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Theoretically the majority of resistance mechanisms
2022-10-02
Theoretically, the majority of resistance mechanisms identified so far could be targeted by compounds that are already available, such as inhibitors of ER, PIK3CA/mTOR or FGFR1. However, the potential therapeutic advantage of combining these agents with standard HER2-targeting treatments must be wei
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The following are the supplementary data related to this
2022-09-30
The following are the supplementary data related to this article. Author contribution Conflict of interest Introduction Thrombosis (arterial and venous) is a major cause of vascular obstructive diseases including myocardial infarction, cerebral infarction and pulmonary embolism. Glycoprote
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A general synthesis of the tetrazole is
2022-09-30
A general synthesis of the tetrazole is shown in . First, a magnesium-halogen exchange reaction quenched with DMF afforded benzo[]thiophene-5-carbaldehyde , which was further decorated with a bromine at the 3-position (). A Suzuki reaction with -tolylboronic 9-amino Camptothecin followed by reduct
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A key limiting factor in the semi quantitative analysis of
2022-09-30
A key limiting factor in the semi-quantitative analysis of changes in the nuclear-to-cytoplasmic distribution of glucokinase is the large intercellular heterogeneity of haspin inhibitor of glucokinase in both isolated hepatocytes in vitro and also in liver in vivo[13], [23], [24], [26], [36]. This n
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Xenobiotic metabolizing enzymes are classified as
2022-09-30
Xenobiotic metabolizing enzymes are classified as being phase I, phase II and transporter enzymes, with phase I enzymes metabolizing lipophyllic xenobiotics to make them more polar so that the phase II enzymes can perform the necessary conjugation reactions that afford elimination. Although the pha
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In the liver ghrelin has opposite
2022-09-30
In the liver, ghrelin has opposite effects to insulin on the expression of the enzyme PEPCK, thereby promoting gluconeogenesis and also causing a decrease in glucose uptake and fatty BS-181 HCl oxidation (Rigault et al., 2007). Ghrelin also stimulates hepatic lipogenesis de novo in a GH-independent
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In a series of experiments the clotrimazole concentration wa
2022-09-30
In a series of experiments, the clotrimazole concentration was varied and the NSVDC channel conductances were calculated from Eq. (1) to obtain the dose-response relation (Fig. 3). The data were fitted to the Michaelis–Menten-type activation curve (Eq. (3)) and gave an EC50 value of 14 μM and a dose
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In perimenstrual catamenial epilepsy there is emerging evide
2022-09-30
In perimenstrual catamenial epilepsy, there is emerging evidence to suggest that P withdrawal plays a key role in seizure exacerbations occurring around the time of menstruation (Backstrom et al., 1984, Bonuccelli et al., 1989, Scharfman and MacLusky, 2006). The mechanisms underlying ovarian cycle-r
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On the contrary the benzhydrol
2022-09-30
On the contrary, the benzhydrol series showed modest activity with EC of two digit micromole. The bulkiness of the AL 8810 tail may be the reason for the low activity. Interestingly, introduction of H-bonding groups, such as OMe in and CF in , slightly improved the activity compared to the unsubst
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br Introduction It is well known that
2022-09-29
Introduction It is well known that conventional cancer treatment strategies, such as surgery, radiotherapy, and chemotherapy all have their own limitations, which lead to an unsatisfactory therapeutic effect. Under this situation, the combination of two or more therapeutic strategies has recently
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It is difficult however to assure that observed
2022-09-29
It is difficult, however, to assure that observed alterations of pro-oxidant/antioxidant levels within the studied organisms are related directly to heavy metal pollution, rather than to other accompanying environmental stressors. Environmental factors like oxygen partial pressure, temperature, sali
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Type diabetes mellitus T DM causes
2022-09-29
Type 2 CPI-169 (T2DM) causes vascular complications and is a major public health problem associated with lifestyle diseases such as obesity, liver steatosis, hypertension, and so on. Although serum lactate is reportedly elevated in diabetic patients [12], [13], the physiological effects remain uncl
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Acute in vivo experiments were performed
2022-09-29
Acute in vivo experiments were performed in normoglycemic 129SVE mice to confirm GPR119 activation and corresponding CB-839 control. GIP release was utilized as a biomarker for target receptor engagement and plasma GIP levels were measured 45min after oral dosing (). Both 3 and 10mg/kg produced an
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br Funding This work was supported by grants of the
2022-09-28
Funding This work was supported by grants of the National Academy of Sciences of Ukraine within the programs “Molecular and cellular biotechnologies for medicine, industry and agriculture” (#35-2018), “Scientific Space Research for 2018-2022” (#19-2018), “Smart sensory devices of a new generation
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br Experimental Procedures br Acknowledgments This work was
2022-09-28
Experimental Procedures Acknowledgments This work was supported by NIH/National Human Genome Research Institute (NHGRI) R00 HG006922 and NIH/NHGRI R01 HG008974 (to J.G.), the Huntsman Cancer Institute, and the Women’s Cancers Disease-Oriented Team at the Huntsman Cancer Institute. Research rep
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