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br Discussion In the present
2022-04-11
Discussion In the present paper it was shown for the first time that the conjugation of ethacrynic BINA receptor and glutathione catalyzed by GSTP1-1 stereospecifically forms one of the diastereoisomers of the glutathione conjugate (EASG). Chemical conjugation results in formation of a mixture o
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CVT 10216 receptor br Other Functions of HCA Receptors HCA
2022-04-11
Other Functions of HCA Receptors HCA receptors, in particular HCA1, are expressed in various primary tumor CVT 10216 receptor 77, 78, 79. This is of interest, as most solid tumors show increased glucose uptake and lactate formation even under normoxic conditions, with lactate concentrations in th
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In addition researchers studying GPR agonists favor the deve
2022-04-11
In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it cell division cycle is unclear why Sanofi-Aventis chose to terminate collaboration with M
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Abiraterone On the basis of their relative Glu transport rat
2022-04-11
On the basis of their relative Glu transport rates and anion currents, EAATs group into two functionally distinct classes, EAAT1–3 being efficient Glu transporters with small associated macroscopic anion currents and EAAT4–5 low-capacity transporters with predominant anion conductance [18]. The diff
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The effects of GHS R
2022-04-09
The effects of GHS-R1a blockade on alcohol-related outcomes have been examined in numerous preclinical experiments, utilizing various GHS-R1a antagonists (JMV 2959, [D-Lys3]-GHRP-6, BIM 28163) and rodent species (prairie vole, mouse, rat). In spite of methodological differences, the results consiste
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br Conclusion and future directions GS
2022-04-09
Conclusion and future directions GS is an important therapeutic target for the treatment of Alzheimer's disease. Its structure and function have been studied during the last years to understand the substrate cleavage mechanism to modulate the Aβ42 peptide production. The recent elucidation of GS
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Interestingly transgenic mice that constitutively express ac
2022-04-09
Interestingly, transgenic mice that constitutively express active FXR in the intestine (iVP16FXR) are protected from chemically-induced and genetically-induced cholestasis. This protective effect is attributed to the induction of intestinal FGF15 and repression of hepatic Cyp7a1 expression, downregu
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pka inhibitor Another small compound targeting IBAT has
2022-04-09
Another small compound targeting IBAT has been evaluated in Phase I clinical trial (EudraCT 2013-001175-21) [86]. The oral administration of A4250 to healthy subjects did not give rise to any serious adverse events, was well tolerated and had a similar safety profile as elobixibat; however, it cause
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In addition to the robust intracellular calcium mobilisation
2022-04-09
In addition to the robust intracellular calcium mobilisation, DHA and TUG-891 also induced MMP-9 granules release and superoxide production, supporting a key role of calcium in bovine neutrophil defense responses (Burgos et al., 2011). Pisani et al. (Pisani et al., 2009) described a reduction of bas
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Bisindolylmaleimide IV Piroxicam belongs to the oxicam famil
2022-04-09
Piroxicam belongs to the oxicam family of NSAIDs and a special attention has been drawn to this drug because of its multifunctional potential [5], [27], [28]. Chemically, piroxicam (4-hydroxy-2-methyl-N-2-pyrimidyl-2H-1,2-benzothiazine-3-carboxyamide) is an enolic Bisindolylmaleimide IV with a size
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Acquiring resistance to the FGFR inhibitor may determine
2022-04-09
Acquiring resistance to the FGFR inhibitor may determine treatment outcomes in patients with GC dependent on FGFR2 amplification, and we investigated the mechanism of AZD4547 resistance in FGFR2-amplified GC cells. We established a FGFR2-amplified GC cell line resistant to the selective FGFR inhibit
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br Acknowledgements This work was in part supported by
2022-04-09
Acknowledgements This work was in part supported by the FöFoLe program by Ludwig-Maximilians-Universität München (to T.S.), the Deutsche Forschungsgemeinschaft (DFG) CO 291/5-2, the Human Frontier Science Program (HFSP) RGP0013, the Helmholtz Validation Funds (Helmholtz Association of German Rese
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The recent identification of new mechanisms for
2022-04-09
The recent identification of new mechanisms for triggering ferroptosis, by compounds termed FIN56 and FINO2, provided new insights into regulation of ferroptosis. FINO2 acts through a distinct mechanism: it promotes lipid peroxidation by oxidizing iron and indirectly inactivating GPX4 [180]. FIN56 w
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Although ALPS type is very rare
2022-04-09
Although ALPS type 0 is very rare with few published cases, we herein report the clinical and immunogenetic characteristics of two additional unrelated patients from highly inbred North African population. Both patients present two rare splicing defects mechanisms in FAS gene inducing the skipping o
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br Results br Discussion A key step in the regulation
2022-04-09
Results Discussion A key step in the regulation of gene Sarpogrelate hydrochloride is the methylation on H3K4, which is added by the multi-component MLL/COMPASS-like histone methyltransferases. Many studies have shown the requirement of shared core subunits for optimal methylation activity of
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