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DNA PK Jackson is activated by
2021-07-20

DNA-PK (Jackson, 1997) is activated by DNA double-stranded breaks (DSBs). It is a trimeric complex composed of the catalytic subunit, DNA-PKcs, and the Ku70/80 heterodimer. DNA-PK mediates non-homologous end joining (NHEJ), which joins programmed DSBs created during V(D)J recombination and class swi
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Recently naphthoquinone derivatives have shown promising res
2021-07-20

Recently, naphthoquinone derivatives have shown promising results as antiparasitic lead compounds [28]. Conjugated hybrid compounds could be an effective path to discovery of new drugs by associating two different pharmacophore groups with different mechanisms of action in a single molecule [29,30],
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br Molecular modeling simulation study Molecular
2021-07-20

Molecular modeling simulation study Molecular modeling study was performed through docking of the test compounds into the binding site of hDHFR enzyme using Discovery Studio 2.5 software. Computational docking is an algorithm designed to determine the suitable position and the orientation of the
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Some limitations to our study should be
2021-07-20

Some limitations to our study should be noted. First, the sample size of our study was limited. As DDR2 mutations are rare in lung SCC, it is possible that the power of our study was insufficient to detect potential associated factors. Second, a significant proportion of the 271 sequenced patients h
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br Results br Discussion The
2021-07-20

Results Discussion The sequence homology-based clustering of the human kinome by Manning et al. (2002) has been extremely useful to organize kinases into MLN2238 by sequence relationship. Since kinases are such prominent drug targets, we expect that clustering of the kinases by their inhibiti
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The synthetic route of R
2021-07-20

The synthetic route of R-changed derivatives is shown in . Compounds – were prepared from commercially available 4-nitro-1-indazole (). After same two steps with , the N-substituted indazole of was produced using the Suzuki reaction in a good yield (85%). Reduction of was performed using Pd/C, and
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br Pre clinical combination studies using CSF CSF R
2021-07-20

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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br Methods Adult male B CRHtklee mice g at the
2021-07-20

Methods Adult male B6, 129 CRHtklee mice (25–30g at the beginning of the experiments) that were wild-type (CRF1R+/+) and recessive homozygous or knockout (CRF1R−/−) were housed six per cage. Mice were 3–5months old and derived from mating CRF1R+/− breeders (Jackson Laboratory, California). Wild-t
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In Murray Darling rainbowfish confirming the expected
2021-07-20

In Murray–Darling rainbowfish, confirming the expected in vivo effects of androgenic progestins could be achieved using short-term exposures and determining expression profiles for androgen-responsive genes, or in longer term exposures by monitoring fecundity or the development of male secondary sex
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We hypothesize that both IGF dependent kinase
2021-07-20

We hypothesize that both IGF-1-dependent kinase activation and locally synthesized neuroestrogens interactively regulate estrogen receptor activity in neuronal CID 2011756 in the absence of exogenously applied estradiol. The Neuro-2A cell line was chosen as the model system for these studies becaus
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br Diverse functions of ERK pathway Same as
2021-07-19

Diverse functions of ERK pathway Same as the other MAPK cascades, the ERK pathway is activated by several extracellular stimuli and different internal routes. ERK vitally tunes the function of various substrates in all cellular components; the nucleus, cytoplasm, membranes and the cytoskeleton. E
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br Effects of culture conditions on drug
2021-07-19

Effects of culture conditions on drug-induced gene BMH-21 in primary human hepatocytes Past progress in elucidating the optimal conditions for the long-term cultivation of rodent hepatocytes has helped define some of the key components in the matrix and medium environment that are most critical
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Autoradiography studies have shown cerebellum to be devoid
2021-07-19

Autoradiography studies have shown E3330 to be devoid of D1-R [40], confirming that this region may serve as reference for estimation of free and non-specifically bound radioligand concentration in tissue (= non-displaceable uptake). In initial human studies using [11C]SCH 23390 and [11C]NNC 112, q
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The human serotonin hydroxytryptamine HT receptor family
2021-07-19

The human serotonin (5-hydroxytryptamine; 5-HT) receptor family consists of 14 receptor subtypes to date, which are primarily G protein-coupled receptors (GPCRs) with 5-HT3 being the sole ligand-gated ion channel (Alexander et al., 2017). These receptors are widely distributed in the central and per
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To study the role of
2021-07-19

To study the role of DNA–PK in the response to replication arrest, we used the DNA replication inhibitor aphidicolin (APH). APH, a mycotoxin isolated from Cephalosporium aphidicola, inhibits DNA replication by interacting with the replicating DNA polymerase α (pol α). APH specifically inhibits the a
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