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In addition to Rabs several proteins have
2022-04-19
In addition to Rabs, several proteins have been shown to interact with Rabphilin3a, for instance the GluN2A subunit of the NMDA receptor, PSD-95 ([56,57] and references therein), Rabaptin-5, α-actinin [16] and SNAP-25 [21,23,41,61]. Only the latter has been reported to participate in the AR. Explori
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Acknowledgments The authors would like to thank members of t
2022-04-19
Acknowledgments The authors would like to thank members of the Department of Discovery Synthesis (DDS) and Biocon-Bristol Myers Squibb Research Center (BBRC) for scaling up key intermediates, analytical team for analytical experiments, lead profiling group for evaluating compounds in an in vitro AD
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br Funding The authors disclose the following support for
2022-04-19
Funding The authors disclose the following support for the research and/or authorship of this article: This work was supported by the Canadian Institutes for Health Research (CIHR). TM is the recipient of a BMS/CTN postdoctoral fellowship and PKQ was funded by a CAHR/CIHR doctoral scholarship. A
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Following the discovery of diketo
2022-04-19
Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent Semaxanib based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase. Bioas
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Spectinomycin hydrochloride hydrate br Discussion Our study
2022-04-19
Discussion Our study found that 62.6% of MSM from Natal had been tested for HIV before. This rate was higher than the national average of 37% estimated for the general Spectinomycin hydrochloride hydrate in 2011 and the 51.6% found by Brito et al. in MSM from 10 Brazilian cities in 2009. These r
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Integrase inhibitors have been licensed for
2022-04-19
Integrase inhibitors have been licensed for use in the UK since 2008. BHIVA now recommend starting all treatment naïve patients on a regimen containing two NRTIs, plus one of the following: a ritonavir boosted PI, an NNRTI, or an integrase inhibitor. They make further recommendations for patients wi
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Although epigenetic mechanisms are implicated in the pathoge
2022-04-19
Although epigenetic mechanisms are implicated in the pathogenesis of hematopoietic malignancies, little is known about the role of lysine-specific histone demethylases and whether manipulation of these enzymes can be translated into targeted therapies. KDM6A is the most frequently mutated histone de
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br Acknowledgements This work was supported
2022-04-19
Acknowledgements This work was supported by grants from the Agencia Nacional de Promoción Científica y Tecnológica (PICT2013-0495, PICT2016-1821), and from CONICET (PIP 2013-562), as well as from Fundación René Barón and Fundación Williams. Introduction Histamine poisoning, also known as scom
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br Results br Discussion Our current study
2022-04-19
Results Discussion Our current study demonstrates that the sustained activation of Yap overrides the p27-mediated checkpoint, at least in part, through the degradation of FoxO family proteins, allowing polyploid cells to proliferate inappropriately with mitotic defects and resulting in centros
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In cancer cells HIF upregulates HK II expression by
2022-04-19
In cancer cells, HIF-1α upregulates HK-II expression by binding to the hypoxia-responsive element in the HK-II promoter region to adapt to hypoxic conditions [20]. In the present study, we observed that mangiferin transiently increased HIF-1α expression in endothelial cells, suggesting another possi
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Eastern Guangdong is a Teochew
2022-04-19
Eastern Guangdong is a Teochew dialect area. We found that subtype 1b (3.1%) in this region was significantly lower than in other areas. Subtype 1b began its spread from the central part of China out into the whole country through illegal blood donation in the mid-1990s (Lu et al., 2013) and is now
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br All platelet agonists acting through specific receptors
2022-04-18
All platelet agonists, acting through specific receptors and triggering different signaling pathways, activate phospholipases (PLCß or PLCγ) and the subsequent messengers inositol 1,4,5-trisphosphate (IP3) and 1,2 diacylglycerol which activate inositol 1,4,5-trisphosphate (IP3) receptors (IP3R) or
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CB-5083 In order to determine whether NF B could interact
2022-04-18
In order to determine whether NF-κB could interact with GSTP1-1 promoter, we performed EMSA. One NF-κB like (−98κB) binding site was previously described in the GSTP1-1 promoter as a regulator element. However, few data about this site have been published and its role in the GSTP1-1 gene regulation
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After the synthesis of methylsulfonyl or tetrazole
2022-04-18
After the synthesis of methylsulfonyl or tetrazole surrogate derivatives, compounds synthesized by introducing hydrogen, fluoro, and methyl groups into the head group of GPR119 agonists were synthesized. Compounds – were synthesized by reacting hydroxybenzaldehyde with fluorine, hydrogen, or a methy
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A high throughput screening campaign
2022-04-18
A high-throughput screening campaign of the Lilly corporate compound collection led to the discovery of as potent and selective inhibitor of GlyT1 (IC=45nM, GlyT2 IC>30,000nM). In addition to the characteristic -methyl glycine moiety as acidic head group and the novel ethanolamine linker, also co
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