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Based on the improved characteristics of the mutant ECDs we
2024-06-19
Based on the improved characteristics of the mutant ECDs we proceeded to crystallization trials, starting with the β1-BPloop as the most promising. We obtained rod shaped hexagonal crystals reproducibly, but with moderate diffraction ability (Fig. 5). Furthermore, the crystals were sensitive in moun
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br Results and discussion br
2024-06-18
Results and discussion Conclusion In summary, a series of indazole-based derivatives were synthesized and SAR studies conducted, with view to the development of a novel Aurora kinases inhibitor. The carboxylic 2-APB group extending from the C-3 position of the aniline and substituted groups at
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The link between HPV infection and neoplasia
2024-06-18
The link between HPV infection and neoplasia has been well established. HPV encodes two oncogenes (E6 and E7) that drive W123 progression by controlling the functions of tumor suppressor proteins p53 and Rb [7]. HPV is associated with more than 99% of cervical CESC cases [8]. CESC remains a major p
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In our H K ATPase assay Fig and
2024-06-18
In our H+, K+-ATPase assay (Fig. 1 and Supplementary Fig. 1), myricetin (IC50 = 0.58μM) was more potent than acid-activated omeprazole (IC50 = 1.50μM). In contrast, in oral administration in mice (Fig. 3), omeprazole (20mg/kg) more effectively inhibited gastric Edrophonium chloride secretion compar
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The allosteric site of class C receptors
2024-06-18
The allosteric site of class C receptors is generally located on the extracellular side of the TM domain (Brauner-Osborne et al., 2007, Christopher et al., 2015, Dore et al., 2014, Gregory et al., 2011, Harpsoe et al., 2017, Kniazeff et al., 2011, Pin and Prezeau, 2007, Urwyler, 2011, Wu et al., 201
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Most of lipid lowering agents have many therapeutic problems
2024-06-18
Most of lipid-lowering agents have many therapeutic problems with severe side effects, while dietary fibers as lipid lowering therapy are safer. Chitosan (CS) is a dietary fiber biodegradable, biocompatible and has many health benefits including wound healing, antiinflammatory, anti-cancers, immune-
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92 8 To further investigate the role of
2024-06-18
To further investigate the role of cholesterol in the Rh2-induced cytotoxicity, we then focused on the U937 cell line, which is cholesterol auxotroph and considered as a valuable model to study the importance of cholesterol in membrane structure and function (Billheimer et al., 1987), and used the e
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Our previous studies and others
2024-06-18
Our previous studies and others have identified that the inhalational anesthetic isoflurane induces neuronal apoptosis via [Ca2+]i overload through the opening of synaptic voltage-dependent calcium channels (VDCCs) and the excessive Ca2+ release from the endoplasmic reticulum (Zhao et al., 2011; Zha
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At Johns Hopkins Aramco Health JHAH
2024-06-18
At Johns Hopkins Aramco Health (JHAH), we started an ASP in 2011 with an educational program of physicians and pharmacist. The program was enhanced mid-2012 with the following interventions: a re-designed antibiotic sensitivity report [2], intravenous to oral conversion program, vancomycin pharmacok
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Under some pathological conditions AT R internalization is d
2024-06-18
Under some pathological conditions, AT1R internalization is decreased when agonist exposure is prolonged. This weakens or removes the AT1R desensitization effect and leads to AT1R and downstream signal overactivation. AT1R overactivation can result in continued biological effects such as sustained v
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An ALK rearrangement was found in
2024-06-18
An ALK rearrangement was found in all the analyzable ‘truly positive’ IHC+/FISH+ samples, and the proportion of the various transcripts was in accordance with the literature [[26], [46], [47], [48]]. In these samples, the RNA-seq technique was therefore 100% sensitive and specific. Additional non-ta
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All desired compounds with a carboxylic acid substituent
2024-06-18
All desired compounds with a carboxylic (+)-Aphidicolin substituent at N1 position of the quinoxalinone scaffold and a variety of aromatic substituents at C3 position were obtained by the syntheses starting from methoxy-substituted 3-chloro-quinoxalin-2(1)-ones () prepared as previously. As shown i
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br Downstream signalling of AKT A consensus
2024-06-18
Downstream signalling of AKT A consensus phosphorylation motif has been described for AKT substrates: R-X-R-X-X-S/T-B where X represents any amino Calcium Ionophore I and B represents bulky hydrophobic residues (Alessi, Caudwell, Andjelkovic, Hemmings, & Cohen, 1996). Numerous AKT substrates hav
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br Regulation of AHR Activity AHR activity is
2024-06-18
Regulation of AHR Activity AHR activity is regulated in various ways. First, AHR protein levels are controlled via ubiquitin-mediated proteosomal degradation: Ligand binding induces AHR ubiquitination and subsequent degradation by the proteasome [5]. AIP, a component of the AHR chaperone complex,
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The lack of specific PARP
2024-06-18
The lack of specific PARP inhibitors prevents our understanding of how TIPARP or perhaps other PARPs affect AHR signaling. Current inhibitors are based on NAM and were designed to inhibit PARP1 [59]. Many of them do not effectively inhibit mono-ADP-ribosyltransferases and their ability to inhibit TI
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