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br FXR Agonists Azepinol b
2021-09-24
FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement i
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Angiotensin 1/2 (1-5) synthesis Wasting syndrome is a common
2021-09-24
Wasting syndrome is a common complication of HIV infection and is marked by progressive weight loss and weakness, often associated with fever (Weinroth et al., 1995). Fever is a highly complex process initiated by the action on the Angiotensin 1/2 (1-5) synthesis thermosensitive cells of a number o
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The expression of heat shock proteins HSPs can be
2021-09-24
The expression of heat-shock proteins (HSPs) can be upregulated by viral infection, nutritional deficiency, TNF-α and oxidative stress in Atovaquone synthesis [44], [45] HSPs are classified in six families (including the HSP10, HSP40, HSP60, HSP70, HSP90 and HSP100 families). HSP90 [46] for example
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We first investigated the influence of the acyl
2021-09-24
We first investigated the influence of the -acyl group of the glycine amide side chain and found that shorter linkers lead to better activities (–); simple -benzoyl substituents were always superior to the 3-arylpropanoyl group present in the high-throughput hit (). Electron withdrawing substituents
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br Discussion Agonist and antagonist action at
2021-09-24
Discussion Agonist and antagonist action at the GluN1/GluN3 topoisomerase inhibitors is known to be complex [4], [10]. Recombinant GluN1/GluN3 receptors produce only small excitatory currents in response to glycine, likely because of a combination of activation via GluN3 and desensitization via
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Among the various delivery strategies in the field
2021-09-24
Among the various delivery strategies in the field of nano-DDS, developing smart targeted nanocarriers has long been a research focus for pharmaceutical scientists11., 12.. The ideal drug delivery outcome must be precisely delivering the therapeutic agents to their sites of action, especially for an
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Glial cells have emerged as important protagonists of the ce
2021-09-24
Glial cells have emerged as important protagonists of the central nervous system (CNS) physiology (Chen and Swanson, 2003; Kettenmann and Verkhratsky, 2008; Parpura and Verkhratsky, 2012). As widely described in the literature, astrocytes regulate glutamatergic synapses by clearance of glutamate in
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Because of the relationship between carbohydrate
2021-09-24
Because of the relationship between carbohydrate consumption and chronic diseases such as obesity and type II diabetes (Hu, van Dam, & Liu, 2001), there is mounting interest to evaluate the quality of Temafloxacin hydrochloride receptor through analysis by glycemic index (GI) and Englyst assay, for
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br Conclusions Temporally controlled disruption of
2021-09-24
Conclusions Temporally-controlled disruption of Gcgr reveals a lack meaningful contribution to the improvement of glycemic control in insulinopenic conditions attributable to the intrinsic loss of GCGR signaling. On the other hand, these data highlight the importance of compensatory systems, incl
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The effects of GHS R a blockade on alcohol related
2021-09-24
The effects of GHS-R1a blockade on alcohol-related outcomes have been examined in numerous preclinical experiments, utilizing various GHS-R1a antagonists (JMV 2959, [D-Lys3]-GHRP-6, BIM 28163) and rodent species (prairie vole, mouse, rat). In spite of methodological differences, the results consiste
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In sharp contrast to these
2021-09-24
In sharp contrast to these genetically altered animals, there are two types of living fish that appear to lack Band 3 in their red blood cells. These are the Lamprey [45] and the Hagfish [46,47]. While these fish normally occupy their respective niches, the presumed compensatory mechanisms, as with
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The structures of KDM A revealed
2021-09-24
The structures of KDM4A revealed a Cys-His Zn(II) binding site that is close to the substrate binding spot, which bioinformatic analyses indicated was not present in any other histone demethylase subfamily. Therefore, an alternative method to inhibit the KDM4 family (95) would be to use compounds th
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Newly identified evidence has put immune checkpoint inhibito
2021-09-23
Newly identified evidence has put immune checkpoint inhibitors into the spotlight. However, even though they have been reported to achieve optimistic outcomes [67], there is still a provocative question about their limitations [68]. The solid evidence above has provided us with translational values
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Fig C presents the secondary
2021-09-23
Fig. 1(C) presents the secondary structure arrangement of the PAS-A and PAS-B domains in both HIF-2α and ARNT. The common scaffold of the PAS domains is a β sheet with numerous flanking α helixes. The PAS-A domains of both HIF-2α and ARNT have A’α, Aβ, Bβ, Cα, Dα, Eα, Fα, Gβ, Hβ, and Iβ from the N t
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br Endogenous and synthetic ligands of GPR There are current
2021-09-23
Endogenous and synthetic ligands of GPR55 There are currently limited commercially available synthetic agonists and antagonists that are specific for GPR55. A large number of studies have investigated the pharmacology of GPR55 4, 23, 25, 30, 31, 32, 33, 34, 35, with contradictory findings reporte
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