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br Introduction Epidermal growth factor
2019-12-17
Introduction Epidermal growth factor receptor (EGFR)-activating-mutant non-small cell lung cancer (NSCLC) often initially responds well to EGFR tyrosine kinase inhibitors (TKIs) (Haber et al., 2011); however, the disease almost always recurs about 10–13 months of therapy. Analysis of clinical spe
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These studies established IAP proteins
2019-12-17
These studies established IAP proteins as dimeric RING E3 ligases, but did not account for the essential role of dimerization. In IAPs and related E3s, such as RNF4 and MDM2, dimerization not only depends on contacts from the core RING domain but also residues N- and C-terminal to the RING domain (B
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N acetylation by N acetyltransferase NAT is an
2019-12-17
N-acetylation by N-acetyltransferase (NAT) is an important metabolic pathway for some substances, and there are 2 functional NAT isoforms in humans—NAT1 and NAT2. Studies of etamicastat in healthy subjects showed an extensive N-acetylation of etamicastat to the inactive metabolite BIA 5-961, and a l
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In our current work we have undertaken
2019-12-17
In our current work, we have undertaken liquid phase combinatorial synthesis methods for the synthesis of 1,2,5-trisubstituted benzimidazole derivatives as hDHODH inhibitors. Synthesised 839 were also screened by molecular docking studies over the reported hDHODH structure. The synthesised molecule
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Although shoulder dub off on gun drills has significant
2019-12-16
Although shoulder dub-off on gun drills has significant influence on chip transportation behavior, most commercial gun drills adhere to a fixed design of 20° that has limited scientific basis. To determine the effects of shoulder dub-off on chip evacuation, 5 different angles ranging from 0° to 30°
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In conclusion we have found that
2019-12-16
In conclusion, we have found that Egr1 can play an inhibitory role on DBH promoter-driven transcription. This inhibition requires a newly identified Egr1 response Amyloid Beta-peptide (25-35) sale at the −227/−224 region of DBH promoter. This inhibition appears to result from Egr1 directly bound to
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We have compared the potency of a series
2019-12-16
We have compared the potency of a series of DNA-directed alkylating agents, including N-mustard-acridine, N-mustard-quinoline, and N-mustard-quinazoline conjugates previously synthesized in our laboratory [7], [13], and currently used drugs (oxaliplatin, cisplatin, or 5-FU) for the treatment of CRC
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Although PQQ has nutritional importance
2019-12-16
Although PQQ has nutritional importance and pharmacological effects in higher organisms, including humans [15], until recently, there was no clear evidence for the use of PQQ as a co-factor in a eukaryotic enzyme. This review presents a novel eukaryotic PQQ-dependent quinohemoprotein recently discov
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In addition we investigated if
2019-12-16
In addition, we investigated if the previously reported papain inhibitor can inhibit rhodesain, and found that it was not active at inhibiting rhodesain. The vinyl sulfone analogue of () was then synthesized and tested, and it was also inactive towards rhodesain. We then determined the time depend
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CXC chemokines are primarily expressed in immune
2019-12-16
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) Otamixaban synthesis (Federsppiel et al., 1993) and cattle locus coeruleus, cerebellum and pons (Ri
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Our results also showed that the highest dose
2019-12-16
Our results also showed that the highest dose of Astressin2-B increased the rewarding effects of cocaine, since non-defeated animals treated with this dose developed CPP with a sub-threshold dose. We monitored the acute effects of 30 µg/kg of Astressin2-B and found an increase of anxiety in the open
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Abha et al reported Natural coumarinolignoids isolated from
2019-12-16
Abha et al. reported Natural coumarinolignoids isolated from the seeds of Cleome viscosa consist of a racemic mixture of cleomiscosins A 19, B 20 and C 21 and were screened for anti-inflammatory activity through mol. docking and QSAR studies by using reported in vivo activity of Swiss albino mice. B
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Several CHK inhibitors have been reported
2019-12-16
Several CHK-1 inhibitors have been reported in the literature. Of these, UCN-01 (7-hydroxystaurosporine) is a potent inhibitor of CHK-1 (=5.6nM), , and has modest selectivity among other kinases. UCN-01 is currently in clinical trials. Other CHK-1 inhibitors reported in the literature include indaz
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To our knowledge this is
2019-12-16
To our knowledge, this is the first report of an oncocytoma expressing alpha-enolase or causing autoimmune retinopathy and optic neuropathy. Although generally considered benign, oncocytomas have rarely been associated with paraneoplastic syndromes, including tumor-induced hypertension, erythrocytos
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Compounds were screened for their activity against the hERG
2019-12-16
Compounds were screened for their activity against the hERG channel, with the 2,3-Cl compounds more active here than the 2,4-F compounds. The homopiperazine examples (, , , ) showed increased hERG activity relative to the corresponding piperazines. The cell data for the 6,7-dimethoxyquinoline compo
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