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Colorectal cancer CRC is the third most common cancer
2022-02-12
Colorectal cancer (CRC) is the third most common cancer in men and the second in women worldwide and almost 55% of the cases occur in more developed areas of the world. In the 2012, more than 1.3 million new cases were reported, which accounts for about 10% of the total cancers worldwide (GLOBOCAN,
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To understand the impact of alterations in brain
2022-02-12
To understand the impact of alterations in SM-164 zinc homeostasis, the role of Zn2+ as a neurotransmitter has to be appreciated. Certain regions of the brain including the neocortex and hippocampus harbour so-called “zincergic” (or “gluzinergic”) neurons, where Zn2+ is co-released with glutamate an
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Despite their undisputed importance however FPR receptors ar
2022-02-12
Despite their undisputed importance, however, FPR receptors are not in the limelight of GPCR-related research (for review [12] and references therein). We, therefore, draw attention to this GPCR receptor family, in order to re-initiate FPR-related research, particularly in the light of biased agonis
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Studies of human and mouse GPR as
2022-02-12
Studies of human and mouse GPR84, as ascertained by mRNA levels in various tissues, have determined that GPR84 is highly expressed on bone marrow cells, splenic T and B cells, and circulating granulocytes/monocytes/macrophages. In the latter cells, mRNA expression of is up-regulated only under infl
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br Acknowledgments We thank Dr
2022-02-11
Acknowledgments We thank Dr Kathleen Sullivan of Merck Research Laboratories for providing the CHO-K1 trp channel expressing an NFAT-β-lactamase reporter and the Gα subunit Gqi5, Dr. Chen Liaw (Arena Pharmaceutical), Ms. Rebecca Kaplan, Mr. Frank Xiaodong Gan for technical assistance, Dr. Andrew
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Several studies have found that GPR
2022-02-11
Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected sglt expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Rimonab
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In addition to gonadotropes GnRHRs have also been detected
2022-02-11
In addition to gonadotropes, GnRHRs have also been detected on somatotropes, lactotropes, thyrotropes, melanotropes, somatolactin (SL) cells, and/or corticotropes using immunohistochemical, radioligand-binding, or mRNA expression approaches across species; including fishes, rats, and humans (La Rosa
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Based on work from our labs with mGlu
2022-02-11
Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]
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In the present study both experimental and theoretical studi
2022-02-11
In the present study, both experimental and theoretical studies were performed to explore the inhibitory mechanisms of indomethacin and its analogues towards GLOI. A remarkable correlation (=0.974) was derived for the four structurally similar NSAIDs and two curcumins between the experimental bindin
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About epilepsy no specific seizure type has been identified
2022-02-11
About epilepsy, no specific seizure type has been identified because GLUT1-DS is associated with a wide range of epilepsies: patients develop seizures in infancy and early childhood, which are, frequently, do not respond to anticonvulsant medication. In infants, seizures are described as brief, sub
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Acute effects of FZ were not altered in
2022-02-11
Acute effects of FZ were not altered in GluR-A−/− mice, thus providing a solid basis for comparing the effects of repeated drug administration. In addition, GluR-A subunit deficiency did not affect the basal behavior of saline-treated animals, despite the GluR-A−/− mice having been described as hype
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The expression of GLUT receptors throughout the body could
2022-02-11
The expression of GLUT receptors throughout the body could be considered a potential source for off-target effects even for engineered glucose-conjugated nanomedicines, as there are at least 12 types of GLUT transporters in the body, including GLUT1 in erythrocytes and the blood-brain barrier, as we
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In patients with type diabetes glucagon receptor
2022-02-11
In patients with type 2 diabetes glucagon receptor antagonism led lowered fasting glucose however not postprandial glucose levels [9], which may reflect that glucagon may not be of particular importance for the diabetic hyperglycemia upon a meal. Current glucagon receptor antagonists have however be
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Dioscin In order to test the influence of
2022-02-11
In order to test the influence of the initial depolarization, experiments were performed, where the degree of chloride substitution was varied, either by adding n-Ringer to Dioscin incubated in a sucrose Ringer or by suspending the cells directly in Ringers identical to the final composition in the
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br The potential of EPA
2022-02-10
The potential of EPA-Ffar4 signaling as a novel intervention for HFpEF Conclusions and future directions Optimization of ω3-PUFA/EPA-therapy based upon titration to achieve therapeutic levels: A pressing clinical challenge is to continue to define the benefit of ω3-PUFA/EPA-therapy. Recent ana
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