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https://www.readbyqxmd.com/read/29454190/potholing-of-the-hydrophobic-heme-oxygenase-1-western-region-for-the-search-of-potent-and-selective-imidazole-based-inhibitors
#1
Loredana Salerno, Emanuele Amata, Giuseppe Romeo, Agostino Marrazzo, Orazio Prezzavento, Giuseppe Floresta, Valeria Sorrenti, Ignazio Barbagallo, Antonio Rescifina, Valeria Pittalà
Here we report the design, synthesis, and molecular modeling of new potent and selective imidazole-based HO-1 inhibitors in which the imidazole nucleus and the hydrophobic groups are linked by a phenylethanolic spacer. Most of the tested compounds showed a good inhibitor activity with IC 50 values in the low micromolar range, with two of them (1b and 1j) exhibiting also high selectivity toward HO-2. These results were obtained by the idea of potholing the entire volume of the principal hydrophobic western region with an appropriate ligand volume...
February 9, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29451361/development-of-a-focused-library-of-triazole-linked-privileged-structure-based-conjugates-leading-to-the-discovery-of-novel-phenotypic-hits-against-protozoan-parasitic-infections
#2
Elisa Uliassi, Lorna Piazzi, Federica Belluti, Andrea Mazzanti, Marcel Kaiser, Reto Brun, Carolina B Moraes, Lucio H Freitas-Junior, Sheraz Gul, Maria Kuzikov, Bernhard Ellinger, Chiara Borsari, Maria Paola Costi, Maria Laura Bolognesi
Protozoan infections caused by Plasmodium, Leishmania, and Trypanosoma spp. contribute significantly to the burden of infectious diseases worldwide, causing severe morbidity and mortality. The inadequacy of available treatments calls for cost- and time-effective drug discovery endeavors. To this end, we envisaged the triazole linkage of privileged structures as an effective drug design strategy to generate a focused library of high-quality compounds. The versatility of this approach was combined with the feasibility of a phenotypic assay, integrated with early ADME-tox profiling...
February 16, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29404794/computational-assessment-of-pharmacokinetics-and-biological-effects-of-some-anabolic-and-androgen-steroids
#3
Marin Roman, Diana Larisa Roman, Vasile Ostafe, Alecu Ciorsac, Adriana Isvoran
PURPOSE: The aim of this study is to use computational approaches to predict the ADME-Tox profiles, pharmacokinetics, molecular targets, biological activity spectra and side/toxic effects of 31 anabolic and androgen steroids in humans. METHODS: The following computational tools are used: (i) FAFDrugs4, SwissADME and admetSARfor obtaining the ADME-Tox profiles and for predicting pharmacokinetics;(ii) SwissTargetPrediction and PASS online for predicting the molecular targets and biological activities; (iii) PASS online, Toxtree, admetSAR and Endocrine Disruptomefor envisaging the specific toxicities; (iv) SwissDock to assess the interactions of investigated steroids with cytochromes involved in drugs metabolism...
February 5, 2018: Pharmaceutical Research
https://www.readbyqxmd.com/read/29398302/organs-on-a-chip-current-applications-and-consideration-points-for-in%C3%A2-vitro-adme-tox-studies
#4
REVIEW
Seiichi Ishida
Assay systems using in vitro cultured cells are increasingly applied for evaluation of the efficacy, safety, and toxicity of drug candidates. In vitro cell-based assays have two main applications in the drug discovery process: searching for a compound that is effective against the target disease (seed investigation) and confirmation of safety during use of the identified compounds (safety assessment). Currently available in vitro cell-based assays have been designed to evaluate the efficacy and toxicity in single organs, but the in vivo pharmacokinetics and pharmacodynamics of the administered drug candidates have not been considered...
January 11, 2018: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29390151/high-co2-hypoxia-responsive-transcription-factor-network-involved-in-persimmon-fruit-deastringency
#5
Qing-Gang Zhu, Zi-Yuan Gong, Miao-Miao Wang, Xian Li, Donald Grierson, Xue-Ren Yin, Kun-Song Chen
Plant responses to anaerobic environments are regulated by ethylene response factors (ERFs) in both vegetative and productive organs, but the roles of other transcription factors (TFs) in hypoxia responses are poorly understood. Here, eight TFs (DkbHLH1, DkMYB9/10/11, DkRH2-1, DkGT3-1, DkAN1-1, DkHSF1) were shown to be strongly up-regulated by AHCA (artificial high CO2 atmosphere, 1 % O2 and 95 % CO2). Dual-luciferase assay indicated some TFs were activators of previously characterized DkERFs, including DkMYB10 for the DkERF9 promoter, DkERF18/19 and DkMYB6 for the DkERF19 promoter, DkERF21/22 for the DkERF10 promoter...
January 30, 2018: Journal of Experimental Botany
https://www.readbyqxmd.com/read/29376224/long-term-efficacy-of-botulinum-neurotoxin-a-treatment-for-essential-blepharospasm
#6
Seunghyun Lee, Sangrye Park, Helen Lew
PURPOSE: In the present study, we investigated the treatment efficacy and clinical outcomes of botulinum neurotoxin-A (BoNT-A) administered for longer than 5 years to patients with essential blepharospasm. METHODS: We retrospectively reviewed 19 patients (male : female = 8 : 11) diagnosed with essential blepharospasm between March 2006 and July 2016 who underwent BoNT-A injections for over 5 years and were followed. Efficacy of 297 injections of Botox (n = 162), Meditoxin (n = 75), Hugel-tox (n = 40), or Dysport (n = 20) was based on the symptom improvement score at the final injection (-1, worse; 0, same; 1, better)...
January 24, 2018: Korean Journal of Ophthalmology: KJO
https://www.readbyqxmd.com/read/29370758/transcriptome-sequencing-of-the-human-pathogen-corynebacterium-diphtheriae-nctc-13129-provides-detailed-insights-into-its-transcriptional-landscape-and-into-dtxr-mediated-transcriptional-regulation
#7
Manuel Wittchen, Tobias Busche, Andrew H Gaspar, Ju Huck Lee, Hung Ton-That, Jörn Kalinowski, Andreas Tauch
BACKGROUND: The human pathogen Corynebacterium diphtheriae is the causative agent of diphtheria. In the 1990s a large diphtheria outbreak in Eastern Europe was caused by the strain C. diphtheriae NCTC 13129. Although the genome was sequenced more than a decade ago, not much is known about its transcriptome. Our aim was to use transcriptome sequencing (RNA-Seq) to close this knowledge gap and gain insights into the transcriptional landscape of a C. diphtheriae tox+ strain. RESULTS: We applied two different RNA-Seq techniques, one to retrieve 5'-ends of primary transcripts and the other to characterize the whole transcriptional landscape in order to gain insights into various features of the C...
January 25, 2018: BMC Genomics
https://www.readbyqxmd.com/read/29369159/substance-associated-elevations-in-monocyte-activation-among-methamphetamine-users-with-treated-hiv-infection
#8
Adam W Carrico, Emily M Cherenack, Margaret E Roach, Elise D Riley, Olorunleke Oni, Samantha E Dilworth, Steven Shoptaw, Peter Hunt, Sabita Roy, Suresh Pallikkuth, Savita Pahwa
OBJECTIVE: Microbial translocation and monocyte activation predict mortality in treated HIV. We examined whether substance use independently contributes to these pathophysiologic processes. DESIGN: Cross-sectional study at baseline for a randomized controlled trial. METHODS: HIV-positive, methamphetamine-using men who have sex with men (MSM) with undetectable HIV viral load (< 40 copies/mL) were enrolled. We examined if plasma biomarkers of monocyte activation and intestinal barrier integrity were associated with the following: 1) reactive urine toxicology results (Tox+) for stimulants (i...
January 23, 2018: AIDS
https://www.readbyqxmd.com/read/29324927/hematopoiesis-is-prognostic-for-toxicity-and-survival-of-223radium-treatment-in-patients-with-metastatic-castration-resistant-prostate-cancer
#9
A Leisser, M Nejabat, M Hartenbach, H Duan, S F Shariat, G Kramer, M Krainer, M Hacker, A R Haug
OBJECTIVE: We evaluated the impact of pre-therapeutic hematopoiesis on survival, hematotoxicity (HT) and number of 223Radium (223Ra) treatments in patients with metastatic castration-resistant prostate cancer. SUBJECTS AND METHOD: Hemoglobin-levels (Hb), the number of platelets (Plts), leukocytes (Leuk), and survival data were collected in 56 patients treated with 223Ra. Pre-therapeutic hematopoiesis as well as adverse events during and after therapy were scored (grade 0-4) according to the CTCAE recommendations...
September 2017: Hellenic Journal of Nuclear Medicine
https://www.readbyqxmd.com/read/29315692/comprehensive-review-of-cardiovascular-toxicity-of-drugs-and-related-agents
#10
REVIEW
Přemysl Mladěnka, Lenka Applová, Jiří Patočka, Vera Marisa Costa, Fernando Remiao, Jana Pourová, Aleš Mladěnka, Jana Karlíčková, Luděk Jahodář, Marie Vopršalová, Kurt J Varner, Martin Štěrba
Cardiovascular diseases are a leading cause of morbidity and mortality in most developed countries of the world. Pharmaceuticals, illicit drugs, and toxins can significantly contribute to the overall cardiovascular burden and thus deserve attention. The present article is a systematic overview of drugs that may induce distinct cardiovascular toxicity. The compounds are classified into agents that have significant effects on the heart, blood vessels, or both. The mechanism(s) of toxic action are discussed and treatment modalities are briefly mentioned in relevant cases...
January 5, 2018: Medicinal Research Reviews
https://www.readbyqxmd.com/read/29286521/impact-of-chronic-blood-viral-infection-on-lymphocyte-telomere-length-in-chornobyl-clean-up-workers-in-a-remote-period-after-radiation-exposure
#11
I M Ilienko, O V Lyaskivska, O A Belayev, O Y Pleskach, V I Shinkarenko, D A Bazyka
OBJECTIVE: To assess whether telomere length in lymphocytes of Chornobyl clean up workers at a late period 30 years after the exposure to ionizing radiation is influenced by a chronic blood viral infection and to determine role of viral carriage in cellular senescence. PATIENTS AND METHODS: Study group included 70 Chornobyl cleanup male workers 30 years after exposure {doses of external exposure (602.67 ± 114.19) mSv (M ± m); age (59.75 ± 0.82) yrs}. Relative telomere length (RTL) was analysed by fluorescence in situ hybridization and flow cytometry, immune cell subsets by standard combinations of monoclonal antibodies (CD45/14, CD3/19, CD4/8, CD3/HLADR, CD3/16/56, TCRγδ) and flow cytometry; antiviral immunity was performed determining the chronic phase antibodies to viruses: Hepatitis C (HCV), Cytomegalovirus (CMV), Toxoplasma gondii (TOX), Herpes simplex (HSV) and Epstein Barr virus (EBV VCA IgG and EBV NA IgG)...
December 2017: Problemy Radiat︠s︡iĭnoï Medyt︠s︡yny Ta Radiobiolohiï
https://www.readbyqxmd.com/read/29286347/anticonvulsant-activity-of-halogen-substituted-cinnamic-acid-derivatives-and-their-effects-on-glycosylation-of-ptz-induced-chronic-epilepsy-in-mice
#12
Ye Cuan, Xirui He, Yuhui Zhao, Jiajun Yang, Yajun Bai, Yin Sun, Qiang Zhang, Zefeng Zhao, Xiaoyang Wei, Xiaohui Zheng
Epilepsy is a common chronic neurological disorder disease, and there is an urgent need for the development of novel anticonvulsant drugs. In this study, the anticonvulsant activities and neurotoxicity of 12 cinnamic acid derivatives substituted by fluorine, chlorine, bromine, and trifluoromethyl groups were screened by the maximal electroshock seizure (MES) and rotarod tests (Tox). Three of the tested compounds (compounds 3, 6 and 12) showed better anticonvulsant effects and lower neurotoxicity. They showed respective median effective dose (ED50) of 47...
December 29, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29286075/genome-expression-profiling-predicts-the-molecular-mechanism-of-peripheral-myelination
#13
Xiaoming Wu
The present study aimed to explore the molecular mechanism of myelination in the peripheral nervous system (PNS) based on genome expression profiles. Microarray data (GSE60345) was acquired from the Gene Expression Omnibus database. Differentially expressed genes (DEGs) were integrated and subsequently subjected to pathway and term enrichment analysis. A protein‑protein interaction network was constructed and the top 200 DEGs according to their degree value were further subjected to pathway enrichment analysis...
December 22, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29242531/long-noncoding-rna-expression-profile-reveals-lncrnas-signature-associated-with-extracellular-matrix-degradation-in-kashin-beck-disease
#14
Cuiyan Wu, Huan Liu, Feng'e Zhang, Wanzhen Shao, Lei Yang, Yujie Ning, Sen Wang, Guanghui Zhao, Byeong Jae Lee, Mikko Lammi, Xiong Guo
Kashin-Beck disease (KBD) is a deformative, endemic osteochondropathy involving degeneration and necrosis of growth plates and articular cartilage. The pathogenesis of KBD is related to gene expression and regulation mechanisms, but long noncoding RNAs (lncRNAs) in KBD have not been investigated. In this study, we identified 316 up-regulated and 631 down-regulated lncRNAs (≥ 2-fold change) in KBD chondrocytes using microarray analysis, of which more than three-quarters were intergenic lncRNAs and antisense lncRNAs...
December 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29237788/naat-quantitation-as-predictor-of-toxin-presence-in-clostridium-difficile-infection
#15
M J T Crobach, N Duszenko, E M Terveer, C M Verduin, E J Kuijper
Multi-step algorithmic testing in which a sensitive nucleic acid amplification test (NAAT) is followed by a specific toxin A and B Enzyme Immunoassay (Tox A/B EIA) is among the most accurate methods for Clostridium difficile infection (CDI) diagnosis. The obvious shortcoming of this approach is that multiple tests must be performed to establish a CDI diagnosis, which may delay treatment. As such, we sought to determine whether a preliminary diagnosis could be made on the basis of the quantitative result of the first test in algorithmic testing, which provides a measure of organism burden...
December 13, 2017: Journal of Clinical Microbiology
https://www.readbyqxmd.com/read/29212448/from-genomes-to-genotypes-molecular-epidemiological-analysis-of-chlamydia-gallinacea-reveals-a-high-level-of-genetic-diversity-for-this-newly-emerging-chlamydial-pathogen
#16
Weina Guo, Martina Jelocnik, Jing Li, Konrad Sachse, Adam Polkinghorne, Yvonne Pannekoek, Bernhard Kaltenboeck, Jiansen Gong, Jinfeng You, Chengming Wang
BACKGROUND: Chlamydia (C.) gallinacea is a recently identified bacterium that mainly infects domestic chickens. Demonstration of C. gallinacea in human atypical pneumonia suggests its zoonotic potential. Its prevalence in chickens exceeds that of C. psittaci, but genetic and genomic research on C. gallinacea is still at the beginning. In this study, we conducted whole-genome sequencing of C. gallinacea strain JX-1 isolated from an asymptomatic chicken, and comparative genomic analysis between C...
December 6, 2017: BMC Genomics
https://www.readbyqxmd.com/read/29211817/qtwist-analysis-of-the-recourse-trial-of-trifluridine-tipiracil-in-metastatic-colorectal-cancer
#17
Josep Tabernero, Eric Van Cutsem, Atsushi Ohtsu, Nadia Amellal, Stéphanie Cadour, Ronan Fougeray, Benjamin Haffemayer, Robert J Mayer
Purpose: A Quality-adjusted Time WIthout Symptoms of disease or Toxicity (QTWiST) analysis was carried out to assess quality-adjusted survival time in the RECOURSE trial of trifluridine/tipiracil versus placebo in pretreated metastatic colorectal cancer (mCRC). Methods: Duration of overall survival in the RECOURSE trial (n=798 patients) was partitioned into three discrete health states: toxicity (TOX), time without symptoms or toxicity (TWIST) and relapse (REL)...
2017: ESMO Open
https://www.readbyqxmd.com/read/29194347/in-vivo-and-in-vitro-activities-and-adme-tox-profile-of-a-quinolizidine-modified-4-aminoquinoline-a-potent-anti-p-falciparum-and-anti-p-vivax-blood-stage-antimalarial
#18
Nicoletta Basilico, Silvia Parapini, Anna Sparatore, Sergio Romeo, Paola Misiano, Livia Vivas, Vanessa Yardley, Simon L Croft, Annette Habluetzel, Leonardo Lucantoni, Laurent Renia, Bruce Russell, Rossarin Suwanarusk, Francois Nosten, Giulio Dondio, Chiara Bigogno, Daniela Jabes, Donatella Taramelli
Natural products are a prolific source for the identification of new biologically active compounds. In the present work, we studied the in vitro and in vivo antimalarial efficacy and ADME-Tox profile of a molecular hybrid (AM1) between 4-aminoquinoline and a quinolizidine moiety derived from lupinine (Lupinus luteus). The aim was to find a compound endowed with the target product profile-1 (TCP-1: molecules that clear asexual blood-stage parasitaemia), proposed by the Medicine for Malaria Venture to accomplish the goal of malaria elimination/eradication...
December 1, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29194289/lack-of-detection-of-new-amphetamine-like-drugs-using-conventional-urinary-immunoassays
#19
A Begeman, E J F Franssen
BACKGROUND: The number of reports of serious adverse effects and intoxication after the use of the new drug 4-fluoroamphetamine (4-FA) increases. At the Emergency Department of the OLVG-Oost Hospital in Amsterdam an on-site drug test, the Triage® TOX Drug Screen, is available to assist in a rapid diagnosis. In less urgent cases, an EMIT® II Plus immunoassay is used to determine semi-quantitatively the presence of drugs of abuse. The antibodies in these immunoassays are designed to detect classic drugs of abuse and its urinary metabolites...
November 29, 2017: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/29193815/introduction-to-special-section-on-using-pools-to-generate-good-laboratory-practice-tox-or-other-non-clinical-material-to-accelerate-development-timelines
#20
Christine DeMaria, Trent Munro
No abstract text is available yet for this article.
November 28, 2017: Biotechnology Progress
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