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https://www.readbyqxmd.com/read/28724178/could-myo-inositol-soft-gel-capsules-outperform-clomiphene-in-inducing-ovulation-results-of-a-pilot-study
#1
A-L Rolland, M Peigné, P Plouvier, A Dumont, S Catteau-Jonard, D Dewailly
OBJECTIVE: Insulin resistance is known to worsen polycystic ovarian syndrome (PCOS). The management of insulin resistance is crucial in the treatment of PCOS and insulin-sensitizing molecule as myo-inositol (MYO) seems to have promising effects. The aim of our pilot study was to study whether supplementation with MYO can improve patients' sensitivity to clomiphene citrate (CC) in terms of ovulation and pregnancy rates. PATIENTS AND METHODS: This study included 26 patients with PCOS, eligible to ovulation induction with CC...
June 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28723681/inhibition-of-necroptosis-attenuates-kidney-inflammation-and-interstitial-fibrosis-induced-by-unilateral-ureteral-obstruction
#2
Xia Xiao, Chunyang Du, Zhe Yan, Yonghong Shi, Huijun Duan, Yunzhuo Ren
BACKGROUND: Inflammation plays a crucial role in renal interstitial fibrosis, the pathway of chronic kidney diseases. Necroptosis is a novel form of regulated cell death, which plays a potential role in inflammation and renal diseases. The small molecule necrostatin-1 (Nec-1) is a specific inhibitor of necroptosis. This study was aimed at determining the role of necroptosis, RIP1/RIP3/mixed lineage kinase domain-like (MLKL) signaling pathway, in renal inflammation and interstitial fibrosis related to primitive tubulointerstitial injury...
July 20, 2017: American Journal of Nephrology
https://www.readbyqxmd.com/read/28723669/multicomponent-analysis-of-the-tumour-microenvironment-reveals-low-cd8-t-cell-number-low-stromal-caveolin-1-and-high-tenascin-c-and-their-combination-as-significant-prognostic-markers-in-non-small-cell-lung-cancer
#3
David Onion, Mark Isherwood, Naveen Shridhar, Mikalena Xenophontos, Madeleine L Craze, Laura J Day, María A García-Márquez, Robert G Pineda, Alexander M Reece-Smith, John H Saunders, John P Duffy, Richard H Argent
The complex interplay of the tumour microenvironment (TME) and its role in disease progression and response to therapy is poorly understood. The majority of studies to date focus on individual components or molecules within the TME and so lack the power correlative analysis. Here we have performed a multi-parameter analysis of the TME in 62 resectable non-small cell lung cancer (NSCLC) specimens detailing number and location of immune infiltrate, assessing markers of cancer-associated fibroblasts, caveolin-1 and tenascin-C, and correlating with clinicopathological details, as well as markers of disease progression such as epithelial-to-mesenchymal transition (EMT)...
June 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28723622/dual-targeting-of-mdm2-and-bcl2-as-a-therapeutic-strategy-in-neuroblastoma
#4
Alan Van Goethem, Nurten Yigit, Myrthala Moreno-Smith, Sanjeev A Vasudevan, Eveline Barbieri, Frank Speleman, Jason Shohet, Jo Vandesompele, Tom Van Maerken
Wild-type p53 tumor suppressor activity in neuroblastoma tumors is hampered by increased MDM2 activity, making selective MDM2 antagonists an attractive therapeutic strategy for this childhood malignancy. Since monotherapy in cancer is generally not providing long-lasting clinical responses, we here aimed to identify small molecule drugs that synergize with idasanutlin (RG7388). To this purpose we evaluated 15 targeted drugs in combination with idasanutlin in three p53 wild type neuroblastoma cell lines and identified the BCL2 inhibitor venetoclax (ABT-199) as a promising interaction partner...
July 4, 2017: Oncotarget
https://www.readbyqxmd.com/read/28723595/pilot-investigation-of-a-topographical-filter-dermal-patch-in-patients-with-tinnitus
#5
Peter Ahnblad
OBJECTIVES: A new topographical filter in a dermal administration patch that organizes water molecules has been suggested as an alternative treatment for manifested tinnitus. The aim of this study was to evaluate this patch in a pilot study. MATERIALS AND METHODS: 12 patients were included (10 completed) in an open study all receiving treatment with daily changed patches. The objectives were to evaluate safety and performance of the patch during and after treatment...
June 1, 2017: International Tinnitus Journal
https://www.readbyqxmd.com/read/28723416/unravelling-the-pharmacologic-opportunities-and-future-directions-for-targeted-therapies-in-gastro-intestinal-cancers-part-2-neuroendocrine-tumours-hepatocellular-carcinoma-and-gastro-intestinal-stromal-tumours
#6
REVIEW
Cindy Neuzillet, Louis de Mestier, Benoît Rousseau, Olivier Mir, Mohamed Hebbar, Hemant M Kocher, Philippe Ruszniewski, Christophe Tournigand
Until the 1990s, cytotoxic chemotherapy has been the cornerstone of medical therapy for gastrointestinal (GI) cancers. Better understanding of the cancer cell molecular biology has led to the therapeutic revolution of targeted therapies, i.e. monoclonal antibodies or small molecule inhibitors directed against proteins that are specifically overexpressed or mutated in cancer cells. These agents, being more specific to cancer cells, were expected to be less toxic than conventional cytotoxic agents. However, their effects have sometimes been disappointing, due to intrinsic or acquired resistance mechanisms, or to an activity restricted to some tumour settings, illustrating the importance of patient selection and early identification of predictive biomarkers of response to these therapies...
July 16, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28723271/development-of-three-orthogonal-assays-suitable-for-the-identification-and-qualification-of-pikfyve-inhibitors
#7
Kylie Fogarty, Mohammed Kashem, Andras Bauer, Alexandra Bernardino, Debra Brennan, Brian Cook, Neil Farrow, Teresa Molinaro, Richard Nelson
FYVE-type zinc finger-containing phosphoinositide kinase (PIKfyve) catalyzes the formation of phosphatidylinositol 3,5-bisphosphate (PI(3,5)P2) from phosphatidylinositol 3-phosphate (PI(3)P). PIKfyve has been implicated in multiple cellular processes, and its role in the regulation of toll-like receptor (TLR) pathways and the production of proinflammatory cytokines has sparked interest in developing small-molecule PIKfyve inhibitors as potential therapeutics to treat autoimmune and inflammatory diseases. We developed three orthogonal assays to identify and qualify small-molecule inhibitors of PIKfyve: (1) a purified component microfluidic enzyme assay that measures the conversion of fluorescently labeled PI(3)P to PI(3,5)P2 by purified recombinant full-length human 6His-PIKfyve (rPIKfyve); (2) an intracellular protein stabilization assay using the kinase domain of PIKfyve expressed in HEK293 cells; and (3) a cell-based functional assay that measures the production of interleukin (IL)-12p70 in human peripheral blood mononuclear cells stimulated with TLR agonists lipopolysaccharide and R848...
July 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28723269/identification-of-antipneumococcal-molecules-effective-against-different-streptococcus-pneumoniae-serotypes-using-a-resazurin-based-high-throughput-screen
#8
Hyung Jun Kim, Namyoul Kim, David Shum, Srigouri Huddar, Chul Min Park, Soojin Jang
Streptococcus pneumoniae is a major human pathogen, causing around 1.6 million deaths worldwide each year. By optimizing a resazurin-based assay to detect S. pneumoniae growth in 384-well microplates, we developed a new high-throughput screening (HTS) system for the discovery of antipneumococcal molecules, which was unsuccessful using conventional absorbance measurements. Before applying our protocol to a large-scale screen, we validated the system through a pilot screen targeting about 7,800 bioactive molecules using three different S...
July 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28723234/flexible-small-molecular-anti-estrogens-with-n-n-dialkylated-2-5-diethoxy-4-morpholinoaniline-scaffold-targets-multiple-estrogen-receptor-conformations
#9
Bethany K Asare, Emmanuel Yawson, Rajendram V Rajnarayanan
Estrogen mediates various cellular processes including cell proliferation, differentiation, growth and mammary gland function. Estrogen Receptors (ERs) are expressed in 70% of breast cancers. Consequently, estrogen mediated ER signaling plays a critical role in breast cancer diagnosis, prognosis, and treatment. Estrogen Receptors are ligand-triggered transcription factors. However, in the absence of a cognate estrogenic ligand, ERs can be activated by a variety of other extracellular signals. Tamoxifen, an anti-estrogen that selectively targets ER, induces substantial regression of breast tumors and an increase in disease-free survival...
July 19, 2017: Cell Cycle
https://www.readbyqxmd.com/read/28723154/interruption-of-hydrogen-bonding-networks-of-water-in-carbon-nanotubes-due-to-strong-hydration-shell-formation
#10
Yoshifumi Oya, Kenji Hata, Tomonori Ohba
We present the structures of NaCl aqueous solution in carbon nanotubes with diameters of 1, 2, and 3 nm based on an analysis performed using X-ray diffraction and canonical ensemble Monte Carlo simulations. Anomalously longer nearest-neighbor distances were observed in the electrolyte for the 1-nm-diameter carbon nanotubes; in contrast, in the 2 and 3 nm carbon nanotubes, the nearest-neighbor distances were shorter than those in the bulk electrolyte. We also observed similar properties for water in carbon nanotubes, which was expected because the main component of the electrolyte was water...
July 19, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28723122/electrochemical-dna-based-immunoassay-that-employs-steric-hindrance-to-detect-small-molecules-directly-in-whole-blood
#11
Sahar S Mahshid, Francesco Ricci, Shana O Kelley, Alexis Vallée-Bélisle
The development of a universal sensing mechanism for the rapid and quantitative detection of small molecules directly in whole blood would drastically impact global health by enabling disease diagnostics, monitoring, and treatment at home. We have previously shown that hybridization between a free DNA strand and its complementary surface-bound strand can be sterically hindered when the former is bound to large antibodies. Here, we exploit this effect to design a competitive antibody-based electrochemical assay, called CeSHHA, that enables the quantitative detection of small molecules directly in complex matrices, such as whole blood or soil...
June 23, 2017: ACS Sensors
https://www.readbyqxmd.com/read/28723086/formation-of-core-shell-ethane-silver-clusters-in-he-droplets
#12
Evgeny Loginov, Luis F Gomez, Boris G Sartakov, Andrey F Vilesov
Ethane core - silver shell clusters consisting of several thousand particles have been assembled in helium droplets upon capture of first ethane molecules, followed by Ag atoms. The composite clusters were studied via infrared laser spectroscopy in the range of C-H stretching vibrations of ethane molecules. The spectra show the splitting of the vibrational bands, which was assigned to different environment of the molecules, such as in contact or devoid of a contact with Ag atoms. The analysis of the band intensities for different number of trapped ethane molecules and Ag atoms indicates that the composite clusters consist of ethane core covered with small Ag clusters having different degree of submergence on the surface...
July 19, 2017: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/28723063/using-cooperatively-folded-peptides-to-measure-interaction-energies-and-conformational-propensities
#13
Maziar S Ardejani, Evan T Powers, Jeffery W Kelly
The rates and equilibria of the folding of biopolymers are determined by the conformational preferences of the subunits that make up the sequence of the biopolymer and by the interactions that are formed in the folded state in aqueous solution. Because of the centrality of these processes to life, quantifying conformational propensities and interaction strengths is vitally important to understanding biology. In this Account, we describe our use of peptide model systems that fold cooperatively yet are small enough to be chemically synthesized to measure such quantities...
July 19, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28722477/advances-toward-lsd1-inhibitors-for-cancer-therapy
#14
Xiaoli Fu, Peng Zhang, Bin Yu
LSD1 has become an important biologically validated epigenetic target for cancer therapy since its identification in 2004. LSD1 mediates many cellular signaling pathways and is involved in the initiation and development of cancers. Aberrant overexpression of LSD1 has been observed in different types of cancers, and inactivation by small molecules suppresses cancer cell differentiation, proliferation, invasion and migration. To date, a large number of LSD1 inhibitors have been reported, RG6016, GSK-2879552, INCB059872, IMG-7289 and CC-90011 are currently undergoing clinical assessment for the treatment of acute myeloid leukemia, small-cell lung cancer, etc...
July 19, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28722474/when-will-small-molecule-lactate-dehydrogenase-inhibitors-realize-their-potential-in-the-cancer-treatment-in-clinic
#15
Reshma Rani, Vinit Kumar
No abstract text is available yet for this article.
July 19, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28722441/harnessing-the-versatility-of-optical-biosensors-for-target-based-small-molecule-drug-discovery
#16
Tim Kaminski, Anders Gunnarsson, Stefan Geschwindner
Optical biosensors entered target-based small-molecule drug discovery more than two decades ago and have since transformed into a value-adding component in the decision-making process. Here, we briefly highlight the major application areas of optical biosensors and focus on desirable profiles of such platforms in order to ensure their effective use in small molecule drug discovery. Furthermore, we will emphasize current technology-based constraints and discuss experimental strategies to address these limitations as well as provide a view of necessary technology improvements for next generation platforms...
January 27, 2017: ACS Sensors
https://www.readbyqxmd.com/read/28722437/surface-plasmon-resonance-clinical-biosensors-for-medical-diagnostics
#17
Jean-Francois Masson
The design and application of sensors for monitoring biomolecules in clinical samples is a common goal of the sensing research community. Surface plasmon resonance (SPR) and other plasmonic techniques such as localized surface plasmon resonance (LSPR) and imaging SPR are reaching a maturity level sufficient for their application in monitoring biomolecules in clinical samples. In recent years, the first examples for monitoring antibodies, proteins, enzymes, drugs, small molecules, peptides, and nucleic acids in biofluids collected from patients afflicted with a series of medical conditions (Alzheimer's, hepatitis, diabetes, leukemia, and cancers such as prostate and breast cancers, among others) demonstrate the progress of SPR sensing in clinical chemistry...
January 27, 2017: ACS Sensors
https://www.readbyqxmd.com/read/28722431/giant-o2-induced-photoluminescence-modulation-in-hierarchical-titanium-dioxide-nanostructures
#18
Deborah K Pallotti, Luca Passoni, Felice Gesuele, Pasqualino Maddalena, Fabio Di Fonzo, Stefano Lettieri
We demonstrate exceptionally large modulation of PL intensity in hierarchical titanium dioxide (TiO2) nanostructures exposed to molecular oxygen (O2). Optical responsivities up to about 1100% at 20% O2 concentrations are observed in hyperbranched anatase-phase hierarchical structures, outperforming those obtainable by commercial TiO2 nanopowders (up to a factor of ∼7 for response to synthetic air) and significantly improving the ones typically reported in PL-based opto-chemical gas sensing using MOXs. The improved PL response is discussed in terms of the specific morphology of hierarchical structures, characterized by simultaneous presence of small nanoparticles, large surface areas, and large voids...
January 27, 2017: ACS Sensors
https://www.readbyqxmd.com/read/28722340/a-novel-small-molecule-inhibitor-of-prion-replication-and-mutant-prion-protein-toxicity
#19
Tania Massignan, Valeria Sangiovanni, Silvia Biggi, Claudia Stincardini, Saioa R Elezgarai, Giulia Maietta, Ivan A Andreev, Nina K Ratmanova, Dmitry S Belov, Evgeny R Lukyanenko, Grigory M Belov, Maria Letizia Barreca, Andrea Altieri, Alexander V Kurkin, Emiliano Biasini
Prion diseases are a class of neurodegenerative disorders characterized by the accumulation in the brain of a self-replicating, misfolded isoform (PrPSc) of the cellular prion protein (PrPC), a cell-surface glycoprotein of uncertain function. Emerging evidence suggests that PrPC may passively serve as a substrate for the replication of PrPSc, and actively transduce its toxic effects to neuronal cells. The vast majority of previous drug screening campaigns have only targeted PrPSc replication, with largely unsuccessful results...
July 19, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28722297/assessing-guest-molecule-diffusion-in-heterogeneous-powder-samples-of-metal-organic-frameworks-through-pfg-nmr
#20
Roland Thoma, Jörg Kärger, Nader de Sousa Amadeu, Sandra Nießing, Christoph Janiak
Investigation of guest diffusion in porous metal-organic frameworks (MOFs) is of major importance since many porosity-related properties of MOFs are influenced by diffusion effects. The diffusion of dimethylsulfoxide (DMSO) in the metal-organic framework (MOF) MIL-53-NH2(Al) was investigated through pulsed-field-gradient (PFG) NMR spectroscopy. The microporous material was synthesized in small crystallites (under 500 nm), which agglomerated in a large range of particle sizes, giving a morphologically very heterogeneous sample...
July 19, 2017: Chemistry: a European Journal
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