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Replacement of the saturated propoxy group
2021-08-13

Replacement of the saturated -propoxy group in compound with the unsaturated allyloxy group to obtain compound resulted in 10-fold decrease in ET receptor antagonism and more than 20-fold decrease in ET-selectivity. Analogous unsaturated allyloxy compound in the tetrazole series was found to have di
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The highest concentrations from several tens to often hundre
2021-08-13

The highest concentrations (from several tens to often hundreds or thousands ng/L) are reported in animal farm flush water, and associated runoffs and lagoons in China and in the U.S. Lower concentrations are reported in WWTP influents and effluents. In WWTP influent waters DRO, LNG, NET and PRG hav
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It is now well accepted that
2021-08-13

It is now well accepted that increased local estrogen levels are associated with both the onset and growth of breast cancer. Tissue concentrations of estradiol (E2) in breast cancer are 10 times higher than that found in plasma [12]. Breast cancer tissues also contain increased activity and expressi
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br Experimental br Results and discussion On
2021-08-13

Experimental Results and discussion On the basis of the information obtained from the studies on RHA/TiO2 nanocomposites, it LDC000067 is expected that this reagent can be used as a catalyst for the promotion of the organic reactions. So this reagent was used in the promotion of the conversio
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DDR although normally expressed in cells
2021-08-12

DDR2, although normally expressed in Hydrocortisone with mesenchymal features, has also been reported to enhance EMT. In A549 lung cancer cells, TGFβ1 increases the expression of type I collagen and DDR2. Knocking-down COL1A1 or DDR2 with siRNA is sufficient to inhibit EMT and cell migration induced
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br Results and discussion br Conclusion Recent studies showe
2021-08-12

Results and discussion Conclusion Recent studies showed that EGFR signaling is involved in inflammatory response in several inflammatory conditions. The normal inflammatory macrophage sirtuins show EGFR-dependent production of inflammatory mediators. Nevertheless, the development of EGFR inhi
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br Results br Discussion Taking advantage of the highly
2021-08-12

Results Discussion Taking advantage of the highly specific protein–protein interactions among cognate acetylcholinesterase inhibitor that mediate SUMO conjugation to substrates, we have developed a novel strategy for achieving inhibition of SUMO conjugation in vivo based on disruption of SUMO
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Protein degradation via UPP involves
2021-08-12

Protein degradation via UPP involves two steps. One step is the conjugation of multiple ubiquitin to a substrate. The other step is the degradation of tagged protein by the downstream 26S proteasome complex. Protein ubiquitination is the E1–E2–E3 enzymatic cascade (Hershko & Ciechanover, 1998). E1-a
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kinesin 5 br Introduction As a strong analgesic morphine
2021-08-12

Introduction As a strong analgesic, morphine is often used to treat acute and chronic pain. However, morphine is a substance with low lipid solubility that slowly enters the nerve tissue through the blood–brain barrier and produces neurotoxicity. Morphine-induced neurotoxicity can be produced aft
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Given the widespread occurrence of
2021-08-12

Given the widespread occurrence of oncogene-induced RS and the increasing clinical interest in small molecule inhibitors that further exacerbate RS in human cancers (such as ATR inhibitors), our findings point to a protective role for RAD52 in the maintenance of cancer cell viability. As such, RAD52
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This project was funded by
2021-08-12

This project was funded by the Deutsche Forschungsgemeinschaft within FOR 2251 (project grants EB 285/2-1 and WI 3272/3-1) and in part by additional contributions from the Bundesministerium für Bildung und Forschung (D.I.S award Nos. BIOSCAT [05K12YE1]) and the Horizon 2020 programme of the European
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Many DNA repair pathways are candidates for
2021-08-12

Many DNA repair pathways are candidates for DPC repair. Nucleotide excision repair (NER) is widely involved in both bacteria and eukaryotes in removing cross-linked protein with low molecular weights (11kDa) (Ide et al., 2011). The predominant pathway chosen by ahr pathway may also depend on the ty
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entospletinib DGK type I http www apexbt
2021-08-12

DGKη1 (type II DGK) has a separated catalytic domain [10], [13], whereas the domains of DGKα, ε and ζ are not split [1], [2], [3], [4], [5]. Therefore, the structural difference may cause the distinct affinity for DG among these isozymes. Because other type II DGKs (η2, δ1, δ2 and κ) also have the s
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A novel series of DHODH inhibitors was developed by
2021-08-12

A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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As part of a program to
2021-08-12

As part of a program to explore the key binding interactions between the core of 1 and DGAT-1 a systematic analysis of the aminopyrimidine subunit was initiated. A potential approach to improving passive permeability within this series would be to increase lipophilicity via incorporation of substitu
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