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Mitochondrial depolarization induced by DHODH inhibition
2021-01-11
Mitochondrial depolarization induced by DHODH inhibition (Figure 5A) may also contribute to the selective effects of DHODH inhibitors on KRAS mutant cells. If so, the effect may arise more from pro-apoptotic effects of mitochondrial depolarization (Lemasters et al., 1998) than from impaired oxidativ
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There have been two reports of tumor
2021-01-11
There have been two reports of tumor shrinkage in response to dasatinib treatment in lung SCC patients harboring the DDR2 kinase domain S768R mutation., In the first case described by Hammerman et al. a combination of erlotinib (an epithelial growth factor receptor inhibitor) and dasatinib was admin
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In addition we investigated if the previously reported
2021-01-11
In addition, we investigated if the previously reported papain inhibitor can inhibit rhodesain, and found that it was not active at inhibiting rhodesain. The vinyl sulfone analogue of () was then synthesized and tested, and it was also inactive towards rhodesain. We then determined the time dependen
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Similar to Bdnf acute administration of
2021-01-11
Similar to Bdnf4, acute administration of RG108 did not alter gene expression of Gria1 and Hdac2, despite their relevance for the task. Gria1 belongs to the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic nk1 receptor antagonist receptor (AMPAR) family that is known to be crucial for LTP and the st
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br Material and methods br Discussion First
2021-01-11
Material and methods Discussion First, we investigated cannabis use, and results showed that the lifetime prevalence of cannabis use in our sample was 29.63%, with a significant difference between males (73.8% of the abusers) and females (26.2%). Moreover, the mean age and age at onset were si
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The crystal structure of full length CHK is still unsolved
2021-01-11
The crystal structure of full-length CHK is still unsolved. However, the close homology between CHK and Csk suggests that these kinases share a similar structure. Therefore, the engagement of the CHK SH2–kinase linker with the αC-helix could control the activity of the CHK kinase domain. Sequence al
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br Discussion EFTs are sarcomas with almost undifferentiated
2021-01-11
Discussion EFTs are sarcomas with almost undifferentiated histologic features, consequently their differentiation from other small, blue, round cell tumors may be difficult. Substantial intracellular (+)-Bicuculline on PAS stain is a useful diagnostic feature. The addition of CD99 and FLI1 immuno
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In mammals ribonucleotide reductase RNR
2021-01-11
In mammals, ribonucleotide reductase (RNR) is a unique enzyme that catalyzes the rate-limiting step of de novo synthesis of deoxyribonucleoside triphosphates (dNTPs).7, 8 Mammalian RNR consists of two homodimer subunits: the large catalytic dimer RRM1 and the small regulatory dimer RRM2 or RRM2B. An
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EP EP and EP receptor expression on HMVEC L
2021-01-11
EP1, EP3 and EP4 receptor expression on HMVEC-L was shown recently by flow cytometry [14]. However, only EP4 mRNA expression was previously described in these cells [49]. Our data obtained with RT-PCR showed EP4 mRNA and very low levels of EP1 mRNA, but no EP2 and EP3 mRNA expression was detectable
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Moxidectin Recoverin is a kDa retinal protein that binds to
2021-01-11
Recoverin is a 23-kDa retinal protein that binds to calcium. It regulates the Moxidectin of rhodopsin during visual transduction within photoreceptor cells. Since the pathogenicity of anti-recoverin antibody is potent, anti-recoverin CAR patients often have progressive visual impairments, character
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Besides EGFR other tyrosine kinase receptors are currently
2021-01-11
Besides EGFR, other tyrosine kinase receptors are currently gaining attention as potential therapeutic targets. Included among these is the fibroblast growth factor receptor (FGFR) family, which is involved in the progression of a variety of cancers.7, 8, 9, 10, 11 In lung cancer, fibroblast growth
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Intriguingly one E residue may serve as a
2021-01-11
Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In
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br Materials and methods br Results
2021-01-09
Materials and methods Results Discussion To date, several reports have suggested an involvement of DGK in bipolar disorder. A splice variant at the COOH-terminus of DGKβ has been related to bipolar disorder [15] and DGKβ KO mice showed hyperactive behavior [17]. For the other DGK isoforms,
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CCT241533 Some pyrimidine analogs are substrate based inhibi
2021-01-09
Some pyrimidine analogs are substrate-based inhibitors that bind to the dihydroorotate binding site, but most reported inhibitors of DHODH bind to the site occupied by the ubiquinone co-factor., , , , , , , , , , , , , , , , , X-ray crystallographic studies of inhibitor complexes with DHODH and DHOD
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br Introduction Analyses of genomic alterations
2021-01-09
Introduction Analyses of genomic alterations in cancer have identified epidermal growth factor receptor (EGFR) as one of the most potent “oncogenic driver” kinases that is present in many epithelial tumors including endometrial, breast, prostate, skin, esophagus, lung, stomach, colorectal, and re
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