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N terminally extended antigenic peptide precursors
2024-01-30

N-terminally extended antigenic peptide precursors that survive cytosolic degradation and enter the ER, need to be further processed by ERAP1 and/or ERAP2, in order to acquire the right length required for MHCI binding. ERAP1 (ERAAP in mouse) is an IFN-γ-inducible, metalloaminopeptidase that trims N
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Recently two distinct small molecule inhibitors
2024-01-30

Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer AH 7614 with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces the growth a
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Compounds and with potent ALR inhibitory activity
2024-01-30

Compounds , and with potent ALR2 inhibitory activity were also tested for their inhibition ability against ALR1, as shown in . They all showed low activity with inhibition percentages no more than 45% at the concentration of 10μM, demonstrating good selectivity for ALR2. To evaluate the antioxidant
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AHR mediated MMP upregulation has
2024-01-29

AHR-mediated MMP1 upregulation has been shown in response to tobacco smoke [32]. Tobacco smoke contains various AHR ligands such as benzo[a]pyrene. Both benzo[a]pyrene [15] and FICZ [13] are high-affinity ligands for AHR and upregulate CYP1A1 and CYP1B1. FICZ is rapidly degraded by CYP1A1 [20], [33]
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Perhaps the discovery of this linkage has
2024-01-29

Perhaps the discovery of this linkage has served to catapult much of the work on ABCA1, leaving its family member in need of a relationship with a defined human pathology. In this regard, there is by now a quite mature literature that suggests that ABCA2 may have been overlooked in terms of its impo
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In brief serotonin can interact with classes
2024-01-29

In brief, serotonin can interact with 7 classes of receptors are differentiated into 14 subtypes (Barnes and Sharp, 1999). Specifically, 5-HT1A and 5-HT2C receptors have been the most widely studied in the modulation of anxiety responses (Deakin et al., 1992; Millan, 2003). However, the studies that
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The most widely recognized effects of adenosine are operated
2024-01-29

The most widely recognized effects of adenosine are operated through inhibiting A1R, one of the most abundant G protein-coupled receptors in all trans retinal mg tissue [53]. A1R are located presynaptically, postsynaptically and nonsynaptically [54]. Effect of adenosine in neuronal circuits of adul
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An alternative approach to the administration
2024-01-29

An alternative approach to the administration of ADO agonists is to amplify the actions of endogenous ADO by inhibiting the ADO-metabolizing enzyme, ADO kinase (AK). Inhibition of AK has the net effect of potentiating the local concentration and the effects of ADO in the extracellular compartment. T
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SCH772984 br Acknowledgment br Introduction Vascular
2024-01-29

Acknowledgment Introduction Vascular smooth muscle cells (VSMC) exhibit the capacity to switch between a differentiated (contractile) and a dedifferentiated (synthetic) phenotype [1]. Synthetic VSMC express a lower amount of contractile proteins such as Smooth muscle 22α (sm22α) and α-Smooth m
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Despite functional studies demonstrating the role of HT in
2024-01-29

Despite functional studies demonstrating the role of 5-HT in ureteral contractility, the source of endogenous 5-HT in the ureter is unclear. Since 5-HT-containing enterochromaffin cells, which are present in the gastrointestinal tract, could not be found in the ureter (Nocito et al., 2007, Ripoche,
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The reductase family is composed of
2024-01-29

The 5α-reductase family is composed of three known isozymes, with the types I and II being the most known. Type I isozyme, which is the dominant form, can be found in the skin, liver, kidney, brain and lung. Furthermore, it has been evidenced that type I activity is several times higher in PC than i
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Some of the earliest LOX inhibitors
2024-01-27

Some of the earliest 12-LOX inhibitors were redox inhibitors, including nordihydroguaiaretic GSK2636771 (NDGA), BW 755C, and baicalein 48, 49, 50. Redox inhibitors block the oxidation of the nonheme iron at the cataylytic site, preventing its conversion from the inactive (Fe2+) to the active (Fe3+)
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br Endoplasmic reticulum protein ERp binds
2024-01-27

Endoplasmic reticulum protein 46 (ERp46) binds to AdipoR1 in HeLa cells ERp46 is localized in the ER and is suggested to act as a chaperone. About 20% of endogenous ERp46 are found at the plasma membrane suggesting that this protein may have additional functions. ERp46 interacts with AZ505 ditrif
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Changes in actin microfilaments are mediated
2024-01-27

Changes in amiodarone hcl microfilaments are mediated by changes in extracellular matrix, mechanical stimulation or growth factors intracellular signaling. We observed significant changes in a number of intracellular signaling pathways associated with changes in actin dynamics during hMSCs differen
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Concerning asthma in a study evaluating the
2024-01-27

Concerning asthma, in a study evaluating the effect of tiotropium in severe asthma, the sputum eosinophil count and exhaled nitric oxide were also assessed. However, evaluation of the anti-inflammatory effect of tiotropium was difficult because these markers were low at baseline and thereafter. In a
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