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The structure of the HOIP
2020-06-13

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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Although our knowledge of the biochemical and biological fun
2020-06-13

Although our knowledge of the biochemical and biological functions of E3 ubiquitin ligases has increased in B-cell malignancies, a deeper characterization of cell-context dependent substrate regulation and biological relevance is needed. The recent approval of a general proteasome inhibitor, VELCADE
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Moreover maintaining the pyrimidine pool is not the only imp
2020-06-13

Moreover, maintaining the pyrimidine pool is not the only important role played by DHODHs. In Toxoplasma gondii, for instance, DHODH plays a second essential function [38] possibly coupled to the mitochondrial respiratory activity, where it replenishes ubiquinol levels and prevents reactive oxygen s
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Asunaprevir Fig D shows that E lagascae
2020-06-13

Fig. 2D shows that E. lagascae VIR E gives two species of radioactive TAG: one represents 45% of total labelled TAG and the smaller more-polar spot (15%) is probably derived from the endogenous 1,2-divernolin instead of the exogenous 1,2-diolein. In this case, the total scintillation counts were gre
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Recently Schenck et al identified an active site asparagine
2020-06-13

Recently, Schenck et al. [25] identified an active site asparagine 222 (N222) residue in the Glycine max TyrAp/PDH (GmPDH1) that is responsible for its prephenate substrate specificity. Mutating the single N222 into an acidic residue (i.e. aspartate, D) in the legume TyrAp/PDH shifted from prephena
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br Proteases with special focus on cysteine
2020-06-13

Proteases with special focus on cysteine proteases Vaccination using cysteine proteases as antigens with special emphasis on DNA-vaccines Concluding remarks In spite of the great potential of DNA vaccines, the technology has not been as revolutionary as expected in higher mammals. In fish,
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Acidic substituents showed moderate biochemical activity but
2020-06-13

Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic PF-04449913 receptor were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their bi
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In a previous study we reported that
2020-06-13

In a previous study we reported that the systemic administration of the α1-adrenergic receptor antagonist prazosin attenuates the deficit in Sirtinol reward function associated with precipitated nicotine withdrawal (Bruijnzeel et al., 2010). One of the aims of the present experiments was to investi
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Partial suppression of the cot ts phenotype by deletion of
2020-06-13

Partial suppression of the cot-1 (ts) phenotype by deletion of gul-1 has been well documented (Seiler et al., 2006). This is now also very clearly evident in the transcriptional profile of the various strains (Fig. 2). Furthermore, the comparative analysis of the single and double mutants revealed,
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The present study sought to determine if chlorodifluoroaceto
2020-06-13

The present study sought to determine if chlorodifluoroacetophenones, such as 3 and 4, were amenable to a radiolabelling methodology to generate potential 18F imaging agents with high cholinesterase affinity. A number of procedures have been reported for the synthesis of trifluoromethyl ketones, inc
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The ACC receptor family appear to be
2020-06-13

The ACC receptor family appear to be attractive targets for the development of novel anthelmintics. With this in mind we also tested the activity of the anthelmintics levamisole and pyrantel which activate the nematode nAChR (Martin and Robertson, 2007). We found both molecules were partial agonists
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So what can we glean from this illuminative foray into
2020-06-13

So what can we glean from this illuminative foray into how Chk1 and MK2 participate in checkpoint control? First and foremost, this work reveals that PF-00562271 deficient in the tumor suppressor p53 contain two spatially distinct G2/M phase checkpoint control kinase networks. This provides compell
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The P H activity and the large
2020-06-12

The P4H activity and the large number of 4-Hyp residues that are formed, amounting to half of all the Pro residues or 10% of all residues, have been identified as having a clear role in the structure and chemistry of the triple helix [3]. The role of the rare 3-Hyp residues is less clear and is stil
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br The modulation of ER from SERMs to TSECs
2020-06-12

The modulation of ERα: from SERMs to TSECs Continued efforts to provide women with efficacious menopausal therapies have generated interest in the development of selective Conoidin A receptor modulators (SERMs). Similar to estrogens, SERMs have been shown to bind to ERs with high affinity, despi
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In mammals ribonucleotide reductase RNR
2020-06-12

In mammals, ribonucleotide reductase (RNR) is a unique enzyme that catalyzes the rate-limiting step of de novo synthesis of deoxyribonucleoside triphosphates (dNTPs).7, 8 Mammalian RNR consists of two homodimer subunits: the large catalytic dimer RRM1 and the small regulatory dimer RRM2 or RRM2B. An
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