Genomes and Genes
Summary: Heterocyclic compounds where the ring system is composed of three CARBON atoms, a SULFUR and NITROGEN atoms.
Publications102 found, 100 shown here
- Raju U, Riesterer O, Wang Z, Molkentine D, Molkentine J, Johnson F, et al. Dasatinib, a multi-kinase inhibitor increased radiation sensitivity by interfering with nuclear localization of epidermal growth factor receptor and by blocking DNA repair pathways. Radiother Oncol. 2012;105:241-9 pubmed publisher
- Khullar V, Amarenco G, Angulo J, Cambronero J, Høye K, Milsom I, et al. Efficacy and tolerability of mirabegron, a ?(3)-adrenoceptor agonist, in patients with overactive bladder: results from a randomised European-Australian phase 3 trial. Eur Urol. 2013;63:283-95 pubmed publisher..Mirabegron, a ?(3)-adrenoceptor agonist, has been developed for the treatment of overactive bladder (OAB)...
- Mohanty J, Barooah N, Dhamodharan V, Harikrishna S, Pradeepkumar P, Bhasikuttan A. Thioflavin T as an efficient inducer and selective fluorescent sensor for the human telomeric G-quadruplex DNA. J Am Chem Soc. 2013;135:367-76 pubmed publisher..This work has implication in designing new generation dyes based on the ThT scaffold, which are highly selective for telomeric DNA, for potential diagnostic, therapeutic, and ion-sensing applications. ..
- Sobel K, Menyhart K, Killer N, Renault B, Bauer Y, Studer R, et al. Sphingosine 1-phosphate (S1P) receptor agonists mediate pro-fibrotic responses in normal human lung fibroblasts via S1P2 and S1P3 receptors and Smad-independent signaling. J Biol Chem. 2013;288:14839-51 pubmed publisher..These data demonstrate that S1PR agonists are pro-fibrotic via S1P2R and S1P3R stimulation using Smad-independent pathways...
- Sano M, Saotome M, Urushida T, Katoh H, Satoh H, Ohnishi K, et al. Pulmonary arterial hypertension caused by treatment with dasatinib for chronic myeloid leukemia -critical alert-. Intern Med. 2012;51:2337-40 pubmed..As notified by U.S. Food and Drug Administration (FDA) in October 2011, we recommend routine cardiopulmonary evaluation before and during treatment with dasatinib in CML patients in terms of the adverse effects of PAH. ..
- Cresswell J, Thompson H. Comment on "A common pesticide decreases foraging success and survival in honey bees". Science. 2012;337:1453; author reply 1453 pubmed..Here, we show that collapse disappears when the model is recalculated with parameter values appropriate to the season when most pesticide-treated flowering crops bloom. ..
- Mendell J, Noveck R, Shi M. Pharmacokinetics of the direct factor Xa inhibitor edoxaban and digoxin administered alone and in combination. J Cardiovasc Pharmacol. 2012;60:335-41 pubmed publisher..Edoxaban PD were consistent with PK. Both drugs were well tolerated alone or in combination. No clinically significant changes in PK, PD, or renal elimination were observed with concomitant administration of edoxaban and digoxin. ..
- Elman J, Madison C, Baker S, Vogel J, Marks S, Crowley S, et al. Effects of Beta-Amyloid on Resting State Functional Connectivity Within and Between Networks Reflect Known Patterns of Regional Vulnerability. Cereb Cortex. 2016;26:695-707 pubmed publisher..They indicate the presence of A?-related dysfunction of neural systems in cognitively normal people well before these areas become hypometabolic with the onset of cognitive decline. ..
- Murad A, Marren P. Prevalence of methylchloroisothiazolinone and methylisothiazolinone contact allergy in facial dermatitis: a single centre Irish study. J Eur Acad Dermatol Venereol. 2016;30:60-2 pubmed publisher..The detection rate of this allergen was increased by 5% in our cohort since the inclusion of MI (0.2%) in the standard series. ..
- Koh E, Hung C, Parker K, Crowley J, Giblin D, Henderson J. Metal selectivity by the virulence-associated yersiniabactin metallophore system. Metallomics. 2015;7:1011-22 pubmed publisher..These results are consistent with yersiniabactin as part of a metallophore system able to prioritize iron(III) complex uptake in high copper environments. ..
- Macchi F, Deleersnijder A, Van den Haute C, Munck S, Pottel H, Michiels A, et al. High-content analysis of Î±-synuclein aggregation and cell death in a cellular model of Parkinson's disease. J Neurosci Methods. 2016;261:117-27 pubmed publisher..The presented analysis approach offers a rapid, objective and multiparametric approach for the screening of compounds and genes that might alter Î±-SYN aggregation and/or toxicity. ..
- Lu C, Makala L, Wu D, Cai Y. Targeting translation: eIF4E as an emerging anticancer drug target. Expert Rev Mol Med. 2016;18:e2 pubmed publisher..This paper reviews the strategies that can be used to target eIF4E, highlighting agents that target eIF4E activity at each distinct level. ..
- Jensen D, Asselah T, Dieterich D, Foster G, Sulkowski M, Zeuzem S, et al. Faldaprevir, pegylated interferon, and ribavirin for treatment-naïve HCV genotype-1: pooled analysis of two phase 3 trials. Ann Hepatol. 2016;15:333-49 pubmed publisher..Addition of faldaprevir to PegIFN/RBV increased SVR12 in patients with HCV genotype-1, and was well tolerated. Faldaprevir 120 mg is effective in the treatment of HCV genotype-1. ClinicalTrials.gov: NCT01343888 and NCT01297270. ..
- Vannini P, Hanseeuw B, Munro C, Amariglio R, Marshall G, Rentz D, et al. Hippocampal hypometabolism in older adults with memory complaints and increased amyloid burden. Neurology. 2017;88:1759-1767 pubmed publisher..Decreased hippocampal metabolism may be a specific marker of subclinical changes in cognition due to amyloid pathology. However, longitudinal studies are needed to determine whether our findings foreshadow clinical decline. ..
- Etzerodt T, Wetterhorn K, Dionisio G, Rayment I. Functional characterization of a soluble NADPH-cytochrome P450 reductase from Fusarium graminearum. Protein Expr Purif. 2017;138:69-75 pubmed publisher..graminearum which most likely is involved in mycotoxin biosynthesis or some primary metabolic pathway such as sterol biosynthesis in F. graminearum. ..
- Watson L, Bamber E, Schnekenberg R, Williams J, Bettencourt C, Lickiss J, et al. Dominant Mutations in GRM1 Cause Spinocerebellar Ataxia Type 44. Am J Hum Genet. 2017;101:451-458 pubmed publisher..Crucially, the gain-of-function mutations could be pharmacologically modulated in vitro using an existing FDA-approved drug, Nitazoxanide, suggesting a possible avenue for treatment, which is currently unavailable for ataxias. ..
- Tomasić T, Barančoková M, Zidar N, Ilas J, Tammela P, Kikelj D. Design, synthesis, and biological evaluation of 1-ethyl-3-(thiazol-2-yl)urea derivatives as Escherichia coli DNA gyrase inhibitors. Arch Pharm (Weinheim). 2017;: pubmed publisher..The most potent DNA gyrase inhibitors in the prepared library of compounds were benzo[1,2-d]thiazoles 32-34, 36, and 37 with IC50 values in the low micromolar range...
- Newman M, Halter L, Lim A, Lardelli M. Mitochondrion to endoplasmic reticulum apposition length in zebrafish embryo spinal progenitors is unchanged in response to perturbations associated with Alzheimer's disease. PLoS ONE. 2017;12:e0179859 pubmed publisher..Future examination of more differentiated, more secretory cell types may reveal measurable responses of M-ER apposition to environmental and genetic manipulation. ..
- Martinez Ariza G, Mehari B, Pinho L, Foley C, Day K, Jewett J, et al. Synthesis of fluorescent heterocycles via a Knoevenagel/[4 + 1]-cycloaddition cascade using acetyl cyanide. Org Biomol Chem. 2017;15:6076-6079 pubmed publisherA concise one-pot three-component reaction that affords fluorescent indolizines, benzo[d]pyrrolo[2,1-b]thiazoles, and pyrrolo[1,2-a]pyrazines is reported...
- Gardner N, Gillespie P, Carrington J, Shanks E, McElroy S, Haagensen E, et al. The High-Affinity Interaction between ORC and DNA that Is Required for Replication Licensing Is Inhibited by 2-Arylquinolin-4-Amines. Cell Chem Biol. 2017;24:981-992.e4 pubmed publisher..We show that RL5a prevents ORC forming a tight complex with DNA that is required for MCM2-7 loading. Formation of this ORC-DNA complex requires ATP, and we show that RL5a inhibits ORC allosterically to mimic a lack of ATP. ..
- Marques Ramos A, Candeias M, Menezes J, Lacerda R, Willcocks M, Teixeira A, et al. Cap-independent translation ensures mTOR expression and function upon protein synthesis inhibition. RNA. 2017;23:1712-1728 pubmed publisher..These results suggest a novel regulatory mechanism for mTOR gene expression that integrates the global protein synthesis changes induced by translational inhibitory conditions. ..
- Irwin D, Brettschneider J, McMillan C, Cooper F, Olm C, Arnold S, et al. Deep clinical and neuropathological phenotyping of Pick disease. Ann Neurol. 2016;79:272-87 pubmed publisher..Pick disease tau neuropathology may originate in limbic/paralimbic cortices. The patterns of tau pathology observed here provide novel insights into the natural history and biology of tau-mediated neurodegeneration. ..
- Eser B, Zhang X, Chanani P, Begley T, Ealick S. From Suicide Enzyme to Catalyst: The Iron-Dependent Sulfide Transfer in Methanococcus jannaschii Thiamin Thiazole Biosynthesis. J Am Chem Soc. 2016;138:3639-42 pubmed publisher..Here, we demonstrate that the Thi4 ortholog from Methanococcus jannaschii uses exogenous sulfide and is catalytic. Structural and biochemical studies on this enzyme elucidate the mechanistic details of the sulfide transfer reactions. ..
- Chen L, Zhang W, Ye R, Hu C, Wang Q, Seemann F, et al. Chronic Exposure of Marine Medaka (Oryzias melastigma) to 4,5-Dichloro-2-n-octyl-4-isothiazolin-3-one (DCOIT) Reveals Its Mechanism of Action in Endocrine Disruption via the Hypothalamus-Pituitary-Gonadal-Liver (HPGL) Axis. Environ Sci Technol. 2016;50:4492-501 pubmed publisher..The reproductive impairments of DCOIT at environmentally realistic concentrations highlights the need for more comprehensive investigations of its potential ecological risks. ..
- Zou J, Yu Y, Li Y, Ji W, Chen C, Law W, et al. Well-defined diblock brush polymer-drug conjugates for sustained delivery of paclitaxel. Biomater Sci. 2015;3:1078-84 pubmed publisher..In summary, the results obtained in this work provide new insight into the structure-dependent properties of brush polymer-based drug delivery systems. ..
- Zwan M, Villemagne V, DorÃ© V, Buckley R, Bourgeat P, Veljanoski R, et al. Subjective Memory Complaints in APOEÉ›4 Carriers are Associated with High Amyloid-Î² Burden. J Alzheimers Dis. 2016;49:1115-22 pubmed publisher..These findings suggest that selection based on the presence of SMC, APOEÉ›4 genotype and age may help identify healthy elderly participants with high AÎ² burden eligible for secondary prevention trials. ..
- Ewida M, Abou El Ella D, Lasheen D, Ewida H, El Gazzar Y, El Subbagh H. Thiazolo[4,5-d]pyridazine analogues as a new class of dihydrofolate reductase (DHFR) inhibitors: Synthesis, biological evaluation and molecular modeling study. Bioorg Chem. 2017;74:228-237 pubmed publisherA new series of 1,3-thiazoles and thiazolo[4,5-d]pyridazine both bearing the 2-thioureido function were designed, synthesized and evaluated for their invitro DHFR inhibition and antitumor activities...
- Zhu X, Yang Y, Xiao G, Song J, Liang Y, Deng G. Double C-S bond formation via C-H bond functionalization: synthesis of benzothiazoles and naphtho[2,1-d]thiazoles from N-substituted arylamines and elemental sulfur. Chem Commun (Camb). 2017;53:11917-11920 pubmed publisher..friendly method for the synthesis of 2-substituted benzothiazoles and 2-substituted naphtho[2,1-d]thiazoles from N-substituted arylamines and elemental sulfur has been developed under metal-free conditions...
- Liu T, Wang X, You X, Chen D, Li Y, Wang F. Oxidative stress and gene expression of earthworm (Eisenia fetida) to clothianidin. Ecotoxicol Environ Saf. 2017;142:489-496 pubmed publisher..Additionally, the present results showed that superoxide dismutase (SOD), DNA damage and heat shock protein 70 (HSP70) may be good indicators for environmental risk assessment of clothianidin to earthworms. ..
- Dos Santos Silva T, Bomfim L, da Cruz Rodrigues A, Dias R, Sales C, Rocha C, et al. Anti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivatives. Toxicol Appl Pharmacol. 2017;329:212-223 pubmed publisher..Together the results indicated the anti-liver cancer activity of 2-pyridyl 2,3-thiazole derivatives. ..
- Lip G, Al Saady N, Jin J, Sun M, Melino M, Winters S, et al. Anticoagulation Control in Warfarin-Treated Patients Undergoing Cardioversion of Atrial Fibrillation (from the Edoxaban Versus Enoxaparin-Warfarin in Patients Undergoing Cardioversion of Atrial Fibrillation Trial). Am J Cardiol. 2017;120:792-796 pubmed publisher..In conclusion, even in this short-term study, TiTR was significantly related to bleeding events. ..
- Loy J, Merry S, Hetrick S, Stasiak K. Atypical antipsychotics for disruptive behaviour disorders in children and youths. Cochrane Database Syst Rev. 2017;8:CD008559 pubmed publisher..This is consistent with current clinical guidelines. ..
- Olwoch I, Greeff O, Jooné G, Steenkamp V. The effects of the natural enzyme, Pectinex Ultra SP-L, on human cell cultures and bacterial biofilms in vitro. BMC Microbiol. 2014;14:251 pubmed publisher..It was therefore deemed unsuitable for the management of either planktonic or biofilm phenotypes of S. aureus or P. aeruginosa. ..
- Tamura K, Kawai Y, Kiguchi T, Okamoto M, Kaneko M, Maemondo M, et al. Efficacy and safety of febuxostat for prevention of tumor lysis syndrome in patients with malignant tumors receiving chemotherapy: a phase III, randomized, multi-center trial comparing febuxostat and allopurinol. Int J Clin Oncol. 2016;21:996-1003 pubmed..Febuxostat demonstrated an efficacy and safety similar to allopurinol in patients with malignant tumors receiving chemotherapy. http://www.clinicaltrials.jp ; Identifier: JapicCTI-132398. ..
- Jiao W, Xiao Y, Qian X, Tong M, Hu Y, Hou R, et al. Optimized combination of dilution and refined QuEChERS to overcome matrix effects of six types of tea for determination eight neonicotinoid insecticides by ultra performance liquid chromatography-electrospray tandem mass spectrometry. Food Chem. 2016;210:26-34 pubmed publisher..3 to 108.0% from tea samples spiked at 0.01-0.5mgkg(-1). Relative standard deviations were below 16% for all recovery tests. The limit of quantification ranged from 0.01 to 0.05mgkg(-1). ..
- Heimbach F, Russ A, Schimmer M, Born K. Large-scale monitoring of effects of clothianidin dressed oilseed rape seeds on pollinating insects in Northern Germany: implementation of the monitoring project and its representativeness. Ecotoxicology. 2016;25:1630-1647 pubmed..Furthermore, the study area was found to be representative for other oilseed rape cultivation regions in Europe. ..
- Tavares D, Dussaubat C, Kretzschmar A, Carvalho S, Silva Zacarin E, Malaspina O, et al. Exposure of larvae to thiamethoxam affects the survival and physiology of the honey bee at post-embryonic stages. Environ Pollut. 2017;229:386-393 pubmed publisher..This study represents the first investigation of the effects of thiamethoxam on the development of A. mellifera following larval exposure. ..
- Zhang H, Lin W, Wu Z, Ruan W, Wen T. Correction: Silver-mediated direct phosphorylation of benzothiazoles and thiazoles with diarylphosphine oxides. Chem Commun (Camb). 2015;51:16871 pubmed publisherCorrection for 'Silver-mediated direct phosphorylation of benzothiazoles and thiazoles with diarylphosphine oxides' by Hui-Jun Zhang et al., Chem. Commun., 2015, 51, 3450-3453.
- Kasai A, Hayashi T, Ohnishi H, Suzuki K, Hayasaka D, Goka K. Fipronil application on rice paddy fields reduces densities of common skimmer and scarlet skimmer. Sci Rep. 2016;6:23055 pubmed publisher..These results suggest that the accumulation of these insecticides in paddy soil reduces biodiversity by eliminating dragonfly nymphs, which occupy a high trophic level in paddy fields. ..
- Ziyaei Halimehjani A, Lotfi Nosood Y. Synthesis of N,S-Heterocycles and Dithiocarbamates by the Reaction of Dithiocarbamic Acids and S-Alkyl Dithiocarbamates with Nitroepoxides. Org Lett. 2017;: pubmed publisher..In addition, substituted thiazoles and 1-(alkylthio)-1-phenylpropan-2-ones were prepared in reactions of S-alkyl dithiocarbamates and nitroepoxides.
- Liaras K, Fesatidou M, Geronikaki A. Thiazoles and Thiazolidinones as COX/LOX Inhibitors. Molecules. 2018;23: pubmed publisher..This review focuses on the biological activity of several thiazole and thiazolidinone derivatives as COX-1/COX-2 and LOX inhibitors. ..
- Alsharif Z, Alam M. Modular synthesis of thiazoline and thiazole derivatives by using a cascade protocol. RSC Adv. 2017;7:32647-32651 pubmed publisherThiazolines and thiazoles are an integral part of numerous natural products, a number of drugs, and many useful molecules such as ligands for metal catalysis...
- Orozco SolÃs M, GarcÃa Ãvalos Y, Pichardo RamÃrez C, TobÃas AzÃºa F, Zapata Morales J, Aragon MartÃnez O, et al. Single dose of diclofenac or meloxicam for control of pain, facial swelling, and trismus in oral surgery. Med Oral Patol Oral Cir Bucal. 2016;21:e127-34 pubmed
- Bahl V, Weng N, Schick S, Sleiman M, Whitehead J, Ibarra A, et al. Cytotoxicity of Thirdhand Smoke and Identification of Acrolein as a Volatile Thirdhand Smoke Chemical That Inhibits Cell Proliferation. Toxicol Sci. 2016;150:234-46 pubmed publisher..This study identified acrolein as a highly cytotoxic VOC in THS which killed cells at high doses and inhibited cell proliferation at low doses. ..
- Kumar M, Chand R, Shah K. Evidences for growth-promoting and fungicidal effects of low doses of tricyclazole in barley. Plant Physiol Biochem. 2016;103:176-82 pubmed publisher..Application of low doses of TCZ can fit in well with environment friendly strategies for sustainable barley crop production, more yield and minimal soil contamination. ..
- Du Y, Song L, Zhang L, Ling H, Zhang Y, Chen H, et al. The discovery of novel, potent ERR-alpha inverse agonists for the treatment of triple negative breast cancer. Eur J Med Chem. 2017;136:457-467 pubmed publisher..All these results suggest that compound 11 represents a novel potent ERR? inverse agonist and is promising in the discovery of antitumor compounds for the treatment of triple negative breast cancer. ..
- Sopha P, Ren H, Grove D, Cyr D. Endoplasmic reticulum stress-induced degradation of DNAJB12 stimulates BOK accumulation and primes cancer cells for apoptosis. J Biol Chem. 2017;292:11792-11803 pubmed publisher..In summary, JB12 is a stress-sensitive Hsp40 whose degradation during severe ER stress provides a mechanism to promote BOK accumulation and induction of apoptosis. ..
- Boost M, Yau P, Yap M, Cho P. Determination of cytotoxicity of traditional Chinese medicine herbs, Rhizoma coptidis, Radix scutellariae, and Cortex phellodendri, by three methods. Cont Lens Anterior Eye. 2016;39:128-32 pubmed publisher..Only flow cytometry was able to accurately predict cytotoxic effects of extracts of TCM herbs on HCEC, demonstrating the importance of using a sensitive method of detection of cytotoxicity. ..
- Oliveira L, Molina E, Moura A, de Faria E, Ciuffi K. Synthesis, Characterization, and Environmental Applications of Hybrid Materials Based on Humic Acid Obtained by the Sol-Gel Route. ACS Appl Mater Interfaces. 2016;8:1478-85 pubmed publisher..These hybrid materials have potential use as adsorbents for the removal of cationic or anionic species and could be viable alternatives to remove various substances present as contaminants in natural environments. ..
- Izushi Y, Takami Y, Shiota N, Tetsunaga T, Ookura Y, Shimada K, et al. Clinical Assessment of Postoperative Anemia Associated with Edoxaban in Patients Undergoing Total Knee Arthroplasty Compared to Fondaparinux. Biol Pharm Bull. 2016;39:516-23 pubmed publisher..Thus, as the frequency of postoperative anemia tended to be higher in E-group, edoxaban 30?mg might require vigilance, and prolonged PT and PT-INR could potentially predict edoxaban-associated postoperative anemia after TKA. ..
- Rossignol J. Nitazoxanide, a new drug candidate for the treatment of Middle East respiratory syndrome coronavirus. J Infect Public Health. 2016;9:227-30 pubmed publisher..Future research should include in vitro mechanism studies, animal models of MERS-CoV infection, clinical trials, including dose-ranging trials, and evaluation of combination therapy with other potential MERS-CoV antivirals. ..
- Lockhart S, Scholl M, Baker S, Ayakta N, Swinnerton K, Bell R, et al. Amyloid and tau PET demonstrate region-specific associations in normal older people. Neuroimage. 2017;150:191-199 pubmed publisher..The spatial relationship between Aβ and tau accumulation does not appear to be specific to Aβ location, suggesting a regional vulnerability of temporal brain regions to tau accumulation regardless of where Aβ accumulates. ..
- Grbčić P, Tomljanović I, Klobučar M, Kraljevic Pavelic S, Lucin K, Sedic M. Dual sphingosine kinase inhibitor SKI-II enhances sensitivity to 5-fluorouracil in hepatocellular carcinoma cells via suppression of osteopontin and FAK/IGF-1R signalling. Biochem Biophys Res Commun. 2017;487:782-788 pubmed publisher
- Vale N, Correia Branco A, Patrício B, Duarte D, Martel F. In vitro studies on the inhibition of colon cancer by amino acid derivatives of bromothiazole. Bioorg Med Chem Lett. 2017;27:3507-3510 pubmed publisher..The ability of bromo substituent in thiazole ring with new sequences of amino acids in inducing cell death and apoptosis in Caco-2 cells (and other cell lines) is now being studied. ..
- Rabhi K, Deisig N, Demondion E, Le Corre J, Robert G, Tricoire Leignel H, et al. Low doses of a neonicotinoid insecticide modify pheromone response thresholds of central but not peripheral olfactory neurons in a pest insect. Proc Biol Sci. 2016;283: pubmed publisher..This correlates with the changes of behavioural responses after clothianidin treatment and suggests the antennal lobe as neural substrate involved in clothianidin-induced behavioural changes. ..
- Bartos C, Szabó Révész P, Bartos C, Katona G, Jójárt Laczkovich O, Ambrus R. The Effect of an Optimized Wet Milling Technology on the Crystallinity, Morphology and Dissolution Properties of Micro- and Nanonized Meloxicam. Molecules. 2016;21:507 pubmed publisher..According to the results, the produced samples could be applied as a basic material (micronized MEL) and intermediate product (micronized and nanonized MEL with PVA) for the design of dosage forms. ..
- Slade L, Chalker J, Kuksal N, Young A, Gardiner D, Mailloux R. Examination of the superoxide/hydrogen peroxide forming and quenching potential of mouse liver mitochondria. Biochim Biophys Acta Gen Subj. 2017;1861:1960-1969 pubmed publisher..We also confirm that catalase plays a role in quenching either exogenous or intramitochondrial H2O2. ..
- Ha S, Oh J, Kim Y, Ham S. Determination of the binding site of 2-aminothiazole derivative with importin ?1 by UV-crosslinking experiment. J Chromatogr B Analyt Technol Biomed Life Sci. 2017;1060:71-75 pubmed publisher..Herein, we report that compound 1 binds strongly to KPNB1, in a pocket centered around serine-476, as shown by UV-crosslinking and tandem mass spectrometry experiments, and supported using a model derived from molecular docking. ..
- Bunyavaree M, Kasemsarn P, Boonchai W. Cosmetic preservative labelling on the Thai market. Contact Dermatitis. 2016;74:217-21 pubmed publisher..Preservatives in cosmetics were significantly different according to source of production and type of cosmetics. ..
- Hou Y, Xing S, Shao J, Yin Z, Hao L, Yang T, et al. Synthesis of seven-membered iminosugars fused thiazolidin-4-one and benzthiazinan-4-one and their HIV-RT inhibitory activity. Carbohydr Res. 2016;429:105-12 pubmed publisher..11?µM and 2.73?µM, respectively. Structure-activity relationship analysis suggested that the phenyl group in the tricyclic azasugars was beneficial for their anti-HIV RT activity. ..
- Andrade Neto V, Pereira T, Canto Cavalheiro M, Torres Santos E. Imipramine alters the sterol profile in Leishmania amazonensis and increases its sensitivity to miconazole. Parasit Vectors. 2016;9:183 pubmed publisher..Using imipramine in combination with azoles may be advantageous for the treatment of leishmaniasis. ..
- Li Z, Zhang J, Liu X, Geng P, Ma J, Wang B, et al. Identification of thiazolo[5,4-d]pyrimidine derivatives as potent antiproliferative agents through the drug repurposing strategy. Eur J Med Chem. 2017;135:204-212 pubmed publisher..Western blot experiments indicated the expression changes of apoptosis-related proteins, including up-regulation of Bax and caspase-3/9, as well as down-regulation of Bcl-2. ..
- Matsuzaki N, Yamamoto Y, Murayama D, Katakawa Y, Mimura H, Kimura S, et al. Evaluation of Maltose-Induced Chemical Degradation at the Interface of Bilayer Tablets. Chem Pharm Bull (Tokyo). 2017;65:478-486 pubmed publisher..The results of this study have shown that chemical degradation can occur at the interface of bilayer tablets and that an alternative strategy is available to formulate more stable MB/SS bilayer tablets. ..
- Jiang M, Yu S, Yu Z, Sheng H, Li Y, Liu S, et al. XBP1 (X-Box-Binding Protein-1)-Dependent O-GlcNAcylation Is Neuroprotective in Ischemic Stroke in Young Mice and Its Impairment in Aged Mice Is Rescued by Thiamet-G. Stroke. 2017;48:1646-1654 pubmed publisher..Boosting prosurvival pathways to counterbalance the age-related decline in the brain's self-healing capacity could be a promising strategy to improve ischemic stroke outcome in aged brains. ..
- Napolitano L, Scalise M, Koyioni M, Koutentis P, Catto M, Eberini I, et al. Potent inhibitors of human LAT1 (SLC7A5) transporter based on dithiazole and dithiazine compounds for development of anticancer drugs. Biochem Pharmacol. 2017;143:39-52 pubmed publisher..Treatment of SiHa cells expressing hLAT1 at relatively high level, with the two most potent inhibitors led to cell death which was not observed after treatment with a compound exhibiting very poor inhibitory effect. ..
- Koifman E, Lipinski M, Escarcega R, Didier R, Kiramijyan S, Torguson R, et al. Comparison of Watchman device with new oral anti-coagulants in patients with atrial fibrillation: A network meta-analysis. Int J Cardiol. 2016;205:17-22 pubmed publisher..44 [0.09-2.14]). NOAC therapy was superior to warfarin for multiple outcomes while Watchman reduced hemorrhagic stroke. Further studies are needed to assess Watchman versus NOAC to optimize therapy for stroke prevention in AF patients. ..
- Leeds J. Antibacterials Developed to Target a Single Organism: Mechanisms and Frequencies of Reduced Susceptibility to the Novel Anti-Clostridium difficile Compounds Fidaxomicin and LFF571. Cold Spring Harb Perspect Med. 2016;6:a025445 pubmed publisher..Although there are several agents in development for treatment of CDI, this review summarizes the frequencies and mechanisms of C. difficile mutants displaying reduced susceptibility to FDX or LFF71. ..
- Asano A, Minoura K, Yamada T, Doi M. Conformational transformation of ascidiacyclamide analogues induced by incorporating enantiomers of phenylalanine, 1-naphthylalanine or 2-naphthylalanine. J Pept Sci. 2016;22:156-65 pubmed publisher..In particular, [d-1Nal]ASC showed the most significant transformation from the folded to the open structure in solution, and exhibited the strongest cytotoxicity toward HL-60 cells. ..
- von Heymann C, Rosenthal C, Kaufner L, Sander M. Management of direct oral anticoagulants-associated bleeding in the trauma patient. Curr Opin Anaesthesiol. 2016;29:220-8 pubmed publisher..Sufficiently powered studies with clinical and safety outcome measures are still missing for all specific antidotes at this time. ..
- Yin J, Babaoglu K, Brautigam C, Clark L, Shao Z, Scheuermann T, et al. Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors. Nat Struct Mol Biol. 2016;23:293-9 pubmed publisher..The orexin-receptor crystal structures are valuable tools for the design and development of selective orexin-receptor antagonists and agonists. ..
- Hanseeuw B, Betensky R, Schultz A, Papp K, Mormino E, Sepulcre J, et al. Fluorodeoxyglucose metabolism associated with tau-amyloid interaction predicts memory decline. Ann Neurol. 2017;81:583-596 pubmed publisher..Entorhinal tau was associated with frontal hypometabolism, but this dysfunction was not associated with memory loss. Ann Neurol 2017;81:583-596. ..
- Muñoz Gutiérrez C, Sepúlveda C, Caballero J, Palomo I, Fuentes E. Study of the interactions between Edaglitazone and Ciglitazone with PPAR? and their antiplatelet profile. Life Sci. 2017;186:59-65 pubmed publisher..Altogether, the more potent PPAR? agonist Edaglitazone seems to be a potent antiplatelet agent. ..
- Hilton M, Jarvis T, Ricketts D. The degradation rate of thiamethoxam in European field studies. Pest Manag Sci. 2016;72:388-97 pubmed publisher..They demonstrate that thiamethoxam will degrade to concentrations that are <10% of the maximum within a year of application, and will not accumulate in soil after repeated applications. ..
- Ma C, Jin S, Liu H, Xia K, Tang J, Wang K, et al. Thioflavin T as a fluorescence probe for label-free detection of T4 polynucleotide kinase/phosphatase and its inhibitors. Mol Cell Probes. 2015;29:500-502 pubmed publisher..01 unit/mL limit of detection, which is better than those with labeled fluorophores. Furthermore, T4 PNKP inhibition by the inhibitor heparin is shown, demonstrating the potential to screen suitable inhibitor drugs for T4 PNKP. ..
- Dan W, Geng H, Qiao J, Guo R, Wei S, Li L, et al. Efficient Synthesis and Antibacterial Evaluation of (Â±)-Yanglingmycin and Its Analogues. Molecules. 2016;21:96 pubmed publisher..91 Î¼gÂ·mL(-1)). The above results might lay the firm foundation for the design and synthesis of novel antibacterial drugs based on (Â±)-Yanglingmycin. ..
- Peters B, Gao Z, Zumkier U. Large-scale monitoring of effects of clothianidin-dressed oilseed rape seeds on pollinating insects in Northern Germany: effects on red mason bees (Osmia bicornis). Ecotoxicology. 2016;25:1679-1690 pubmed..High reproductive output and low parasitization rates indicated that Elado®-dressed oilseed rape did not cause any detrimental effects on the development or reproduction of mason bees. ..
- Wehling M, Collins R, Gil V, Hanon O, Hardt R, Hoffmeister M, et al. Appropriateness of Oral Anticoagulants for the Long-Term Treatment of Atrial Fibrillation in Older People: Results of an Evidence-Based Review and International Consensus Validation Process (OAC-FORTA 2016). Drugs Aging. 2017;34:499-507 pubmed publisher..For other vitamin-K antagonists regionally used in Europe, the lack of evidence should challenge current practice. ..
- Dornic N, Ficheux A, Bernard A, Roudot A. Adequacy of the default values for skin surface area used for risk assessment and French anthropometric data by a probabilistic approach. Food Chem Toxicol. 2017;106:386-392 pubmed publisher..This is of importance given that some studies show an increasing risk of developping skin sensitization among women. The disparities in anthropometric data across Europe should be taken into consideration. ..
- Nong W, Zhao A, Wei J, Lin X, Wang L, Lin C. Synthesis and biological evaluation of a new series of cinnamic acid amide derivatives as potent haemostatic agents containing a 2-aminothiazole substructure. Bioorg Med Chem Lett. 2017;27:4506-4511 pubmed publisher..22?mol/L). Furthermore, the relationship between the functional groups of the compounds and the corresponding blood coagulant activity was explored in this study. ..
- Ogawa H, Takyu R, Morimoto H, Toei S, Sakon H, Goto S, et al. Cell proliferation potency is independent of FGF4 signaling in trophoblast stem cells derived from androgenetic embryos. J Reprod Dev. 2016;62:51-8 pubmed publisher..In conclusion, the paternal genome facilitated the proliferation of trophoblast cells without FGF4 signaling. ..