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Bupivacaine is one of the local anesthetics commonly
2021-09-10
Bupivacaine is one of the local anesthetics commonly used in spinal anesthesia. Previous studies had shown that bupivacaine induced neuronal apoptosis and axon degeneration among various neuronal populations in spinal cord, such as sciatic nerves and dorsal root AMG 487 (DRG) neurons [5], [6], [7],
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br Funding This work was partially supported by the National
2021-09-10
Funding This work was partially supported by the National Institute on Alcohol Abuse and Alcoholism, award R00AA021264, startup funds from the Department of Immunology, Herbert Wertheim College of Medicine, and the Office of Research and Economic Development at FIU, and pilot funds from Dr. Werth
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Elimination of the Q R bridge significantly affected the pro
2021-09-10
Elimination of the Q234–R244 bridge significantly affected the protein perifosine but had little effect on its activity at a permissive temperature, which may seem contrary to the known functional importance of this motif in Fpg. However, since the mutants fully or partially retained the bound zinc
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Capillary monolithic columns obtained by in
2021-09-10
Capillary monolithic columns obtained by in situ polymerization have been developed rapidly as an efficient chromatographic stationary phase, which exhibits excellent reproducibility, reliable stability and fast transfer kinetics [18]. Recently, it has been extensively applied in capillary liquid ch
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The regulation of the stem cell compartment in
2021-09-09
The regulation of the stem cell compartment in CML is dynamic, in particular, during disease progression to a blast crisis and might involve a complex cross-regulation of Hh, Wnt, Notch, and hox signaling pathways (). Significant upregulation of Ptch1 and cyclin D1, upon other proteins, marks the bl
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The usefulness of GIP R antagonism for the
2021-09-09
The usefulness of GIP-R antagonism for the treatment of obesity-diabetes has been revealed in numerous studies employing knockout or chemical blockade of GIP-R signalling.*88, 89, *90, 91, 92, 93, 94, 95, 96, *97 For example, sub-chronic daily administration of (Pro3)GIP to ob/ob mice results in sig
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br Signals transmitted via MEGJ MEGJ
2021-09-09
Signals transmitted via MEGJ MEGJ facilitate the direct transfer of ion currents or small molecules between EC and VSMC. Molecules passing through MEGJ are mainly second messengers such as Ca2+, IP3, and cAMP [31,32,] or endothelium-derived hyperpolarization (EDH) signals [34, 35, 36]. Moreover,
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Primidone Many neutral and acidophilic galactosidases have b
2021-09-09
Many neutral and acidophilic β-galactosidases have been purified from microorganisms [14], while only a few alkalophilic β-galactosidases have been reported [19]. An alkalophilic β-galactosidase, BGal_375, was obtained and researched for the characterization of its hydrolytic activity. BGal_375 show
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br Acute host defense Inflammation the host
2021-09-09
Acute host defense Inflammation, the host response to infection and tissue injury, is crucial for survival and restoration of tissue structure and function. This acute response is mediated and governed by a variety of pro-inflammatory circuits to ensure recognition of invading pathogens, coordina
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br Conclusions and perspectives In conclusion offering duly
2021-09-09
Conclusions and perspectives In conclusion, offering duly validated and highly performing assays for measuring DiXaIs in plasma is a step, but not the final issue. More dedicated and individual assays will continue this innovative development, which witnesses the need for collaboration between co
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Given the overexpression of HO
2021-09-09
Given the overexpression of HO-1 in some tumors, such as CML, and its potential involvement in chemoresistance to classical chemotherapeutic agents, compounds 4 and 8f were tested in CML cell lines resistant to IM, a classical TK inhibitor used in CML. Compounds 4 and 8f, in combination with IM, sho
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In human platelets only and isoforms
2021-09-08
In human platelets, only α1 and β1 isoforms of sGC are expressed in equimolar concentrations (3700 copies for β1, and 3500 copies for α1 per platelet) [57] [62]. sGC, is usually a heterodimer and contains heme as cofactor which is required for high-affinity NO binding and stimulation of its activity
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Third we performed correlation analysis
2021-09-08
Third, we performed correlation analysis between the results obtained using DMR agonist assay in HT-29 and Tango assay in the engineered U2OS cells. First, we compared their relative efficacy, the maximal responses after normalized to the maximal responses of zaprinast obtained using both DMR and Ta
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br FXR Agonists Azepinol b indole hEC nM
2021-09-08
FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in
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We also explored various nitrogen substituents with an
2021-09-08
We also explored various nitrogen substituents with an aim toward modulating sterics and basicity within the ABH series. No glycine uptake inhibition was detected with non-basic bicycles (data not shown). Isopropyl was the best compromise between desired on-target effect and clearance, however, eff
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