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Given the molecular pharmacology and in vitro metabolism dat
2021-08-04
Given the molecular pharmacology and in vitro metabolism data, we proceeded to evaluate the in vivo pharmacokinetics of . Mice (=3) were subsequently administered a subcutaneous dose (5mg/kg) with intermittent plasma collections to measure systemic levels of (). Compound achieved a maximum plasma co
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Previous studies demonstrated that cPLA translocates to the
2021-08-04
Previous studies demonstrated that cPLA2α translocates to the phagosomal membrane during macrophage phagocytosis through mechanisms that, in humans, involve phosphorylation of the enzyme by c-Jun N-terminal kinases and membrane association via the cationic cluster of four lysine residues present at
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During the course of enzymatic
2021-08-04
During the course of enzymatic digestion, protein is digested into large peptides and these large peptides are then further digested into small fragments. αs1-Casein f15–39, which contains 25 amino telomerase inhibitors residues was the longest iTRAQ-labelled peptide identified in the samples diges
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Pursuant to our in vitro data that
2021-08-04
Pursuant to our in vitro data that neutrophilic elastase activated the elastase-dependent oncolytic virus, we initially hypothesized that tumor-infiltrating neutrophils could be the source for elastase in tumor tissue. However, we did not detect neutrophils in the PANC-1 tumor tissue where we observ
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The loss of secondary mutation T M mutation
2021-08-04
The loss of secondary mutation T790M mutation after AR and SCLC transformation was also reported for Rociletinib. Piotrowska et al. using the MGH NGS platform recently reported in 13 biopsies among 12 EGFR T790M+ patients progressing after treatment with Rociletinib the loss of EGFR T790M mutation i
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Main Text Post translational modifications by ubiquitin Ub a
2021-08-04
Main Text Post-translational modifications by ubiquitin (Ub) and ubiquitin-like proteins (Ubl) regulate a diverse array of cellular and physiological processes including protein degradation, localization, and activation. While ubiquitination has primary responsibility for targeting substrates for p
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In normal cells the apoptotic stimuli lower the expression l
2021-08-04
In normal cells, the apoptotic stimuli lower the expression level of antiapoptotic proteins by increasing turnover rate and preventing the constant degradation of proapoptotic proteins. Thus, the dysregulation of anti-/pro-apoptotic proteins will confer the survival of cancer Diperodon HCl via enhan
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The ability of minor groove binding agents to inhibit
2021-08-04
The ability of minor groove binding agents to inhibit the activity of DNA helicases is not without precedence. Similar effective inhibition of the unwinding of DNA by the BLM and Werner's DNA helicases by the minor groove binder distamycin A has been observed. Further, and similar to RecBCD, interca
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Cyclophosphamide monohydrate receptor Diacylglycerol kinases
2021-08-04
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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The presence of external NAD P H dehydrogenases
2021-08-03
The presence of external NAD(P)H dehydrogenases (NDE) on the outer surface of the inner mitochondrial membrane enables the mitochondria to oxidize cytosolic NAD(P)H (Moller 2001). A porin (a voltage-dependent anion-selective channel, VDAC) that is abundant in the outer mitochondrial membrane permits
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br Pre clinical combination studies using CSF CSF R inhibito
2021-08-03
Pre-clinical combination studies using CSF-1/CSF-1R inhibitors In preclinical models, the CSF-1R pathway can be blocked by using either small molecule kinase inhibitors (GW2580 [30], PLX3397 [31], Ki20227 [32], BLZ945 [33] and CYC11645 [34]), antibody-mediated inhibition of CSF-1 using 5A1 [35] o
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Under optimized assay conditions very low concentrations pM
2021-08-03
Under optimized assay conditions, very low concentrations (20pM) of [125I]YP20 bound to hCRF1-CHO chemokine receptor antagonist membranes with high specificity (>95% inhibited by 1μM astressin) and in a membrane protein-dependent manner. Specific binding was selective vs. the hCRF2α subtype because
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Using characteristic features of ECM proteins and a computat
2021-08-03
Using characteristic features of ECM proteins and a computational pipeline combining interrogation of protein and gene databases, we previously defined the matrisome as the ensemble of ECM and ECM-associated proteins [[16], [17], [18]]. In mammals, the matrisome represents 4% of the genome, or appro
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kras-pdeδ inhibitor Due to its several industrial applicatio
2021-08-03
Due to its several industrial applications, the recombinant production of collagen and all its derivatives as gelatins has been pursued for many years in different biological systems as mammalian kras-pdeδ inhibitor (Toman et al., 1999), tobacco plants (Ruggiero et al., 2000), silkworms (Tomita et a
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FGF ERK signaling has been implicated in epithelial mesenchy
2021-08-03
FGF/ERK signaling has been implicated in epithelial-mesenchymal interactions in a wide range of tissues (Huh et al., 2015, Klein et al., 2006, Rice et al., 2004, Zhang et al., 2006, El Ramy et al., 2005, Volckaert and Langhe, 2015). During embryonic organogenesis and in adult organs, we often observ
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