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Within the X CX PX RX
2019-10-02

Within the X1CX3PX5RX7 motif of several prokaryotic FGE substrates, the residues of X3, X5, and X7 are variably found as mixtures of alanine, glycine, threonine, or serine residues [26], [27]. The docked model of our identified HCTPRRP motif revealed that position X1 (H1) and position X7 (P7) were n
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STO-609 acetate Although many of the hepatic responses
2019-10-02

Although many of the hepatic responses observed on the first day of recovery attenuated over the course of the recovery period, minimal-to-mild centrilobular hepatocellular hypertrophy tended to persist. Mean absolute and relative liver weights had returned to control levels after 28 days of recover
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new product Cancer patients may develop cachexia a deleterio
2019-10-01

Cancer patients may develop cachexia, a deleterious wasting syndrome that is associated with muscle atrophy and has an impact on the well-being of patients and on the response to the treatment. Indeed, cachexia is a devastating and often irreversible syndrome observed in up to 80% of cancer patients
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Dipeptidyl peptidase inhibitors DPP is or gliptins stimulate
2019-10-01

Dipeptidyl peptidase-4 inhibitors (DPP-4is or gliptins) stimulate both post-meal insulin secretion and inhibit L189 secretion in a glucose-dependent manner, rendering the risk of hypoglycaemia minimal [10]. They are weight-neutral or may even induce slight weight loss. Their good efficacy has been d
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van Linden et al developed a
2019-10-01

van Linden et al. developed a comprehensive guide that describes drug and ligand binding to more than 1200 human and mouse protein kinase domains [77]. Their KLIFS (kinase–ligand interaction fingerprint and structure) directory includes an alignment of 85 potential ligand binding-site residues occur
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The identification of a functional leucine rich NES mediatin
2019-10-01

The identification of a functional leucine-rich NES mediating 8E7 nuclear export led us to analyze the interaction between 8E7 and CRM1 nuclear export receptor. HeLa cell lysates containing EGFP-8E7, EGFP–8cE7, EGFP-16E7–NES (as a positive control), or EGFP (as a negative control) were incubated wit
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MTT results show that both pancreatic cell
2019-10-01

MTT results show that, both pancreatic cell lines were quite sensitive to camptothecin (CPT), a well known topoisomerase I poison. Interestingly, CPT does not show any selectivity over cancer cell lines probably due to the duplication times for cancerous (MIA PaCa-2) and immortalized healthy (HPDEC)
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Many studies have used paradigms based
2019-10-01

Many studies have used paradigms based on animal models to understand human emotional behavior because it appears to be correlated with fear- and anxiety-related defensive patterns in non-human mammals (Blanchard et al., 2001). In this case, defensive reactions are used to study the neural substrate
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The inhibition of CYP activity
2019-10-01

The inhibition of CYP11β activity by NOR was 11- and 2.5-fold higher than those reported for the antifungal agents ketoconazole (IC50: 4.4μM) and clotrimozole (IC50: 1.0μM) (Fernandes and Porte, 2013). Furthermore, NOR was able to inhibit P450 aromatase activity in carp ovaries, although at a rather
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Kinetic isotope effects KIEs inform on bond vibrational chan
2019-10-01

Kinetic isotope effects (KIEs) inform on bond vibrational changes between the ground state (GS) and TS of a chemical reaction and remain one of the most powerful experimental techniques for interrogating TS structure. KIEs on enzyme reactions measured by the internal AZD-3463 pathway of labeled subs
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br Mass spectrometry based technologies Oxysterols tend not
2019-10-01

Mass spectrometry-based technologies Oxysterols tend not to be observed in global lipidomic analysis, whether shot-gun based electrospray ionisation – mass spectrometry (ESI-MS) or liquid chromatography (LC)-MS based. This is because of their comparatively low-abundance and poor ionisation charac
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SCH772984 HCl kinase From a mechanistic standpoint the BCL R
2019-10-01

From a mechanistic standpoint, the BCL6 RD2 domain represses the GPR183 and S1PR1 loci by recruiting HDAC2, but not MTA3-NuRD, to suppress the enhancer activation mark H3K27ac at their distal regulatory elements. However, these data do not exclude the possibility that other as yet unknown corepress
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Collectively our results indicate that
2019-10-01

Collectively, our results indicate that GSK682753A functions as a competitive antagonist and binds to the receptor in the same region as 7α,25-OHC. First, we observe linearity in the Schild plot analysis (Fig. 2B). Second, GSK682753A is highly dependent on F111 at position III:08/3.32 in TM-III (Fig
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DL-AP5 p as a cyclin dependent kinase inhibitor exert
2019-10-01

p21, as a cyclin-dependent kinase inhibitor, exert significant negative regulator of proliferation, and it could be transcriptional upregulated by p53 in order to impel transient DL-AP5 arrest (Romanov et al., 2010). Using western blotting, we found that the protein expression of p21 upgrades first
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br E mediated E discharge E ligases simultaneously
2019-10-01

E3-mediated E2 discharge E3 ligases simultaneously interact with the substrate and the SUMOD charged E2 enzyme to catalyze the discharge of the thioester-bound SUMOD from the E2 to the substrate. E3 interaction with SUMOD via a SIM results in a closed conformation which is highly reactive and lea
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