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gli protein A variety of quinazoline or fused pyrimidine
2023-09-20
A variety of quinazoline or fused pyrimidine-substituted diaminotriazoles showed sub-100nM inhibition of Axl (). Diaminotriazoles similarly substituted with quinolines, isoquinolines and benzothiazoles also showed potent Axl activity (data not shown), but generally exhibited potent cytotoxicity and
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The allosteric site of class C receptors is
2023-09-20
The allosteric site of class C receptors is generally located on the extracellular side of the TM domain (Brauner-Osborne et al., 2007, Christopher et al., 2015, Dore et al., 2014, Gregory et al., 2011, Harpsoe et al., 2017, Kniazeff et al., 2011, Pin and Prezeau, 2007, Urwyler, 2011, Wu et al., 201
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Two critical determinants of receptor
2023-09-20
Two critical determinants of receptor trafficking are found within the GABAB1 cytoplasmic tail: the di-leucine internalization signal (EKSRLL) (Margeta-Mitrovic et al., 2000, Restituito et al., 2005) and the ER retention signal (RSRR) (Calver et al., 2001, Margeta-Mitrovic et al., 2000, Pagano et al
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TLX may promote survival and prevent apoptosis in NB cells
2023-09-20
TLX may promote survival and prevent apoptosis in NB Adarotene australia [12]. Here, we ask whether the survival-promoting effects of TLX are mediated by Apoptosis Signal-regulating Kinase-1 (ASK1, MAP3K5). ASK1 is a member of the Mitogen-Activated Protein (MAP) kinase family and it preferentially a
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Mitochondria are key organelles involved in the mechanism of
2023-09-20
Mitochondria are key organelles involved in the mechanism of apoptosis (Xiong et al., 2014), and loss of ΔΨm is an important marker associated with mitochondrial dysfunction and cell death. We found that Mino induced ΔΨm impairment and nuclear fragmentation in Jurkat blz in a concentration-dependent
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MADS box proteins are combinatorial
2023-09-20
MADS box proteins are combinatorial transcription factors in that they often derive their regulatory specificity from other DNA binding or accessory factors. In many cases, the cofactor with which MADS box proteins interact specifies which genes are regulated, when they are regulated and if these ge
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Protein arrays provide a new approach for the
2023-09-20
Protein arrays provide a new approach for the identification of substrates for several protein-modifying enzymes. For example, protein kinase substrate identification, which constitutes an important aspect of pathway mapping because of the prevalence of these substrates in biological pathways. MacBe
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Physical and chemical preservatives such as ultraviolet and
2023-09-20
Physical and chemical preservatives such as ultraviolet and ɣ-rays irradiation, sulphur and aluminium phosphide fumigation, etc, have been introduced to inhibit the growth of fungi. Nevertheless, due to the potential decomposition reactions and residues, as well as their own potential toxicity, and
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Of the infants in the study there were twin deliveries
2023-09-20
Of the 580 infants in the study, there were 106 twin deliveries and 10 triplet deliveries. There was no difference in prenatal antibiotic exposure between multiple and singleton births. Nevertheless, analysis of maternal antibiotic use was based on the 309 individual mothers who were provided Tubast
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br Conclusions br Funding This
2023-09-20
Conclusions Funding This work was supported by a Finnish government subsidy for health science research [grant numbers TYH2012141, TYH 2013218, and TYH 2014216]; the SSAC Foundation [grant numbers SLS-504141 and SLS-693781]; and the Paulo Foundation. The funding sources had no involvement in s
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ERAP has been crystallized in two different conformations wh
2023-09-19
ERAP1 has been crystallized in two different conformations, wherein the C-terminal domain IV is either closely interacting with domains I/II and enclosing the active site (termed ‘closed’), or is rotated away in a hinge motion which exposes the active site (‘open’). This large motion correlates with
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Despite extensive studies on the expression
2023-09-19
Despite extensive studies on the expression of T. pallidum-induced pro-inflammatory cytokines, very little is known about T. pallidum-mediated intracellular signaling pathway activation, that leads to cytokine expression in macrophages. A network of signaling molecules, transcription factors, epigen
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In addition to the above mentioned synaptic mechanisms the
2023-09-19
In addition to the above-mentioned synaptic mechanisms, the serotonergic system also has a critical role in the antidepressant effects of mGlu2/3 receptor antagonists. Indeed, we previously reported that mGlu2/3 receptor antagonists increased the firing rate of serotonin neurons in the dorsal raphe
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br Functional consequences of ADK regulation on
2023-09-19
Functional consequences of ADK regulation on astrocyte function As outlined above (see introduction), ADK critically regulates the extracellular adenosine levels in Apoptosis Inhibitor (Boison, 2006, Etherington et al., 2009). Changes in the levels of adenosine, as a result of the regulation of A
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In this paper we describe the formation
2023-09-19
In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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