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https://www.readbyqxmd.com/read/29332593/facile-synthesis-crystal-structure-dft-calculation-and-biological-activities-of-4-2-fluorophenyl-3-3-methoxybenzyl-1h-1-2-4-triazol-5-4h-one-5
#1
Muhammad Saleem, Muhammad Rafiq, Yeon Ki Jeong, Dae Won Cho, Chong-Hyeak Kim, Sung-Yum Seo, Chang-Shik Choi, Seong-Karp Hong, Ki-Hwan Lee
BACKGROUND: In the past few decades, the design, synthesis and characterization of novel heterocyclic compounds with auspicious biological profile received the considerable attention of scientific community. Among them, the small and simple organic molecular backbone like triazole moiety have broad spectrum of applications in the medicinal as well as diagnostic areas. OBJECTIVE: The objective of present study was the synthesis, characterization and exploration of biological profile of 4-(2-fluorophenyl)-3-(3-methoxybenzyl)-1H-1,2,4-triazol-5(4H)-one (5)...
January 12, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29332579/alzheimer-s-disease-a-systemic-review-of-substantial-therapeutic-targets-and-the-leading-multi-functional-molecules
#2
Tarana Umar, Nasimul Hoda
Alzheimer's disease (AD) is a fatal neurodegenerative disorder, having a complex aetiology with numerous possible drug targets. There are targets that have been known for years while more new targets and theories have also emerged. Beta amyloid and cholinesterases are the most significant biological targets for finding curative treatment of AD. The major class of drugs used for AD till now has been the Cholinesterase (ChE) inhibitors. Other prevailing models of molecular pathogenesis in AD include neurofibrillary tangles (NFTs) and amyloid deposition, tryptophan degradation pathway, kinase and phosphatase activity imbalance and neuroinflammation...
January 12, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29332402/monitoring-antimicrobial-mechanisms-of-surface-immobilized-peptides-in-situ
#3
Minyu Xiao, Joshua Jasensky, Leanna L Foster, Kenichi Kuroda, Zhan Chen
Antimicrobial peptides (AMPs) free in solution can kill bacteria by disrupting bacterial cell membranes. Their modes of action have been extensively studied and various models ranging from Pore formation to Carpet-like mechanism were proposed. Surface immobilized AMPs have been used as coatings to kill bacteria and as sensors to capture bacteria, but the interaction mechanisms of surface immobilized AMPs and bacteria are not fully understood. In this research, an analytical platform, SFG-microscope, which is composed of a sum frequency generation (SFG) vibrational spectrometer and a fluorescence microscope, was used to probe molecular interactions between surface immobilized AMPs and bacteria in situ in real time at the solid/liquid interface...
January 15, 2018: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/29332383/developing-pantetheinase-resistant-pantothenamide-antibacterials-structural-modification-impacts-on-pank-interaction-and-mode-of-action
#4
Leanne Barnard, Konrad Johannes Mostert, Willem A L van Otterlo, Erick Strauss
Pantothenamides (PanAms) are analogues of pantothenate, the biosynthetic precursor of coenzyme A (CoA), and show potent antimicrobial activity against several bacteria and the malaria parasite in vitro. However, pantetheinase enzymes that normally degrade pantetheine in human serum also act on the PanAms, thereby reducing their potency. In this study, we designed analogues of the known antibacterial PanAm N-heptylpantothenamide (N7-Pan) to be resistant to pantetheinase by using three complementary structural modification strategies...
January 14, 2018: ACS Infectious Diseases
https://www.readbyqxmd.com/read/29330859/differential-effects-of-phototherapy-adalimumab-and-betamethasone-calcipotriol-on-effector-and-regulatory-t-cells-in-psoriasis
#5
I S Kotb, B J Lewis, R N Barker, A D Ormerod
BACKGROUND: Psoriasis is a chronic T cell-mediated skin disease with marked social and economic burdens. Current treatments are unsatisfactory, with unpredictable remission times and incompletely understood modes of action. Recent advances in our understanding of the pathogenesis of psoriasis identify the imbalance between CD4+ T effector cells, particularly the T helper (Th) 17 subset, and regulatory T cells (Treg) as key to the development of psoriatic lesions, and therefore a novel therapeutic target...
January 12, 2018: British Journal of Dermatology
https://www.readbyqxmd.com/read/29330776/second-hand-exposure-of-staff-administering-vaporised-cannabinoid-products-to-patients-in-a-hospital-setting
#6
Nadia Solowij, Peter Galettis, Samantha J Broyd, Peter de Krey, Jennifer H Martin
BACKGROUND: In many health settings, administration of medicinal cannabis poses significant implementation barriers including drug storage and safety for administering staff and surrounding patients. Different modes of administration also provide different yet potentially significant issues. One route that has become of clinical interest owing to the rapid onset of action and patient control of the inhaled amount (via breath timing and depth) is that of vaporisation of cannabinoid products...
January 12, 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29330449/lithium-chloride-effectively-kills-the-honey-bee-parasite-varroa-destructor-by-a-systemic-mode-of-action
#7
Bettina Ziegelmann, Elisabeth Abele, Stefan Hannus, Michaela Beitzinger, Stefan Berg, Peter Rosenkranz
Honey bees are increasingly important in the pollination of crops and wild plants. Recent reports of the weakening and periodical high losses of managed honey bee colonies have alarmed beekeeper, farmers and scientists. Infestations with the ectoparasitic mite Varroa destructor in combination with its associated viruses have been identified as a crucial driver of these health problems. Although yearly treatments are required to prevent collapses of honey bee colonies, the number of effective acaricides is small and no new active compounds have been registered in the past 25 years...
January 12, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29329451/epidermal-growth-factor-receptor-signaling-disruption-by-endocrine-and-metabolic-disrupting-chemicals
#8
Josiah E Hardesty, Laila Al-Eryani, Banrida Wahlang, K Cameron Falkner, Hongxue Shi, Jian Jin, Brad Vivace, Brian P Ceresa, Russell A Prough, Matthew C Cave
Background: The purpose of this study is to identify an environmentally relevant shared receptor target for endocrine and metabolism disrupting chemical pollutants. A feature of the tested chemicals was that they induced Cyp2b10 in vivo implicating activation of the constitutive androstane receptor (CAR). Recent studies suggest that these compounds could be indirect CAR activators via epidermal growth factor receptor (EGFR) inhibition. Methods: Assays included a CAR activity reporter assay, EGF endocytosis assay, and EGFR phosphorylation assay...
January 10, 2018: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/29329291/ovule-identity-mediated-by-pre-mrna-processing-in-arabidopsis
#9
Encarnación Rodríguez-Cazorla, Samanta Ortuño-Miquel, Héctor Candela, Lindsay J Bailey-Steinitz, Martin F Yanofsky, Antonio Martínez-Laborda, Juan-José Ripoll, Antonio Vera
Ovules are fundamental for plant reproduction and crop yield as they are the precursors of seeds. Therefore, ovule specification is a critical developmental program. In Arabidopsis thaliana, ovule identity is redundantly conferred by the homeotic D-class genes SHATTERPROOF1 (SHP1), SHP2 and SEEDSTICK (STK), phylogenetically related to the MADS-domain regulatory gene AGAMOUS (AG), essential in floral organ specification. Previous studies have shown that the HUA-PEP activity, comprised of a suite of RNA-binding protein (RBP) encoding genes, regulates AG pre-mRNA processing and thus flower patterning and organ identity...
January 12, 2018: PLoS Genetics
https://www.readbyqxmd.com/read/29329238/long-chain-metabolites-of-vitamin-e-metabolic-activation-as-a-general-concept-for-lipid-soluble-vitamins
#10
REVIEW
Martin Schubert, Stefan Kluge, Lisa Schmölz, Maria Wallert, Francesco Galli, Marc Birringer, Stefan Lorkowski
Vitamins E, A, D and K comprise the class of lipid-soluble vitamins. For vitamins A and D, a metabolic conversion of precursors to active metabolites has already been described. During the metabolism of vitamin E, the long-chain metabolites (LCMs) 13'-hydroxychromanol (13'-OH) and 13'-carboxychromanol (13'-COOH) are formed by oxidative modification of the side-chain. The occurrence of these metabolites in human serum indicates a physiological relevance. Indeed, effects of the LCMs on lipid metabolism, apoptosis, proliferation and inflammatory actions as well as tocopherol and xenobiotic metabolism have been shown...
January 12, 2018: Antioxidants (Basel, Switzerland)
https://www.readbyqxmd.com/read/29328974/novel-approach-for-evaluating-pharmaceuticals-toxicity-using-daphnia-model-analysis-of-the-mode-of-cytochrome-p450-generated-metabolite-action-after-acetaminophen-exposure
#11
Ryeo-Ok Kim, Min-A Jo, Jinhaeng Song, Il-Chan Kim, Seokjoo Yoon, Woo-Keun Kim
Because of its widespread use, the pharmaceutical acetaminophen (APAP) is frequently detected in aquatic environments. APAP can have serious physiological effects, such as reduced reproduction, low growth rates, and abnormal behavior, in aquatic organisms. However, the methods available for evaluation of the aquatic toxicity of APAP are of limited usefulness. The present study aimed to develop reliable and sensitive markers for evaluation of APAP toxicity using Daphnia as a model organism. We focused on N-acetyl-p-benzoquinoneimine (NAPQI) production from APAP via cytochrome P450 metabolism because NAPQI causes APAP toxicity...
December 30, 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/29327915/multispectral-atomic-force-microscopy-infrared-nano-imaging-of-malaria-infected-red-blood-cells
#12
David Perez-Guaita, Kamila Kochan, Mitchell Batty, Christian Doerig, Jose Garcia-Bustos, Shirley Josefina Espinoza Herrera, Don McNaughton, Philip Heraud, Bayden R Wood
Atomic Force Microscopy-Infrared (AFM-IR) spectroscopy is a powerful new technique that can be applied to study molecular composition of cells and tissues at the nano-scale. AFM-IR maps are acquired using single wavenumber value: they show either the absorbance plotted against a single wavenumber value, or a ratio of two absorbance values. Here we implement multivariate image analysis to generate multivariate AFM-IR maps, and use this approach to resolve subcellular structural information in red blood cells infected with Plasmodium falciparum at different stages of development...
January 12, 2018: Analytical Chemistry
https://www.readbyqxmd.com/read/29326493/renal-mitochondria-can-withstand-hypoxic-ischemic-injury-secondary-to-renal-failure-in-uremic-rats-pretreated-with-sodium-thiosulfate
#13
Dhivya Mohan, Eswari Dhivya Balasubramanian, Sriram Ravindran, Gino A Kurian
BACKGROUND: Sodium thiosulfate (STS) is a potent drug used to treat calcific uremic arteriopathy in dialysis patients and its mode of action is envisaged by calcium chelation and antioxidant potential. STS's action on mitochondrial dysfunction, one of the major players in the pathology of vascular calcification is yet to be explored. METHODS: Adenine (0.75%, 28 days)-treated vascular calcified rat kidney was used to isolate mitochondria, where the animal was administered with or without STS for 28 days...
July 2017: Indian Journal of Pharmacology
https://www.readbyqxmd.com/read/29325885/9-aminoacridine-based-agents-impair-the-bovine-viral-diarrhea-virus-bvdv-replication-targeting-the-rna-dependent-rna-polymerase-rdrp
#14
Roberta Loddo, Valeria Francesconi, Erik Laurini, Silvia Boccardo, Suzana Aulic, Maurizio Fermeglia, Sabrina Pricl, Michele Tonelli
Bovine viral diarrhea virus (BVDV) infection is still a plague that causes important livestock pandemics. Despite the availability of vaccines against BVDV, and the implementation of massive eradication or control programs, this virus still constitutes a serious agronomic burden. Therefore, the alternative approach to combat Pestivirus infections, based on the development of antiviral agents that specifically inhibit the replication of these viruses, is of preeminent actuality and importance. Capitalizing from a long-standing experience in antiviral drug design and development, in this work we present and characterize a series of small molecules based on the 9-aminoacridine scaffold that exhibit potent anti-BVDV activity coupled with low cytotoxicity...
January 4, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29325777/data-driven-model-reference-control-of-mimo-vertical-tank-systems-with-model-free-vrft-and-q-learning
#15
Mircea-Bogdan Radac, Radu-Emil Precup, Raul-Cristian Roman
This paper proposes a combined Virtual Reference Feedback Tuning-Q-learning model-free control approach, which tunes nonlinear static state feedback controllers to achieve output model reference tracking in an optimal control framework. The novel iterative Batch Fitted Q-learning strategy uses two neural networks to represent the value function (critic) and the controller (actor), and it is referred to as a mixed Virtual Reference Feedback Tuning-Batch Fitted Q-learning approach. Learning convergence of the Q-learning schemes generally depends, among other settings, on the efficient exploration of the state-action space...
January 8, 2018: ISA Transactions
https://www.readbyqxmd.com/read/29325769/the-structural-determinants-of-the-bitopic-binding-mode-of-a-negative-allosteric-modulator-of-the-dopamine-d2-receptor
#16
Christopher J Draper-Joyce, Mayako Michino, Ravi Kumar Verma, Carmen Klein Herenbrink, Jeremy Shonberg, Anitha Kopinathan, Peter J Scammells, Ben Capuano, David M Thal, Jonathan A Javitch, Arthur Christopoulos, Lei Shi, J Robert Lane
SB269652 is a negative allosteric modulator of the dopamine D2 receptor (D2R) yet possesses structural similarity to ligands with a competitive mode of interaction. In this study, we aimed to understand the ligand-receptor interactions that confer its allosteric action. We combined site-directed mutagenesis with molecular dynamics simulations using both SB269652 and derivatives from our previous structure activity studies. We identify residues within the conserved orthosteric binding site (OBS) and a secondary binding pocket (SBP) that determine affinity and cooperativity...
January 8, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29325211/uptake-and-intracellular-fate-of-engineered-nanoparticles-in-mammalian-cells-capabilities-and-limitations-of-transmission-electron-microscopy-polymer-based-nanoparticles
#17
REVIEW
Martin Reifarth, Stephanie Hoeppener, Ulrich S Schubert
In order to elucidate mechanisms of nanoparticle (NP)-cell interactions, a detailed knowledge about membrane-particle interactions, intracellular distributions, and nucleus penetration capabilities, etc. becomes indispensable. The utilization of NPs as additives in many consumer products, as well as the increasing interest of tailor-made nanoobjects as novel therapeutic and diagnostic platforms, makes it essential to gain deeper insights about their biological effects. Transmission electron microscopy (TEM) represents an outstanding method to study the uptake and intracellular fate of NPs, since this technique provides a resolution far better than the particle size...
January 11, 2018: Advanced Materials
https://www.readbyqxmd.com/read/29324336/new-1-5-and-2-5-disubstituted-tetrazoles-dependent-activity-towards-surface-barrier-of-candida-albicans
#18
Monika Staniszewska, Małgorzata Gizińska, Ewa Mikulak, Klaudia Adamus, Mirosława Koronkiewicz, Edyta Łukowska-Chojnacka
A series of novel tetrazole derivatives was synthetized using N-alkylation or Michael-type addition reactions, and screened for their fungistatic potential against Candida albicans (the lack of endpoint = 100%). Among them, the selected compounds 2d, 4b, and 6a differing in substituents at the tetrazole ring were non-toxic to Galleria mellonella larvae in vivo and exerted slight toxicity against Caco-2 in vitro (CC50 at 256 μg/mL). An antagonistic effect of tetrazole derivatives 2d, 4b, and 6a respectively in combination with Fluconazole was shown using the checker board and colorimetric methods (fractional inhibitory concentration indexes FICIs >1)...
December 30, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29324251/potential-role-of-plasmodium-falciparum-exported-protein-1-in-the-chloroquine-mode-of-action
#19
Andreas Martin Lisewski, Joel Patrick Quiros, Monica Mittal, Nagireddy Putluri, Arun Sreekumar, Jesper Z Haeggström, Olivier Lichtarge
In the human malaria parasite Plasmodium falciparum, membrane glutathione S-transferases (GST) have recently emerged as potential cellular detoxifying units and as drug target candidates with the artemisinin (ART) class of antimalarials inhibiting their activity at single-digit nanomolar potency when activated by iron sources such as cytotoxic hematin. Here we put forward the hypothesis that the membrane GST Plasmodium falciparum exported protein 1 (PfEXP1, PF3D7_1121600) might be directly involved in the mode of action of the unrelated antimalarial 4-aminoquinoline drug chloroquine (CQ)...
December 27, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29324050/the-roles-of-adjuvant-supplements-in-colorectal-cancer-patients-on-chemotherapy-reaping-benefits-from-metabolic-crosstalk
#20
Babak Golkhalkhali, Audra Shaleena Paliany, Kin Fah Chin, Retnagowri Rajandram
The prevalence of colorectal cancer (CRC) is on a steady rise over the years, with the World Health Organization (WHO) reporting CRC as the fourth leading cause of cancer-related death worldwide. While treatment modalities may differ in accordance to the staging and severity of the disease itself, chemotherapy is almost unavoidable in most cases. Though effective in its mode of action, chemotherapy is commonly associated with undesirable side effects that negatively affects the patient in terms of quality of life, and in some cases may actually interfere with their treatment regimens, thus escalating to poor prognosis...
January 11, 2018: Nutrition and Cancer
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