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br Materials and methods br Results
2021-08-05

Materials and methods Results Discussion DUSP1 is a member of the subfamily of the Dusl specific phosphatases (DUSPs). High levels of DUSP1 observed in lung, liver and placenta, and low levels have been found in the mCAP and kidney. DUSP1 has been shown to be elevated in various diseases [
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To study systemic potential of the selected compounds
2021-08-05

To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,
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The discoidin domain receptors DDR
2021-08-05

The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases that are activated by different types of collagen (Shrivastava et al., 1997, Vogel et al., 1997). Both receptors interact with a number of fibrillar collagens, and DDR1, but not DDR2, is also activated by the network-formin
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br Materials and methods br Results br Discussion In
2021-08-05

Materials and methods Results Discussion In addition, the responses of CYP450s induced by metalaxyl are species-specific in the four cells. For example, metalaxyl lead to induction of CYP1A1, CYP1A2, and CYP2B1 in HepG2 cells, CYP1A2 and CYP2B1 in H4IIE cells, CYP1A1 and CYP2B1 in LMH cells
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br Guidance of B cell localization by EBI br EBI
2021-08-05

Guidance of B cell localization by EBI2 EBI2 expression and B cell disease Although chemoattractant receptors of the GPR family play essential roles in coordinating the migration of lymphocytes for efficient responses against pathogens, their dysregulation can result in the initiation or progr
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br Results br Discussion The ubiquitin system has in
2021-08-05

Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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Verapamil a calcium channel blocker used clinically
2021-08-05

Verapamil, a calcium channel blocker used clinically as a coronary vasodilator, was amongst the first compounds identified that could reverse MDR and potentiate the effects of MDR1 substrates such as vincristine [15], [16]. Verapamil, along with a number of other MDR1 blockers, have proved largely u
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ag1478 br Introduction A variety of means including UV irrad
2021-08-05

Introduction A variety of means, including UV irradiation, dNTP depletion, and oncogene activation at precancerous lesions, induce replication stress, which causes replication errors if left undealt with (Hills and Diffley, 2014, Zeman and Cimprich, 2014). Eukaryotic cells have developed the DNA
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Diacylglycerol kinases DGK and are lipid kinases that
2021-08-05

Diacylglycerol kinases (DGK) α and ζ are lipid kinases that limit diacylglycerol (DAG)-dependent activation pathways downstream of the TCR (Merida et al., 2015). Their upregulation in tumor infiltrating lymphocytes (TIL) has been linked to generation of hyporesponsive states that contribute to immun
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br Fragment based drug discovery FBDD is a powerful
2021-08-04

Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical Ezatiostat hydrochloride sale space with libraries which are smaller in size, producing drug leads with high ligand-bind
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Unlike CRM exportins Cse and
2021-08-04

Unlike CRM1, exportins Cse1 and Xpot lack a C-extension and instead rely primarily on changes in HEAT-repeat conformation and direct Ran-cargo contacts to ensure low cargo-binding affinity in the cytosol and cooperative assembly of the exportin/Ran/cargo complex in the nucleus (Cook et al., 2005, Co
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Therapeutic options targeting intrahepatic resistance are
2021-08-04

Therapeutic options targeting intrahepatic resistance are very limited. Theoretically, the NO-cGMP pathway may be influenced at several sites. Yet, most strategies did not reach clinical practice or yielded disappointing results, such as activators of soluble guanylate cyclase [14], NO releasing der
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Astrocytes play a key role in the
2021-08-04

Astrocytes play a key role in the brain, as these cells are involved in fluid, ion, pH, and neurotransmitter homeostasis, synapse function, energy and metabolism and blood-brain barrier (BBB) maintenance (Sofroniew and Vinters, 2010). PA is able to activate different damaging responses in astrocytes
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5-Formyl-UTP br Results and discussion Analysis of experimen
2021-08-04

Results and discussion Analysis of experimental data indicates that the radon 5-Formyl-UTP coefficient in OPC blended with RHA varies from 0.15 × 10−6 m2 s−1 for pure cement to 0.26 × 10−6 m2 s−1 for cement mixed with 50% RHA by weight. The value of diffusion coefficient first decreases in cemen
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PET CT static images of F CJ acquired at
2021-08-04

PET/CT static images of F-CJ-042794 acquired at 1h p.i. from LNCaP tumour-bearing mice with/without co-injection of non-radioactive CJ-042794 (50μg) are shown in . The LNCaP tumours were clearly visualized in PET images with a moderate tumour-to-background contrast. High radioactivity accumulation w
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