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DIDS The occurrence of MDR in cancer patients undergoing che
2021-10-15

The occurrence of MDR in cancer patients undergoing chemotherapy can be mimicked in the laboratory by culturing cancer DIDS in the presence of chemotherapeutic drugs, thereby enforcing the evolution of acquired drug resistance. This has been described in multiple model systems including the rhabdomy
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To further investigate if GPR was the functional target
2021-10-15

To further investigate if GPR40 was the functional target of these phenylpropiolic Actinomycin D analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux [15]. HEK293-GP
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Hyperhomocysteinemia HHcy is a clinical condition
2021-10-14

Hyperhomocysteinemia (HHcy) is a clinical condition characterized by increased levels of plasma homocysteine (Hcy) and a well-known risk factor for CVDs. Hcy is a sulfur-containing non-protein amino N6-Methyl-dATP mg formed during the intracellular conversion of methionine to cysteine. Previous stu
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The present experimental study identified remarkable protect
2021-10-14

The present experimental study identified remarkable protective effects for celecoxib against renal toxicity caused by CSA. All aspects of CSA nephrotoxicity, functional, inflammatory, fibrotic, and structural, were improved by celecoxib. Mechanistically, pharmacological and immunostaining protein e
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With the aim to identify potential
2021-10-14

With the aim to identify potential novel targets in CVD, we applied proteome analyses on vascular tissue of these frequently used mouse models of atherosclerotic disease in the presence and/or absence of diabetes. Potential targets for intervention identified with this approach were validated in hum
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Histone acetylation is regulated by two groups of enzymes hi
2021-10-14

Histone acetylation is regulated by two groups of enzymes, histone acetyltransferases (HATs) and deacetylases (HDACs), with antagonizing functions (Wang et al., 2009b). Among members of HATs, p300 and CBP are homologous. Both are global transcriptional co-activators (Ogryzko et al., 1996), and play
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br Hippo Signaling in Autoimmunity
2021-10-14

Hippo Signaling in Autoimmunity An imbalance of T cell subsets, such as immunosuppressive regulatory T a good thing (Treg) and inflammatory TH17, has a key role in autoimmune diseases. Recently, investigations found that TAZ but not YAP enhances TH17 differentiation but attenuates Treg different
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SB 239063 sale The physiological and pharmacological roles o
2021-10-14

The physiological and pharmacological roles of GPR81 remain largely unclear because of several reasons. The low potency of lactate agonizing GPR81 in the millimolar range, together with its fast metabolic turnover, renders as a challenge in in vivo studies using lactate. Furthermore, there are no po
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In normal tissues the expression patterns of
2021-10-14

In normal tissues, the expression patterns of GPR120 and GPR40 are not uniform. GPR120 is highly expressed in adipocytes, lung and intestinal tract, while GPR40 is shown to be expressed in pancreatic islet 8-pCPT-2-O-Me-cAMP-AM and intestinal tract [7], [20]. It is considered that the distribution
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br Conclusions In summary we have designed an ultrasensitive
2021-10-14

Conclusions In summary, we have designed an ultrasensitive electrochemical assay for hOGG1 based on a ratiometric strategy and HCR assisted amplification. The hOGG1 can specifically identify 8-oxo G site on the DNA probes modified on the electrode surface. The subsequent cleavage reaction trigger
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In the GLUT family glucose transporter GLUT
2021-10-14

In the GLUT family, glucose transporter 1(GLUT1) is primarily responsible for basal glucose uptake and maintenance of glucose basal metabolism in cells (Olson and Pessin, 1996). High GLUT1 expression occurred in various types of human cancers, like brain tumor, lung cancer and esophageal cancer (Nis
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In a follow up study the same research group
2021-10-13

In a follow up study, the same research group further characterized FFA4 involvement in DU145 and PC-3 cancer cell lines by demonstrating that the anti-proliferative and anti-migration activities of FFA4 require the presence of LPA1 receptor (LPA1R), suggesting a mechanism consistent with negative c
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GPR which is also known as FFA receptor FFAR
2021-10-13

GPR40, which is also known as FFA receptor 1 (FFAR1 or FFA1), was identified as an orphan receptor in the search for novel human galanin receptor (GALR) subtypes in 1997. Using reverse pharmacology approaches measuring calcium transients, GPR40 were deorphanized and characterized as being activated
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LIMKi 3 depicts the synthesis of series with a four step
2021-10-13

depicts the synthesis of series with a four-step sequence. First, the commercially available 4-hydroxybenzaldehyde () was condensed with 2-bromoethanol through Mitsunobu reaction to give the key intermediate (). Next, conventional nucleophilic substitution reaction with the privileged structures (
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Several other assay parameters were also explored First the
2021-10-13

Several other assay parameters were also explored. First, the thermal dependence of the assay was investigated by measuring the specific activity at different temperatures (Fig. 7). That data show that enzymatic activity increases with increasing temperature. Interestingly, the observed rate increas
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