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Drug resistance to both pathogens and cancer has been
2021-04-15

Drug resistance to both pathogens and cancer has been a big hindrance in healthcare. Integrated research undertakings are being pursued to find the exact causes of the lack of response towards drugs. Surprisingly, host pumps are the key factors in failure of most drugs. The pumps either do not allow
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Immunomodulation effects of certain oxysterols
2021-04-15

Immunomodulation effects of certain oxysterols were previously shown to depend on activation of oxysterol-binding liver X receptors (LXRs). Recent work from our labs as well as from others has shown additional receptors linking oxysterols and immunity. For example, we found that 7α,25-dihydroxychole
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br Ubiquitin Capture by the Mobile APC
2021-04-15

Ubiquitin Capture by the Mobile APC11 RING Domain Contributes to Processive Substrate Ubiquitylation Although the rules of Ub-mediated proteolysis are only beginning to emerge, the rate and order in which different APC/C substrates are degraded during the GSK503 mg correlates with processivity o
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br RING dimerization RING type domains are
2021-04-14

RING dimerization RING-type domains are found in many different structural contexts. While many exist as single-chain K-7174 (Fig. 3A), a notable feature of RING-type E3s is their tendency to form homodimers and heterodimers (Fig. 3C–F). Homodimeric RING-type E3s include cIAP, RNF4, BIRC7 (shown
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The pseudo DUBs KIAA and Abraxas are required
2021-04-14

The pseudo DUBs KIAA0157 and Abraxas are required for the catalytic function of BRCC36. Comparison of the BRCC36–KIAA0157 heterodimer structure with an inactive BRCC36 homodimer structure provides a model for understanding how this functional interplay is achieved. As shown in schematic form in Figu
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In general graphene nanoplatelets have many
2021-04-14

In general, graphene nanoplatelets have many useful features for the design of multifunctional composite materials, including excellent electrical and thermal conductivities, considerable weight-saving lightness, and high mechanical strength [26]. Moreover, they are characterized by a high specific
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br Diacylglycerol kinases and T cell responses br Diacylglyc
2021-04-14

Diacylglycerol kinases and T cell responses Diacylglycerol kinases and cancer Several studies implicate DGKα in tumor progression, but its function is debated, as it might also have roles as a tumor suppressor. Diminished DGKα expression is linked to malignant transformation in epithelia. High
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QSAR based on the D structures of ligands plays
2021-04-14

QSAR based on the 3D structures of ligands plays an important role in the ligand-based drug discovery and design [12]. Comparative molecular field analysis, CoMFA [11], and comparative molecular similarity index analysis, CoMSIA [12] are among the most popular QSAR models. They focus on changes in 3
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Besides degrading cholesterol the cholesterol degradation pa
2021-04-14

Besides degrading cholesterol, the cholesterol degradation pathway also offers a route to obtain useful starting materials for the production of steroid drugs and hormones. Indeed, steroids are among the most marketed pharmaceuticals with about 300 approved steroid drugs [15] and a worldwide market
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To date the role of CRF and CRF
2021-04-14

To date, the role of CRF and CRF1+ neurons within the amygdala in the expression of anxiety-like behavior and conditioned fear, and the place where these cell populations fit into the fear-related microcircuitry already identified in the CeA, have not been fully characterized. Recent evidence suppo
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Population genetic summary statistics for five super and sub
2021-04-14

Population genetic summary statistics for five super- and 26 sub-populations, including haplotype and diplotype frequencies (analogous to allele and genotype frequencies), observed (Ho) and expected (He) heterozygosities, pairwise genetic distances, and tests for detection of departures from Hardy W
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It is very important to decide what
2021-04-14

It is very important to decide what the best time of NIR laser irradiation is for the optimized PTT. So the best way is to monitor the biodistribution of the nanoparticles in various tissues (specially, in tumors) temporally and spatially after iv injection. Based on the combined functions of therap
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Compounds and possessed relatively low clogP
2021-04-14

Compounds 11–13 and 15 possessed relatively low clogP values and tended to show relatively weak antagonist activity regardless of their potent EP1 receptor affinity. Compounds 2–4, which were selected based on their potent in vivo antagonist activity, were found to be effective in an animal model.
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Several studies have demonstrated that
2021-04-13

Several studies have demonstrated that αSyn specifically associates with lipid rafts (Cole et al., 2002), raising the possibility that the perturbation of rafts can affect the aggregation and phosphorylation of αSyn (Fortin et al., 2004). Schneider et al. (2010) described the potential involvement o
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Historically covalent drugs have had great
2021-04-13

Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form
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