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Recently two distinct small molecule inhibitors of PHGDH wer
2023-02-13
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 Lisinopril dihydrate with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces
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AR is an enzyme involved in
2023-02-13
AR is an enzyme involved in conversion of glucose into sorbitol using NADPH as a cofactor [46]. This AR polyol pathway generates sorbitol accumulation and NADPH depletion. NADPH participates in detoxification via glutathione (GSH) reductase pathway [47]. Therefore, reduction of NADPH attenuates remo
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Previous studies to investigate the functions of AHR in Treg
2023-02-13
Previous studies to investigate the functions of AHR in Treg EPZ5676 have employed a loss-of-function approach, using AHR complete-null mice, or a gain-of-function approach by ligand administration. However, these approaches may confound the interpretation of the results. For example, the broad exp
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Among all the compounds the novel L derivative d showed
2023-02-13
Among all the compounds, the novel L-748,337 derivative (23d) showed the potent human β3-AR antagonist activity and high lipolysis inhibitory activity in vitro. The SYN-117 23d displayed 23-fold more potent β3-AR antagonist activity (EC50 = 0.5117 nM) than that of L-748,337 (EC50 = 11.91 nM) and hi
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br Mechanisms of specific immunotherapy Several mechanisms m
2023-02-13
Mechanisms of specific immunotherapy Several mechanisms may be involved in specific immunotherapy of EAMG by active immunization with the therapeutic vaccine in IFA. During the therapy, the therapeutic benefits result from diversion of autoantibody specificities away from pathogenic extracellular
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The gene SRD A encodes the reductase enzyme
2023-02-13
The gene SRD5A2 encodes the 5-α-reductase enzyme, which converts testosterone into dihydrotestosterone. Although dihydrotestosterone levels are considerably lower than testosterone, dihydrotestosterone has a five-fold stronger binding capacity to the androgen receptor and, thereby, a considerably mo
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In this study in an effort to explore the possible
2023-02-13
In this study, in an effort to explore the possible role of 5-HT6 receptors in mediating the memory-enhancing effects of YL-0919, we first assessed the memory-enhancing effects of YL-0919 in the Morris water maze, object recognition test and step-down passive avoidance task. In addition, we then inv
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Young disease transitioning B Sle mice
2023-02-10
Young disease-transitioning B6·Sle1 mice show partial loss of leukocyte Axl versus B6 controls (data not shown). Further, BMDM from diseased B6·Sle1.Yaa mice do not express detectable levels of ADAM10 and TACE (ADAM17) but do express basal levels of Axl similar to wild type B6-derived BMDM (Suppleme
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lcq Pompe disease is accompanied by the deficiency of the
2023-02-10
Pompe disease is accompanied by the deficiency of the lysosomal α-1,4-glucosidase that makes the lcq unable to hydrolyze glycogen to glucose, thereby resulting in the accumulation of glycogen in lysosomes, especially in skeletal muscles and cardiac tissues. This accumulation results in the structura
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Jesus et al discovered a new
2023-02-10
Jesus et al. discovered a new series of azaindole as Aurora inhibitors through various modification of GSK1070916 (47). They synthesized series from modification of the GSK1070916 and evaluated for in-vitro Aurora-B/INCENP and Aurora-A/TPX2 inhibition assays. Modified Cefpodoxime Proxetil synthesis
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br Discussion Herein we demonstrate
2023-02-10
Discussion Herein, we demonstrate that mice deficient in L-12/15 LO are more sensitive to 3-NP-induced toxicity although a substantial individual variability in striatal lesion size in response to 3-NP in both genotypes was observed. This variability is not atypical; several studies demonstrate s
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CGRP (rat) The known crystal structures of class C GPCR
2023-02-10
The known crystal structures of class C GPCR VFTs do not include attached TM domains, therefore current conformational data may not accurately reflect the dynamics of extracellular domains in full-length receptors. Nevertheless, compelling mechanisms of signal transduction can still be postulated. S
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In our study caspase and DRAM were
2023-02-10
In our study, caspase3 and DRAM were identified as being involved in full-length AIFM1-induced apoptosis. Caspase3 is best known for its role in the execution phase of apoptosis in both intrinsic and extrinsic apoptotic pathways [17]. The members of the caspase family are generally in inactive pro-f
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Tedizolid australia Despite their different effects on cell
2023-02-10
Despite their different effects on cell survival, the functions of autophagy and apoptosis are not completely independent. Additionally, Cho et al. (2009) suggested that the mediation of caspase-3 links the apoptotic and autophagic signaling pathways. Consequently, to illuminate the correlation, exc
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AT signaling is distinct to
2023-02-10
AT2 signaling is distinct to that of AT1 (Kaschina and Unger, 2003). As shown here, opposite to the stimulating effect of AT1 signaling, it inhibits apelin secretion. Activation of AT2 receptor, which is also G-protein coupled, is known to decrease cAMP and cGMP levels by inhibiting adenylyl cyclase
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