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https://www.readbyqxmd.com/read/29668110/phenylbutyl-isoselenocyanate-induces-reactive-oxygen-species-to-inhibit-androgen-receptor-and-to-initiate-p53-mediated-apoptosis-in-lncap-prostate-cancer-cells
#1
Wei Wu, Deepkamal Karelia, Kartick Pramanik, Shantu G Amin, Arun K Sharma, Cheng Jiang, Junxuan Lu
Previous studies have established the in vivo bioavailability and efficacious dosages of phenylbutyl isoselenocyanate (ISC-4), a selenium-substituted isothiocyanate, against mouse xenograft models of human melanoma and colorectal cancer. To explore its potential attributes against prostate cancer, we treated human LNCaP prostate cancer cells with ISC-4 and examined their apoptosis responses, and interrogated the signaling mechanisms through pharmacological and siRNA knockdown approaches. Our results show that ISC-4 was more potent at inducing apoptosis than its sulfur analog phenylbutyl isothiocyanate (PBITC) without suppressing protein kinase AKT Ser473 phosphorylation...
April 18, 2018: Molecular Carcinogenesis
https://www.readbyqxmd.com/read/29668081/lipocalin-type-prostaglandin-d-synthase-is-a-novel-phytocannabinoid-binding-protein
#2
Matthew W Elmes, Anthony D Volpe, Simon d'Oelsnitz, Joseph M Sweeney, Martin Kaczocha
Lipocalin-type prostaglandin D synthase (L-PGDS; EC:5.3.99.2) is an enzyme with dual functional roles as a prostaglandin D2 -synthesizing enzyme and as an extracellular transporter for diverse lipophilic compounds in the cerebrospinal fluid (CSF). Transport of hydrophobic endocannabinoids is mediated by serum albumin in the blood and intracellularly by the fatty acid binding proteins, but no analogous transport mechanism has yet been described in CSF. L-PGDS has been reported to promiscuously bind a wide variety of lipophilic ligands and is among the most abundant proteins found in the CSF...
April 18, 2018: Lipids
https://www.readbyqxmd.com/read/29667555/synthesis-cytotoxicity-and-antioxidant-activity-of-new-analogues-of-rc-121-synthetic-derivatives-of-somatostatin
#3
Diana Wesselinova, Emilia D Naydenova, S Staykova, I G Goshev, L Vezenkov
BACKGROUND: Based on the structure of RC-121 (D-Phe-c (Cys-Tyr-D-Trp-Lys-Val-Cys)-Thr-NH2, - synthetic derivatives of somatostatin), some analogs were synthesized and tested for in vitro cytotoxic and antioxidant activity. OBJECTIVES: The new analogs were modifyed at position 5 with Dap (diaminopropanoic acid), Dab (diaminobutanoic acid) and Orn and at position 6 with the unnatural amino acids Tle (t-leucine). METHODS: The in vitro cytotoxic effects of the substances were investigated against a panel of human tumor cell lines HT-29 (human colorectal cancer cell line), MDA-MB-23 (human breast cancer cell line), Hep G-2 (human hepatocellular carcinoma cell line) and HeLa (cervical cancer cell line)...
April 17, 2018: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29667397/asymmetric-synthesis-of-silanediol-inhibitors-for-the-serine-protease-coagulation-cascade-enzyme-fxia
#4
Hoan Quoc Duong, Scott McN Sieburth
Silanediol peptidomimetics have been prepared, designed to inhibit the serine protease enzyme Factor XIa (FXIa) for treatment of thrombosis without complete interruption of normal hemostasis. These Arg-[Si]-Ala analogs of the FXIa substrate (FIX) are the first silanediol dipeptide analogs to carry a basic guanidine group. Control of stereochemistry was accomplished using catalytic asymmetric hydrosilylation and addition of a silyllithium intermediate to the Davis-Ellman sulfinimine.
April 18, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29667288/a-brief-bedside-visual-art-intervention-decreases-anxiety-and-improves-pain-and-mood-in-patients-with-haematologic-malignancies
#5
J J Saw, E A Curry, S L Ehlers, P D Scanlon, B A Bauer, J Rian, D R Larson, A P Wolanskyj
Treatment of cancer-related symptoms represents a major challenge for physicians. The purpose of this pilot study was to determine whether a brief bedside visual art intervention (BVAI) facilitated by art educators improves mood, reduces pain and anxiety in patients with haematological malignancies. Thirty-one patients (21 women and 10 men) were invited to participate in a BVAI where the goal of the session was to teach art technique for ~30 min. Primary outcome measures included the change in visual analog scale, the State-Trait Anxiety Inventory and the Positive and Negative Affect Schedule scale, from baseline prior to and immediately post-BVAI...
April 17, 2018: European Journal of Cancer Care
https://www.readbyqxmd.com/read/29667255/nonvolatile-memory-materials-for-neuromorphic-intelligent-machines
#6
REVIEW
Doo Seok Jeong, Cheol Seong Hwang
Recent progress in deep learning extends the capability of artificial intelligence to various practical tasks, making the deep neural network (DNN) an extremely versatile hypothesis. While such DNN is virtually built on contemporary data centers of the von Neumann architecture, physical (in part) DNN of non-von Neumann architecture, also known as neuromorphic computing, can remarkably improve learning and inference efficiency. Particularly, resistance-based nonvolatile random access memory (NVRAM) highlights its handy and efficient application to the multiply-accumulate (MAC) operation in an analog manner...
April 18, 2018: Advanced Materials
https://www.readbyqxmd.com/read/29667134/two-phase-i-pharmacokinetic-and-pharmacodynamic-studies-of-dfp-10917-a-novel-nucleoside-analog-with-14-day-and-7-day-continuous-infusion-schedules
#7
Kamalesh Sankhala, Chris H Takimoto, Alain C Mita, Henry Xiong, Jordi Rodón, Amir Mehrvarz Sarshekeh, K Burns, Kenzo Iizuka, Scott Kopetz
Purpose DFP-10917 is a novel deoxycytidine analog with a unique mechanism of action. Brief exposure to high concentrations of DFP-10917 inhibits DNA polymerase resulting in S-phase arrest, while prolonged exposure to DFP-10917 at low concentration causes DNA fragmentation, G2/M-phase arrest, and apoptosis. DFP-10917 demonstrated activity in tumor xenografts resistant to other deoxycytidine analogs. Experimental design Two phase I studies assessed the safety, pharmacokinetic, pharmacodynamic and preliminary efficacy of DFP-10917...
April 18, 2018: Investigational New Drugs
https://www.readbyqxmd.com/read/29666607/exploring-biogeochemistry-and-microbial-diversity-of-extant-microbialites-in-mexico-and-cuba
#8
Patricia M Valdespino-Castillo, Ping Hu, Martín Merino-Ibarra, Luz M López-Gómez, Daniel Cerqueda-García, Roberto González-De Zayas, Teresa Pi-Puig, Julio A Lestayo, Hoi-Ying Holman, Luisa I Falcón
Microbialites are modern analogs of ancient microbial consortia that date as far back as the Archaean Eon. Microbialites have contributed to the geochemical history of our planet through their diverse metabolic capacities that mediate mineral precipitation. These mineral-forming microbial assemblages accumulate major ions, trace elements and biomass from their ambient aquatic environments; their role in the resulting chemical structure of these lithifications needs clarification. We studied the biogeochemistry and microbial structure of microbialites collected from diverse locations in Mexico and in a previously undescribed microbialite in Cuba...
2018: Frontiers in Microbiology
https://www.readbyqxmd.com/read/29666478/two-new-spliceostatin-analogs-from-the-strain-pseudomonas-sp-hs-nf-1408
#9
Yue Zhao, Junwei Zhao, Chang Lu, Hui Zhang, Huan Qi, Shanwen Jiang, Xiaowei Guo, Jidong Wang, Wensheng Xiang
Two new spliceostatin derivatives, designed as spliceostatin H (1) and spliceostatin I (2), and one known compound FR901464 (3), were isolated from the strain Pseudomonas sp. HS-NF-1408. Their structures were determined by the comprehensive spectroscopic data, including 1D, 2D NMR, MS spectral analysis and comparison with data from the literature. Compound 1 exhibited potent cytotoxicity activity against A549 and HepG2 with IC50 values of 3.57 and 16.72 μg/ml, respectively.
April 17, 2018: Journal of Antibiotics
https://www.readbyqxmd.com/read/29666423/generalized-concurrence-in-boson-sampling
#10
Seungbeom Chin, Joonsuk Huh
A fundamental question in linear optical quantum computing is to understand the origin of the quantum supremacy in the physical system. It is found that the multimode linear optical transition amplitudes are calculated through the permanents of transition operator matrices, which is a hard problem for classical simulations (boson sampling problem). We can understand this problem by considering a quantum measure that directly determines the runtime for computing the transition amplitudes. In this paper, we suggest a quantum measure named "Fock state concurrence sum" C S , which is the summation over all the members of "the generalized Fock state concurrence" (a measure analogous to the generalized concurrences of entanglement and coherence)...
April 17, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29666272/human-n-acetylglucosaminyltransferase-ii-substrate-recognition-uses-a-modular-architecture-that-includes-a-convergent-exosite
#11
Renuka Kadirvelraj, Jeong-Yeh Yang, Justin H Sanders, Lin Liu, Annapoorani Ramiah, Pradeep Kumar Prabhakar, Geert-Jan Boons, Zachary A Wood, Kelley W Moremen
Asn-linked oligosaccharides are extensively modified during transit through the secretory pathway, first by trimming of the nascent glycan chains and subsequently by initiating and extending multiple oligosaccharide branches from the trimannosyl glycan core. Trimming and branching pathway steps are highly ordered and hierarchal based on the precise substrate specificities of the individual biosynthetic enzymes. A key committed step in the synthesis of complex-type glycans is catalyzed by N -acetylglucosaminyltransferase II (MGAT2), an enzyme that generates the second GlcNAcβ1,2- branch from the trimannosyl glycan core using UDP-GlcNAc as the sugar donor...
April 16, 2018: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/29666111/decreasing-an-offloading-device-s-size-and-offsetting-its-imposed-limb-length-discrepancy-lead-to-improved-comfort-and-gait
#12
Ryan T Crews, Joseph Candela
OBJECTIVE: Patient adherence is a challenge in offloading diabetic foot ulcers (DFUs) with removable cast walkers (RCWs). The size and weight of an RCW, changes to gait, and imposed limb length discrepancies may all discourage adherence. This study sought to determine whether RCW size and provision of a contralateral limb lift affected users' comfort and gait. RESEARCH DESIGN AND METHODS: Twenty-five individuals at risk for DFUs completed several 20-m walking trials under five footwear conditions: bilateral standardized shoes, a knee-high RCW with shoe with or without an external shoe lift contralaterally, and an ankle-high RCW with shoe with or without an external shoe lift contralaterally...
April 17, 2018: Diabetes Care
https://www.readbyqxmd.com/read/29666030/resection-arthroplasty-compared-with-total-hip-arthroplasty-in-treating-chronic-hip-pain-of-patients-with-a-history-of-substance-abuse
#13
William Curtis, Meir Marmor
BACKGROUND: Retrospective comparison of surgical management of severe hip pain in patients with a history of substance abuse treated by modified Girdlestone resection arthroplasty (RA) vs delayed total hip arthroplasty (THA) following yearlong sobriety pathway. METHODS: Patients were identified using charts, current procedural terminology (CPT) code query, and THA sobriety pathway registry. The primary outcome was adequate pain control following surgery, defined as visual analog scale ≤ 5 or verbal description of "moderate" or lower pain...
March 16, 2018: Journal of Arthroplasty
https://www.readbyqxmd.com/read/29665953/key-molecules-in-the-gaba-signalling-pathway-are-present-in-mouse-and-human-cervical-tissue
#14
Marta Skelin, Danijel Bursać, Viviana Kozina, Tristan Winters, Marija Macan, Marija Ćurlin
Cervical mucus modulates fertility by cyclical changes of its biophysical and functional properties. Based on an analogy with bronchial goblet cells we set out to investigate the possible role of the gamma-aminobutyric acid (GABA) signalling pathway in the mediation of oestrogen-induced mucus secretion from endocervical secretory cells. The aim of the study was to examine the existence of GABAA receptor (GABAAR), glutamic acid decarboxylase 65/67 (GAD65/67) and vesicular GABA transporter (VGAT) in human and mouse cervical tissue...
April 18, 2018: Reproduction, Fertility, and Development
https://www.readbyqxmd.com/read/29665764/unicompartmental-knee-arthroplasty-for-spontaneous-osteonecrosis-of-the-knee-a-meta-analysis
#15
Julio J Jauregui, Christopher L Blum, Neil Sardesai, Craig Bennett, R Frank Henn, Farshad Adib
BACKGROUND: Spontaneous osteonecrosis of the knee (SONK) is a poorly understood but debilitating disease entity. Total knee arthroplasty (TKA) is the standard of care for those patients who fail conservative management, but considering SONK's predilection for affecting a single knee compartment, unicompartmental knee arthroplasty (UKA) appears to be a more tailored option. Unfortunately, conflicting data exist on the utility of UKA in SONK. Thus, the purpose of this study was to evaluate functional outcomes and revision rates of UKA in the setting of SONK...
May 2018: Journal of Orthopaedic Surgery
https://www.readbyqxmd.com/read/29665717/selective-peripheral-nerve-resection-for-treatment-of-persistent-pain-around-the-knee-joint-after-total-knee-arthroplasty
#16
Guangjun Zhong, Zhu Liang, Jiang Kan, Aikeremujiang Muheremu
Objective This study was performed to determine the efficacy of selective peripheral nerve resection for treatment of persistent neuropathic pain after total knee arthroplasty (TKA). Methods Patients who underwent TKA in our department from January 2013 to July 2016 and experienced persistent pain around the knee joint after TKA were retrospectively included in the current study. Sixty patients were divided into experimental and control groups according the treatment they received. The treatment effect was evaluated by the Hospital for Special Surgery (HSS) knee score and visual analog scale (VAS) pain score preoperatively and at 1, 2, 3, 6, and 12 months postoperatively...
January 1, 2018: Journal of International Medical Research
https://www.readbyqxmd.com/read/29665681/synthesis-of-symmetric-and-unsymmetric-secondary-amines-from-the-ligand-promoted-ruthenium-catalyzed-deaminative-coupling-reaction-of-primary-amines
#17
Pandula T Kirinde Arachchige, Hanbin Lee, Chae S Yi
The catalytic system generated in-situ from the tetranuclear Ru-H complex with a catechol ligand (1/L1) was found to be effective for the direct deaminative coupling of two primary amines to form secondary amines. The catalyst 1/L1 was highly chemoselective for promoting the coupling of two different primary amines to afford unsymmetric secondary amines. The analogous coupling of aniline with primary amines formed aryl-substituted secondary amines. The treatment of aniline-d7 with 4-methoxybenzylamine led to the coupling product with significant deuterium incorporation on CH2 (18% D)...
April 18, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29665367/suppression-of-akt-mediated-hdac3-expression-and-cdk2-t39-phosphorylation-by-a-bichalcone-analog-contributes-to-s-phase-retardation-of-cancer-cells
#18
Kuang-Chen Hung, Meng-Liang Lin, Shih-Wei Hsu, Chuan-Chun Lee, Ren-Yu Huang, Tian-Shung Wu, Shih-Shun Chen
Targeting cell cycle regulators has been a suggested mechanism for therapeutic cancer strategies. We report here that the bichalcone analog TSWU-CD4 induces S phase arrest of human cancer cells by inhibiting the formation of cyclin A-phospho (p)-cyclin-dependent kinase 2 (CDK2, threonine [Thr] 39) complexes, independent of mutant p53 expression. Ectopic expression of CDK2 (T39E), which mimics phosphorylation of the Thr 39 residue of CDK2, partially rescues the cells from TSWU-CD4-induced S phase arrest, whereas phosphorylation-deficient CDK2 (T39A) expression regulates cell growth with significant S phase arrest and enhances TSWU-CD4-triggered S phase arrest...
April 14, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29665236/a-tryptophan-prenyltransferase-with-broad-substrate-tolerance-from-bacillus-subtilis-subsp-natto
#19
Ikuro Abe, Tomotoshi Sugita, Masahiro Okada, Yu Nakashima, Tian Tian
Bacillus subtilis subsp. natto secrets the ComXnatto pheromone as a quorum sensing pheromone to produce poly-γ-glutamate for biofilm formation. The amino acid sequence of the pheromone is Lys-Trp-Pro-Pro-Ile-Glu, and the tryptophan residue is post-translationally modified with a farnesyl group to form a tricyclic scaffold. Unlike other Bacillus ComX pheromones, the tryptophan residue is distant from the C-terminal end of the precursor peptide ComXnatto. Here we report the functional analysis of ComQnatto, which catalyzes a unique farnesyl-transfer reaction...
April 17, 2018: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/29665225/objective-and-quantitative-equilibriometric-evaluation-of-individual-locomotor-behaviour-in-schizophrenia-translational-and-clinical-implications
#20
Svetlozar Haralanov, Evelina Haralanova, Emil Milushev, Diana Shkodrova, Claus-Frenz Claussen
Psychiatry is the only medical specialty that lacks clinically applicable biomarkers for objective evaluation of the existing pathology at a single-patient level. On the basis of an original translational equilibriometric method for evaluation of movement patterns, we have introduced in the everyday clinical practice of psychiatry an easy-to-perform computerized objective quantification of the individual locomotor behaviour during execution of the Unterberger stepping test. For the last 20 years, we have gradually collected a large database of more than 1000 schizophrenic patients, their relatives, and matched psychiatric, neurological, and healthy controls via cross-sectional and longitudinal investigations...
April 17, 2018: Journal of Evaluation in Clinical Practice
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