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A number of chemical strategies have been developed to desig
2021-08-23
A number of chemical strategies have been developed to design activatable optical imaging probes and have been summarized in several excellent reviews 11., 12., 13., 14., 15.. Fluorogenic enzyme substrates are one of the most explored activatable probe types for enzyme detection. These probes contai
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The EGFR belongs to the
2021-08-23
The EGFR belongs to the ErbB family of receptor tyrosine kinases (RTKs), comprised of four members: EGFR (ErbB1, HER1), HER2 (ErbB2), HER3 (ErbB3) and HER4 (ErbB4) [24]. HER receptors are activated by a group of epidermal growth factor (EGF) ligands and undergo homo- or hetero-dimerization during th
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The expression of EBI has been
2021-08-23
The expression of EBI2 has been found to be dysregulated in several types of B cell malignancies and is thus reduced in e.g. diffuse large B-cell lymphomas [12] and chronic lymphocytic leukemia [13] and increased in post-transplantation lymphoproliferative disorders (PTLDs) [14]. EBI2 is also highly
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br The ubiquitin proteasome system The ubiquitin proteasome
2021-08-23
The ubiquitin proteasome system The ubiquitin proteasome system (UPS) plays a significant role in the regulation of cell growth and survival, in addition to maintaining cellular homeostasis. By means of the UPS, GW0742 can precisely and temporally degrade approximately 80% of the entire proteome.
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The mesolimbic dopamine system is believed to be
2021-08-20
The mesolimbic dopamine system is believed to be highly important for evaluating environmental stimuli in order to generate an adaptive behavioral response. Thus, not surprisingly these functions appear to have been highly conserved across the vertebrate subphylum. Even though teleost fish lack midb
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br Introduction The discoidin domain receptors DDRs
2021-08-20
Introduction The discoidin domain receptors (DDRs), DDR1 and DDR2, are unique among the receptor tyrosine kinases (RTKs) in being activated by interaction with the extracellular matrix [1], [2]. Binding to triple-helical collagen is mediated by the receptor extracellular domains that include an N
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Etoposide In conclusion the magnitude of the
2021-08-20
In conclusion, the magnitude of the association between prenatal exposure to MeHg and child neuropsychological development appears to be modified by polymorphisms in CYP3A7 and CYP3A5 genes in some of the populations studied. These results provide some support for the hypothesis that CYP3A genes may
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AV-951 br Additional CDKs with a role in
2021-08-20
Additional CDKs with a role in cancer Small molecule CDK inhibitors The majority of protein kinase inhibitors developed to date are type I inhibitors: they bind at the ATP–binding site, are ATP-competitive and target the kinase in its active state; with the activation loop DFG motif in the ‘in
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Prostaglandins PGs are lipid mediators that exhibit
2021-08-20
Prostaglandins (PGs) are lipid mediators that exhibit a variety of physiological properties by interacting specific G protein-coupled receptors (GPCRs) [10]. PGD2 is synthesized from PGH2 through two distinct PGD synthases; lipocalin-type PGD synthase (L-PGDS) and hematopoietic PGD synthase (H-PGDS)
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Compound A and Compound B Fig were found in
2021-08-20
Compound A and Compound B (Fig. 4) were found in our in vitro screening assays and have similar CRF1 receptor in vitro profiles (Table 1). When binding was investigated using [125I]-CRF in ex vivo assay, Compound A inhibited binding of [125I]-CRF both in the frontal cortex and the pituitary; however
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The inhibition of FAS by C produces an accumulation
2021-08-20
The inhibition of FAS by C75 produces an accumulation of malonyl-CoA which is difficult to reconcile with the activation of CPT1 reported by others [2], [16], [17], [18]. To unravel this paradox the mechanism of action of C75 needs to be examined. We recently demonstrated that C75 is converted in vi
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In the context of our ongoing studies to define
2021-08-20
In the context of our ongoing studies to define the phytochemical and biological properties of oxyprenylated secondary metabolites of plant and fungal origin, we wish to report herein the investigation on the interaction of some natural and semisynthetic O-alkylcoumarins with promising ChE inhibitor
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br Conclusions and future perspectives It is now
2021-08-20
Conclusions and future perspectives It is now evident that selective ETA or nonselective endothelin receptor antagonism provides therapeutic potentials against a variety of cardiovascular diseases such as hypertension, PAH, and diabetic microvascular dysfunction (Fig. 1). However, PAH is currentl
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Nocodazole australia All these results indicate that cleavin
2021-08-20
All these results indicate that cleaving embryos possess a regulative mechanism, sensing the number of inner Nocodazole australia and controlling the proportion of conservative and differentiative divisions of blastomeres. The current observations agree with the results from other laboratories and
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br Methods An ongoing prospective study at the Princess Marg
2021-08-19
Methods An ongoing prospective study at the Princess Margaret Cancer Centre is enrolling consenting patients with stage IV EGFRm NSCLC for longitudinal blood collection. Patients may enrol at any point in their treatment. In this study, we performed a cross-sectional analysis of 72 patient liquid
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