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Cholera Toxin Cytochrome P CYP enzymes plays an
2021-08-12
Cytochrome P450 (CYP-450) enzymes plays an essential role in pharmacology of drugs and toxicology of xenobiotics. Inhibition of these enzymes may lead to increase plasma levels of a concomitantly administered drug (Lee et al., 2013). It may prolong or reduce the pharmacological effects and increase
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Compounds were screened for their activity against the
2021-08-11
Compounds were screened for their activity against the hERG channel, with the 2,3-Cl compounds more active here than the 2,4-F compounds. The homopiperazine examples (, , , ) showed increased hERG activity relative to the corresponding piperazines. The cell data for the 6,7-dimethoxyquinoline compo
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Kumar et al studied Umbelliferone
2021-08-11
Kumar et al. studied Umbelliferone β-D-galactopyranoside (UFG) (benzopyrone), found in many plants exhibiting numerous pharmacological actions. The results of the study showed that UFG in a dose of 10, 20 or 40mgkg-1 per day, helps to prevent paw edema and arthritic score development for arthritis i
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Second when considering the Poisson point process the high d
2021-08-11
Second, when considering the Poisson point process, the high-density or large-radius limit of the percolation probability tends to 1 exponentially fast and is governed by the isolation probability. In the random environment, the picture is more subtle since the regime of a large radius is no longer
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br Agonist binding ETA activation
2021-08-11
Agonist binding ETA activation is promoted by binding of the endogenous peptidergic agonists to their orthosteric binding site on the receptor. ET1 and ET2 (Trp6-Leu7-ET1) bind with equal high affinity to ETA, whereas the third endogenous isopeptide ET3 (Thr2-Phe4-Thr5-Tyr6-Lys7-Tyr14-ET1) binds
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br Funding This work was supported by the National Natural
2021-08-11
Funding This work was supported by the National Natural Science Foundation of China (grant number 81671411); Beijing Natural Science Foundation (grant number 7162062); Beijing Nova Program Interdisciplinary Cooperation Projects (grant number Z161100004916045); Beijing Municipality Health Technolo
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br Materials and methods br Results
2021-08-11
Materials and methods Results and discussion Conclusions The current research work deals with preparation of CES from RHA and comparative study of Ni (II) ion adsorption on CES and RHA. It was observed that carbon embedded silica shows more porous structure and more surface area as compared
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Other studies have investigated the role
2021-08-11
Other studies have investigated the role of HDAC inhibitors in particular signaling pathways mediated by EWS–FLI1 (Matsumoto et al., 2001). A recent investigation, showed a physical association of EWS–FLI1 and HDAC1 that helps mediate a disruption in the p53 activation of downstream targets (Li et a
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The majority of serpins inhibit
2021-08-11
The majority of serpins inhibit serine proteases, but serpins that inhibit caspases or papain-like cysteine proteases have also been identified [4], [5]. Inhibitory serpins are ‘suicide’ or ‘single use’ inhibitors that use a unique conformational change to inhibit proteases. This conformational tran
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br Effects of culture conditions on drug
2021-08-11
Effects of culture conditions on drug-induced gene Tazobactam sodium salt in primary human hepatocytes Past progress in elucidating the optimal conditions for the long-term cultivation of rodent hepatocytes has helped define some of the key components in the matrix and medium environment that ar
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Introduction CYP is a superfamily
2021-08-11
Introduction CYP450 is a superfamily of heme-containing monooxygenases, many of which are expressed in the liver, and they are significant phase-I Carmofur in drug metabolism and detoxification. There are three subfamilies (CYP1, CYP2 and CYP3) that are mainly involved in the metabolism of drugs i
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Adenosine Kinase Inhibitor hydrate Ubiquitination can occur
2021-08-11
Ubiquitination can occur on a single (monoubiquitination) or several (multiubiquitination) lysine residues, or the same lysine residue can be subjected to several rounds of Ub conjugation (polyubiquitination). Ub bonds within polyUb chains are formed through 1 of 7 lysine residues in Ub, and the typ
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Structural changes within the heteromer induced by agonist a
2021-08-11
Structural changes within the heteromer induced by agonist administration show a high level of complication. The presented results obtained in quantitative FLIM-FRET measurements with two selective ligands match the qualitative conclusions indicated by changes in the intracellular calcium level. The
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An even more striking difference is observed when comparing
2021-08-11
An even more striking difference is observed when comparing active site residues, which are evolutionarily very well conserved in other soluble PPases 18, 19. In 31 known PPase sequences, 13 functionally important active site residues are conserved in all sequences, but only two of them (D70 and D97
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Substitutions on the benzene ring of the
2021-08-10
Substitutions on the benzene ring of the phenyl acetic BEC sale moiety were evaluated to study their effect on DP and CRTH2 selectivity (). Compound has strong affinity for CRTH2, but it only has moderate affinity for DP. Small substitutions such as methoxy () and fluorine () next to the aryloxy gro
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