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Another possible effect of niacin is in altering
2022-08-11
Another possible effect of niacin is in altering immune cell trafficking; as it has been suggested that niacin therapy quells endothelial cell activation (Digby et al., 2010, Ganji et al., 2009) and thereby suppresses inflammatory cell recruitment (Wu et al. 2010). However, the impact of niacin on l
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Necrosulfonamide Piezo channels can be activated by many mec
2022-08-10
Piezo channels can be activated by many mechanical stimuli . While some of these stimulations directly mimic physiological forces experienced by Necrosulfonamide , such as shear stress applied in a microfluidic chamber, the most commonly used modes of stimulation consist of stretching the membrane
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How changes in APP processing by secretase lead
2022-08-10
How changes in APP processing by γ-secretase lead to AD is still not well understood. Deposition of amyloid beta (Aβ) peptide fragments of the amyloid precursor protein (APP) in amyloid plaques and hyperphosphorylated tau in neurofibrillary tangles are the cellular hallmarks of AD (O’Brien and Wong,
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Ionotropic aminobutyric acid GABA receptors GABARs belong to
2022-08-10
Ionotropic γ-aminobutyric BIO-acetoxime (GABA) receptors (GABARs) belong to the Cys-loop ligand-gated ion channel (LGIC) superfamily and play an important role in the rapid inhibitory synaptic transmission in nervous systems of both vertebrate and invertebrate (Buckingham et al., 2005). Insect iono
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MLN8237 In case where an extreme loop of up to
2022-08-10
In case where an extreme loop (of up to 45 nt) is allowed, as in G3 + E3 + XX, however, a G3+GQ loop maximum of 3 was adequate to reach high J-statistic. It continued to increase only up to 6 as the loop maximum. (Fig. 1A) Hence we suggest using a G3+GQ loop maximum between 3 and 6 where an extreme
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TMC647055 Choline salt receptor As a part of our continuing
2022-08-10
As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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Liver and muscle isozymes have been found
2022-08-10
Liver and muscle isozymes have been found in vertebrate tissues [2], [5], [6]. The liver FBPase is recognized as a regulatory enzyme of gluconeogenesis. The muscle isozyme participates in the glycogen synthesis from lactate and in the regulation of glycolysis [7], [8], [9]. The basic difference betw
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pp2 Dysregulation of the HPA axis resulting in alteration to
2022-08-10
Dysregulation of the HPA axis, resulting in alteration to both baseline and stress-induced glucocorticoid levels (e.g., cortisol and corticosterone), has been implicated in several diseases and psychopathologies, including anxiety (McEwen et al., 2015, 2016; Shin and Liberzon, 2010). For example, ba
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With LML methyl oxo dihydropyridazin yl piperidin
2022-08-09
With LML-134 (1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl 4-cyclobutylpiperazine-1-carboxylate) containing drug-likeness properties (MW 375.47, five HBA, and MLogP 1.88), Novartis presents an additional drug-candidate to treat excessive sleepiness. A phase I clinical study was perform
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RS testing has been extensively validated in patients
2022-08-09
RS testing has been extensively validated in patients with early stage, ER+, HER2− patients. TAILORx, a randomized controlled trial to evaluate the role of adjuvant chemotherapy by RS, found no recurrence or survival benefit to the addition of chemotherapy to endocrine therapy in patients with inter
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These agents can be divided into three categories
2022-08-09
These agents can be divided into three categories based upon the therapeutic agent conjugated to the antibody; the most frequently explored are ADCs using a cytotoxic agent to be delivered directly to the tumor site. The second class has not been broadly used and consists of radionucleotides (Wong e
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Prolonged sGC oxidative inhibition occurs in many diseases K
2022-08-09
Prolonged sGC oxidative inhibition occurs in many diseases [46,[86], [87], [88]]. Keeping sGC membrane-bound and functional under conditions of high oxidative stress requires a mechanism for restoring oxidized sGC (Fe3+) heme iron to its reduced (Fe2+) state. Without this redox regulation, the sGC e
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br GSNOR regulates SA synthesis and SA signalling
2022-08-09
GSNOR1 regulates SA synthesis and SA signalling The phenolic metabolite salicylic tetrandrine (SA) is a powerful immune activator in plants. Moreover, mutations that disable SA biosynthesis or transgenes that result in its depletion compromise both resistance (R) gene-mediated and basal resistan
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Historically pharmacological investigations have been carrie
2022-08-09
Historically, pharmacological investigations have been carried out by first identifying a biological response to a ligand, and then subsequently using that ligand to identify the receptor(s) responsible for the response (Wilson et al., 1998). However, this approach needed revision with the discovery
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The atherosclerosis development requires additional pro infl
2022-08-09
The atherosclerosis development requires additional pro-inflammatory response in the vascular tissue, promoting increased levels of adhesion molecules such as VCAM-1 (vascular cell adhesion molecule-1) and ICAM-1 (intercellular adhesion molecule-1). Cytokines such as TNF-α and IL-1β are able to upre
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