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According to the Nomenclature Committee of
2021-06-10
According to the Nomenclature Committee of the International Union of Biochemistry and Molecular Biology (NC-IUBMB, 1992), peptidases are divided into two classes, namely exopeptidases and endopeptidases, based on their actions on substrates and their active sites, respectively. Endopeptidases inclu
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br The role of TNFs and
2021-06-09
The role of TNFs and AD The TNF superfamily includes 19 members that can bind 29 different receptors [56, 57]; the 19 members are Lta, TNF-α, lymphotoxin-β (LTβ), OX40L, TNF associated activation protein (TRAP, also named CD40L or gp39), factor associated suicide ligand (FasL), CD70, CD153, 4-1BB
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The CRTH inhibitory activities of
2021-06-09
The CRTH2 inhibitory activities of the synthesized compounds are listed in , . At first we introduced halogen or other substituents at the 4,4′-position of phenyl rings in the benzhydryl moiety in order to obtain SAR and to improve the metabolic stability at this moiety (–). It is well-known that in
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Although the phase I clinical trial of LMB was
2021-06-09
Although the phase I clinical trial of LMB was unsuccessful, the detailed review of this trial only mentions some malaise and anorexia as side effects, which are common for most effective chemotherapeutic drugs. These side effects may diminish if lower doses are administered. In view of the novel CR
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Another well established visceral action of CRF and
2021-06-09
Another well-established visceral action of CRF and urocortin administered peripherally is the long-lasting lowering of blood pressure observed in various species ranging from rodents to humans [22]. Existing evidence suggests that the hypotensive action of CRF and urocortin is mediated by the inter
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The synthesis of tricyclic analogs is described in
2021-06-09
The synthesis of tricyclic analogs 28–33 is described in Scheme 3. Oxidative C–C bond cleavage of the terminal olefin of 39i afforded a tricyclic product 52 without isolation of an aldehyde expected as an intermediate. Aminolysis of the chloride 52 with optionally substituted anilines afforded 28–30
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br Conclusion br Acknowledgement The project was supported
2021-06-09
Conclusion Acknowledgement The project was supported by National Natural Science Foundation of China, China (No. 31872535); Natural Science Foundation of Shandong Province, China (ZR2018MC027, ZR2016CQ29); and Funds of Shandong "Double Tops" Program, China. Introduction High-altitude hypox
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The BDNF Val Met polymorphism is also
2021-06-09
The BDNF Val66Met polymorphism is also associated with decreased dendritic arborization and impaired long-term potentiation [25]. This is particularly important for the hippocampus, and healthy individuals with a BDNF Val66Met allele have decreased hippocampal volumes [30]. Hippocampal atrophy is co
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br Objectives br Study design
2021-06-09
Objectives Study design Thirty KTx recipients were enrolled in this pilot study from December 2015 to May 2016. Patient demographics are presented in Table 1. The inclusion criteria were: age ≥ 18 years and CMV-IgG serostatus (D+/R−, D+/R+, D−/R+) pre-Tx. All patients were enrolled during the
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The four other mutations S T V I
2021-06-09
The four other mutations (S281T, V317I, T328A and A329S) were not detected in the absence of the A286S. This could suggest that when all of them are present, there would be a tri-dimensional structural modification that would interfere with the binding of the insecticide and produce different levels
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To develop novel EPAC inhibitors Zhou and co
2021-06-09
To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock
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br Cytochrome P monooxygenases Cytochrome P
2021-06-09
Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are o
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SynaptoRedTM C2 br Conclusion The past few years have witnes
2021-06-09
Conclusion The past few years have witnessed substantial progress in understanding the structural mechanisms of substrate recognition and the reactions catalyzed by the O-GlcNAc-cycling enzymes, but more work remains. In particular, future research will be needed to establish how OGT and OGA inte
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A comparative analysis of the
2021-06-09
A comparative analysis of the cleavage activity of different forms of the BoNT/A endopeptidase in reduced conditions with SNAPtide and full-length SNAP-25 substrate is summarized in Fig. 5, Fig. 6. The BoNT/A LC was found to be the most active against SNAPtide, a small peptide segment of the SNAP-25
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In vitro studies in NSCLC cell
2021-06-09
In vitro studies in NSCLC cell lines expressing EGFR mutants (T790M mutation, exon 19 deletion E746-A750, L858R/T790M double mutation), demonstrated that Rociletinib potently inhibits proliferation in the mutant EGFR NSCLC potassium hydrochloride with Growth inhibition (GI50) values ranging from 7 t
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