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In the nineties we knew that
2023-10-30
In the nineties we knew that (-)baclofen was the stereo-selective ligand for the GABAB receptor which had been recognised by Norman Bowery as a receptor for GABA, which was different from the GABAA receptor (Hill and Bowery, 1981). GABAB receptor antagonists were also synthesised and made available
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Enhanced arginase activity and the resultant
2023-10-30
Enhanced arginase activity and the resultant decreases in L-arginine levels can also impair T cell mediated immune function and allow tumor growth by limiting the supply of L-arginine needed for the formation of cytotoxic levels of NO by iNOS [10]. Increased arginase expression/activity may also lim
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In our study we provide evidence for the
2023-10-27
In our study we provide evidence for the existence of an endosome-lysosomal pathway for the proteolytic degradation of AR triggered by its interaction with the ESCRT-I component TSG101. The following findings of this study support this notion: (1) We showed that TS101 interacts with endogenous or ec
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br Depletion of serum amino acids Currently the only antican
2023-10-27
Depletion of serum amino acids Currently, the only anticancer agents that directly target amino PDK1 inhibitor mg metabolism are bacterial l-asparaginases (from Escherichia coli and Erwinia chrysanthemi), which are FDA-approved for treatment of pediatric and adult ALL. A potential complication o
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Recently two distinct small molecule inhibitors of PHGDH wer
2023-10-27
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 serine threonine protein kinase with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5
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Interestingly our transgenic mouse model with
2023-10-27
Interestingly, our transgenic mouse model with macrophages expressing AdipoR1 showed not only improved insulin sensitivity and inflammation in skeletal muscle and adipose tissues, but fat mass, macrophage and plasma lipid accumulation and foam cell formation was also favorably reduced resulting from
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Introduction Mammalian cells express the seven STAT family m
2023-10-27
Introduction Mammalian Cy5 TSA express the seven STAT family members STAT1, −2, −3, −4, −5A, −5B, and −6 [1], [2]. All STATs exert physiologically important roles as homo- and heterodimers [2], [3], [4]. Cytokines and growth factors activate STATs through the activation of kinases that phosphoryla
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Both subcutaneous s c and mucosal
2023-10-27
Both subcutaneous (s.c.) and mucosal administration of short synthetic peptide derivatives of AChR prevent the onset of EAMG, but do not treat ongoing EAMG [80], [81], [82], [83], [84], [85]. The selection of peptides for treatment is mainly based on the identification of immunodominant T- and B-cel
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Although CP has been an important
2023-10-27
Although CP has been an important research subject in the field of antigen processing and presentation, the mechanisms of presentation of intracellular Kaempferol receptor by MHC II received considerably less attention. Interestingly, pioneering work by the Münz laboratory has pointed to an involvem
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We have recently reported a regulatory effect of
2023-10-27
We have recently reported a regulatory effect of quercetin on the AChE activity in the brainstem during the demyelination and remyelination process [17]. It has also been observed that there is a protective effect on lipid peroxidation and worsening of motor functions caused by loss of myelin in the
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In bacteria H gler et
2023-10-27
In bacteria (Hügler et al., 2007, Kanao et al., 2001), a glaucophyte alga (Ma et al., 2001), green algae/land plants (Fatland et al., 2002), and filamentous fungi (Nowrousian et al., 2000), ACL enzyme activity requires ACLA, and ACLB (referred to here as dual-subunit ACL, or dsACL) (Kanao et al., 20
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br ACL Regulation and Role in Lipid Metabolism ACL is
2023-10-27
ACL Regulation and Role in Lipid Metabolism ACL is a ubiquitous enzyme at the nexus of nutrient catabolism and synthesis of cholesterol and fatty acids. In mammals, it is highly expressed in lipogenic tissues including adipose, liver, and lactating mammary glands [9]. In the presence of ATP and C
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A high throughput screening campaign
2023-10-27
A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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The compounds containing beryllium act as
2023-10-27
The compounds containing beryllium act as strong Lewis acids because of electron deficiency of the Be Trehalose mg []. Interactions of X-Be-Y compounds with different Lewis bases have been studied by Yanez and co-workers [], extensively. Recently, they proposed a class of extremely strong bidentate
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Experimentally the ECD spectrum of showed
2023-10-26
Experimentally, the ECD spectrum of 1 showed three ECD bands: positive ones at 260 and 200nm, and a negative one at 230nm (Fig. 4). Meanwhile, there is only one broad positive ECD band starting from 300nm in the ECD spectrum of 2. ECD spectra of 1 and its derivatives attracted great interest because
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