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br Rationale and hypothesis To discover an allosteric inhibi
2021-06-07
Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be
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Dihydrotestosterone Two primary members of the TRIM
2021-06-07
Two primary members of the TRIM family – TRIM5α and TRIM25 – function as antiviral effector and immune regulator, respectively. TRIM5α is one of the best characterized members of the TRIM family (both structurally and functionally) and reported to be an important ubiquitin-mediated regulator of a ma
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br Materials and methods br Results br Discussion br
2021-06-07
Materials and methods Results Discussion Conflict of interest Introduction Dopamine-β-hydroxylase (DβH) deficiency is a rare autosomal recessive disorder characterized by the congenital absence of DβH, the enzyme converting dopamine to noradrenaline in sympathetic nerve terminals and
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For the SAR optimization of the right hand side it
2021-06-07
For the SAR optimization of the right hand side, it was decided to explore the inclusion of the key carboxylic Digoxin receptor moiety present in the original DGAT-1 inhibitors from . Analogs were constructed by the synthetic routes outlined in , . In , the methylene-oxy linker was introduced by co
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br Acknowledgements br Introduction Laryngeal cancers
2021-06-07
Acknowledgements Introduction Laryngeal cancers are the most frequent cancers of the head and neck region and their occurrence is strongly associated with the exposure to cigarette smoke and the consumption of strong alcohols. Almost all laryngeal cancers are squamous cell carcinomas. Usually
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Recently we have demonstrated that the synthesis of cysteiny
2021-06-07
Recently we have demonstrated that the synthesis of cysteinyl-LTs from LTA4 by human umbilical vein endothelial cells (HUVECs) is directly associated with the activation of the CysLT2 receptor (CysLT2R) in a typical autocrine fashion, and that solely the CysLT2R is responsible for the increase in in
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Park et al expanded their own model
2021-06-07
Park et al. [34] expanded their own model as hydrogen- bonding lattice fluid EOS (NLF-HB) [35] for calculating the activity coefficients of aqueous amino Birinapant solution. Further, Pazuki et al. [36] extended the perturbed hard chain theory which has been proposed by Beret and Prausnitz [37] for
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The majority of pro inflammatory cytokines are regulated by
2021-06-07
The majority of pro-inflammatory cytokines are regulated by NFκB, and recently, it has been found that p38 MAPK partly regulates NFκB-driven gene AZ3146 by increasing the association of the basal transcriptional factor, TATA-binding protein, with the C terminus of p65 subunit of NFκB and increasing
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CD is a key co stimulation surface
2021-06-07
CD28 is a key co-stimulation surface marker that can be detected in all peripheral T Gemcitabine sale in newborns, and the proportion of CD28bearing T cells reduces progressively with age [reviewed by (Fagnoni et al., 1996; Weng et al., 2009)]. Therefore, CD28nullCD8+ T cells are one of the most ac
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Estrogen receptors ERs belong to
2021-06-07
Estrogen receptors (ERs) belong to the third class of nuclear receptors (NR3) [23]. Two different forms of ER have been described, ERα and ERβ. They are coded by two distinct genes (ESR1 and ESR2, respectively) containing 8 transcribed exons that give rise to six conserved protein domains: domains A
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br Acknowledgements The authors thank Drs C Klein I Canisso
2021-06-05
Acknowledgements The authors thank Drs. C. Klein, I. Canisso and A. Claes with assistance in obtaining tissues. Supported by the Albert G. Clay Endowment, University of Kentucky. Introduction Neoplastic cells often develop drug resistance during tumor progression or cancer treatment (Turner a
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Since the dideoxy analogues and served
2021-06-05
Since the 1,2-dideoxy analogues, and , served as substrates for TgTCEA and TgTCEB, respectively, with the higher affinity (lower ) and lower turnover number (lower ) than their authentic substrates, PosA and PosB (such trend was more evident on analogue for TgTCEB than on analog for TgTCEA), an i
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br Orthotopic liver transplantation OLT
2021-06-05
Orthotopic liver transplantation (OLT) is the only curative therapy available for patients with end-stage liver disease. The surgical procedure of liver transplantation inherently involves cold ischemia during graft preservation , followed by reperfusion of the transplanted graft which results in
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Central to the mechanism of cold I R
2021-06-05
Central to the mechanism of cold I/R-associated liver injury is the activation of the pro-inflammatory cascade resulting in the release of pro-inflammatory cytokines. In agreement with the present study, serum and hepatic mRNA levels of TNF-α, IL-6, and ICAM-1 were all significantly up-regulated ear
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A study profiling chemokine expression in LCLs revealed high
2021-06-05
A study profiling chemokine expression in LCLs revealed high expression levels of CCR6, CCR7, and CCR10 and low expression of CXCR4 and CXCR5 in EBV immortalized cells. Accordingly, LCLs showed a markedly increase in migration in response to the ligands of CCR6 (CCL20), CC7 (CCL21), and CCR10 (CCL28
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