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The requisite extended benzyl alcohols and and
2020-07-01
The requisite extended benzyl alcohols –, , and and final potential DFG-out binding hybrid inhibitors – and – were prepared as shown in , . Benzaldehyde was alkylated with -methoxybenzyl chloride and then reduced with sodium borohydride to give benzyl alcohol . Pyridine derivative was prepared by
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We have previously disclosed the discovery of a azaindole ac
2020-07-01
We have previously disclosed the discovery of a 7-azaindole-3-acetic t-type calcium channel CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to disclosure of
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br Materials and methods br Results br Discussion Intra BNST
2020-07-01
Materials and methods Results Discussion Intra-BNST injections of NOC-9 (at all doses) were able to produce freezing and anxiogenic-like effects. Freezing was observed immediately after the NO donor injection and lasted about 2–3min (data not shown). When exposed to the EPM 5min after intra
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The V V process of the
2020-07-01
The V&V process of the FPGA development includes equivalence checking (Huang and Cheng, 1998, Huang et al., 2000, Kuehlmann and Krohm, 1997, Kuehlmann et al., 1995, Burch et al., 1994) as well as the simulation techniques. The equivalence checking can prove that two given designs have the same funct
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Our earlier experimental studies showed neutral i e non
2020-07-01
Our earlier experimental studies showed \"neutral\", i.e. non-proliferative, effects of progesterone but a large increase in proliferation using certain progestins; however, this was only in the presence of PGRMC1 [[13], [14], [15], [16], [17], [18], [19]]. The next step was to investigate whether
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7ACC2 Future advances in the in vivo molecular imaging of
2020-07-01
Future advances in the in vivo molecular imaging of enzyme activity will greatly benefit from the progress towards the quantitative detection of enzymes. Quantitative imaging requires knowledge of both the location and concentration of a specific enzyme, which is dependent on the simultaneous measur
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The importance of AAE in enhancing the survival of plants
2020-07-01
The importance of AAE3 in enhancing the survival of plants and yeast when confronted with certain environmental stresses has been documented in recent reports. In response to biotic stress such as oxalate-secreting micro-organisms, AAE3 was found to reduce the inhibitory growth effects of the secret
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ELUXA HM EMSI is an ongoing pivotal Phase II global
2020-07-01
ELUXA 1 (HM-EMSI-202) is an ongoing pivotal Phase II global clinical trial, designed to further investigate the efficacy and safety of Olmutinib in patients T790M-positive NSCLC with acquired resistance after first-line EGFR TKIs. Primary endpoint is ORR according to RECIST 1.1, while secondary endp
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br Materials and Methods br
2020-07-01
Materials and Methods Acknowledgements Authors would like to thank Mr. Pritam Naskar and Mr. Dibya Mukherjee for their help. Authors also acknowledge the help of Mr. Barun Mahata and Dr. Kaushik Biswas, Division of Molecular Medicine, Bose Institute, for human cDNA samples. P.A.B. and A.B.D. w
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A number of factors have been shown to
2020-07-01
A number of factors have been shown to remove blocking end groups in order to make the termini of DSBs ligatable. A common non-ligatable end is one that contains either a 3′ phosphate or 5′ hydroxyl. The polynucleotide kinase/phosphatase (PNKP) is the NHEJ processing enzyme responsible for removing
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Our finding that the ATRX
2020-07-01
Our finding that the ATRX-DAXX-H3.3 complex promotes a form of HR is likely to have important implications for our understanding of the ALT recombination process that takes place at telomeres. We were surprised to observe that ATRX promotes a form of HR, since loss of the ATRX-DAXX-H3.3 complex is n
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FK-228 Protein expression and purification A
2020-07-01
Protein expression and purification. A 3 mL overnight culture of E. coli BL21 (DE3) pLysS pGEX-6P-3-A1S_0222 was grown in Luria-Bertani (LB)-Medium (10 g/L tryptone, 5 g/L yeast extract, 5 g/L NaCl, pH 7.4, 100 μg/mL Amp) at 37 °C and 160 rpm. The overnight culture was diluted 1:100 into 200 mL LB (
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br Results and discussion br Conclusion A new series of
2020-07-01
Results and discussion Conclusion A new series of 2-mercapto-quinazolin-4-one analogues is designed and synthesized to possess electron withdrawing or donating functional groups (Cl or CH3O) at position 6- or 7-, 4-methoxyphenyl function at position 3. The 2-mercapto function is used to connec
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br Materials and methods br Results br Discussion GOS potent
2020-07-01
Materials and methods Results Discussion GOS potently inhibited SRD5A1 in COS-1 cells (Fig. 4A) and rat Leydig cells (Fig. 4B), possibly attenuating testosterone activation into DHT. It has been reported that gossypol inhibited human SRD5A1 with IC50 of 7 × 10−6 M [28]. Interestingly, gossy
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br Methods br Results Our study focused on
2020-06-30
Methods Results Our study focused on consecutive postural adjustments (CPAs) between IS and BS (the shaded areas on Fig. 2); that is to say, the Rx kinetics that occur after the end of an upper limb movement. It was dedicated to examining the main features of CPAs and the influence of movement
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