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On the basis of the structure of the Rab
2022-01-12

On the basis of the structure of the Rab35/ACAP2 complex, the authors identified Thr76 in switch II of Rab35 as one key specificity determinant (Lin et al., 2019). The crystal structure shows that the hydroxyl group of Thr76 forms a Fusidic Acid sodium salt with Asp756 in ACAP2, while the methyl gr
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In the pathogenesis of insulin resistance chronic
2022-01-12

In the pathogenesis of insulin resistance, chronic activation of inflammatory pathways plays an important role, and the macrophage/adipocyte inter-communication provides a key mechanism underlying the common disease states of decreased insulin sensitivity [10]. This involves the migration of macroph
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br Results and discussion br Conclusions br Introduction The
2022-01-12

Results and discussion Conclusions Introduction There is no effective treatment for HIV-associated neurocognitive disorder (HAND) which affects about half of the over 36 million people infected (Saylor et al., 2016). HIV can remain in the LEE011 during combination antiretroviral therapy (El
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br Conclusion br Acknowledgments br
2022-01-12

Conclusion Acknowledgments Introduction The gyloxalase pathway is a well-conserved antioxidant defense system found in all cells of the body [1], [2], [3], [4]. The glyoxalase pathway facilitates the neutralization of highly reactive and oxidizing dicarbonyl molecules, with methylglyoxal (M
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No other lacZ mutant showed a marked difference in mutation
2022-01-12

No other lacZ mutant showed a marked difference in mutation rate between fpg and fpg backgrounds (that is, rates were comparable between HS101 and CSH1191, HS102 and CSH1192, etc.). The number of reversion mutants was much higher in HS1194 than in any other fpg strain. The inclusion of the pTRC99a p
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To date glycine receptors have
2022-01-11

To date, glycine receptors have been found in five distinct transmembrane protein subunits (one β subunit and four α subunit (α1–α4)), combining to form two different types of functional receptors [4], [14], either α homomeric, the immature extrasynaptic glycine receptor subtype, or αβ heteromeric,
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Mycophenolic acid receptor Introduction Glucose is the most
2022-01-11

Introduction Glucose is the most important energy carrier of the brain. Glucose transporter type 1 (Glut1) is located at the blood–brain barrier and assures the energy-independent, facilitative transport of glucose into the brain [1]. Twelve transmembrane segments of the protein and an intracellula
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br Acknowledgments The authors would like to thank
2022-01-11

Acknowledgments The authors would like to thank principal investigator Edward John Pratt, MD (Lilly-NUS Centre for Clinical Pharmacology, Singapore) and study investigator Martha Hernandez-Illas MD (QPS-MRA) along with site staff, and trial participants and their families. We thank Zvonko Milicev
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Recently a lot of synthetic FFA agonists containing acidic
2022-01-11

Recently, a lot of synthetic FFA1 agonists containing acidic moieties have been reported (Fig. 1) [13], [14], [15], [16], [17], [18], [19], [20], [21]. Notably, most of FFA1 agonists usually have the common biphenyl scaffold, which resulted in a relative deprivation in structure types of agonists [2
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In the previous paper we described
2022-01-11

In the previous paper, we described the design and synthesis of tricyclic thiazoles as FBPase inhibitors, and a series of SAR studies led to the identification of phosphate 3 and difluoromethylenephosphonate 4 exhibiting potent FBPase inhibitory activities (IC50=13, 47nM, respectively) (Fig. 2). In
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Focal adhesion kinase Fakir et al also known as
2022-01-11

Focal adhesion kinase (Fakir et al., 2006), also known as non-receptor tyrosine kinase (PTK2), is a 125-kDa protein that regulates cell migration, adhesion, proliferation, and survival (Tavora et al., 2014; Yang et al., 2016; Tian et al., 2017). Many studies have observed FAK overexpression and/or h
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ci-1033 Compounds and were evaluated for their
2022-01-11

Compounds and were evaluated for their pharmacokinetic properties in rats and the results are summarized in . Following intravenous (IV) administration, both compounds displayed low clearance (CL), short half-lives (t) and low volumes of distribution (V). When dosed orally as a solution, exposure
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A complimentary approach with Per Luc cells exposed to hypox
2022-01-11

A complimentary approach with Per2:Luc Ferulenol mg exposed to hypoxia as well as with mBmal1:Luc circadian reporter cells in which we overexpressed variants of HIF-1α and HIF-2α revealed that hypoxia and HIFs can not only shorten the period but also decrease the amplitude of the clock (Figures 2 a
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Cells undergoing EMT display a
2022-01-11

Cells undergoing EMT display a downregulation of E-cadherin and dissociation of their junctional complexes that associates cell-cell contacts with the Furegrelate sodium salt australia cytoskeleton, known as the adherens junction (Berx and van Roy, 2009, Birchmeier and Behrens, 1994). Adherens junc
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Despite the rapid development of synthetic ligands
2022-01-11

Despite the rapid development of synthetic ligands, the endogenous ligands of GPR109A, GPR109B and GPR81 remained elusive until recently. This is probably the result of their relatively low potencies and their metabolite character (Table 1). Traditionally, agonists of GPCRs were believed to belong t
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