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In the current study although EP agonist was the
2019-07-29
In the current study, although EP4 agonist was the most effective in relaxing corpus cavernosum, it did not affect the neuronally-mediated relaxation. On the other hand, both alprostadil and iloprost, which were less effective as direct relaxants, potentiated EFS-induced relaxation of rat corpus cav
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chemokine receptor antagonist Although the control group and
2019-07-29
Although the control group and tinnitus group do not significantly differ based on age, gender or hearing loss, a limitation of this study is that the control group is only group-matched, and not individually matched. Furthermore, we only tested hearing acuity in tinnitus patients via standard pure
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Due to the high attractiveness of E and E ligases
2019-07-29
Due to the high attractiveness of E2 and E3 ligases as drug targets, a number of drug discovery assays have been published, based on detection by fluorescence (Dudgeon et al., 2010, Krist et al., 2016, Zhang et al., 2004), Glycyrrhizic acid (Davydov et al., 2004, Huang et al., 2005, Kenten et al., 2
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Calcium dependence of CaM target interaction was analyzed us
2019-07-27
Calcium dependence of CaM/target interaction was analyzed using a titration matrix in which both Ca2+ and CaM concentrations were changed. This gave us access to different parameters characterizing the interaction and namely to the number of bound Ca2+ required for the interaction to occur. Our app
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Since free testosterone diffuses into a target organ
2019-07-27
Since free testosterone diffuses into a target organ [1], a remarkable increase in free testosterone in plasma is expected to enhance androgen response in target organs including the prostate. In fact, the results of the present study showed testosterone and DHT levels, and mRNA expression levels of
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SPR was used to measure
2019-07-27
SPR was used to measure biomolecular kinetic interactions between TERRA G-quadruplex and ligand in the present study. SPR is a widely used method, but cannot tell which specific type of interaction happened. Compounds with similar structures probably have similar mechanism of interaction, while comp
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In summary we have identified a series of
2019-07-27
In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als
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br Materials and methods br Results
2019-07-27
Materials and methods Results Discussion Cisplatin, as one member of a class of platinum-containing anti-cancer drugs, which displays a great deal of clinical activity on a wide variety of solid tumors. In addition, cisplatin often used in combination with other chemotherapy drugs to treat
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In sum although it is reasonable to
2019-07-27
In sum, although it is reasonable to assume that the activities of an enzyme on alternative (metabolically available) substrates may often depend on neutral drift, the point is difficult to prove because various types of selective pressures can be at play, and these will be different in different or
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Fig D shows that E lagascae VIR E gives two
2019-07-27
Fig. 2D shows that E. lagascae VIR E gives two species of radioactive TAG: one represents 45% of total labelled TAG and the smaller more-polar spot (15%) is probably derived from the endogenous 1,2-divernolin instead of the exogenous 1,2-diolein. In this case, the total scintillation counts were gre
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Experimentally measured DGAT activity was first reported by
2019-07-26
Experimentally measured DGAT activity was first reported by Weiss et al. (1960) and several different types of DGAT enzyme have since been described in plants [12,41,42]. As recently as 2011 there appeared to be just two DGAT enzymes both in plants and in other eukaryotes, namely DGAT1 and DGAT2 [43
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DDR was originally cloned by the group of Michele de
2019-07-26
DDR1 was originally cloned by the group of Michele de Luca, at the time named TrkE. The Genoa-based research team identified the skin, and the keratinocytes in particular, as a major site of DDR1-binding activity [20]. DDR1 is also expressed in kidney, liver and lung (Fig. 2). The functional role of
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br Materials and methods br Acknowledgments br Introduction
2019-07-26
Materials and methods Acknowledgments Introduction Proton pumps convert the energy of high-energy compounds into the Cystamine dihydrochloride of protons across biomembranes. They play two physiological roles: pH regulation and the formation of proton-motive forces in their membranes. The
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Moreover a ligand for fusin has recently been
2019-07-26
Moreover, a ligand for fusin has recently been found: the lymphocyte chemoattractant stromal-derived factor-1 (SDF-1) binds to CHO 5-Azacytidine transfected with fusin and promotes secondary messenger production (Bleul et al., 1996; Oberlin et al., 1996). A new name, CXCR-4, has been proposed for t
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PR-171 where From the general synthetic route we first
2019-07-26
From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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