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During the course of our ACK inhibitor program a high
2023-10-25
During the course of our ACK1 inhibitor program, a high-throughput screening (HTS) campaign of our internal sample collection was conducted. A series of -aryl pyrimidine-5-carboxamides of the general structure () was identified. Earlier studies of the structure–activity relationship (SAR) of ident
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We found that several anticancer drugs inhibit HT receptor c
2023-10-24
We found that several anticancer drugs inhibit 5-HT3 ddhGTP current in vitro. Several studies have suggested that 5-HT3 receptor antagonists have anti-mitogenic and apoptotic effects on colorectal and breast cancer cell lines (Ataee et al., 2010, Hejazi et al., 2015). Irinotecan is used frequently
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Finasteride has been shown to be a mechanism based
2023-10-24
Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a
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Regarding brain tumors AXL has been
2023-10-24
Regarding nor-Binaltorphimine dihydrochloride tumors, AXL has been implicated in gliomagenesis and chemoresistance [39]. Previous investigations found that AXL is constitutively phosphorylated in many glioma cell lines, murine xenograft tumors and primary patient tumor samples [40]. Immunohistochem
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Song et al reported series of triazolylsalicylamide derivati
2023-10-24
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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Purification of Rv c In order to investigate the
2023-10-24
Purification of Rv2477c. In order to investigate the catalytic capabilities of Rv2477c, we expressed the protein as an N-terminal histidine-tagged fusion protein in E. coli BL21 cells and purified the protein by cobalt-affinity chromatography. As shown in Fig. 2A, the 65 kDa fusion protein was expre
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The protective role of HMW HA in inflammatory
2023-10-24
The protective role of HMW-HA in inflammatory diseases and pulmonary damage led us to investigate whether PM2.5-induced ALI could be attenuated by HMW-HA and the underlying mechanisms. In this study, we used a rat model to evaluate the effect of HMW-HA on pulmonary histology, lung inflammation, oxid
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Based on our findings in this work as
2023-10-24
Based on our findings in this work as well as the previous published data in the experimental mice model of RSV infection, we suggest that modulation of 12/15 LOX expression and/or blocking of LOX products such as 12(S)-HETE may represent potential pharmacological approaches to prevent or treat vira
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Quinidine br Materials and method br Result and discussion
2023-10-24
Materials and method Result and discussion Conclusion Acknowledgments This work is partly supported by the University Research Committee (URC) of the Senate of The Federal University of Technology, Akure. The authors thanked IFS for the funds (F/4449 1F and F/4449-2F) used to purchase th
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Globally the total number of patients included
2023-10-24
Globally, the total number of patients included in the meta-analysis was 1885, ranging from 40 to 442 patients per study. All eligible studies reported the association between ALDH1 expression and patients' OS [24-26, 3241], whereas nine studies evaluated the relationship between ALDH1 expression an
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The decreased AR mediated response
2023-10-24
The decreased βAR-mediated response has been attributed to different mechanisms, including an attenuation of PKA activation, an impaired generation of cyclic AMP, a reduced receptor density, and a less efficient coupling to adenylyl-cyclase [10]. However, currently there is no single molecular or ce
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In summary the different types of interstitial cells
2023-10-24
In summary, the different types of interstitial cells found in the current study are illustrated in Fig. 7A (see legend for further details), which is suggestive of a heterogeneous complex network of interstitial cells communicating with each other. The possible signaling pathways involving this int
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br Conclusion The HT receptor family is
2023-10-24
Conclusion The 5-HT receptor family is complex, and one may ask as does Bryan Roth et al. [205] whether this is useless BI-847325 (i.e. too much redundancy) or an embarrassment of the riches (i.e. many potential targets to choose from to affect normal or pathological function); molecular biology
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The use of a single well
2023-10-23
The use of a single well-identified molecule to induce AChR clusters formation can simplify complicated cell manipulation procedures and may provide a more efficient means of developing biological substitutes for functional muscle tissue restoration in vivo. Pharmacological approaches dealing with b
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Regarding androgens it is known that they are also
2023-10-23
Regarding androgens, it is known that they are also essential for reproductive success (Walters et al., 2010). At the molecular level, their effects are produced mainly by dihydrotestosterone (DHT), arising from the conversion of testosterone by the enzyme 3-oxo-5-alpha-steroid-4-dehydrogenase (enco
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