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The optimization of the lead compound was initiated and the
2019-12-05
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic GSK461364 moiety with other functional groups led to loss of functional activity against EP4 receptor. A
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br Material and Methods br Results
2019-12-05
Material and Methods Results and Discussion Conclusions Two chemical coupling agents, BTDE and CDI, were used to activate the free hydroxyl groups of plant cellulose powder and OPH from Flavobacterium ATCC 27551 immobilized on modified carriers by covalent linkages. The highest immobilizati
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br Materials and methods BAECs
2019-12-05
Materials and methods BAECs (CAB30405, Toyobo Life Science, Osaka, Japan) were cultured in Dulbecco’s Modified Eagle Medium supplemented with 10% Fetal Bovine Serum (04-001-1A-US, Biological Industries, Kibbutz Beit Haemek, Israel) and 1% antibiotic-antifungal agent containing 10,000-μg/mL penici
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Introduction Taenia solium is the causative agent of human t
2019-12-05
Introduction Taenia solium is the causative agent of human taeniasis/cysticercosis and porcine cysticercosis, a major health problem and a veterinary economic challenge in developing countries of Latin America, Africa, and Asia. In Mexico, approximately 500 human neurocysticercosis cases were repor
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br Funding This work was partly
2019-12-05
Funding This work was partly supported by the grant ‘Maria Grazia Cuccoli’ from Fondazione Cassa di Risparmio di Bologna. Declarations of interest Acknowledgements Introduction The main strategy of oncolytic viral therapy is based on the fact that naturally occurring or engineered virus
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The differences between ground and
2019-12-05
The differences between ground and transition state properties are exemplified by a comparison of our human–yeast results with those of a structural study of possible differences in ubiquitin-Uba-1 binding in yeast (known structure) with human (simulated in [12]). Their discussion focuses on Ubiquit
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Acknowledgments br Introduction Diabetes mellitus DM is
2019-12-05
Acknowledgments Introduction Diabetes mellitus (DM) is a multifactorial disease [1] associated with serious comorbidities. This condition has recently reached epidemic proportions, as its occurrence has exponentially increased in the general population. Over 400 million people worldwide were est
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Two primary members of the TRIM family TRIM and
2019-12-04
Two primary members of the TRIM family – TRIM5α and TRIM25 – function as antiviral effector and immune regulator, respectively. TRIM5α is one of the best characterized members of the TRIM family (both structurally and functionally) and reported to be an important ubiquitin-mediated regulator of a ma
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Historically covalent drugs have had great success e
2019-12-04
Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form
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Vacuolin-1 br Materials and methods br Results
2019-12-04
Materials and methods Results Discussion Regardless of obvious beneficial effects of GC on acceleration of foetal lung and cardiomyocytes maturation (Kamath-Rayne et al., 2012; Rog-Zielinska et al., 2015), the current study revealed that GC exposure during late pregnancy induces IR and alte
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br Materials and methods br Results
2019-12-04
Materials and methods Results Discussion Drug of abuse induces widespread Disulfiram changes in the molecular and cellular functions in circuits between VTA and its neighbored regions such as NAC, and amygdala. It is belived that these changes result behavioral phenotype that characterize
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br Conclusions Present work comprehensively characterizes th
2019-12-04
Conclusions Present work comprehensively characterizes the inhibitory activity of Yersinia enterocolitica against cysteine proteases. All tested strains, regardless of their bioserotype, genotype and the presence of virulence markers, synthesized the high-molecular-weight inhibitors of papain an
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Acknowledgments br Introduction Various researches have been
2019-12-04
Acknowledgments Introduction Various researches have been made in the field of the treatment of cancer and inflammatory diseases. Different mechanisms are involved in the progression of cellular damage that gives an idea about new drug targets. There are always some efforts to improve efficacy,
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br Acknowledgements The study was supported by grant no
2019-12-04
Acknowledgements The study was supported by grant no. 501-003-11043 from the Institute of Psychiatry and Neurology in Warsaw. The authors thank Mrs. Ala Biegaj for the excellent technical assistance. Introduction In an effort to identify hIFN receptor molecules encoded by a gene(s) within hum
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br Role of CRF receptors
2019-12-04
Role of CRF1 receptors in the BNST in stress-induced relapse to cocaine seeking The seminal work of Stewart and co-workers [19] showed that rats that have extinguished their auto-administration of different drugs of abuse relapse to drug-seeking behaviour when exposed to footshock, even after a 4
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