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During preparation of this manuscript
2024-05-06
During preparation of this manuscript, some studies investigating effects of Sunitinib on Axl activity in renal cancer have been published [44], [45], [46], [47]. However, there are several important considerations to take into account interpreting results of these studies. First, Sunitinib doses th
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Here we report discovery of highly selective pan Aurora
2024-05-06
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of SB505124 bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. To ide
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Adenine HCl What are the in situ effects of multi site CaM
2024-05-06
What are the in-situ effects of multi-site CaM associations with AT1R? Kai et al. showed that synthetic peptides corresponding to residues 125–137 (rat sequence) in SMD2, 217–227 in the N-terminal side of SMD3, and 304–316 in SMD4JM inhibit to various degrees AngII-induced GTPase activity of isolate
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Furthermore to address the concern
2024-05-06
Furthermore, to address the concern that the observed positive in vitro activity results might be stymied by the propensity of such assays to display false positives due to the inherent noxiousness of the tested compounds, all analogs were evaluated against Vero cells in an MTT assay. Some of the mo
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For hippocampal asymmetry two SNPs rs and rs showed
2024-05-06
For hippocampal asymmetry, two SNPs (rs1476679 and rs4147929) showed significant interaction with diagnosis. They have an inverse effect on asymmetry, which is consistent with their different roles as preventative or risk loci in AD. rs1476679 is intronic in the ZCWPW1 gene, is a histone modificatio
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Although several ARIs have reached
2024-05-06
Although several ARIs have reached various phases of clinical experimentation however most of them have been withdrawn either due to an insufficient bioavailability, their poor efficacy or adverse side effects. Currently Epalrestat is in clinical use for the treatment of diabetic neuropathy. The sid
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Mt a known to be upregulated
2024-05-06
Mt2a, known to be upregulated by ozone (Inoue et al., 2008), was also increased in vehicle-pretreated rats exposed to ozone, however, this effect was markedly reduced by both PROP and MIFE, suggesting that the neuroendocrine response is linked to ozone-induced acute phase protein expression. In huma
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Lipotoxicity is the accumulation of
2024-05-06
Lipotoxicity is the accumulation of excess lipids in non-adipose tissues that leads to cell dysfunction or cell death. It may play an important role in the pathogenesis of diabetes, and contributes to the rate of progression of CKD [7,8]. Emerging evidence indicates that renal lipid dysregulation is
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Since natural and recombinant glycoprotein hormones exhibit
2024-05-06
Since natural and recombinant glycoprotein hormones exhibit some differences in their carbohydrate structures, we checked whether this could affect the permissive effect on FSK-induced cyclic AMP response in MLTC-1 cells. Fig. 6 shows that the same sensitizing effect to FSK is observed with pituitar
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The relatively high concentration of HT
2024-05-03
The relatively high concentration of 5-HT used in this study (100 µM) is consistent with the concentrations used in other published ex vivo studies (Ropert and Guy, 1991, Passani et al., 1994, Shen and Andrade, 1998). In our paradigm 5-HT was focally applied at the surface of the slice via a fast pe
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The role of DHT in
2024-05-03
The role of DHT in early teleost embryogenesis is not entirely clear or established, however additional studies that treat fish embryos to DHT or to specific srd5a inhibitors at critical stages of development (i.e. prior to sex differentiation) will shed light on the early functions of this androgen
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Song et al reported series of triazolylsalicylamide derivati
2024-05-03
Song et al. reported series of 1,2,3-triazolylsalicylamide derivatives and screened over kinase panel and found compound 31 as most potent which inhibited Aurora-A, specifically with IC50 of 0.37 μM. Compound 31 was about 10-fold more active for Aurora-A than for Aurora-B (IC50 = 3.58 μM reported se
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In many cells AR mediated activation of PLC
2024-05-03
In many RG7112 α1-AR mediated activation of PLC has been shown to be the downstream process for NA-induced signalling. The activated PLC initiates subsequent signalling by breakdown of PIP2 to IP3 and DAG (Fisher and Agranoff, 1987) and the process continues. To confirm if such mechanism exists in r
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Whole body loss of ACLY is
2024-05-03
Whole-body loss of ACLY is early embryonic lethal, indicating that it serves non-redundant roles during development (Beigneux et al., 2004). Silencing or inhibition of ACLY suppresses the proliferation of many cancer cell lines and impairs tumor growth (Bauer et al., 2005, Hanai et al., 2012, Hatziv
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br Discussion Herein we demonstrate that mice deficient in
2024-05-03
Discussion Herein, we demonstrate that mice deficient in L-12/15 LO are more sensitive to 3-NP-induced toxicity although a substantial individual variability in striatal lesion size in response to 3-NP in both genotypes was observed. This variability is not atypical; several studies demonstrate s
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