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In the past few years neuroprotection via GLP R
2021-07-16

In the past few years, neuroprotection via GLP-1R activation has been shown in several animal models of stroke, Alzheimer's, Parkinson's, Huntington's, ALS and traumatic HC-030031 mg injury. This research field is rapidly growing and several reviews have been recently published (Darsalia et al., 201
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br Phylogenetic analysis KSTDs have rather
2021-07-16

Phylogenetic analysis — Δ1-KSTDs have rather diverse amino CRT0044876 sale sequences. A sequence distance analysis using the program MEGA6 [75] of all currently biochemically characterized Δ1-KSTDs yielded a largest p-distance [76] of 0.67 (on a scale of 0-1) for the Δ1-KSTDs from the actinobacter
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SR1078 br Authors contributions br Acknowledgements br Intro
2021-07-16

Authors’ contributions Acknowledgements Introduction Retinoic SR1078 is a key signalling molecule in healthy development and in differentiation of stem cells, albeit uncontrolled levels of retinoic acid can lead to mutagenesis [1]. In eukaryotes retinoic acid is made by oxidation of all-tr
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We have previously reported DAPK
2021-07-16

We have previously reported DAPK inhibitors discovered through our structure-based virtual screening (SBVS) research program. In this paper, we describe the general protocol of our in silico approach, and the strategy used to develop hit compounds. In addition, the studies conducted on the structure
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Atg cleaves Atg at the peptide bond on the
2021-07-16

Atg4 cleaves Atg8 at the peptide bond on the glycine residue at the C-terminus, thus allowing the conjugation of Atg8 to phosphatidylethanolamine (PE) with the participation of other autophagy molecules. Atg4 can also serve as a deconjugating enzyme, which cleaves the amide bond of the conjugated At
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br Results and discussion br Conclusion Novel
2021-07-16

Results and discussion Conclusion Novel and selective aziridine-based inhibitors for the Leishmania mexicana protease LmCBP2.8 were discovered. Compounds 7d (Ki = 0.8 μM), 9d (Ki = 1.36 μM), 12d (Ki = 0.77 μM), 14d (Ki = 0.9 μM) and 18 (Ki = 0.441 μM) showed the highest potency and selectivity
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CXC chemokines are primarily expressed in immune organs and
2021-07-16

CXC chemokines are primarily expressed in immune organs and the central nervous system: the mouse thymus and spleen (Heesen et al., 1996), chicken bursa (Liang et al., 2001), primate (Macaca mulatta) EPZ004777 (Federsppiel et al., 1993) and cattle locus coeruleus, cerebellum and pons (Rimland et al.
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br Advantages of modified proteins over unmodified ones In
2021-07-16

Advantages of modified proteins over unmodified ones In contrast to small-molecule drugs, proteins are readily amenable to site-specific alterations through genetic engineering. In principle, therefore, it is possible to build in features that allow them to remain active for longer in the body an
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br Materials and methods br Results br Discussion
2021-07-15

Materials and methods Results Discussion In this study, we first showed that fluxametamide, a novel isoxazoline insecticide, inhibits agonist responses in two types of LGCCs, the M. domestica GABACl and GluCl, with higher potency in the former channel versus the latter one (Fig. 3). In addi
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br Dienogest DNG Dienogest is a nortestosterone derivative w
2021-07-15

Dienogest (DNG) Dienogest is a 19-nortestosterone derivative with two special structural changes [Fig. 1a]: [a] At the cabon-17 position there is a cyanomethyl group instead of an ethinyl group; [b] A double bond is present between carbons 9 and 10. DNG is the only progestogen that combines prope
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IOX4 Studies using SERPINB deficient mice established
2021-07-15

Studies using SERPINB1-deficient mice established the significant role for SERPINB1 in protecting lung antimicrobial proteins from proteolysis during microbe infection and its regulatory role in sustaining the balance of neutrophil reserve [15]. Neutrophil serine proteases (NSPs) (elastase, cathepsi
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As in our earlier observations the PTPN SNP
2021-07-15

As in our earlier observations, the PTPN22 SNP affected the appearance of β-cell autoimmunity, but in contrast to our earlier report, only a borderline effect of the PTPN22 SNP on the progression to clinical disease was observed in the current analysis [22], [27]. The finding of an effect of the PTP
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Two parameters were extracted from these experiments to comp
2021-07-15

Two parameters were extracted from these experiments to compare the interactions of the three compounds with ct-DNA. The association constant K for the binding of the naphthalimide derivatives to ct-DNA was calculated by fitting the evolution of the fluorescence spectra with a 1:1 binding model usin
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Recently a sandwich cultured hepatocyte model has
2021-07-14

Recently, a sandwich-cultured hepatocyte model has been proved to be a valuable in vitro system that maintains specific hepatic cytomorphology and function relevant to drug metabolism, disposition and toxicity, and thus, closely resembles the in vivo setting. This hepatocyte model was recognized as
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Previously published results on this topic are inconsistent
2021-07-14

Previously published results on this topic are inconsistent. Stressin1-A, a novel CRF1 receptor agonist, increased anxiety-like behavior in the social interaction and shock-probe tests [51]. Pharmacological blockade of CRF1 (NBI-30775) reversed both CRF-induced increases in startle and CRF-induced d
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