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br Materials and methods br Results Estimations of OMP gener
2021-10-07
Materials and methods Results Estimations of OMP generated by the proposed mechanism (Fig. 1) were first performed for the range of 0.001–2 mM of alkaline phosphatase inhibitor concentration in the cytosol. It was assumed that only 5% of all VDACs in MOM form the ANT-VDAC1-HKI contact sites,
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Organisms can adapt to increasing ROS production
2021-10-07
Organisms can adapt to increasing ROS production by up-regulating antioxidant defences, such as the activities of antioxidant enzymes (Livingstone, 2003). Failure of antioxidant defences to detoxify excess ROS production can lead to significant oxidative damage including enzyme inactivation, protein
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Both GPR A and GPR are located
2021-10-07
Both GPR109A and GPR81 are located on chromosome 12q24 [3] and mediate anti-lipolytic effects through coupling to Gi-type G proteins [17]. It is important to note that with the recent deorphanization of these receptors, there has been a recommendation to the International Union of Basic and Clinical
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br Acknowledgments This work was supported by
2021-10-06
Acknowledgments This work was supported by the NIH (R01DK103884 to JMZ, R01DK100659 to JKE, and F32DK104659 and K01DK111644 to CMC), the Diana and Richard C. Strauss Professorship in Biomedical Research, the Mr. and Mrs. Bruce G. Brookshire Professorship in Medicine, the Kent and Jodi Foster Dist
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br Neural circuits that control hunger
2021-10-06
Neural circuits that control hunger Ghrelin & cognitive control of feeding Ghrelin is a 28 amino GNE-317 orexigenic peptide that stimulates food intake in rodents and patients (Andrews, 2011, Cummings, 2006, Horvath et al., 2001, Müller et al., 2015, Nakazato et al., 2001, Tschöp et al., 2000
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However the clinical development of was terminated in due
2021-10-04
However, the clinical development of was terminated in 2013 due to the concerns over liver toxicity, raising important questions regarding the long-term safety and viability of targeting GPR40 and, more specifically, about our understanding of the pharmacobiology and signaling spectrum of this recep
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Preliminary explorations focused on the linker
2021-10-04
Preliminary explorations focused on the linker of 2 (Table 1). Lilly reported that the methylene between the phenyl and the piperidyl group was metabolically susceptible to N-dealkylation, so we replaced the methylene with a carbonyl moiety to block the metabolic site [23,48] (Fig. 2). In addition,
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TH287 The membrane metalloendopeptidase MME gene is located
2021-10-03
The membrane metalloendopeptidase (MME) gene is located at human chromosome 3q21-27. It encodes a 100-kD type II transmembrane glycoprotein, a widely expressed membrane metalloendopeptidase that degrades a number of substrates. The active site of the enzyme faces the extracellular space. MME is wide
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As for all DOACs measurement of DiXaIs activity
2021-10-03
As for all DOACs, measurement of DiXaIs activity requires the use of dedicated specific calibrators and controls. Each drug needs its own calibration and control material in a like to like manner. In no case can a drug concentration be extrapolated with the use of a calibrator established for anothe
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Compounds that induce exocytosis in cultured cells include C
2021-10-03
Compounds that induce exocytosis in cultured nor-Binaltorphimine dihydrochloride 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 recruiti
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Thus our data demonstrate that polymorphisms of GSTP differe
2021-10-02
Thus, our data demonstrate that polymorphisms of GSTP1-1 differentially mediate activation of Prdx6 peroxidase activity, providing a platform to imply that contingent upon their GSTP genotype, individuals will have significant differences in mounting an antioxidant response, particularly affecting p
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br Positive regulation of gene
2021-10-02
Positive regulation of gene chronic conditions by Nrf2 Repression of Nrf2 by Keap1 Because many xenobiotic inducers of NQO1 and GST enzyme activities contain a thiol-reactive electrophilic moiety (i.e. are soft electrophiles), Paul Talalay and colleagues predicted in 1988 that they would be r
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br Acknowledgments We thank Dr Kathleen Sullivan of Merck
2021-10-02
Acknowledgments We thank Dr Kathleen Sullivan of Merck Research Laboratories for providing the CHO-K1 lasofoxifene expressing an NFAT-β-lactamase reporter and the Gα subunit Gqi5, Dr. Chen Liaw (Arena Pharmaceutical), Ms. Rebecca Kaplan, Mr. Frank Xiaodong Gan for technical assistance, Dr. Andre
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LPCs have been previously described as
2021-10-02
LPCs have been previously described as potential anti-diabetic factors due to stimulation of secretory activity from the isolated rodent pancreas, L-type cells, ands insulin-producing cell lines, with LPC 18:1 as the main structure of interest (Soga et al., 2005, Sakamoto et al., 2006, Overton et al
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Hepcidin expression was not affected under
2021-10-02
Hepcidin expression was not affected under GlyT1 inhibition. Hepcidin downregulation is well documented in conditions of ineffective erythropoiesis and dyserythropoietic anemias, including sideroblastic anemia 33, 34. Systemic iron acquisition under these types of anemia is obviously independent fro
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