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br Conclusions The PQQ dependent CcPDH is the first PQQ
2021-03-26

Conclusions The PQQ-dependent CcPDH is the first PQQ-dependent enzyme identified in eukaryotes. The PQQ cofactor binds the enzyme with high affinity, reflected in a Kd of 1.1 nM, and the enzyme oxidizes 2KG, l-fucose, and rare sugars such as d-arabinose and l-galactose. The AA8 cytochrome b domai
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GSK1016790A Calcium dependence of CaM target interaction
2021-03-26

Calcium dependence of CaM/target interaction was analyzed using a titration matrix in which both Ca2+ and CaM concentrations were changed. This gave us access to different parameters characterizing the interaction and namely to the number of bound Ca2+ required for the interaction to occur. Our app
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br Fragment based drug discovery FBDD is a powerful method
2021-03-26

Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical hqn sale space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency. It al
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br Results br Discussion br Experimental Procedures
2021-03-26

Results Discussion Experimental Procedures Acknowledgments In the preceding paper, we reported 3-amido-4-anilinoquinolines as highly selective inhibitors of CSF-1R kinase, along with our initial efforts to optimize the series. Examples from the 6,7-dimethoxyquinoline series were very p
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Considering all these facts in
2021-03-26

Considering all these facts, in the present study, we investigated the effects of two highly selective CRF receptor 2 antagonists (antisavaugine-30, ASV-30; and astressin-2B, AST-2B) on anxiety behavior in rats. The rationale for such an experimental approach was based on the premise that fear and s
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Converging evidence suggests that reduced glutamate
2021-03-26

Converging evidence suggests that reduced glutamate transmission in the LS is linked to increased anxiety-like behaviors (Radulovic et al., 1999, Henry et al., 2006, Bakshi et al., 2002, Liu et al., 2004). Therefore, attenuated CRF1 receptor-mediated excitatory transmission in the LS following ASV-t
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In summary our findings indicate that bFGF stimulates
2021-03-26

In summary, our findings indicate that bFGF stimulates CPT1 expression, FA oxidation and lactate production with the participation of PPARβ/δ activation. On the other hand, this investigation shows that FSH concomitantly regulates the expression of genes involved in FA metabolism and in mitochondria
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br Acknowledgments br Introduction Cholesterol is an essenti
2021-03-26

Acknowledgments Introduction Cholesterol is an essential lipid for the development, growth, and wellbeing of humans. In newborn children, cord blood cholesterol concentration is 1.5 mmol/l, on average [[1], [2], [3], [4]]. During the first year of life, cholesterol concentration in serum incre
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Interest in the PGE EP
2021-03-25

Interest in the PGE2/EP4 pathway is increasing given its diverse capability of regulating central nervous system activity [13]. EP4 has a protective function by reducing cerebral injury and improving functional outcome after stroke [14], and in suppressing UO 126 inflammation [15]. The EP4 receptor
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MG-132 Enhanced responses to varying concentrations of
2021-03-25

Enhanced responses to varying concentrations of bronchoconstrictors, such as MCh, and airway obstruction are characteristic of MG-132 and common to other clinical states, including chronic obstructive pulmonary disease, lung transplantation, and infection- or chemical agent-induced airway inflammat
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The structure of the HOIP RBR LDD module bound to
2021-03-25

The structure of the HOIP RBR–LDD module bound to UbcH5~Ub reveals insights into an activated HOIP component [47]. Contacts between the E2~Ub and the non-cognate RBR module in the crystal suggest how a structure in which the active sites of the E2 and the E3 are in close proximity might look. In thi
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HCV has evolved mechanisms to evade humoral
2021-03-25

HCV has evolved mechanisms to evade humoral immune responses including high functional flexibility and variability of immunogenic portions of its envelope proteins. The highest sequence variability occurs in the first 27 vitamin k3 of the N-terminus of E2, which is referred to as the hypervariable r
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In vitro study indicated the cell
2021-03-25

In vitro study indicated the cell death of hippocampal neurons was mediated by DAPK1 following ceramide-3 treatment (Pelled et al., 2002). the same study showed that DAPK1-deficient mice treated by acyl ceramide exhibit a less sensitivity to apoptosis, this proposed that DAPK1 plays a central role i
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In cancer interactions between the transformed cancer
2021-03-25

In cancer, interactions between the transformed cancer AP1903 and other cell types recruited to the tumor are important. Tumor associated macrophages provide cancer cells with a suitable low-grade inflammatory milieu including growth promoting factors. Our results suggest a novel pro-tumorigenic me
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95 9 P H is a nonheme iron II dioxygenase
2021-03-24

P4H is a nonheme iron(II) dioxygenase that uses O2 and α-ketoglutarate as co-substrates (Fig. 1A). The three-dimensional structure of mammalian P4H is unknown. We reasoned that an electrophilic analog of α-ketoglutarate could serve as an irreversible inhibitor of the enzyme and, hence, a useful prob
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