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BMS 195614 The G R mutation is located
2024-12-24
The G1202R mutation is located at the solvent front of the ALK kinase domain adjacent to the inhibitor's binding pocket. Although barely reported in the setting of crizotinib resistance, it has emerged as the most refractory mutation to both the first- and second-generation ALK inhibitors. The large
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The correlation in the increase of BADH mRNA protein levels
2024-12-24
The correlation in the increase of BADH mRNA, protein levels, and enzyme activity, demonstrate that oxidation of betaine aldehyde by BADH is primordial to regulate the GB accumulation during physiological cardiac hypertrophy induced by pregnancy, this implies a major role because GB levels enhance c
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Mechanistically NAergic signaling in the VTA
2024-12-24
Mechanistically, NAergic signaling in the VTA modulates neuronal activity presumably via α1-AR. The majority of α1-ARs are found in the VTA are located presynaptically on unmyelinated Dopamine receptor agonist and axon terminals of glutamatergic and GABAergic neurons. However, α1-ARs are also found
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Given these findings above we hypothesized that hypernocicep
2024-12-24
Given these findings above, we hypothesized that hypernociception produced by intra-amygdala 8-OH-DPAT is result of hyperpolarization in this area. This neuronal inhibition of the amygdaloid complex might result in an inactivation of crucial neurotransmitter systems of the descending inhibitory pain
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The anorexic effect observed when AR is infused
2024-12-23
The anorexic effect observed when AR231630 is infused into the VTA could be the result of the DA release inhibition, as previously described [11]. However, there is also a hedonic aspect in feeding that possibly involves dopaminergic mechanisms of reward. Helm et al. showed a functional link between
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Several dehidropregnenolone derivatives functionalized at C
2024-12-23
Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic
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Another important question concerns the mechanism by which a
2024-12-23
Another important question concerns the mechanism by which a polyubiquitinated substrate is released from the Cdc48 complex and passed on to downstream components, such as the proteasome. There are at least three proposed models. In the first, a ubiquitinated substrate is transferred by ubiquitin-bi
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It has been reported that
2024-12-23
It has been reported that Daxx, an interacting partner of MCRS2/MSP58, promotes ASK1 activation following direct interaction with ASK1 [10], [11]. However, it has not been determined whether MCRS2 is involved in ASK1 signalling. In this study, we identified the direct interaction between MCRS2 and A
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It is now well established that the
2024-12-23
It is now well established that the cumulative exposure to endogenous estrogens throughout a woman's life, mainly due to her reproductive history, has an impact on the risk of hormone-dependent breast cancer (Lambertini et al., 2016). Prolonged exposure to estrogens in the case of early age at menar
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br Funding This work was supported
2024-12-23
Funding This work was supported by the National Natural Science Foundation of China (grant No. 81573664). Thanks to Jing-xian Yang from the Pharmacology Laboratory of Liaoning University of Traditional Chinese Medicine for support with technology and experimental equipment. Disclosure Conf
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br Experimental section br Acknowledgements The authors than
2024-12-23
Experimental section Acknowledgements The authors thank Prof. Yongbing Cao from School of Pharmacy, the Second Military Medical University, for providing the fluconazole-resistant strains of Candida albicans(strain 100 and strain 103). This work was supported by Program for Innovative Research
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For patients who have taken
2024-12-21
For patients who have taken advantage of the anti-TKIs and whose follow-up has been succeeded, some partial response has been noticed with 45% (9/20) for gefitinib, 39% (9/23) for erlotinib and 56.5% (13/23) for crizotinib. A disease progression has also been observed with 35% (7/20) for gefitinib,
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br Results br Discussion Utilizing a proteomic
2024-12-21
Results Discussion Utilizing a proteomic approach, we identified HSP90β as a protein that becomes associated with surface AChR in agrin-stimulated muscle cells. We demonstrate that HSP90β does not interact with the AChR directly; instead, via direct interaction with rapsyn, HSP90β becomes asso
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ARG I is one of the most important mammalian enzymes
2024-12-20
ARG I is one of the most important mammalian enzymes responsible for nitrogen metabolism since it comprises the main route for the elimination of excess nitrogen resulting from amino L-NMMA citrate and nucleotide metabolism [18]. ARG I deficiency leads to hyperargininemia, characterized by progress
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MMP-2 Inhibitor I receptor Apelin APJ triggers a variety of
2024-12-20
Apelin/APJ triggers a variety of cellular signaling pathways (Fig. 1). Recent studies from our laboratory showed that apelin-13 induces vascular smooth muscle cell (VSMC) proliferation by the upregulation of Cyclin D1 expression, which is involved in an ERK-dependent activation of Jagged-1/Notch3 si
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