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Our previous high throughput screening HTS campaign using au
2020-09-19
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based GS-9973 assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22], [23],
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br Materials and methods br Results br Discussion In rodent
2020-09-18
Materials and methods Results Discussion In rodent species, CYP2E1 and CYP2B have been implicated in CCl4 metabolism. In this study, we used expressed human CYP2E1 to show that this enzyme is a high-affinity catalyst responsible for low-dose CCl4 metabolism. Studies employing an inhibitory
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Studies have focused on a hydrophobic
2020-09-18
Studies have focused on a hydrophobic cage at the CULT domain, conserved from bacteria to mammals, as it binds to substrates and IMiDs (Chamberlain et al., 2014, Lupas et al., 2015). In addition, CRBN ligand-mediated protein degradation was highly conserved, which was confirmed in vertebrates by foc
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Neurons in the striatum unlike those in the cerebral
2020-09-18
Neurons in the striatum, unlike those in the Ifosfamide mg and cerebellum, do not form a layered or columnar structure. Although they appear to be randomly distributed, they are actually scattered in two embryologically different compartments called striosomes (often referred to as “patches” in rod
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The other interesting observation made during this study rel
2020-09-18
The other interesting observation made during this study relates to the differences between the discrete IR-induced γH2AX foci and the robust H2AX phosphorylation observed during apoptotic DNA fragmentation. The pattern of H2AX phosphorylation observed during DNA fragmentation possibly reflects the
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ML133 HCl br UVC induced DNA damage a
2020-09-18
UVC-induced DNA damage: a model to study DNA damage tolerance The UV components of sunlight that reaches the Earth surface are one of the most carcinogenic agents humans are exposed to, and the leading cause of skin cancer [4,12]. UV light causes different types of DNA damage through indirect and
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br Materials and methods br Statistical
2020-09-18
Materials and methods Statistical analysis All statistical analyses were performed using SPSS software version 20. Protein Linifanib data of DNMTs and clinicopathological parameters were collected. Mann-Whitney U Test was used to assess the differential expression of nonparametric data of DNMT
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Z-LEHD-FMK Extracellular uridine can be transported across
2020-09-18
Extracellular uridine can be transported across the cell membrane to enter the nucleotide salvage pathway. A colon cancer cell line supplemented with uridine was capable of growing normally in the presence of 1 μM brequinar (Peters et al., 1992). The supplemented uridine may be transported into the
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Introduction DHFR is an important enzyme in both mammals
2020-09-18
Introduction DHFR is an important enzyme in both mammals and microorganism including Mycobacterium tuberculosis (Mtb). It catalyzes folic glasdegib conversion to dihydro and tetrahydro folic acid which is a crucial step in folate pathway [1]. Inhibition of folate pathway leads to interruption of t
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An AmDH is engineered by mutating two conserved amino
2020-09-18
An AmDH is engineered by mutating two conserved amino Dronedarone mg residues in the active site of an amino acid dehydrogenase (AADH). Starting from the leucine dehydrogenase (LeuDH) from Bacillus stearothermophilus, substituting a serine and leucine at the K68 and N261 positions, respectively, re
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We aim to apply the
2020-09-18
We aim to apply the same technology to target other collagen-binding proteins using motifs from collagens that are specific for other receptors or matrix components. Previously, we synthesized THP libraries, called Toolkits, composed of an active guest sequence flanked by five GPP host triplets that
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One possible explanation for differences
2020-09-18
One possible explanation for differences in the binding ability of monomeric versus dimeric forms of DDR2 ECD to collagen could be that the monomeric form only binds to the primary GVMGFO site, whereas dimeric (and oligomeric) DDR2 ECD binds to additional sites on the collagen triple-helical molecul
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br Introduction Lung cancer is
2020-09-18
Introduction Lung cancer is the leading cause of cancer-related death worldwide, accounting for more than 1.5 million deaths in 2012. Non–small-cell lung cancers represent approximately 85% of lung neoplasms; among these, squamous cell carcinomas (SCC) account for approximately 30% of cases. The
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Calcium dependence of CaM target interaction was analyzed
2020-09-18
Calcium dependence of CaM/target interaction was analyzed using a titration matrix in which both Ca2+ and CaM concentrations were changed. This gave us access to different parameters characterizing the interaction and namely to the number of bound Ca2+ required for the interaction to occur. Our app
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Each nsP plays a distinct defined and indispensable role
2020-09-18
Each nsP plays a distinct, defined and indispensable role in the replication of viral genome. nsP1 is a membrane associated protein which possesses S-adenosyl-L-methionine (SAM)-dependent methyltransferase (MTase) and guanylyltransferase (GTase) activities to catalyze the viral RNA capping reaction
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