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br Materials and methods br Results Metabolic stability
2021-07-23
Materials and methods Results Metabolic stability of compounds was studied by incubation with pooled human liver microsomes. Piperine was the metabolically most stable compound, with a t1/2 of 141min (Fig. 2, and Table 1). SCT-29 and LAU 397 showed t1/2 of approx. 45min, whereas a t1/2 of only
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br Experimental section br Results br Discussion In our
2021-07-22
Experimental section Results Discussion In our previous work (Rashidi et al., 2018) we isolated a novel glucarpidase whose raised Liproxstatin-1 HCl did not cross-react with the one in clinical use. In principle, therefore, it would be possible to delay the production of antibodies in a pa
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This review aims to examine the literature
2021-07-22
This review aims to examine the literature on chloride leukotriene receptor antagonists in the context of transplacental transport. After a short overview of the general cellular functions of Cl− channels in epithelia and the molecular classifications of these channels, it will focus on the evidenc
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Data on optimal hormone formulations routes of
2021-07-22
Data on optimal hormone formulations, routes of administration, doses and duration of hormone use in young women with POF are lacking (Box 1). Transdermal PPACK Dihydrochloride sale administration, which avoids the first-pass hepatic circulation and the increase in inflammatory markers such as C-re
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Of all ES cases approximately are metastatic diseases
2021-07-22
Of all ES cases, approximately 26–28% are metastatic diseases at diagnosis with the remainder being localized disease [14]. Instituting a systemic chemotherapy regimen in combination with surgery and/or radiotherapy has significantly increased the survival of patients with localized disease. The 5-y
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ATP binding cassette transporters such
2021-07-22
ATP-binding cassette transporters such as ABCA1 and ABCG1 are expressed on cell membranes to transport cholesterol from AAK1 dual inhibitor to HDL. These transporters help to improve RCT and reduce atherosclerosis. ABCA1 and ABCG1 gene expression are primarily induced by the stimulation of liver X
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br Materials and methods br Results br Discussion
2021-07-22
Materials and methods Results Discussion In particular, we showed that pancreatic neuroendocrine tumor GYY 4137 morpholine salt recognize cAMP as a stimulatory signal for cell proliferation. Conversely, cAMP was found to have an inhibitory effect on cell proliferation in bronchial carcinoid
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The monomeric oligomeric states of DDR V His and
2021-07-22
The monomeric/oligomeric states of DDR2-V5-His and DDR2-Fc were confirmed by Western blotting under reducing and non-reducing conditions. As shown in Fig. 1b, DDR2-V5-His exhibited a relative molecular mass of ~60 kDa under both reducing and non-reducing conditions, consistent with this protein bein
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Currently two approaches can be used individually or
2021-07-22
Currently, two approaches can be used individually or combinedly to overcome weak immunogenicity of subunit RGDfK (Bookstaver et al., 2018; Moyle, 2017; Vartak and Sucheck, 2016). The first is to design particulate antigens. Virus-like particles (VLPs), for example—mainly derived from the capsid pr
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The authors identified inhibitors of
2021-07-22
The authors identified inhibitors of SUMOylation using two assays to monitor the conjugation of SUMO1 to RanGAP1 by E1 and E2 enzymes: a fluorescence resonance energy transfer (FRET) primary screen that evaluated over 250,000 compounds and a chemiluminescence secondary screen. A counter screen was u
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br Activity based probes br
2021-07-22
Activity-based probes Characterization of coronavirus-encoded DUBs with activity-based probes To study the activity of specific DUBs, investigators frequently take advantage of the ~10kDa (monoUb or Ubl ABP) or ~20kDa (DiUb ABP) increase in MW on probe labeling. SDS-PAGE analysis or blotting f
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A second advance came with the discovery that conformational
2021-07-22
A second advance came with the discovery that conformationally-flexible benzamide analogs having an N-phenylpiperazine moiety possessed good affinity and modest selectivity for D3 versus D2 receptors [3,[14], [15], [16]]. This observation spawned a significant effort by medicinal chemists to develop
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A summary of the drug CDK hydrophobic hydrogen bonding
2021-07-21
A summary of the drug-CDK2/6/9 hydrophobic (Φ), hydrogen-bonding (H), and polar-bonding (P) interactions based upon the KLIFS residue numbers is provided in Table 5. The KLIFS system gives comparable residues from different GANT61 the same value [77], which facilitates comparisons among different p
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In the course of our program which was aimed
2021-07-21
In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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Our results also showed that the highest dose of
2021-07-21
Our results also showed that the highest dose of Astressin2-B increased the rewarding effects of cocaine, since non-defeated animals treated with this dose developed CPP with a sub-threshold dose. We monitored the acute effects of 30 µg/kg of Astressin2-B and found an increase of anxiety in the open
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