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The compounds were ranked based
2020-09-27
The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR
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br Electron transfer pathway Intramolecular or inter domain
2020-09-27
Electron transfer pathway Intramolecular (or inter-domain) electron transfer (IET) in CDH has been studied in much depth [], and similar IET occurs in CcPDH, from the PQQ cofactor in the AA12 domain to the heme b in the AA8 domain. When two kinds of electron acceptors are used for measuring enzym
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Functionally all members of the IL family have
2020-09-27
Functionally, all members of the IL-12 family have been annotated along major inflammatory signaling axes but their roles have often weighed on opposing sides of the immunological balance. For instance, IL-12 and IL-23 are classified as pro-inflammatory cytokines [10] as opposed to the rather protec
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Moreover recent structural studies of VEEV nsP pro
2020-09-27
Moreover, recent structural studies of VEEV nsP2pro in complex with E-64d revealed an important molecular interaction at the interface of two subdomains. In this structure, Asn475 which is in polar contact with carbonyl oxygen of Asp507 of the protease subdomain makes an H-bond with Arg662 of the MT
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Introduction Robust evidence suggests that genetic factors i
2020-09-27
Introduction Robust evidence suggests that genetic factors influence an individual\'s susceptibility to BD (Craddock and Sklar, 2013). Yet, no single, high penetrance gene has been identified with direct causality (Craddock and Sklar, 2009). The largest GWAS to date for identifying genes conferring
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br System description and data
2020-09-27
System description and data collection Fig. 1 shows the arrangement of the system studied. It provided cooling TNKS 49 to maintain thermal conditions in an institutional building. The locations of the measured variables (, and ) relating to temperature and flow rate are indicated in Fig. 1. The
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br Progestogens and autoimmune diseases
2020-09-25
Progestogens and autoimmune diseases Conclusion Take-home messages Introduction The benefits of breastfeeding for both women and their infants are considerable [1], [2], [3]. The World Health Organization (WHO) recommends infants breastfeed exclusively during the first months of life [4]
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Among the different factors that modulate Schwann cell biolo
2020-09-25
Among the different factors that modulate Schwann cell biology, several studies pointed out the role played by neuroactive steroids, in particular progesterone (P4) and its derivatives dihydroprogesterone (DHP) and allopregnanolone (ALLO). Schwann cam kinase are steroidogenic, possessing the entire
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EP receptors belong to the family of G protein
2020-09-25
EP1–4 receptors belong to the family of G protein-coupled receptor (GPCR). Trafficking events such as externalization, internalization, recycling and degradation dynamically regulate GPCR cell surface density. A fast-rate of internalization and degradation reduces GPCR surface density to desensitize
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Previously we have reported that magnitude of the disruption
2020-09-25
Previously, we have reported that magnitude of the disruption of the blood–aqueous barrier after paracentesis was reduced by 82% in EP4 receptor knockout mice (Biswas et al., 2006). In the present study, we observed that pretreatment of EP1 receptor knockout mice with EP4 receptor antagonist, reduce
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The strand domain swap in the UbV XR
2020-09-25
The β strand domain swap in the UbV.XR dimer appears to be a unique arrangement for a Ub-based dimer. In solution, free Ub has a KD of ∼5 mM for the monomer-dimer equilibrium, and the two subunits in the dimer adopt a range of relative orientations involving residues from Ub’s β sheet (Liu et al., 2
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br APC C Uses a
2020-09-25
APC/C Uses a Dynamic Cullin–RING Mechanism to Elongate Polyubiquitin Chains Human APC/C generates Lys11-linked poly-Ub chains through an entirely different mechanism, via the distinctive E2 enzyme, UBE2S 30, 31, 32. Although APC2 and APC11 are necessary and sufficient to activate UBE2S, the mecha
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It was hypothesized that if modafinil
2020-09-25
It was hypothesized that if modafinil acts primarily via a noradrenergic mechanism, Dbh −/− mice should be non-responsive since they completely lack NE. In contrast, if modafinil acts mainly through DA systems, these mice should be hypersensitive. Modafinil was tested in Dbh −/− mice using both loc
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Tailoring pharmacological treatment to the genetic backgroun
2020-09-25
Tailoring pharmacological treatment to the genetic background of a person can enhance therapeutic response (), increase compliance (), and decrease drug toxicity (, , ). Because cocaine addiction has a strong genetic basis, with the vulnerability to develop an addiction estimated to be as high as 72
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The Lysine mutant is located in the tail region
2020-09-25
The Lysine429 mutant is located in the tail region of 5-HT2A, which is predicted to be unstructured. This region has been shown to interact, in vitro, with PSD95 and leads to differences in signaling (Xia et al., 2003). The ASK motif, a component of the tail region, is also important for regulation
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