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Our structures also provide new insights into
2021-06-28
Our structures also provide new insights into CRTH2 drug development. The ligand binding pocket revealed by our structures comprises many aromatic residues and a few polar residues at the distal end. Correspondingly, most CRTH2 antagonists share a similar structural feature characterized by an aceta
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gdc 0941 Self Determination Theory SDT as
2021-06-28
Self-Determination Theory (SDT), as described by Ryan and Deci (2000) is “an approach to human motivation and personality that uses traditional empirical methods while employing an organismic metatheory highlighting the importance of humans' evolved inner resources for personality development and be
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br When Does Activity with Alternative Substrates
2021-06-25
When Does Activity with Alternative Substrates Depend on Neutral Drift? In a final scenario, the alternative reaction catalyzed by an enzyme might have no significant (positive or negative) effects on the system fitness, and thus it would be invisible to natural selection and essentially subject
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Against this backdrop we set out to identify synthetic
2021-06-25
Against this backdrop, we set out to identify synthetic and endogenous ligands that bind directly to and regulate the activity of Nurr1. Owing to the pivotal role Nurr1 plays in producing and processing dopamine, and the need for neurons to tightly regulate dopamine levels, we postulated that the re
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Diacylglycerol kinase was one of the hits identified from
2021-06-25
Diacylglycerol kinase was one of the hits identified from the RNAi screen. Diacylglycerol kinases are conserved across a Ro3306 of species with more complex, multicellular organisms possessing several DGKs with differing protein domains, expression patterns and functions [61], [62], [63]. Some of t
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The folate pathway plays an essential role
2021-06-25
The folate pathway plays an essential role in cell survival by generating 5, 10-methylene tetrahydrofolate as a one-carbon donor for the synthesis of deoxythymidine monophosphate (dTMP), purines, methionine and histidine. Disruption of this pathway leads to the critical deficiency of these key molec
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Our results implicate a critical role
2021-06-24
Our results implicate a critical role for CXCR-1 in promoting the migration of colonic tumor cells. Expression of this receptor, but not CXCR-2, increased significantly because of the EMT (Fig. 3). Moreover, although Clone A 5-hme-CTP express comparable levels of both IL-8 receptors, only CXCR-1 in
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As described above we designed and synthesized
2021-06-24
As described above, we designed and synthesized a new 1,4-di-substituted isoquinoline lead compound, and was identified as a ligand with moderate potency for the CRTH2 receptor. We initially we examined the effects of the steric factor of R group on the CRTH2 binding potency (). When the methyl gro
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Introduction The inflammation process involves sequential ac
2021-06-24
Introduction The inflammation process involves sequential activation of signaling molecules, pro-inflammatory mediators, such as prostaglandins, leukotrienes, and oxygen free radicals [1]. Two cyclooxygenases substance p receptor were responsible for activation of the production of prostaglandins
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Neuroinflammation is the one of the emerging
2021-06-24
Neuroinflammation is the one of the emerging causal factors contributing to these cognitive deficits. Therefore, we further tested the hypothesis that neuroinflammation is a key component contributing to the progression of spatial memory deficits during HH. Spatial memory deficits were observed afte
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More recently it was discovered
2021-06-24
More recently, it was discovered that BChE hydrolyzes the neuropeptide gut hormone, ghrelin [25], [26], [27], [28]. Nonetheless, because the enzyme reaction is very slow, those who first reported this finding were initially reluctant to attribute a real physiological role for that phenomenon. Our ow
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It was reported that IVM modulates various ion
2021-06-24
It was reported that IVM modulates various ion channels, such as type-A GABACls, α7 acetylcholine-gated cation channels, P2X4 ATP-gated cation channels, and glycine-gated chloride kinesin spindle protein in vertebrates (Adelsberger et al., 2000, Khakh et al., 1999, Krause et al., 1998, Krůšek and Ze
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Perturbations in cell cycle are
2021-06-24
Perturbations in leucine enkephalin are known to induce apoptosis. Our results show that a fraction of the DT40YB-1b+/− cells, in addition to becoming tetraploids, undergo apoptotic cell death. Similar observations linking polyploidy and apoptosis have been made in the past [23], [30], [31], [32],
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br Progestogens and venous thromboembolism
2021-06-24
Progestogens and venous thromboembolism: clinical data Progestogens and haemostatis: biological studies For many years, the effect of HT on haemostatis has been largely investigated in observational studies as well as in high evidence level studies among users of oral and transdermal estrogens
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br Most reported binding data are
2021-06-24
Most reported binding data are obtained by performing heterologous competition binding experiments and expressing the results as relative binding affinity (RBA). The constructed binding curves should theoretically be sigmoidal in shape with a Hill slope value of one, for a single ligand binding to
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