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Dihydrofolate reductase DHFR is an excellent molecular targe
2021-03-17
Dihydrofolate reductase (DHFR) is an excellent molecular target for this study because it has been and is currently studied by using different molecular modeling techniques [6], [7], [8], [9]. Kerrigan et al. have reported an interesting review about recent progress in molecular dynamics simulations
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Our finding that activating DDR variants
2021-03-17
Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho
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CYP A is involved in the
2021-03-17
CYP3A is involved in the enzymatic (Z)-4-Hydroxytamoxifen of many therapeutic agents [29]. The activity of BFCOD has been used to monitor CYP3A activity in humans [30], pigs [31], mice [32], and fish [23]. The predominant isoform expressed in the human liver is CYP3A4 [33]. In pigs, CYP3A29 contrib
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br Author contributions br Conflicts of interest br
2021-03-17
Author contributions Conflicts of interest Introduction Current the 5-year survival rates for lung and pancreatic cancers are 18% and 8%, respectively. These low survival rates are partially because of the late diagnosis of one-half of cases, in which 5-year survival decrease to 4% and 3%,
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In rats exposed to day of nicotine withdrawal
2021-03-17
In rats exposed to 1 day of nicotine withdrawal (24 h after the last nicotine administration) we expected a decrease of general locomotor activity and a decrease of global striatal dopamine release, which were assessed in a previous study following 14 days of nicotine exposure and 24 h of nicotine w
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Numerous small molecule CRF receptor antagonists
2021-03-17
Numerous small molecule CRF receptor antagonists have been reported in the literature. Some representative examples are shown in . In preclinical studies (DMP696), , was found to be efficacious in preclinical behavioral models for anxiety and depression. In an open label clinical trial with (R121
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Estrogen receptor related receptor ERR like other members of
2021-03-16
Estrogen receptor-related receptor γ (ERRγ), like other members of the ERR subfamily, is a constitutively active orphan nuclear receptor, though unlike ERRα and β, it is more selectively expressed in metabolically active and highly vascularized tissues such as heart, kidney, brain, and skeletal musc
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In SLO permeabilized human sperm the AR elicited by calcium
2021-03-16
In SLO-permeabilized human sperm, the AR elicited by calcium, persistently active Arf6 [41] and Rab3A, 8-pCPT-2′-O-Me-cAMP [8], diacylglycerol and a non-hydrolyzable analog [35], is sensitive to the PLC blocker U73122. Furthermore, 8-pCPT-2′-O-Me-cAMP elicits a calcium signal in non-permeabilized sp
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br Materials and Methods br Results br Discussion The spatia
2021-03-16
Materials and Methods Results Discussion The spatial properties of receptor-ligand interactions can influence receptor activation and signal propagation, but studying this phenomenon requires the development of systems capable of recapitulating complex biophysical traits. In this study, we
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Based upon these findings on portions A and B
2021-03-16
Based upon these findings on portions A and B, novel scaffolds of EP4 antagonist, and (R & R=()-Me; =Cl; R=H), shown in , were identified. We next focused on optimizing portion C of these scaffolds. We utilized for an alternative synthesis of nicotinamide scaffold , which is quite effective for der
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br Results and discussion The
2021-03-16
Results and discussion The effects of hypoxia, a combination of shear stress and hyperoxia, and a combination of shear stress and hypoxia in BAECs were assessed at 0, 15, 30, 60, 120, and 180 min. Changes in phosphorylation levels of eNOS at Ser635 were investigated using immunoblotting, and repr
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br Transparency document br Introduction Cigarette smoke
2021-03-16
Transparency document Introduction Cigarette smoke is modifiable factors to alter the neurovascular functions. Now a day, cigarette smoking in public place is offense due to toxic exposure cause the neurological and respiratory system damage to non-smoker population [1]. A literature survey ex
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The cytoplasmic domain of classical cadherins is highly
2021-03-16
The cytoplasmic domain of classical cadherins is highly conserved and can interact with different cytosolic proteins. Typically this domain is associated with catenin family members, including p120 catenin, β-catenin, and α-catenin, which form a cadherin-catenin complex (Fig. 1). The catenin family
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In this report we describe studies of the effects of
2021-03-16
In this report we describe studies of the effects of peroxisome proliferator-activated receptor γ (PPARγ) and acyl-CoA synthetase (ACSL1) on palmitate-induced ER stress in the human cardiomyocyte-like cell line AC16 [22], which was derived from adult ventricular heart tissue. PPARγ is a nuclear rece
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In conclusion we have shown that the cellular effects
2021-03-16
In conclusion, we have shown that the cellular effects produced by SFN in NSCLC Cladribine are largely mediated by SFN-induced production of ROS. Cells with higher levels of EGFR were more resistant to SFN treatment and showed resistance to SFN-induced apoptosis, suggesting that high EGFR levels pr
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