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Acknowledgments br Introduction Diabetes mellitus DM is a mu
2021-08-02
Acknowledgments Introduction Diabetes mellitus (DM) is a multifactorial disease [1] associated with serious comorbidities. This condition has recently reached epidemic proportions, as its occurrence has exponentially increased in the general population. Over 400 million people worldwide were est
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Structural homology modelling Intensive Phyre modelling was
2021-08-02
Structural homology modelling. Intensive Phyre2 modelling [44] was performed using the primary amino latrunculin sequence of A1S_0222 as input to generate an atomistic 3D-homology model of A1S_0222. The fit to the SAXS data of the homology model as well as the fit to the data of the E. coli adenine-
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5-Methoxy-CTP The presence of H PPases in parasitic protists
2021-08-02
The presence of H+-PPases in parasitic protists raises the question of the physiological role of these proteins. So far, they had been extensively characterized mainly in higher plants, and some prokaryotes [1], [2], [3], [4], [5], [6], [7], [16], [20]. A common feature to all these organisms is tha
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R co localizes Golgi marker GM
2021-08-02
R co-localizes Golgi marker GM130 (Fig. 5). Our metabolic pulse-chase studies carried out in the presence of CSF-1 exposed the newly synthesized CSF-1R to its ligand, which promoted its rapid degradation. While this was clearly seen in control BMDMs, the mature band of CSF-1R remained intact for the
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The paper is organized as follows http
2021-08-02
The paper is organized as follows. Section 2 gives a brief presentation of the JPEG-LS algorithm and respective hardware implementation. In Section 3 the fault injection model and the simulation-based susceptibility analysis method are reviewed. Section 4 provides a discussion on the susceptibility
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Since PTKs are involved in numerous aspects of cell
2021-08-02
Since PTKs are involved in numerous aspects of cell function, their regulation is critical for cell survival and function. The carboxyl-terminal tyrosine of Src-family PTKs is a key site of regulation. Phosphorylation on this carboxyl-terminal tyrosine contributes to the induction of a conformationa
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MAPKs are a family of phosphorylating enzymes that orchestra
2021-08-02
MAPKs are a family of phosphorylating enzymes that orchestrate various cellular response in proliferation, apoptosis, inflammation, stress response, and energy metabolism [11]. There are at least four major members including extracellular signal-regulated kinase 1 and 2 (ERK1/2), p38 mitogen-activat
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While previously reported optimizations on compound focused
2021-08-02
While previously reported optimizations on Rosiglitazone maleate focused on the phenyl ring A () and substituents on isoxazole ring, other alternatives to replace isoxazole ring were never explored. Herein, we propose to replace the isoxazole with its bioisosteric substituted phenyl ring B () to e
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The ADME profile of AAT was very promising with high
2021-08-02
The ADME profile of AAT-008 () was very promising, with high stability in HLM. The pre-clinical pharmacokinetic properties of AAT-008 were also assessed in rats (Sprague-Dawley, male), dogs (beagle, male), and monkeys (cynomolgus, male). The experimentally determined parameters are summarized in .
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N Cyclopentylmethyl analog exhibited fold less potent recept
2021-08-02
N-Cyclopentylmethyl analog 25 exhibited 2.3-fold less potent receptor affinity and 1.6-fold less potent antagonist activity. Among the compounds tested, the N-isobutyl analog 23 showed the most potent EP1 receptor affinity and antagonist activity. In summary, a series of 4-( 2-[alkyl(phenylsulfonyl
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br Activatable photoacoustic probes Photoacoustic PA imaging
2021-08-02
Activatable photoacoustic probes Photoacoustic (PA) imaging is a recently developed technique [47]. The imaging approach uses probes that absorb a pulsed laser beam and convert light energy into acoustic signals. It combines the advantages of the high sensitivity offered by optical imaging and th
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br Conflicts of interest br Financial support NZ
2021-07-31
Conflicts of interest Financial support NZ is an Established Investigator of the Dutch Heart Foundation (2013T111) and is supported by an ERC Consolidator grant (617376) from the European Research Council and by a Vici grant from the Netherlands Organization for Scientific Research (NWO; 91818
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We next focused our design building into
2021-07-31
We next focused our design building into the ribose binding site, which had not been yet utilized in this effort. Compounds bearing a series of five-membered aromatic heterocycles (compound , ) showed reduced inhibition of the Gram-positive isozymes compared with compound , but a 20-fold improved po
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br Acknowledgements Thanks are due to Science
2021-07-31
Acknowledgements Thanks are due to Science and Technology Development Fund – Egypt for the Research Support Technology Development Grant (RSTDG) no. 12626. Our deep thanks and gratitude is also extended to National Cancer Institute (NCI), Bethesda, Maryland, USA for performing the anticancer eval
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Multiple sequence alignment of the proteins in the DGAT
2021-07-31
Multiple sequence alignment of the proteins in the DGAT1 sub-family shows that there are about 41 conserved amino AGK7 residues distributed over seven sequence motifs [74]. Unlike DGAT2, a large number of DGAT1 residues, including a majority of the conserved residues, are found in a loop on the lumi
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