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Data are expressed as means SE Statistical significance was
2021-12-28
Data are expressed as means±SE. Statistical significance was determined by the Student's -test or ANOVA with post hoc Bonferroni test. A value of U87MG Metronidazole expressing human FPPS. Western blot analysis showed a clear band, which indicated the overexpression of FPPS, in U87MG cells (A, inser
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br Development of calibrators and
2021-12-28
Development of calibrators and controls for DiXaIs Method validation and comparison with reference technique (LC:MS) At this stage, anti-Factor Xa bioassays can be established for reliably measuring DiXaI concentrations in plasma, with the available appropriate drug specific calibrators and co
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Compounds and were evaluated for their pharmacokinetic
2021-12-28
Compounds and were evaluated for their pharmacokinetic properties in rats and the results are summarized in . Following intravenous (IV) administration, both compounds displayed low clearance (CL), short half-lives (t) and low volumes of distribution (V). When dosed orally as a solution, exposure
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br STAR Methods br Author
2021-12-28
STAR★Methods Author Contributions Introduction Hyaluronan, a major constituent of the extracellular matrix (ECM), is produced by hyaluronan synthases (HASs) and degraded by hyaluronidases (HYALs) (Vigetti et al., 2014). Physiologically, hyaluronan exists in a form with a molecular weight of
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Given the major differences between the molecular regulation
2021-12-28
Given the major differences between the molecular regulation of the genes encoding HO-1 (HMOX1) in mice and humans, it is not appropriate to utilize mouse models for mechanistic analyses of human HMOX1[35]. In addition, it has been reported that drugs, such as statins, as well as stressors and the r
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Human immunodeficiency virus type HIV is responsible for
2021-12-28
Human immunodeficiency virus type 1 (HIV-1) is responsible for the emca pandemic; notification is compulsory in Brazilian blood banks since 1988. From 1980 to 2016, the Brazilian MH reported 882,810 HIV/AIDS cases, with 52.3% in the southeast region. HIV/HCV co-infection has been associated with p
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Background Chronic hepatitis C virus HCV infection
2021-12-28
Background Chronic hepatitis C virus (HCV) infection is a major public health concern, with 71 million people infected worldwide [1]. Treatment options have improved with the availability of interferon-free direct-acting antiviral (DAA) therapies with cure in >95% of people [2]. However, broadening
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To identify structurally novel autophagy inhibitors a medium
2021-12-28
To identify structurally novel autophagy inhibitors, a medium throughput screen of our in-house library of approximately 160,000 compounds was performed. In the screening assay, MCF7 SR3335 stably transfected with eGFP-tagged light chain 3 (LC3), were employed, which can be detected by automated fl
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The characterization of Da CTSL
2021-12-28
The characterization of Da-CTSL1 shows that it preferentially cleaves Z-FR-AFC (Fig. 8), which has a bapta sale phenylalanine at P2 and Da-proCTSL1 is autocatalyzed at pH 8.0 releasing an activated Da-CTSL1 that exhibits optimal activity at pH 8 indicating that the enzyme when secreted by the foreg
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Compared with the tetrazole derivative the potency of analog
2021-12-28
Compared with the tetrazole derivative , the potency of analogs – was 3- to 17-fold improved. Of the range of heterocycles prepared, 1,2,4-thiadiazol-5(4)-one and 1,3,4-oxadiazol-2(3)-one showed the best potencies of 0.52μM and 0.61μM, respectively. Introduction of a second hydrogen bond donor, su
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In the Toc Regulator Mode Fig recognition of the transit
2021-12-28
In the “Toc34 Regulator Mode” (Fig. 6), recognition of the transit peptide by Toc159 monomer (step 4) leads to heterodimer-formation [18]. Subsequently, preprotein interaction with the Toc34G homodimer (step 1) regulates the Toc34G homodimer (step 2, 3). However, this mode requires a parallel induct
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GSK can function in regulating insulin
2021-12-28
GSK-3 can function in regulating insulin signaling and glucose metabolism. Inactivation of GSK-3 activity results in dephosphorylation and activation of GS that leads to improved glucose tolerance. However, there are additional mechanisms that can lead to increases in GS activity and improve insulin
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Vacquinol-1 Throughout our studies we used CBD under the ass
2021-12-28
Throughout our studies we used CBD under the assumption that it binds to the GPR55 receptor and has antagonist properties at the GPR55 receptor, as previously suggested (Whyte et al., 2009). To clarify whether the GPR55 receptor is involved in the O-1602-mediated effects on GI motility, we performed
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FSH and LH are glycoprotein
2021-12-28
FSH and LH, are glycoprotein dimers that are comprised of two subunits, a common α-subunit (αGSU) and a distinct β-subunit (FSHβ or LHβ, respectively), which determines the biological specificity of the gonadotropins (Ciccone and Kaiser, 2009, Gharib et al., 1990). The Lithocholic Acid synthesis of
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H together with T also forms a binding site
2021-12-28
H109, together with T112, also forms a binding site for H+ (Chen et al., 2004; Harvey et al., 1999). H+-binding at this site also inhibits GlyR-mediated currents. Notably, the vicinity of neurons experiences changes in pH, to a mild extent in physiological conditions such as when neurons fire (Chesl
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