affect their structure and function. We tested this hypothesis. Immortalized (i) HMGECs were cultured with brimonidine, as well as clonidine (α2 agonist), phenylephrine (α1 agonist), RX821002 (inverse α2 agonist) and MK912 (neutral α2 agonist) for up to 7 days...
February 13, 2018: Experimental Eye Research
https://www.readbyqxmd.com/read/29452095/the-role-of-free-fatty-acid-receptor-4-ffa4-in-human-cancers-and-cancer-cell-lines
#19
REVIEW
Ilya S Senatorov, Nader H Moniri
A dietary influence on cancer progression has been evident for many decades, and dietary fatty acids, particularly long chain mono- and polyunsaturated fatty acids, have been shown to play significant roles in influencing growth of a variety of human cancers. The discovery of the family of cell-surface free-fatty acid receptors, which include the long-chain fatty acid receptors FFA1 and FFA4, suggest that many of the effects of dietary fats could be receptor-mediated. FFA4 is ubiquitously expressed and has recently been shown to modulate a variety of important anti-inflammatory and metabolic processes...
February 13, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29451997/poly-lactic-co-glycolic-acid-as-a-slow-release-drug-carrying-matrix-for-methotrexate-coated-onto-intraocular-lenses-to-conquer-posterior-capsule-opacification
#20
Stefan A Kassumeh, Christian M Wertheimer, Annabel von Studnitz, Anna Hillenmayer, Claudia Priglinger, Armin Wolf, Wolfgang J Mayer, Daniel Teupser, Lesca M Holdt, Siegfried G Priglinger, Kirsten H Eibl-Lindner
PURPOSE: Posterior capsule opacification (PCO) still represents the main long-term complication of cataract surgery. Research into pharmacologic PCO prophylaxis is extensive. One promising candidate drug is methotrexate (MTX). Our aim is to determine the in vitro feasibility of MTX-loaded poly(lactic-co-glycolic) (PLGA) biomatrices sprayed on intraocular lenses (IOLs) as a drug-delivery implant. METHODS: Hydrophilic and hydrophobic acrylic IOLs were spray-coated with MTX-loaded PLGA...
February 16, 2018: Current Eye Research
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