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ML 277 Another strategy adopted to enhance the action of end
2021-10-07

Another strategy adopted to enhance the action of endocannabinoids is indirectly through blocking their metabolism. Indeed, amplifying the action of anandamide and 2-AG by inhibiting their enzymatic degradation has emerged to develop the endocannabinoid system for medicinal purposes. It is interesti
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We conclude that a combination
2021-10-07

We conclude that a combination of GD2-specific CAR T cell therapy with pharmacological EZH2 inhibition deserves investigation as a new therapeutic strategy in EwS and potentially other cancers with heterogeneous GD2 expression, including osteosarcoma, various soft tissue sarcomas, melanoma, lung can
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Compounds that induce exocytosis in cultured cells include
2021-10-07

Compounds that induce exocytosis in cultured chronic health condition include Ca2+-dependent [14] or Ca2+-independent [15] mechanisms. Ca2+-dependent exocytosis releases soluble enzyme content from lysosomes [16] operating by increasing the cytosolic concentration of Ca2+[13] by recruiting extracel
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In addition The present study was designed to
2021-10-07

The present study was designed to clarify the distribution and the function of the endothelin receptors in the guinea-pig urinary bladder. We found that endothelin-1 produced a clear tonic contraction via both In addition subtypes, the endothelin ETA and ETB receptor, and that sarafotoxin S6c also
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br Introduction The period around birth is a risky time
2021-10-07

Introduction The period around birth is a risky time for stroke in infants. Ischemic stroke has been diagnosed in about 1/4000 full-term infants (Nelson and Lynch, 2004) and perinatal stroke represents the second most frequent cause of acute seizures in this age group (Levy et al., 1985). Further
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Following the discovery of diketo compounds S and L
2021-10-07

Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent voltage gated sodium channel based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of H
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br Conclusion br Disclosure of
2021-10-07

Conclusion Disclosure of interest Introduction The Joint United Nations Program on HIV and AIDS (UNAIDS) proposed the ambitious global goal of achieving the "90-90-90" target by 2020 and ending the HIV epidemic by 2030 (Barton-Knott, 2014). One important measure is to monitor the incidence
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br The HDC knockout mouse as a pathophysiological model
2021-10-07

The HDC knockout mouse as a pathophysiological model of TS The implication of a hypomorphic allele of the Hdc gene as a rare cause of TS (Ercan-Sencicek et al., 2010) created a rare opportunity for the generation of a pathophysiologically grounded model of the disorder. Modeling pathophysiology o
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The therapeutic potential of acetate
2021-10-07

The therapeutic potential of acetate has been advocated by research on neurodegenerative disorders such as Canavan's disease (Arun et al., 2010, Mathew et al., 2005), where oral acetate improved motor function in a genetic model of the disorder, and in studies of behavioural phenotypes associated wi
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FSH and LH are glycoprotein dimers that are comprised
2021-10-07

FSH and LH, are glycoprotein dimers that are comprised of two subunits, a common α-subunit (αGSU) and a distinct β-subunit (FSHβ or LHβ, respectively), which determines the biological specificity of the gonadotropins (Ciccone and Kaiser, 2009, Gharib et al., 1990). The WY-14643 mg of the gonadotropi
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The synthesis of is shown in The Boc
2021-10-07

The synthesis of is shown in . The ---Boc--diaminopropanoic acid--butyl ester () fragment was synthesized in four steps from Boc--asparagine (). The key step in this synthesis was a Hofmann rearrangement of the terminal carboxamide, which was performed according to the elegant protocol of Zhang tha
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In summary we have developed an efficient
2021-10-07

In summary, we have developed an efficient synthetic route to the required urea-isostere containing hydroxamic acid-based inhibitor . The target molecule, , was found to retain the inhibitory potency of the corresponding carbo-analog against glyoxalase-I while possessing resistance to cleavage by γ
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RHPS4 In the light of the above
2021-10-04

In the light of the above-mentioned considerations, it is interesting to note that the FPR-related research with regards to bias agonism did not prosper during considerably during the last decade (possible exceptions are [[8], [9], [10], [11]]. However, with new insights in receptor chemistry and fu
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Two recently developed highly specific
2021-10-03

Two recently developed, highly specific EZH2 enzymatic inhibitors, GSK126 and EPZ-6438, are currently in clinical trials for treating lymphomas (Kim and Roberts, 2016). Although these EZH2 inhibitors have shown antitumor effects in lymphoma cells with enzyme-activating mutations of EZH2 (Knutson et
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H O induced astrocyte ATP release through
2021-10-03

H2O2 induced astrocyte ATP release through lysosome exocytosis. The LDH assay and electric microscope results indicated that the increase of extracellular ATP concentration was not due to the cell rupture, but the alternations in cell activities. In addition, when lysosome exocytosis was blocked by
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