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Studies have focused on a hydrophobic
2021-05-28

Studies have focused on a hydrophobic cage at the CULT domain, conserved from bacteria to mammals, as it binds to substrates and IMiDs (Chamberlain et al., 2014, Lupas et al., 2015). In addition, CRBN ligand-mediated protein degradation was highly conserved, which was confirmed in vertebrates by foc
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We also identified Ubc as a functional
2021-05-28

We also identified Ubc13 as a functional E2 for LNX1 and determined the complex structure of LNX1–Ubc13~Ub, which depicts the first step of the ubiquitination process (Fig. 3a.). Comparing structural alignment of the RNF4 RING: Ubc13~Ub: Ube2V2 complex (PDB code 5AIU) [33] and the RNF4:Ubc13~Ub comp
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br Materials and methods br Results
2021-05-28

Materials and methods Results Discussion To date, several reports have suggested an involvement of DGK in bipolar disorder. A splice variant at the COOH-terminus of DGKβ has been related to bipolar disorder [15] and DGKβ KO mice showed hyperactive behavior [17]. For the other DGK isoforms,
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With regard to the DGATs
2021-05-28

With regard to the DGATs, we have found that the majority of algal species encode at least one DGAT1, although it appears to be absent from Ostreococcus and Micromonas, as is the case for yeast, S. cerevisiae. More surprising is the presence of multiple DGAT2 genes in algae, with the exception of C.
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One possible explanation for differences in the binding
2021-05-28

One possible explanation for differences in the binding ability of monomeric versus dimeric forms of DDR2 ECD to collagen could be that the monomeric form only binds to the primary GVMGFO site, whereas dimeric (and oligomeric) DDR2 ECD binds to additional sites on the collagen triple-helical molecul
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Several highly potent CysLT receptor antagonists with large
2021-05-28

Several highly potent CysLT1 receptor antagonists with large structural Fmoc-Asp-OAll have been developed. Beyond antagonists with structures analogous to cysteinyl leukotrienes, other subclasses comprise: (a) hydroxyacetophenones, (b) indoles and indazoles, (c) quinolines, benzothiazoles, and thiaz
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To be a qualified non specific CYP inhibitor
2021-05-28

To be a qualified non-specific CYP inhibitor used as an in vitro or in vivo screening tool to distinguish CYP involvement in the overall metabolism, a complete inhibition of the entire metabolism catalyzed by CYPs in a simple experiment is desired. Based on our results, 100 μM atipamezole can comple
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With the narrow SAR of the tail
2021-05-28

With the narrow SAR of the tail favouring the ortho sulfone group, we examined the remaining position open to substitution at the pyrazole 3-position, in an attempt to at least moderate the excessive human PPB (). Lipophilic groups in this position maintained huge shifts in potency in the absence or
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br Acknowledgements We thank A
2021-05-27

Acknowledgements We thank A. Devia-Barros and S.A. Barrios Latorre for invaluable technical support during the collection, maintenance and exposure of oysters. We are, furthermore, grateful to the municipal marina of Santa Marta for authorizing access to their facilities and to A. Franco for faci
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Because of the lack of sequence
2021-05-27

Because of the lack of sequence, current knowledge on the cellular regulation of CoA-IT is scarce. However, recent work has suggested an interesting new role for CoA-IT in regulating the extent of the AA mobilization response in primed macrophages. Bacterial lipopolysaccharide (LPS) is a poor trigge
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Lavallee et al reported that PREG could be esterified by
2021-05-27

Lavallee et al. [30] reported that PREG could be esterified by lecithin:cholesterol acyltransferase (LCAT). LCAT uses cholesterol and phosphatidyl choline present in the newly formed high-density lipoprotein (HDL) as substrates and convert them into cholesteryl esters and lysophosphatidyl choline. T
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DNA bound Ku proteins recruit DNA PKcs and thereby transloca
2021-05-27

DNA-bound Ku proteins recruit DNA-PKcs; and thereby translocate into the duplex by one helical turn, leaving DNA-PKcs near the DNA terminus to assist in tethering the broken ends together [25]. In addition to keeping the DSBs in close proximity, DNA-PKcs may prevent exonucleolytic degradation of the
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STRING protein interactions were used to highlight enzymes
2021-05-27

STRING protein interactions were used to highlight enzymes directly associated with DHODH (Fig. 10) (Szklarczyk et al., 2015). The reported protein-protein associations are primarily within the de novo nucleotide synthesis pathways (CAD, carbamoyl phosphate synthetase 1, uridine monophosphate synthe
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WAY 208466 dihydrochloride A range of inhibitors were
2021-05-27

A range of inhibitors were therefore synthesized containing either carboxylic WAY 208466 dihydrochloride or ester functionality at the ‘tail’ group as well as variations in the ‘head.’ These were assayed in vitro using the DCIP assay for binding affinity against and human DHODH at 50μM, respective
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The recombinant Scl collagen system has shown
2021-05-27

The recombinant Scl2 collagen system has shown capability as a biomaterial as well because of its adaptability and scalability. Scl2 was functionalized to crosslink into a hydrogel without disrupting its triple helix [130]. The Scl2–hydrogel crosslinking also did not disrupt cell adhesion and integr
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