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The first rationally designed dual mPGES
2024-06-21
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic calmodulin dependent protein kinase - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted deri
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Taniyama et al reported a female
2024-06-21
Taniyama et al. reported a female with infertility who had a homozygous T-to-A transversion at nucleotide position g.2472 in exon 3 of the CYP17A1 gene (mutation Y201N) and decreased 17-hydroxylase and 17,20-lyase activities of SMIP004 was initiated using dexamethasone to control adrenal P productio
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Having established the structural requirements for potency i
2024-06-21
Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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Defining the multiple roles of autophagy in stroke has
2024-06-21
Defining the multiple roles of autophagy in stroke has been a rapidly evolving and exciting venue for translational research, with innovative products being applied from bench to bedside. Spanning pharmacological pathway manipulation and functional experimental validation, altered autophagy activati
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Many ruthenium complexes were tested as potential anticancer
2024-06-21
Many ruthenium complexes were tested as potential anticancer agents and two complexes, namely NAMI-A (trans-[imH] [RuCl4(dmso-S)(im)]; im, imidazole) and KP1019 (trans-[indH][RuCl4(ind)2]; ind, indazole) have successfully entered clinical trials [27], [28]. NAMI-A is selectively active against meta
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Finally we argue that the estimated penetrance
2024-06-21
Finally, we argue that the estimated penetrance of 0.45% (95% CI 0.02%, 9.35%) calculated by leveraging the gnomAD (Lek et al., 2016) population data indicate that T201S is at most a low-risk gene variant for CJD. If we arbitrarily consider a central estimate of 10% or higher as the clinically signi
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2 nbdg The fluorescence in a fluorescent antibiotic
2024-06-21
The fluorescence in a fluorescent antibiotic can be derived either from functional groups with intrinsic fluorescence in an existing antibiotic, or via synthetic conjugation of a fluorophore to an antibiotic core to enable visualisation. Attachment of fluorophore to an antibiotic should ideally not
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While there is much in
2024-06-21
While there is much in vivo work on prion-like Aβ, it has not been shown that one can induce inclusions of Aβ in cultured cells as has been shown for tau and α-synuclein. One reason is practical; Aβ is a low molecular weight metabolite cleaved from within the larger amyloid precursor protein (APP) a
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RO 4929097 Several reports of single cases of MG
2024-06-20
Several reports of single cases of MG patients treated with Rituximab have claimed a favourable response (Baek et al., 2007, Gajra et al., 2004, Hain et al., 2006, Thakre et al., 2007, Wylam et al., 2003, Zaja et al., 2000). We report our experience with Rituximab in 6 patients with severe MG, 3 pa
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The sequence of our reconstructed Anc
2024-06-20
The sequence of our reconstructed βAnc is inferred based on probabilities, and the estimated probability of inferring the actual ancestral sequence is the product of the posterior probabilities for each site within the reconstructed sequence. Although the posterior probabilities (PP) for the majorit
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A review has recently been published
2024-06-20
A review has recently been published to evaluate the potential effects of food, alcohol and DMPO juices on the pharmacokinetics and pharmacodynamics of the drugs for BPH. The authors reviewed the PubMed database during the years 1991–2015. In addition, a digital version of Stockley on drug interact
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br Material and methods br
2024-06-20
Material and methods Results Discussion Clinical gene therapy trials with viral vectors have been in use for treatment of various genetic disorders and diseases, however efficacious, targetable and highly reliable non-viral delivery systems are needed for safe and long-term applications. De
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Acl converts cytosolic citrate CoA and ATP
2024-06-20
Acl converts cytosolic citrate, CoA and ATP into acetyl-CoA, ADP+Pi and oxaloacetate (Fig. 1). This cytosolic enzyme is present in few Prokaryotes and in all Eukaryotes, but not in non-oleaginous yeasts [14]. Thus, this enzyme was presumed to be essential for FA synthesis [1], [13], [15]. In most mi
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To the best of our knowledge there
2024-06-19
To the best of our knowledge, there have been only a few reports on antiangiogenic activities about C. sanki, and its antiangiogenic constituents as well as its mechanism of action are worthy of further exploring and studying. Therefore, we carried out a bioassay-guided investigation of C. sanki in
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Recent results suggest that TARPs
2024-06-19
Recent results suggest that TARPs are not the only auxiliary AMPAR subunits. Using a proteomic strategy (affinity purification of native AMPAR complexes followed by mass-spectrometric analysis), cornichon-related proteins (CNIHs) have been recently identified as components of the AMPAR protein micro
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