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br Fragment based drug discovery FBDD
2020-12-16
Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical cytochrome p450 inhibitors space with libraries which are smaller in size, producing drug leads with high ligand-binding
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br Materials and methods Male Hartley guinea pigs g were
2020-12-16
Materials and methods Male Hartley guinea pigs (300–350g) were obtained from National Laboratory Animal Center, Taiwan. LTD4, LTC4, LTE4, LTB4, montelukast and BAY u9773 were purchased from Cayman Chemical, Ann Arbor, Michigan; Carbachol, atropine, l-serine, boric acid, l-cysteine and all buffer
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The in vitro enantioselective metabolism
2020-12-16
The in vitro enantioselective metabolism of pesticides has been investigated by employing human liver microsomes, which are a reliable resource to perform MCL enantioselective risk assessment in humans (Carrão et al., 2019; de Albuquerque et al., 2018, 2016; Yao et al., 2016). The enantioselective m
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Taking into account that Gr dysfunction is involved in
2020-12-16
Taking into account that Gr dysfunction is involved in the molecular mechanisms underlying HPA axis disorder (Li et al., 2017b) and Gr activity has been reported to be lowered in patients with severe mood disorders (Rush et al. 1996) and in adult rats (Green et al. 2016), PFOS could alter HPA axis a
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Finally the recent work to define the microcircuitry of the
2020-12-16
Finally, the recent work to define the microcircuitry of the central amygdala and the role of specific cell populations in fear conditioning can stand as a useful model for advances in preclinical alcohol research. To date, the role of the amygdala in alcohol-related behaviors, and reward-related be
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These cognitive deficits may suggest that cognitive therapy
2020-12-15
These cognitive deficits may suggest that cognitive therapy and pharmacotherapy for gambling behavior may ultimately wish to consider genotyping as a means of better targeting treatment approaches. If core cognitive deficits are shown consistently in certain subgroups of gamblers based on genotype,
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br Materials and methods br
2020-12-15
Materials and methods Results Discussion In this study, we first showed that fluxametamide, a novel isoxazoline insecticide, inhibits agonist responses in two types of LGCCs, the M. domestica GABACl and GluCl, with higher potency in the former channel versus the latter one (Fig. 3). In addi
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In recent years there has been much
2020-12-15
In recent years, there has been much interest within the endothelin community regarding the possibility that ETA and ETB receptors may form homo- and heterodimers. Heterodimerization of endothelin receptors may provide an explanation for the results mentioned in the previous paragraph and might als
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First of all two assumptions
2020-12-15
First of all, two assumptions just as in Ref. [30] are need to simplify the penetration process: (1) The crater phases is short and the dpp-iv inhibitors of EFP is consumed little; thus, the influence of crater on penetration can be ignored; (2) the initial stagnation radial pressure is equal to ax
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Palomid 529 CM AVM and VOGM are
2020-12-15
CM-AVM and VOGM are thought to be two distinct disorders, with CM-AVM characterized by atypical CMs, with or without AVM in variable body parts, while VOGM is a type of cerebral AVM [16]. The fact that VOGM is infrequently reported as the AVM in CM-AVM patients, and CMs are quite often identified in
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To identify and characterize new possible molecular targets
2020-12-15
To identify and characterize new possible molecular targets, the mechanisms of various kinds of TCDD toxicities that occur by abnormal regulation in the downstream of AhR signals have been studied (Yoshioka et al., 2011). Experimental evidence has revealed that prostanoids (i.e., prostaglandins and
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Neonatal hydronephrosis induced by TCDD exposure via
2020-12-15
Neonatal hydronephrosis induced by TCDD exposure via lactation has a critical window for onset: the incidence of this disease peaks around PNDs 1–4, followed by a rapid decrease to a substantially null level in adulthood (Couture-Haws et al., 1991; Yoshioka et al., 2016). The EP1 protein was localiz
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Early VL diagnosis makes it possible to formulate a quicker
2020-12-15
Early VL diagnosis makes it possible to formulate a quicker and more effective treatment against the disease, which could increase the possibility of a cure for the patients, as well as reduce the toxicity of the drugs (Coelho et al., 2009); however, conventional and molecular parasitological method
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Our previous work has demonstrated that two
2020-12-15
Our previous work has demonstrated that two glutamate residues (Glu-305 and Glu-331 in murine and human TPP II) in the active site are important for exopeptidase activity in mTPP II [17]. At least one of these, Glu-331, seems to form a salt bridge to the N-terminal amino group of the substrate, posi
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In principle in vitro techniques for assessing
2020-12-15
In principle, in vitro techniques for assessing enzyme induction might include the use of cultured hepatocytes, precision-cut liver slices, immortalized HAT Inhibitor II lines (such as those derived from hepatomas) and reporter gene constructs (where appropriate cells are transfected with recombina
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