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endothelin receptor antagonists br Background In resource li
2022-05-10
Background In resource-limited countries, many HIV patients currently do not have reliable access to essential diagnostic laboratory tests, including CD4, clinical chemistry, hematology, viral load, and diagnosis of common co-infections. CD4 T cell count monitoring remains an important surrogate
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Introduction Substantial body of evidence supports the notio
2022-05-10
Introduction Substantial body of evidence supports the notion that GABA, the dominant inhibitory neurotransmitter in the hypothalamus of mammals, affects GnRH release by two classes of membrane receptors: GABAA (GABAAR) [1] and GABAB (GABAB R) [2]. Studies in rodents and sheep have documented that
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We were able to obtain
2022-05-10
We were able to obtain several crystalline forms of CHAV Gth. The first one corresponded to the post-fusion conformation [14]. The comparison of this structure with that of VSV-Gth post-fusion conformation revealed that the PHD is the most divergent domain, with the largest differences confined to t
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As a part of our
2022-05-10
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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Epidemiological evidence indicates that neuroinflammation pl
2022-05-10
Epidemiological evidence indicates that neuroinflammation plays a pivotal role in pathogenesis of AD (Heneka et al., 2015, Heneka et al., 2013, Holmes et al., 2009, Liu et al., 2016). For example, prolonged treatment with nonsteroidal anti-inflammatory drugs reduces the risk of developing AD (In et
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Rifampicin that is methyl piperazinyl imino methyl
2022-05-10
Rifampicin, that is 3-[[(4-methyl-1-piperazinyl) imino] methyl]-rifamycin (Fig. 1), is a semisynthetic antibiotic drug. It is one of the most potent and broad drug against bacterial pathogens and tuberculosis [9]. In recent years, rifampicin has also been reported to have inhibitory effects on Taq R
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br Glucose metabolism and diet Glucokinase is essential for
2022-05-09
Glucose metabolism and diet Glucokinase is essential for sensing blood glucose levels, thus controls metabolism (Iynedjian, 1993, Iynedjian, 2009, Postic et al., 2001, Agius, 2008). Loss of glucokinase activity in humans and mice leads to diabetes (Printz et al., 1993b, Postic et al., 2001, Agius
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The Growth Hormone Secretagogue Receptor GHSR also known
2022-05-09
The Growth Hormone Secretagogue Receptor (GHSR), also known as the ghrelin receptor, is a G protein-coupled receptor (GPCR) expressed widely throughout the body and brain, with particular enrichment in hydrazone regions concerned with homeostatic and motivational function such as the hypothalamus, h
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A model substance often used in the
2022-05-09
A model substance often used in the studies of oxidative processes in erythrocytes is tert-butyl hydroperoxide (t-BHP), which, being lipophilic, passes easily across the erythrocyte membrane [9]. In erythrocytes treated with t-BHP (0.1–3mM) for less than 1h, a dramatic decline in the reduced glutath
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br Conclusions There are a number of factors
2022-05-09
Conclusions There are a number of factors that affect the transit of solutes through gap junction channels. Fig. 4 provides a simplified illustration of those factors. First is the cytoplasmic vestibule through which all permeable solutes must pass to gain access to the pore. In an equivalent cir
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It must be noted that while the accumulated
2022-05-09
It must be noted that while the accumulated evidence on molecular mechanisms has resulted in well-established experimental methods to externally act on single-cell characteristics and networks, safe and efficient external methods to modify multicellular states are still a matter of basic research. C
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Clinical trials of all GSIs have
2022-05-09
Clinical trials of all GSIs have ended prematurely, raising the question on our understanding of their target, the γ-secretase/presenilin. Development of compounds to target γ-secretase and reduce Aβ production is complicated by the fact that γ-secretase/presenilin has critical biological function,
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Photoincorporation of pTFDBzox AP occurred predominantly in
2022-05-09
Photoincorporation of 21-pTFDBzox-AP occurred predominantly in the β3 subunit, very modestly in the α1 subunit and not at all in the γ2 subunit. These observations taken together with the sensitivity of 21-pTFDBzox-AP enhancement of GABA currents to the α1 M1 mutation Q242 W4 suggest that the 21-pTF
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br Discussion br Concluding remarks There are
2022-05-09
Discussion Concluding remarks There are potentially hundreds or thousands of G-quadruplexes which form within promoters, telomeres, RNA transcripts, and even LINEs and SINES [9,11,121,122]. As articulated previously [27], G-quadruplexes are easily targetable with heterocyclic aromatic compound
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melanin inhibitor Interestingly we have shown that OA requir
2022-05-09
Interestingly, we have shown that OA required FFAR4 to induce osteoblast gene expression in MC3T3-E1 pre-osteoblasts, but not to inhibit osteoclastogenesis in RAW264.7 murine macrophages. As previously suggested, FFAR1 may mediate the effects of OA in osteoclasts. However, FFAR1 has also been shown
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