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It was hypothesized that if
2021-01-20

It was hypothesized that if modafinil acts primarily via a noradrenergic mechanism, Dbh −/− mice should be non-responsive since they completely lack NE. In contrast, if modafinil acts mainly through DA systems, these mice should be hypersensitive. Modafinil was tested in Dbh −/− mice using both loco
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DGK is distributed exclusively in the brain particularly in
2021-01-20

DGKβ [9] is distributed exclusively in the brain, particularly in the striatum, cerebral cortex, olfactory bulb, and hippocampus [9,10]. This isozyme accumulates at the perisynaptic sites of medium spiny neurons in the striatum [11]. The Mifepristone of DGKβ rapidly increases after 14 days of age,
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Other karyopherins besides CRM must bind
2021-01-20

Other karyopherins besides CRM1 must bind to FG-Nups in a similar fashion. However, at an atomic resolution, only the interaction of importin β with isolated FG motifs has been analyzed (Bayliss et al., 2000, Bayliss et al., 2002, Liu and Stewart, 2005). Despite similarities in the FG-binding pocket
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Considering all these facts in the present
2021-01-20

Considering all these facts, in the present study, we investigated the effects of two highly selective CRF receptor 2 antagonists (antisavaugine-30, ASV-30; and astressin-2B, AST-2B) on anxiety behavior in rats. The rationale for such an experimental approach was based on the premise that fear and s
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To extend these toxicity minimization
2021-01-20

To extend these toxicity minimization strategies to 3D tissues, a more complicated mass transfer model is necessary to account diffusion in the interstitial space, as well as transport across cell membranes. Until recently, tissue mass transport in cryobiology was modeled using classic spatially dep
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Finally considering the encouraging inhibitory and selectivi
2021-01-20

Finally, considering the encouraging inhibitory and selectivity properties of compound and against isolated CK1δ, we have also acquired a very preliminary cytotoxicity profile on human ovarian carcinoma cell line (2008) and on its cisplatin-resistant clone (C13). Results showed that after 48h of e
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The action of pt PGE as an EP receptor
2021-01-20

The action of 17-pt-PGE2 as an EP1 receptor agonist [34] was demonstrated in several experimental settings, including cancer, neurons, vascular system, kidney and was confirmed by application of EP1 receptor selective antagonists [35], [36], [37], [38], [39], [40], [41]. Receptor binding studies in
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Upon assembly of HLA tetramers loaded
2021-01-20

Upon assembly of HLA tetramers loaded with either of the two peptide versions, we could query the T cell repertoires of RA subjects and healthy individuals for the presence of cognate T Cilengitide recognizing the respective peptide-HLA complexes. We found no significant difference in frequencies o
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The most significant finding was the inhibition of EROD
2021-01-20

The most significant finding was the inhibition of EROD and BFCOD activity by CLO. Inhibition of EROD and BFCOD were reversible, as pre-incubation did not enhance CLO inhibitory potency, and no reductions in IC50 values were observed. We further characterized the kinetic pattern of inhibition using
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br Lymphoplasmacytic lymphoma Waldenstrom macroglobulinemia
2021-01-20

Lymphoplasmacytic lymphoma/Waldenstrom macroglobulinemia Lymphoplasmacytic lymphoma (LPL) and its subgroup Waldenstrom macroglobulinemia (WM) are rare and indolent lymphomas that arise from fully differentiated B cells. The only family of GPCRs that has been well studied in LPL/WM is the chemokin
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Our study provides proof of principle for dimerizing
2021-01-19

Our study provides proof of principle for dimerizing two different E3 ligases as a novel approach to inducing one ligase to degrade the other one. The outcome of ‘ligase versus ligase’ PROTAC-mediated activity might be unpredictable a priori, but could reveal a new mechanism for proximity-mediated h
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In conclusion we have found that Egr can play an
2021-01-19

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 tnf-a at the −227/−224 region of DBH promoter. This inhibition appears to result from Egr1 directly bound to the DBH promoter. We specula
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Previous in vitro studies have
2021-01-19

Previous in vitro studies have demonstrated that DNA-PK-deficient cell line (MO59J) is approximately 30-fold more sensitive to radiation than DNA-PK-proficient cell line (MO59K) [31]. Moreover, specific DNA-PK inhibitors SU11752 and wortmannin have been shown to sensitize GBM apexbt dilution calcula
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Cysteine protease inhibitors representing several chemical s
2021-01-19

Cysteine protease inhibitors representing several chemical scaffold types are effective in halting parasite replication without toxicity to the host (Renslo and McKerrow, 2006). A vinyl sulfone cysteine protease inhibitor, K11777, is completing final Good Laboratory Practice (GLP) preclinical tests
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Another well established visceral action
2021-01-19

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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