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br Material and methods br
2021-12-08
Material and methods Results Discussion Organisms have developed a variety of anti-glycation defense mechanisms. In gaba receptor antagonist to the aldose-reductase-pathway or 2-oxoaldehyde dehydrogenase-pathway, the glyoxalase system is the only mechanism, which is not restricted to liver
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It should be noted that the applied steered unfolding of
2021-12-08
It should be noted that the applied steered unfolding of the i-motif and G-quadruplex satisfies the conditions of Jarzynski inequality for computations of the free energy change. [41] However, in order to reproduce the free energy with an adequate quality a number of nonequilibrium unfolding transit
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CUDC-907 In the light of the above mentioned
2021-12-08
In the light of the above-mentioned considerations, it is interesting to note that the FPR-related research with regards to bias agonism did not prosper during considerably during the last decade (possible exceptions are [[8], [9], [10], [11]]. However, with new insights in receptor chemistry and fu
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p-Cresyl sulfate receptor Our results are consistent with th
2021-12-08
Our results are consistent with the hypothesis that reduced Fas-mediated apoptosis in maternally activated T-lymphocytes could result in insufficient trophoblast invasion of the spiral p-Cresyl sulfate receptor as the activated T-lymphocytes become able to enhance the destruction of the cytotrophobl
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Continuing studies of endocannabinoid ligands at GPR reveal
2021-12-07
Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as ort
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As a part of our continuing efforts towards discovery
2021-12-07
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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Solid tumors usually present insufficient supply
2021-12-07
Solid tumors usually present insufficient supply of oxygen, activating the hypoxia inducible factor-1 (HIF-1) pathway, which prompts an adaptive response on genes that regulate glycolytic metabolism, promoting glucose uptake through the transcription of GLUTs [54]. Increasing evidence indicates that
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The biological actions of ghrelin are mainly due to
2021-12-07
The biological actions of ghrelin are mainly due to its interaction with GHSR-1a (Howard et al., 1996). The pharmacological properties of D-Lys3-GHRP-6, a selective antagonist of GHSR-1a, have been extensively studied (Beck et al., 2004, Benso et al., 2007, Sibilia et al., 2006). To study the recept
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GHSR A s have high levels of constitutive
2021-12-07
GHSR-1A's have high levels of constitutive activity and recent investigations show that constitutively active GHSR-1As in the absence of ligand (ghrelin) binding can have effects on feeding and energy balance (Mear et al., 2013, Petersen et al., 2009). Furthermore, GHSR-1As are capable of dimerizing
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Optimization of the tetrahydroindazole series led to the
2021-12-07
Optimization of the tetrahydroindazole series led to the discovery of two moderately potent γ-secretase modulators, 2-cyclobutane and 2-hydroxy-2-methylpropane which were subsequently evaluated in a kinetic aqueous solubility assay. Unfortunately, neither analog demonstrated improved solubility ()
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The first GSM was identified from
2021-12-06
The first GSM was identified from the discovery of non-steroidal anti-inflammatory drugs (NSAIDs). An amyloid reducing GSM that also suppresses inflammation is desirable. Inflammatory response is an invariable characteristic of AD pathogenesis, in part triggered by Aβ. During AD onset and progressio
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FFA expression was also noted to be upregulated in eight
2021-12-06
FFA4 expression was also noted to be upregulated in eight human CRC cell lines. Compared to two normal colon cell lines with relative one-fold expression of FFA4, CRC cell lines HCT116 (3.5-fold higher), Colo205 (3-fold), Caco-2 (2.2-fold), HT-29 (2.3-fold), RKO (2.8-fold), DLD-1 (2.9-fold), SW480 (
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In recent years it was
2021-12-06
In recent years, it was discovered in animals that certain types of non-apoptotic cell death are strictly dependent on iron and ROS. The term ‘ferroptosis’, derived from the Greek word ‘ptosis’ (falling) and the Latin word ‘ferrum’ (iron), is coined to describe such cell death phenomena. Cytoplasmic
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br Introduction Ovarian cancer patients have the highest
2021-12-06
Introduction Ovarian cancer patients have the highest mortality rate amongst patients with gynecologic cancers. The 10-year survival rate of ovarian cancer patients is DY131 receptor with BRCA1/2 mutation [2]. Several studies have indicated the role of dysregulation of histone methylation in ca
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br Results br Discussion HIV reservoirs
2021-12-06
Results Discussion HIV reservoirs represent a major barrier to HIV eradication (Archin et al., 2014, Kimata et al., 2016), and substantial research efforts are being directed toward the goal of identifying and eliminating this obstacle to cure (Archin and Margolis, 2014, Pitman et al., 2018).
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