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Recently two distinct small molecule inhibitors of PHGDH wer
2025-01-03
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 desogestrel mg with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces the
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DCG IV We next considered the effect of alkyl chain length o
2025-01-03
We next considered the effect of alkyl chain length on the inhibitory activity. As can be seen from , it is obvious that there is no proportional relationship between the methylene chain length and activity. The activity decreased when the chain length increased from 1 to 3 and increased with elonga
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A clear link between ADR stimulation and
2025-01-03
A clear link between α2-ADR stimulation and decreased respiration in β-cells is established and consistent with proteomics data. Current discoveries in islets have identified physical interactions between ADR-coupled G proteins and cellular components such as insulin vesicles and ion channels (Zhao
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NLX a k a F or befiradol exhibits nanomolar
2025-01-03
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in Type 2 diabetes compound to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Addit
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The AR signalling pathways play important roles in several p
2025-01-03
The AR signalling pathways play important roles in several physiopathological processes associated with ischaemia, inflammation, and tumourigenesis [35]. Moreover, A3AR is overexpressed in different tumour A 350619 hydrochloride and seems implicated in pro- or anti-apoptotic effects [36]. In partic
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A borderline significant effect of women s age has
2025-01-03
A borderline significant effect of women's age has been observed for ADA6 only. For ADA2 the proportion of the *1/*1 genotype is 69.4% in women aged ≤36 years vs. 66.9% in women aged ≥36 years (p=0.944). The proportion of ADA6*1 allele carriers is 32.6% in women aged ≤36 years vs. 49. 8 in women age
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Apoptosis or programmed cell death
2025-01-03
Apoptosis or programmed cell death is a function of biochemical mechanisms, which are energy-dependent. It is considered to be a vital component of many processes such as normal cell cycle, immune mechanism, atrophy, embryonic development and toxin-induced cell death (Elmore, 2007). In addition, apo
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LO is a soluble kDa enzyme composed of an helix
2025-01-03
5-LO is a soluble 78 kDa enzyme, composed of an α-helix-rich catalytic domain and a regulatory β-sheet-rich C2-like domain. Depending on the cell type, 5-LO may be located in the cytosol, in the nucleoplasm, or in both compartments (Werz, 2002). Upon cell stimulation by agents that elevate intracell
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The acidification of endocytic compartments is closely relat
2025-01-02
The acidification of endocytic compartments is closely related to endocytic activity, although the mechanism linking acidification and membrane dynamics is largely unknown. In a recent RNA interference (RNAi)-based screen, V-ATPase depletion blocked the formation of clathrin-coated vesicles, an effe
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br ASK in Huntington s disease and other polyglutamine disea
2025-01-02
ASK1 in Huntington's disease and other polyglutamine diseases The polyglutamine (polyQ) diseases are a group of inherited neurodegenerative disorders caused by the expansion of cytosine-adenine-guanine (CAG) trinucleotide repeats in the coding regions of specific genes, leading to the production
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br Metabolic effects of apelin in obesity and type
2025-01-02
Metabolic effects of apelin in obesity and type 2 diabetes Mice fed a high fat diet (HFD) for several weeks become obese, hyperglycemic, hyperinsulinemic and insulin resistant. Acute apelin treatment by intravenous injection or by infusion during a hyperinsulinemic–euglycemic clamp in obese and i
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Introduction Enzymatic browning degrades quality safety and
2025-01-02
Introduction Enzymatic browning degrades quality, safety, and nutritional values of various fruits or vegetable products. For example, the color of apple or potato is generally yellowish, representing freshness. However, they are extremely susceptible to enzymatic browning because of abundant poly
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To the best of our knowledge only cases of
2025-01-02
To the best of our knowledge, only 3 cases of an E196K mutation have been described since it was first identified in 2000 [15], [16], [17], although 5 cases, accounting for 1.1% of all genetic TSE cases, were reported with no precise data on the clinical phenotypes in the EUROCJD collaborative surve
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br Conflict of interest statement br Introduction Tanshinone
2025-01-02
Conflict of interest statement Introduction Tanshinone IIA (Tan IIA) is a major active component of Salvia miltiorrhiza (S. miltiorrhiza), a well-known Chinese traditional medicine that is used for the treatment of cardiovascular and cerebrovascular diseases [1]. Tan IIA exhibits diverse pharm
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Introduction AMP activated protein kinase AMPK is
2025-01-02
Introduction AMP-activated protein kinase (AMPK) is mainly known as a highly conserved and ubiquitously expressed energy sensor that is highly sensitive to changes in cellular energy levels (by sensing increases in AMP:ATP and ADP:ATP ratios) and makes appropriate adjustment to balance the consumpt
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