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Verapamil a calcium channel blocker used clinically as
2020-12-15
Verapamil, a calcium channel blocker used clinically as a coronary vasodilator, was amongst the first compounds identified that could reverse MDR and potentiate the effects of MDR1 substrates such as vincristine [15], [16]. Verapamil, along with a number of other MDR1 blockers, have proved largely u
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br Materials and methods br
2020-12-15
Materials and methods Results Discussion In this work, we have studied the contribution of different pathways to the slow but stable progression of replication forks through DNA damaged by MMS [15]. The in vivo analysis of DNA replication forks along a specific chromosome of S. cerevisiae h
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P7C3 We also discovered important clues to domain binding si
2020-12-14
We also discovered important clues to domain P7C3 of DGKs and how to exploit these regions for development of DGKα-selective inhibitors. The identification of a probe-modified site at the C1 domain provided the first evidence of a ligand binding site remote from the ATP binding region of DGKs. Alth
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Real time PCR as described previously with minor modificatio
2020-12-14
Real-time PCR, as described previously with minor modifications, was used to detect DNA . The PCR mixture (Qiagen) was as follows: 5mM MgCl2, 2.5μl of 10x PCR Buffer, 0.125μl of HotStarTaq DNA Polymerase, 0.25mM of each dNTP, 0.4μM of each primer and 0.1μM of FAMlabelled probe (‘5-aacaattggagggcaag
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NMR was employed for the determination of
2020-12-14
NMR was employed for the determination of un-ligated domain 1 structure of DDR2 receptor. The collagen-binding site on the same was identified by cross saturation experiment and mutagenesis [40]. Birgit leitinger identified the binding site of collagen with DDR2 receptor, which was three spatially a
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br Results br Discussion The structures presented here were
2020-12-14
Results Discussion The structures presented here were solved at high Edrophonium chloride and show in detail how DDR1 achieves high affinity for imatinib and ponatinib, respectively. Both type II inhibitors bind in their more potent extended conformations to the inactive DFG-out conformation
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br Materials and methods br
2020-12-14
Materials and methods Results Discussion NB has been shown to induce cancers in many tissues including the kidney, liver, and thyroid, following chronic inhalation in animals (Hsu et al., 2007). The available data indicate that a lager majority of studies on NB evaluate the effects of toxic
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Six substrate recognition sites SRS
2020-12-14
Six substrate recognition sites (SRS1-SRS6) have been identified at positions 102-123, 204-209, 238-244, 301-319, 374-382 and 483-492 (Table 2, underlined residues) based on Gotoh's proposal [30]. CYP3A163 displays the similar characteristic long sequences between helices F and G presenting two addi
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br Introduction Alzheimer s disease AD is the progressive
2020-12-14
Introduction Alzheimer’s disease (AD) is the progressive version of mild cognitive impairment and usually met by the elderly population. It falls into the class of neurodegenerative disorders that attacks the Dioscin synthesis nerves cells, or neurons, resulting in loss of memory, impairment of
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One specific brain region that
2020-12-14
One specific CPI-203 region that may be involved in the reduction of anxiety after anti-SVG-30 treatment is the lateral septum which contains a high density of CRF2 receptors [5], [44]. The lateral septum often exhibits increased immediate early gene expression in response to stress and anxiety [14
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Epigenetic silencing of genes that determine tumor invasiven
2020-12-14
Epigenetic silencing of genes that determine tumor invasiveness, growth patterns of tumors, and tumor-cell apoptosis12, 29 may also affect the expression of drug-metabolizing enzymes, thereby providing an additional genetic mechanism in pharmacogenomics. Trisomy 8 that contains wild-type GGH could b
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Autophagy is a dynamic process that primarily involves autop
2020-12-14
Autophagy is a dynamic process that primarily involves autophagosome formatting and lysosomal degradation, and these processes are controlled by autophagy-related genes (Atg) (Klionsky et al., 2012). The related protein SQSTM1/p62 (sequestosome 1) importantly serves as a signalling director in sever
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Interestingly from our consensus SBVC protocol only few comp
2020-12-14
Interestingly, from our consensus SBVC protocol only few compounds (less than 150) have been scored with a full ‘ consensus’. That means that these compounds appear in the top 5% of the database when ranked by every scoring function independently. After visual inspection, we have realized that two a
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Replacement of the saturated propoxy group
2020-12-14
Replacement of the saturated -propoxy group in compound with the unsaturated allyloxy group to obtain compound resulted in 10-fold decrease in ET receptor antagonism and more than 20-fold decrease in ET-selectivity. Analogous unsaturated allyloxy compound in the tetrazole series was found to have
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br Introduction Rhabdomyosarcoma RMS is
2020-12-14
Introduction Rhabdomyosarcoma (RMS) is a myogenic tumor that accounts for approximately 50% of all pediatric soft tissue sarcomas. Diagnostic criteria for RMS Pentamidine on the validation of proteins of the skeletal muscle lineage, such as Desmin, MyoD or Myogenin [1]. RMS cells are persistentl
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