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https://www.readbyqxmd.com/read/28107776/activity-based-probes-for-the-multicatalytic-proteasome
#1
REVIEW
David S Hewings, John A Flygare, Ingrid E Wertz, Matthew Bogyo
Proteasomes are multisubunit protease complexes responsible for degrading most intracellular proteins. In addition to removing damaged proteins, they regulate many important cellular processes through the controlled degradation of transcription factors, cell cycle regulators and enzymes. Eukaryotic proteasomes have three catalytic subunits, β1, β2 and β5, that each have different substrate specificities. Additionally, although we know that diverse cell types express proteasome variants with distinct activity and specificity profiles, the functions of these different pools of proteasomes are not fully understood...
January 20, 2017: FEBS Journal
https://www.readbyqxmd.com/read/28107773/safety-and-effectiveness-of-tofogliflozin-in-elderly-japanese-patients-with-type-2-diabetes-mellitus-a-post-marketing-study-j-step-el-study
#2
Kazunori Utsunomiya, Naoki Shimmoto, Masayuki Senda, Yuji Kurihara, Ryoji Gunji, Shoko Fujii, Seigo Kakiuchi, Hisataka Fujiwara, Hiroyuki Kameda, Masahiro Tamura, Kohei Kaku
AIMS/INTRODUCTION: While sodium glucose cotransporter 2 inhibitors are a promising treatment for type 2 diabetes mellitus, they are associated with concerns about specific adverse drug reactions. We conducted a 1-year post-marketing study of tofogliflozin, a novel agent in this class, in Japanese elderly patients with type 2 diabetes mellitus. MATERIALS AND METHODS: This was a prospective, observational, and multicenter post-marketing study conducted in the context of routine clinical practice...
January 20, 2017: Journal of Diabetes Investigation
https://www.readbyqxmd.com/read/28107768/arabidopsis-protein-s-acyl-transferase4-mediates-root-hair-growth
#3
Zhi-Yuan Wan, Sen Chai, Fu-Rong Ge, Qiang-Nan Feng, Yan Zhang, Sha Li
Polar growth of root hairs is critical for plant survival and necessitates fine-tuned ROP signaling. Multiple ROP regulators participate in root hair growth. However, protein S-acyl transferases (PATs), mediating the S-acylation and membrane partitioning of ROPs, are yet to be found. By using a reverse genetic approach, combining fluorescence probes, pharmacological drugs, site-directed mutagenesis, and genetic analysis with related root-hair mutants, we have identified and characterized an Arabidopsis PAT, which may be responsible for ROP2 S-acylation in root hairs...
January 20, 2017: Plant Journal: for Cell and Molecular Biology
https://www.readbyqxmd.com/read/28107750/effect-of-clinically-approved-hdac-inhibitors-on-plasmodium-leishmania-and-schistosoma-parasite-growth
#4
Ming Jang Chua, Megan S J Arnold, Weijun Xu, Julien Lancelot, Suzanne Lamotte, Gerald F Späth, Eric Prina, Raymond J Pierce, David P Fairlie, Tina S Skinner-Adams, Katherine T Andrews
Malaria, schistosomiasis and leishmaniases are among the most prevalent tropical parasitic diseases and each requires new innovative treatments. Targeting essential parasite pathways, such as those that regulate gene expression and cell cycle progression, is a key strategy for discovering new drug leads. In this study, four clinically approved anti-cancer drugs (Vorinostat, Belinostat, Panobinostat and Romidepsin) that target histone/lysine deacetylase enzymes were examined for in vitro activity against Plasmodium knowlesi, Schistosoma mansoni, Leishmania amazonensis and L...
December 23, 2016: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/28107736/crystal-structures-binding-interactions-and-adme-evaluation-of-brain-penetrant-n-substituted-indazole-5-carboxamides-as-subnanomolar-selective-monoamine-oxidase-b-and-dual-mao-a-b-inhibitors
#5
Nikolay T Tzvetkov, Hans-Georg Stammler, Beate Neumann, Silvia Hristova, Liudmil Antonov, Marcus Gastreich
The pharmacological and physicochemical analysis of structurally optimized N-alkyl-substituted indazole-5-carboxamides, developed as potential drug and radioligand candidates for the treatment and diagnosis of Parkinson's disease (PD) and other neurological disorders, is reported. Recent efforts have been focused on the development of subnanomolar potent, selective MAO-B (N1-alkyl-substituted compounds 12a-14a and 15) and dual active MAO-A/B (N2-methylated compounds 12b-14b) inhibitors with nanomolar potency towards MAO-B and moderately active against MAO-A enzyme, respectively...
January 11, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28107705/incorporation-of-antimicrobial-peptides-in-nanostructured-lipid-membrane-mimetic-bilayer-cubosomes
#6
Thomas G Meikle, Alexandru Zabara, Lynne J Waddington, Frances Separovic, Calum J Drummond, Charlotte E Conn
The inverse bicontinuous lipidic cubic phase offers a simple and robust membrane mimetic with the ability to encapsulate peptides, potentially increasing bioavailability, while also offering a platform from which functionalized, targeted nanoparticles can be developed. Herein we have investigated the use of a number of cubic phase nanoparticle systems with encapsulated antimicrobial peptides gramicidin A', melittin, and alamethicin. The optimal peptide loading ranges, over which cubic symmetry was retained, were determined using small angle X-ray scattering...
January 8, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28107700/comparative-pharmacokinetics-of-eight-major-bioactive-components-in-normal-and-bacterial-diarrhea-mini-pigs-after-oral-administration-of-gegen-qinlian-decoction
#7
Xiao Ling, Yuqiang Xiang, Qingfa Tang, Feilong Chen, Xiaomei Tan
Healthy animals are most widely used in current pharmacokinetic(PK) studies. However, neglecting the effects of specific diseases on drug absorption results in the PK parameters of those experiments not accurately reflecting in vivo drug concentration changes during treatment. In this study, an E. coli infective diarrheal minipig model was applied to explore the pharmacokinetics of Gegen Qinlian decoction (GQD). A simple and rapid ultrahigh performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method was developed to determine the concentrations of the eight GQD components in minipig plasma after intragastric administration of GQD...
January 11, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28107698/the-natural-flavonoid-apigenin-sensitizes-human-cd44-prostate-cancer-stem-cells-to-cisplatin-therapy
#8
Suat Erdogan, Kader Turkekul, Rıza Serttas, Zeynep Erdogan
Prostate cancer (PCa) is the second most common type of cancer and the fifth leading cause of cancer-related death among men. Development of chemoresistance, tumor relapse and metastasis remain major barriers to effective treatment and all been identified to be associated with cancer stem cells (CSCs). Natural flavonoids such as apigenin have been shown to have the ability to improve the therapeutic efficacy of common chemotherapy agents through CSCs sensitization. Thus, the aim of this study was to evaluate the combination of apigenin with cisplatin on CD44(+) PCa stem cell growth and migration...
January 17, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28107695/antibacterial-activity-computational-analysis-and-host-toxicity-study-of-thymol-sulfonamide-conjugates
#9
Shasank S Swain, Sudhir K Paidesetty, Rabindra N Padhy
Methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin resistant Enterococcus faecalis (VRE) are notorious pathogenic multidrug resistant (MDR) bacteria in both hospital and community sectors, and today the first antibacterial drug sulfamethoxazole is ineffective. The monoterpene phenol, thymol was conjugated with seven sulfa drug derivatives individually, adopting the dye-azo synthesis protocol, and conjugates were characterized using spectral analysis techniques such as, UV, FTIR, MS, HPLC, (1)H NMR, (13)C NMR and SEM...
January 17, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28107690/time-domain-nmr-as-a-new-process-monitoring-method-for-characterization-of-pharmaceutical-hydrates
#10
Stefanie Ulrike Schumacher, Benno Rothenhäusler, Alf Willmann, Jürgen Thun, Regina Moog, Martin Kuentz
Hydrates are of great pharmaceutical relevance and even though they have been characterized thoroughly by various analytical techniques, there is barely literature available on molecular mobility of the hydrate water studied by NMR relaxation in the time domain. The aim of this work was to examine the possibility of differentiating hydration states of drugs by (1)H time domain NMR (TD-NMR) regarding spin-spin and spin-lattice relaxation times (T2 and T1) using benchtop equipment. Caffeine and theophylline were selected as model compounds and binary mixtures of hydrate to anhydrate were analyzed for each drug using a spin echo and inversion recovery pulse sequence...
January 9, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28107680/a-randomized-clinical-trial-of-buprenorphine-for-prisoners-findings-at-12-months-post-release
#11
Michael S Gordon, Timothy W Kinlock, Robert P Schwartz, Kevin E O'Grady, Terrence T Fitzgerald, Frank J Vocci
BACKGROUND: This study examined whether starting buprenorphine treatment prior to prison and after release from prison would be associated with better drug treatment outcomes and whether males and females responded differently to the combination of in-prison treatment and post-release service setting. METHODS: Study design was a 2 (In-Prison Treatment: Condition: Buprenorphine Treatment: vs. Counseling Only)×2 [Post-Release Service Setting Condition: Opioid Treatment: Program (OTP) vs...
January 11, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28107674/mitochondrial-serine-hydroxymethyltransferase-2-is-a-potential-diagnostic-and-prognostic-biomarker-for-human-glioma
#12
Bo Wang, Wei Wang, ZhiZhong Zhu, XueBin Zhang, Fan Tang, Dong Wang, Xi Liu, XiaoLing Yan, Hao Zhuang
OBJECTIVE: Scholars have gradually come to appreciate the relevance of serine and glycine metabolism. Recently, researchers have discovered that mitochondrial serine hydroxymethyltransferase 2 (SHMT2) is overexpressed in various types of cancer. However, the function of SHMT2 in glioma is not clear. In this study, we sought to examine the expression of SHMT2 in glioma, the association between SHMT2 expression and clinicopathological characteristics, and the association of SHMT2 expression with prognosis in glioma patients...
January 16, 2017: Clinical Neurology and Neurosurgery
https://www.readbyqxmd.com/read/28107670/pharmaceutical-opioid-use-among-oral-and-intravenous-users-in-australia-a-qualitative-comparative-study
#13
George Dertadian, Jenny Iversen, Thomas C Dixon, Katrina Sotiropoulos, Lisa Maher
BACKGROUND: Between 1992 and 2012 dispensing episodes for pharmaceutical opioids (PO) in Australia increased from 500000 to 7500000. In the US, increases in the prescription of PO have been linked to increases in opioid-related morbidity and mortality and transitions to heroin injection. However, Australian data indicate that morbidity and mortality related to PO are relatively low, particularly when compared to heroin and other drugs. This paper explores the characteristics and patterns of non-medical pharmaceutical opioid (NMPO) use among a sample of young people in Sydney, Australia...
January 17, 2017: International Journal on Drug Policy
https://www.readbyqxmd.com/read/28107651/one-ring-to-fight-them-all-the-sulfazecin-story
#14
Daniel Braga, Gerald Lackner
In this issue of Cell Chemical Biology, Li et al. (2017) report on the biosynthesis of the monobactam sulfazecin by Pseudomonas acidophila and hypothesize a novel mechanism of β-lactam ring formation. As monobactam antibiotics are unaffected by some emerging resistance mechanisms (particularly metallo-β-lactamases), this discovery opens prospects to engineer β-lactam antibiotics against multi-drug resistant pathogens.
January 19, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/28107633/binding-and-proton-blockage-by-amantadine-variants-of-the-influenza-m2wt-and-m2s31n-explained
#15
Christina Tzitzoglaki, Anna K Wright, Kathrin-Maria Freudenberger, Anja Hoffmann, Ian Tietjen, Ioannis Stylianakis, Felix Kolarov, David Fedida, Michaela Schmidtke, Guenter Gauglitz, Timothy A Cross, Antonios Kolocouris
While aminoadamantanes are well-established inhibitors of the influenza A M2 proton channel, the mechanisms by which they are rendered ineffective against M2S31N are unclear. Solid state NMR, isothermal titration calorimetry, electrophysiology, anti-viral assays and molecular dynamics simulations suggest stronger binding interactions for aminoadamantanes to M2WT compared to negligible or weak binding to M2S31N. This is due to reshaping of the M2pore when N31 is present, which in contrast to WT, leads: A) to the loss of the V27 pocket for the adamantyl cage and to a predominant orientation of the ligand's ammonium group toward the N-terminus and, B) to the lack of a helical kink upon ligand binding...
January 20, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28107624/tocilizumab-alendronate-conjugate-for-treatment-of-rheumatoid-arthritis
#16
Hwiwon Lee, Suk Ho Bhang, Jeong Ho Lee, Hyemin Kim, Sei Kwang Hahn
An autoimmune disease of rheumatoid arthritis (RA) causes severe inflammation on the synovial membrane, which results in the destruction of articular cartilage and bone. Here, Tocilizumab (TCZ) - Alendronate (ALD) conjugate is synthesized for the early intervention of RA. A humanized monoclonal antibody of TCZ shows an immunosuppressive effect, targeting interleukin-6 (IL-6) receptor in the RA pathogenesis. ALD is an anti-inflammatory bisphosphonate drug which can bind to the exposed bone surface. ALD is conjugated selectively to N-glycan on Fc region of TCZ using a chemical linker of 3-(2-pyridyldithio) propionyl hydrazide (PDPH) - poly(ethylene glycol) - N-hydroxysuccinimide (PDPH-PEG-NHS)...
January 20, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28107617/fabrication-of-nanostructured-mesoporous-germanium-for-applications-in-laser-desorption-ionization-mass-spectrometry
#17
Hazem H Abdelmaksoud, Taryn M Guinan, Nicolas H Voelcker
Surface-assisted laser desorption/ionization mass spectrometry (SALDI-MS) is a high-throughput analytical technique ideally suited for small molecule detection from different bodily fluids (e.g. saliva, urine, and blood plasma). Many SALDI-MS substrates require complex fabrication processes and further surface modifications. Furthermore, some substrates show instability upon exposure to ambient conditions and need to be kept under special inert conditions. We have successfully optimized mesoporous germanium (meso-pGe) using bipolar electrochemical etching (BEE) and efficiently applied meso-pGe as a SALDI-MS substrate for the detection of cocaine in the context of workplace, roadside, and anti-addictive drug compliance...
January 20, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28107598/dropout-in-clinical-trials-of-pharmacologic-treatment-for-methamphetamine-dependence-the-role-of-initial-abstinence
#18
Ryan Cook, Brendan Quinn, Keith Heinzerling, Steve Shoptaw
BACKGROUND AND AIMS: High rates of loss to follow-up represent a significant challenge to clinical trials of pharmacologic treatments for methamphetamine (MA) use disorder. We aimed to estimate and test the relationship between achieving and maintaining abstinence in the initial weeks of study participation and subsequent retention in such trials, hypothesizing that participants able to achieve early abstinence would be less likely to drop out. DESIGN: Data from four randomized controlled trials (RCTs) of pharmacologic treatments for MA use disorder were pooled and analyzed using a random-effects approach...
January 20, 2017: Addiction
https://www.readbyqxmd.com/read/28107585/treatment-and-primary-prevention-in-people-who-inject-drugs-for-chronic-hepatitis-c-infection-is-elimination-possible-in-a-high-prevalence-setting
#19
I Gountas, V Sypsa, O Anagnostou, N K Martin, P Vickerman, E Kafetzopoulos, A Hatzakis
AIMS: To project the impact of scaling up oral antiviral therapy and harm reduction on chronic hepatitis C (CHC) prevalence and incidence among people who inject drugs (PWID) in Greece, to estimate the relationship between required treatment levels and expansion of harm reduction programs to achieve specific targets and to examine whether hepatitis C viruse (HCV) elimination among PWID is possible in this high prevalence setting. DESIGN: A dynamic discrete time, stochastic individual-based model was developed to simulate HCV transmission among PWID incorporating the effect of HCV treatment and harm reduction strategies, and allowing for reinfection following treatment...
January 20, 2017: Addiction
https://www.readbyqxmd.com/read/28107576/non-invasive-anaesthetic-methods-for-dermatological-laser-procedures-a-systematic-review
#20
REVIEW
K Greveling, E P Prens, L Liu, M B A van Doorn
Pain is a common side-effect of dermatological laser procedures. Non-invasive anaesthetic drugs and anaesthetic procedures can be used to provide pain relief and increase patient satisfaction and treatment efficacy. However, it remains unclear which method provides the best pain relief. The objective of this systematic review was therefore to assess the efficacy and safety of non-invasive anaesthetic methods during dermatological laser procedures. A systematic literature search was conducted. Randomized and non-randomized controlled clinical trials (RCTs and CCTs) were included...
January 20, 2017: Journal of the European Academy of Dermatology and Venereology: JEADV
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