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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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br Results and discussion br Conclusions
2021-12-28
Results and discussion Conclusions TZDs represent a well-studied group of antidiabetic agents. Based on previous observations of the ability of some TZDs to activate FFAR1, we designed five scaffolds consisting of the TZD head, a linker, and a carefully selected privileged structure. For the p
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Herein we report the discovery
2021-12-28
Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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Cx mimetic peptides short synthetic
2021-12-27
Cx mimetic peptides, short synthetic peptides corresponding to intracellular amino flumethasone sequences of diverse Cx have better specificity compared to traditional GJ blockers and openers. In particular, it was reported that Cx mimetic peptides reversibly inhibited GJ channel function in a conc
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Some clinical reports have suggested that
2021-12-27
Some clinical reports have suggested that galanin has a role in the neurobiology of mood disorders [[6], [7], [8], [9], [10]]. In behavioral studies, contradictory results have been reported [11,12]. For example, systemic administration of non-selective galanin receptor agonists, such as galmic [13]
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